Amitriptyline tablets - Instructions for Use, Dosage, Side Effects, Reviews

Synonyms: ADTzimaia, Amiline, Amiplin, Amitone, Amitrac, Amitrac-CZ (Amitriptyline and Chlordiazepoxide), Amitrip, Amitriptilina Andromaco, Amitriptilina Cevallos, Amitriptilina L.CH., Amitriptilina La Santé, Amitriptilina Luar, Amitriptilina MK, Amitriptilina, Amitriptiline, Amitriptyline GM, Amitriptyline Remedica, Amitriptyline, Amitriptyline-Grindeks, Amitriptyline-IKA, Amypres, Amypres-C (Amitriptyline and Chlordiazepoxide), Amyzol, Apo-Amitriptyline, Axeptyl (Amitriptyline and Chlordiazepoxide), Conmitrip, Cuait-D (Amitriptyline and Trifluoperazine), Dapaz Compuesto (Amitriptyline and Chlordiazepoxide), Emotrip (Amitriptyline and Chlordiazepoxide), Fiorda, Kamitrin, Latilin, Limbival Forte (Amitriptyline and Chlordiazepoxide), Limbritol (Amitriptyline and Chlordiazepoxide), Maxitrip, Mitryp, Mitryp Forte (Amitriptyline and Chlordiazepoxide), Odep, Tadamit, Tiperin (Amitriptyline and Chlordiazepoxide), Trepiline, Tryptanol, Adepril, ADT, Amilavil, Amilin, Amineurin, Amineurin retard, Amiplin, Amirol, Amit, Amitin, Amitrip, Amitriptilin R. Desitin, Amitriptilina Clorhidrato Mintlab, Amitriptilinã, Amitriptilino, Amitriptylin beta, Amitriptylin beta retard, Amitriptylin Dak, Amitriptylin Desitin, Amitriptylin Leciva, Amitriptylin Nycomed, Amitriptylin Slovakofarma, Amitriptylin Valeant, Amitriptylin, Amitriptylin-CT, Amitriptylin-dura, Amitriptyline Changzhou Siyao, Amitriptyline Chen Ho, Amitriptyline Glaxo, Amitriptyline HCl Actavis, Amitriptyline HCl Apotex, Amitriptyline HCl CF, Amitriptyline HCl Mylan, Amitriptyline HCl PCH, Amitriptyline HCl ratiopharm, Amitriptyline HCl Sandoz, Amitriptyline HCl Teva, Amitriptyline Hydrochloride Caraco, Amitriptyline Hydrochloride Medopharm, Amitriptyline Hydrochloride Mutual, Amitriptyline Hydrochloride Mylan, Amitriptyline Hydrochloride Sandoz, Amitriptyline Hydrochloride Vintage, Amitriptyline Hydrochloride, Amitriptyline Jinup, Amitriptyline Nycomed, Amitriptyline Update, Amitriptyline, Amitriptyline-Grindeks, Amitriptylin-neuraxpharm, Amitriptylin-neuraxpharm retard, Amitriptylin-Sandoz, Amitriptylinum ICN Polfa, Amitriptylinum, Amitriptylinum VP, Amitriptylin-Zentiva, Amitryp, Amixide (Amitriptyline and Chlordiazepoxide), Amixide H (Amitriptyline and Chlordiazepoxide), Amotrip, Amyline, Amytril, Amyzol, Anapsique, Antalin (Amitriptyline and Chlordiazepoxide), Apo-Amitriptyline, Chlordiazepoxide and Amitriptyline Hydrochloride Mylan (Amitriptyline and Chlordiazepoxide), Deprelio, Diapatol (Amitriptyline and Chlordiazepoxide), Elatrol, Elatrolet, Elavil, Endep, Klotriptyl (Amitriptyline and Chlordiazepoxide), Laroxyl, Libotryp-XL (Amitriptyline and Chlordiazepoxide), Limbitrol (Amitriptyline and Chlordiazepoxide), Limbitrol-H (Amitriptyline and Chlordiazepoxide), Limbitryl (Amitriptyline and Chlordiazepoxide), Limbival (Amitriptyline and Chlordiazepoxide), Maxitrip-CZ (Amitriptyline and Chlordiazepoxide), Maxivalet, Minitran (Amitriptyline and Perphenazine), Modup, Morelin (Amitriptyline and Chlordiazepoxide), Mutabase (Amitriptyline and Perphenazine), Mutabon (Amitriptyline and Perphenazine), Neo Amitriptilin, Neuragon (Amitriptyline and Perphenazine), Nobritol Forte (Amitriptyline and Medazepam), Nobritol (Amitriptyline and Medazepam), Normaln, Perphenazine and Amitriptyline Hydrochloride Mylan (Amitriptyline and Perphenazine), Pertriptyl (Amitriptyline and Perphenazine), Pinsaun, Polybon (Amitriptyline and Perphenazine), Polytanol, Protanol, Qualitriptine, Redomex, Sandoz Amitriptyline, Saroten, Saroten Retard, Sarotex, Sarotex Retard, Sedans (Amitriptyline and Chlordiazepoxide), Stelminal, Syneudon, Teperin, Thymontil, Trip, Tripta, Triptafen (Amitriptyline and Perphenazine), Triptilin, Triptizol, Triptyl, Triptyline, Tripyline, Trynol, Tryptanol, Tryptin, Tryptizol, Uxen Retard.

Active substance: Amitriptyline.

What is amitriptyline?

Amitriptyline is a tricyclic antidepressant. Amitriptyline affects chemicals in the brain that may be unbalanced in people with depression.

Amitriptyline is used to treat symptoms of depression.

Important information about amitriptyline

You should not use this medicine if you have recently had a heart attack.

Do not use amitriptyline if you have used an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine.

Before taking amitriptyline, tell your doctor if you have used an "SSRI" antidepressant in the past 5 weeks, such as citalopram (Celexa), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, Symbyax), fluvoxamine (Luvox), paroxetine (Paxil), or sertraline (Zoloft).

You may have thoughts about suicide when you first start taking an antidepressant such as amitriptyline, especially if you are younger than 24 years old. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

Report any new or worsening symptoms to your doctor, such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

ATC - N06AA09 amitriptyline

Pharmacological group - Antidepressants.

Nosological classification (ICD–10)

F10.3 abstinence;

F20 Schizophrenia;

F29 Inorganic psychosis, unspecified;

F32 Depressive episode;

F33 Recurrent depressive disorder;

F41.2 Mixed anxiety and depressive disorder;

F50.2 Bulimia Nervosa;

F60.3 Emotionally unstable personality disorder;

F90.0 disturbance of activity and attention;

F91.9 Conduct disorder, unspecified;

F92.0 Depressive conduct disorder;

F98.0 Enuresis inorganic nature;

G43.9 Migraine, unspecified;

G53.0 neuralgia after herpes zoster (B02.2 +);

G62.9 Polyneuropathy, unspecified;

G63.2 Diabetic polyneuropathy (E10-E14 + with common fourth character.4);

K25 Gastric;

K26 Duodenal Ulcer;

M79.0 Rheumatism, unspecified;

M79.2 Neuralgia and neuritis unspecified;

R51 Headache;

R52.1 Constant non stopped pain;

R52.2 Other constant pain;

R52.9 Pain unspecified;

T14.4 Injury of nerve (nerve) of unspecified body region.

Pharmacological action

Pharmacological action - sedative, timoleptic, antidepressant.

Antidepressant from the group of tricyclic compounds derived dibenzocyclogeptadine.

The mechanism of antidepressant action is associated with increased concentration of norepinephrine in the synapses and/or serotonin in the central nervous system by inhibiting reverse neuronal capture of these mediators. Prolonged use reduces the functional activity of β-adrenergic receptors and serotonin receptors of the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, impaired in depressive states. When anxiety and depressive states, reduces anxiety, agitation and depressive symptoms.

Also has some analgesic effect, which is believed to be associated with changes in the concentrations of monoamines in the central nervous system, especially serotonin, and effects on endogenous opioid system.

Possesses strong peripheral and central anticholinergic action, due to a high affinity for m-cholinergic receptors; strong sedative effect connected with affinity for histamine H1 receptors and alpha-adrenoceptor blocking action.

Has antiulcer effect mechanism is due to the ability to block histamine H2 receptors in the parietal cells of the stomach and provide a sedative and m-anticholinergic action (if gastric ulcer and duodenal ulcer reduces pain, promotes healing of ulcers).

Efficiency in bedwetting is caused, apparently, anticholinergic activity, which leads to an increase in the ability of the bladder to stretch, direct β-adrenergic stimulation, the activity of α-adrenergic agonists, accompanied by increased tone of the sphincter and the central blockade of serotonin reuptake.

The mechanism of therapeutic action for bulimia nervosa is not installed (possibly similar to that for depression). It shows the distinct efficacy of amitriptyline in bulimia patients without depression, as well as when it is available, while reducing bulimia can be observed without a concomitant weakening of the most depressed.

With general anesthesia reduces blood pressure and body temperature. Does not inhibit MAO.

Antidepressant effect develops within 2–3 weeks after the start of the application.

Pharmacokinetics of amitriptyline

Bioavailability of amitriptyline is 30–60%. Plasma protein binding is 82–96%. Vd - 5–10 l/kg. Metabolized to the active metabolite nortriptyline.

T 1/2 - 31–46 hours. Excreted mainly by the kidneys.

Amitriptyline Dosage

For oral starting dose is 25–50 mg at night. Then, within 5–6 days the dose is increased to individually 150–200 mg/day (most of the dose is taken at night). If during the second week of no improvement occurred, the daily dose increased to 300 mg. With the disappearance of symptoms of depression to reduce the dose of 50–100 mg/day and continue therapy for at least 3 months. In elderly patients with lung disorders the dose is 30–100 mg/day is usually 1 time/at night, after achieving the therapeutic effect switching to the minimum effective dose - 25–50 mg/day.

When nocturnal enuresis in children aged 6–10 years - 10–20 mg/day for the night, at the age of 11–16 years - 25–50 mg/day.

IM - the initial dose is 50–100 mg/day in 2–4 administration. If necessary, the dose may be gradually increased to 300 mg/day, in exceptional cases - up to 400 mg/day.

Amitriptyline Drug Interactions

While the use of drugs, providing a depressing effect on the central nervous system, may significantly increased inhibitory action on the central nervous system, hypotensive effect, respiratory depression.

While the use of drugs having anticholinergic activity may increase anticholinergic effects.

With simultaneous use may increase the action of sympathomimetic funds for the cardiovascular system and increase the risk of cardiac arrhythmias, tachycardia, severe hypertension.

While the use of antipsychotic drugs (neuroleptics) are relatively suppressed metabolism, with a reduction in the threshold of convulsive readiness.

While the use of antihypertensive drugs (except clonidine, guanethidine and their derivatives) may increase the antihypertensive action and the risk of orthostatic hypotension.

With the simultaneous use with MAO inhibitors may develop a hypertensive crisis; with clonidine, guanethidine - may decrease the hypotensive effect of clonidine or guanethidine; with barbiturates, carbamazepine - may decrease the action of amitriptyline due to increasing its metabolism.

Described a case of serotonin syndrome with concomitant use of sertraline.

In an application with sucralfate decreases absorption of amitriptyline; with fluvoxamine - increases the concentration of amitriptyline in blood plasma and the risk of toxic action; with fluoxetine - increased concentration of amitriptyline in plasma and develop toxic reactions due to inhibition of isoenzyme CYP2D6 under the influence of fluoxetine; with quinidine - may slow metabolism of amitriptyline; cimetidine - possibly slowing down the metabolism of amitriptyline, increasing its plasma concentration and the development of toxic effects.

While the use of ethanol increases the effects of ethanol, especially during the first few days of therapy.

Pregnancy and lactation

Amitriptyline should not be used during pregnancy, especially in the I and III trimester, except in cases of extreme necessity. Adequate and well-controlled clinical studies safety of amitriptyline during pregnancy was conducted.

Acceptance of amitriptyline should be gradually canceled at least 7 weeks prior to delivery to avoid the development of withdrawal syndrome in the newborn.

In experimental studies, amitriptyline is teratogenic.

Contraindicated during lactation. Excreted in breast milk and may cause drowsiness in infants.

Amitriptyline Side effects

CNS and peripheral nervous system: drowsiness, fatigue, fainting, anxiety, confusion, agitation, hallucinations (especially in elderly patients and in patients with Parkinson’s disease), anxiety, restlessness, mania, hypomania, aggressiveness, impaired memory, depersonalization, increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of psychosis symptoms, headache, myoclonus, dysarthria, tremor (especially of hands, head and tongue), peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, acceleration and intensification of epileptic seizures, EEG changes.

Cardio-vascular system: orthostatic hypotension, tachycardia, conduction disturbances, dizziness, nonspecific ECG changes (ST interval or tooth T), arrhythmias, blood pressure lability, impaired intraventricular conduction (widening complex QRS, change the interval PQ, block bundle-branch block).

From the digestive system: nausea, heartburn, vomiting, gastralgia, increase or decrease in appetite (increase or decrease in body weight), disease, change in taste, diarrhea, darkening of the tongue; rarely - liver dysfunction, cholestatic jaundice, hepatitis.

From the Endocrine: testicular swelling, gynecomastia, breast enlargement, galactorrhea, changes in libido, reduced potency, hypo-or hyperglycemia, hyponatremia (decreased production of vasopressin), a syndrome of inappropriate secretion of ADH.

Hematopoietic system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.

Allergic reactions: skin rash, pruritus, urticaria, photosensitivity, swelling of the face and tongue.

Effects due to the anticholinergic activity: dry mouth, tachycardia, accommodation disturbances, blurred vision, mydriasis, increased intraocular pressure (only those with a narrow anterior chamber angle), constipation, paralytic ileus, urinary retention, decreased sweating, confusion, delirium or hallucinations.

Other: hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, pollakiuria, hypoproteinemia.

Indications

Depression (especially with anxiety, agitation and sleep disorders, including childhood, endogenous, involutional, reactive, neurotic, drug, with organic brain damage, alcohol withdrawal), schizophrenic psychoses, mixed emotional disorders, behavioral disorders (activity and attention), nocturnal enuresis (except in patients with hypotonia of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic pain, atypical facial pain, postherpetic neuralgia, posttraumatic neuropathy, diabetic neuropathy, peripheral neuropathy), prophylaxis of migraine, peptic ulcer and duodenal ulcer.

Contraindications

The acute period and early recovery period after myocardial infarction, acute alcohol intoxication, acute intoxication with soporific, analgesic and psychotropic drugs, angle-closure glaucoma, severe violations AV- and intraventricular conduction (bundle-branch block, AV-block II degree), lactation, Children under 6 years of age (for oral administration), children under the age of 12 years (for the/m and/in the introduction), simultaneous treatment with MAO inhibitors, and the period of 2 weeks prior to their use, increased sensitivity to amitriptyline.

Cautions

With careful use in ischemic heart disease, arrhythmias, heart block, heart failure, myocardial infarction, hypertension, stroke, chronic alcoholism, thyrotoxicosis, against the background of therapy with thyroid cancer.

The therapy amitriptyline caution is needed with a sharp transition in the vertical position from the “lying” or “sitting”.

In a dramatic reception may develop withdrawal symptoms.

Amitriptyline in doses greater than 150 mg/day lowers the threshold of convulsive readiness; should take into account the risk of seizures in susceptible patients, as well as the presence of other factors that increase the risk of seizures (including with traumatic brain injury of any etiology, concomitant use of antipsychotic drugs in the period of refusal or withdrawal of ethanol drugs possessing anticonvulsant activity).

It should be borne in mind that patients with depression may attempt suicide.

In conjunction with electroconvulsive therapy should only be used with careful medical supervision.

In predisposed patients and elderly patients may provoke the development of drug psychosis, mainly at night (after the withdrawal of the drug are within a few days).

Can cause paralytic ileus, mainly in patients with chronic constipation who are elderly or in patients who have to comply with bed rest.

Prior to the general or local anesthesia, the anesthetist should be warned that the patient is taking amitriptyline.

With prolonged use, an increase the frequency of dental caries. May increase the need for riboflavin.

Amitriptyline can be applied not earlier than 14 days after discontinuation of MAO inhibitors.

Should not be used simultaneously with adrenergic and sympathomimetic, including epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine.

Used with caution in conjunction with other drugs, anticholinergic effect.

During the reception, amitriptyline to avoid drinking alcohol.

Effects on ability to drive vehicles and management mechanisms

During the period of treatment should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Amitriptyline Review

Now I try to tell my story about amitriptyline in brief. I took this drug half a year ago, as she was in a terrible depression. First, as usual happens to normal people is that they disagree with their loved ones. That's how I happened at that time, I met a long time, was eventually betrayed. Plus, the long time I could not find a job, it is very much affected my stress. Plus family have problems. Eternal emotions, tears, frustration dragged me into the black fabric of the pool every day without meaning, without goals and desires, without appetite, lethargy overtook me, everything irritated me every detail, frustrated at all, and at all times. Not happy just nothing. Even girlfriends could not calm, in on itself, no longer smiling, enjoy, just there and gasped. The moral of all I was disgusted. I experience the first fear when fainted from exhaustion on hunger, because the appetite and exhaustion that night did not sleep, for days on end just like a plant, silent and barely breathing. I bought my mother the drug, so the spacecraft need to have at least something to do. It helped. Two weeks later came back to me the meaning of life, the joy of all things, appetite and rather brutal, ate everything that I wanted. The nerves have calmed down, and I fell in love again, my life and everyone around. Therefore, those who give up and is going through, take, do not be afraid, too, will be the most happy. Now I am very happy, I have a favorite guy, favorite work, and a family favorite.

Medicinal antidepressants serious thing and take them, of course, need to by a physician.
I have been prescribed "Amitriptyline" many years ago, since then periodically accept it. Why periodically, because to him with a long reception habituation occurs.
Now convinced of their own experience. Somehow it did not stop taking it for a year, then there was a strong withdrawal symptoms. Two months were very bad (here will not go into details).
Generally, "Amitriptyline" are usually intended for long-term treatment with the tablets of the reception at different doses three times a day.
I also saw under the scheme. But for myself I decided it was too.
And it limits one tablet at night.
Despite the fact that the drug amitriptyline quite old (about it because a lot of criticism), but still knows his stuff. Well calms the nervous system, resulting in a sense, it helps to cope with depression.
It has weak hypnotic effect, and therefore accept for the night.
I have not had adverse events (with the exception of the worst-addictive). But when the measure courses, then everything is fine.
The only thing I want to add, I prefer to import "Amitriptyline" (preferably Austria). The jar of 50 tablets.

With antidepressant "Amitriptyline" I pushed once the fate of my mother. Her brother died and nerves began to develop neurosis. I bought her all kinds of drugs, spent a lot of money, but did not really help. The internal tension, tremors, body aches, burning sensation in the chest, insomnia, chronic headaches, bad mood mother was tortured for six months. And most importantly the adrenaline went beyond the norm, confusion, restlessness in one place, constantly she wanted to run somewhere, pursued a constant feeling of fear. A few months later it added to the neuroses and even depression, as her mother began to feel that this cure is no longer possible. I had to leave work because she could not be in the team, among the people. Then one day a friend of my mother therapist advised to use this drug is very inexpensive. Taking these pills for a month will remove all of the above symptoms. It is well soothes and relaxes the nervous system. Currently this drug Mom uses at bedtime, in those moments when difficult to sleep, and in the general state of her normal. Of course this drug is not candy, but the functions it performs well. Its main side action-is a dry mouth and slight numbness of the tongue. Other side effects have been observed. With this drug Mom went back to normal life.

Anafranil (Clomipramine) tablets - Instructions for Use, Dosage, Side Effects, Reviews

Synonyms: Anafranil, Atenual, Ausentron, Clomip, Clomipramin, Clonil, Depnil, Ocifril, Ocifril-XR, Praminex, Syconil, Anafranil, Anafranil retard, Anafranil SR, Anafril, Apo-Clomipramine, Chemmart Clomipramine, Clofranil, Clomi, Clomicalm (veterinary use), Clomidep, Clomine, Clomipramin-CT, Clomipramine (chlorhydrate) Mylan, Clomipramine HCl Actavis, Clomipramine HCl CF, Clomipramine HCl Mylan, Clomipramine HCl PCH, Clomipramine HCl ratiopharm, Clomipramine HCl Sandoz, Clomipramine Hydrochloride, Clomipramine Mylan, Clomipramine Sandoz, Clomipramine Teva, Clomipramine, Clomipraminhydrochlorid 2care4, Clomipramin-neuraxpharm, Clomipramin-neuraxpharm retard, Clomipramin-ratiopharm, Clopran, Clowin, CO Clomipramine, Cosinic, Equinorm, For-You, GenRX Clomipramine, Gromin, Hydiphen, Klomipramin Merck NM, Klomipramin Mylan, Klomipramin, Maronil, Pashin, Placil, Promil, Terry White Chemists Clomipramine, Trianil.

Active substance: Clomipramine.

ATC - N06AA04 clomipramine

Pharmacological group - Antidepressants.

Nosological classification (ICD–10)

F32 Depressive episode;

F40.0 Agoraphobia;

F42 Obsessive-compulsive disorder;

F44 Dissociative [conversion] disorders;

G47.4 Narcolepsy and cataplexy;

R32 Urinary incontinence, unspecified;

R52.2 Other constant pain.

Anafranil Composition, structure and packing

Anafranil (25 mg): Coated tablets pale yellow sugar; round, biconcave.

Excipients: lactose, corn starch, colloidal silicon dioxide, stearic acid, talc, magnesium stearate, glycerol 85%, hydroxypropyl methylcellulose, vinylpyrrolidone/vinyl acetate, titanium dioxide, crystalline sucrose, polyvinylpyrrolidone K30, disperse yellow 15093 ansted (iron oxide yellow (EES172) + 5% titanium dioxide (EES171) 95%), polyethylene glycol 8000 (Macrogol 8000), microcrystalline cellulose.

Anafranil SR (75 mg): Sustained-release tablets, film-coated pink capsules, biconcave, with Valium on both sides, one side embossed “C/G”, on the other - “G/D”.

Other ingredients: calcium hydrogen phosphate dihydrate, polyacrylate dispersion 30%, calcium stearate, colloidal silicon dioxide, hydroxypropyl cellulose, talc, titanium dioxide, polyoxyl 40 hydrogenated castor oil, iron oxide red.

Pharmacological action

Tricyclic antidepressant, an inhibitor of the reuptake of norepinephrine and serotonin. It is believed that the therapeutic action is carried Anafranil due to its ability to inhibit neuronal noradrenaline (NA) and serotonin (5-HT), released into the synaptic cleft, and the most important is the inhibition of serotonin reuptake.

Anafranil furthermore inherent in a wide variety of other pharmacological activities: alpha 1-adrenolytic, anticholinergic, antihistaminic and anti-serotoninergic (blockade of 5-HT-receptors).

Anafranil works on the depressive syndrome as a whole, including especially in its typical symptoms such as psychomotor retardation, depressed mood and anxiety. The clinical effect is usually observed after 2–3 weeks of treatment.

In addition, Anafranil has a specific (different from its antidepressant effect) effect in obsessive-compulsive disorders.

Action Anafranil for chronic pain syndromes, as due and not due to physical illness, probably due to relief transmission of nerve impulses, mediated by serotonin and noradrenaline.

Pharmacokinetics

Absorption

After oral clomipramine completely absorbed from the gastrointestinal tract. Systemic bioavailability of unchanged clomipramine is about 50%. Such a reduction in bioavailability due to the effect of “first pass” through the liver to the active metabolite of N-dezmethylclomipramine. Food intake does not significantly affect the bioavailability of clomipramine. Perhaps only a slowing its absorption and hence increase the time to reach C max in the blood plasma. Anafranil (coated tablets) and Anafranil SR (sustained-release tablets, coated tablets) is bioequivalent.

After oral administration in a constant daily dose of clomipramine Css in plasma varies greatly from patient to patient.

With daily administration of 75 mg/day Css of clomipramine in the plasma is established in the range from 20 to 175 ng/ml. C ss values of the active metabolite of N-dezmethylclomipramine at 40–85% higher than that of clomipramine.

Distribution

Clomipramine binding to plasma proteins is 97.6%. The apparent Vd is about 12–17 L/kg of body weight. Concentrations of clomipramine in the cerebrospinal fluid is approximately 2% of its level in blood plasma. Clomipramine penetrates into breast milk, where it is determined at concentrations similar to the concentrations in the blood plasma.

Metabolism

Clomipramine is metabolized mainly by demethylation to the active metabolite N-decmetilklomipramina. In this reaction involves several cytochromeP–450 isozymes, but mainly CYP3A4, CYP2C19 and CYP1A2. Clomipramine and N-dezmethylclomipramine hydroxylated to 8 hydroxyclomipramine and 8-hydroxy-N-dezmethylclomipramine. Activity of hydroxy-metabolite in vivo is not defined. Clomipramine also hydroxylated in position 2; N-dezmethylclomipramine can be further demethylated to dezmethylclomipramine. 2 and 8-hydroxy metabolites are excreted predominantly in the urine as glucuronides. The elimination of the two active components - clomipramine and N-dezmethylclomipramine by forming 2 and 8 hydroxyclomipramine catalyzed CYP2D6.

Excretion

Approximately 2/3 of a single dose of clomipramine is output as the water-soluble conjugates in urine and approximately one third dose - feces. Unchanged in the urine output of about 2% of the dose of clomipramine and about 0.5% dezmethylclomipramine. T 1/2 plasma clomipramine averaging 21 hours (range of variation from 12 to 36 hours) and dezmethylclomipramine - average 36 hours.

Pharmacokinetics in special clinical situations

In elderly patients, regardless of the dose used Anafranil, due to the reduction of metabolic rate in the plasma concentration of clomipramine higher than in younger patients.

Data on the effect of functional disorders of the liver and kidneys on the pharmacokinetic parameters of clomipramine has not yet been received.

Clomipramine (Anafranil) Dosage

Doses were selected individually, taking into account the patient’s condition. The goal of treatment is to achieve an optimal effect on the background of the lowest possible doses of the drug, as well as their gentle increase, especially in elderly patients and adolescents, which are generally more sensitive to Anafranil than those of intermediate age groups.

Before therapy should eliminate hypokalemia.

In depression, obsessive-compulsive syndrome and phobias initial daily dose is 75 mg (25 mg 2–3 times/day) or Anafranil 75 mg 1 time/day Anafranil Wed Then, during the first week of treatment, the dose was gradually increased, e.g., 25 mg every several days (depending on tolerance) to achieve the daily dose is 100–150 mg. In severe cases, the daily dose may be increased to a maximum of 250 mg. Once improvement is achieved, the patient is transferred to a maintenance dose of the drug, is 50–100 mg (2–4 tablets. Anafranil or 1 tab. Anafranil SR).

For panic disorder, agoraphobia, the initial dose is 10 mg/day. Then, depending on the tolerability Anafranil, the dose was increased to achieve the desired effect. The daily dose varies considerably and may range from 25 mg to 100 mg. When necessary, may increase the dose to 150 mg/day. It is recommended not to stop the treatment for at least 6 months, slowly decreasing during this time a maintenance dose of the drug.

When cataplexy accompanying narcolepsy, a daily dose of 25–75 mg Anafranil.

In chronic pain syndromes Anafranil dose should be adjusted individually. The daily dose varies considerably and may range from 10 mg to 150 mg. It should take into account the concomitant analgesics and the ability to reduce the use of the latter.

In elderly patients, the initial dose is 10 mg/day. Then slowly, for about 10 days, the daily dose is increased to an optimum level which is 30–50 mg.

Children and adolescents

For obsessive-compulsive syndromes, the initial dose is 25 mg/day. During the first 2 weeks the dose was gradually increased, as tolerated, until a daily dose of 100 mg, or the calculated rate of 3 mg/kg body weight, depending on whether the dose is less. Over the next several weeks of dosage continuing to gradually increase until reaching a daily dose of 200 mg, or the calculated rate of 3 mg/kg body weight, depending on whether the dose is less.

When nocturnal enuresis initial daily dose of Anafranil for children aged 5–8 years is 20–30 mg; for 9–12 year olds - 25–50 mg; for children over 12 years - 25–75 mg. The use of higher doses indicated for patients who have no clinical effect complete after 1 week of treatment. Usually, all the daily dose administered in one go after dinner, but when involuntary urination noted in the early hours of the night, the dose prescribed Anafranil before - in 16 hours. After achieving the desired effect of treatment should be continued for 1–3 months, gradually reducing the dose of Anafranil.

Anafranil Overdose

Symptoms developing in overdose Anafranil, are similar to those described in cases of overdose of other tricyclic antidepressants. The main complications are violations of the activity of the heart and neurological disorders. Children welcome random drug at any dose should be considered as inside a very serious and threatening fatal event.

Symptoms usually appear within 4 hours after administration and reaches a maximum expression after 24 hours. Due depot (anticholinergic drug action), a prolonged half-life and hepato-enteric recycling of active substance, the time period during which the patient remains in the “risk zone” is 4–6 days.

CNS: drowsiness, stupor, coma, ataxia, restlessness, agitation, increased reflexes, muscle rigidity, horeoatetoidnye movement, convulsions. In addition, there may be manifestations of serotonin syndrome (fever, myoclonus, delirium, coma).

Cardio-vascular system: marked reduction in blood pressure, tachycardia, prolongation of the interval QT c, arrhythmia (including ventricular arrhythmias such as “pirouette”) breach of intracardiac conduction, shock, heart failure; in very rare cases - cardiac arrest.

Other: possible respiratory depression, cyanosis, vomiting, fever, mydriasis, sweating, oliguria or anuria.

Treatment: No specific antidote does not exist, the treatment is mainly symptomatic and supportive. If you suspect an overdose of Anafranil, especially in children, the patient should be hospitalized and closely monitored for a minimum of 72 hours.

If the patient is conscious, you should as soon as possible to gastric lavage or induce vomiting. If the patient is unconscious, before the start of gastric lavage for the prevention of aspiration should be performed tracheal intubation using a tube with a cuff; vomiting in this case do not cause. These measures are recommended in case of overdose has passed since 12 hours and even more, since anticholinergic effects Anafranil may slow gastric emptying. To slow the absorption of the drug is useful to use activated carbon.

Treatment is based on the application of modern methods of intensive therapy with constant monitoring of heart function, gas composition, and blood electrolytes, as well as on the application, if necessary urgent measures such as anticonvulsant therapy, mechanical ventilation and resuscitation techniques. Since then, as it was reported that physostigmine may cause severe bradycardia, asystole, and seizures, use of this drug for the treatment of overdose Anafranil is not recommended. Hemodialysis and peritoneal dialysis are not effective because clomipramine concentration in plasma is low.

Drug Interactions

Pharmacodynamic interaction

Anafranil can reduce or completely eliminate the antihypertensive effect guanethidine, betanidina, reserpine, clonidine and alpha-methyldopa. Therefore, in cases where both the reception Anafranil requires treatment of hypertension, it is necessary to use other classes of drugs (e.g., vasodilators and beta blockers).

Tricyclic antidepressants, including Anafranil may potentiate the effect of anticholinergic agents (eg, phenothiazines, antiparkinson drugs, atropine, biperiden, antihistamines) on the organ of vision, central nervous system, intestines and bladder.

Tricyclic antidepressants may potentiate the effects of ethanol and other agents having a depressing effect on the central nervous system (eg, barbiturates, benzodiazepines or anesthetic drugs).

Anafranil should not be administered for at least 2 weeks after discontinuation of MAO inhibitors because of the risk of such severe symptoms and conditions such as hypertensive crisis, increased body temperature, as well as the symptoms of serotonin syndrome: myoclonus, agitation, seizures, delirium and coma. The same rule should be followed in the event that an MAO inhibitor is administered after previous treatment of Anafranil. In any of these cases, the initial dose or Anafranil MAO inhibitors should be low, they should increase gradually under constant drug effects.

The existing experience shows that Anafranil may be appointed not earlier than 24 hours after discontinuation of MAO inhibitors type A reversible actions (such as moclobemide). However, if MAO inhibitor type A is assigned after the abolition of Anafranil, recess should be at least 2 weeks.

The combined use of Anafranil with selective serotonin reuptake inhibitors may lead to increased action on the serotonin system.

With simultaneous use of Anafranil with selective serotonin reuptake inhibitors or serotonin reuptake inhibitors and noradrenaline (norepinephrine), tricyclic antidepressants and lithium therapy may develop serotonin syndrome with symptoms such as fever, myoclonus, agitation, convulsions, delirium, and coma.

The appointment of fluoxetine is recommended to do a two-week break between the use of Anafranil and fluoxetine - finish fluoxetine to 2–3 weeks prior to initiation of therapy with Anafranil or assign fluoxetine 2–3 weeks after completion of treatment of Anafranil.

Anafranil may potentiate the cardiovascular system sympathomimetics (epinephrine, norepinephrine, isoprenaline, phenylephrine and ephedrine), including: and when these materials are part of local anesthetics.

Pharmacokinetic interactions

The active ingredient of the drug Anafranil - clomipramine - mainly excreted as metabolites. The main metabolic pathway - demethylation to the active metabolite of N-dezmethylclomipramine followed by hydroxylation and conjugation of N-dezmethylclomipramine with clomipramine. In demethylation involves several cytochromeP–450, mainly CYP3A4, CYP2C19 and CYP1A2. The elimination of two active components by hydroxylation is catalyzed by CYP2D6.

Co-administration with inhibitors of CYP2D6 isoenzyme may lead to increased concentrations of both active ingredients to three times the value of the phenotype in patients with rapid metaboliser debrisoquine/sparteine. In this case, the metabolism in these patients is reduced to the level typical for people with poor metabolizer phenotype.

It is assumed that co-administration with inhibitors of CYP1A2, CYP2C19 and CYP3A4 may lead to increased concentrations of clomipramine and lower concentrations of N-dezmethylclomipramine.

MAO inhibitors (eg moclobemide) are contraindicated when taking klomipamina because in vivo, they are potent inhibitors of CYP2D6.

Antiarrhythmic drugs (eg quinidine and propafenone) should not be used in conjunction with tricyclic antidepressants, since they are potent inhibitors of CYP2D6.

Selective serotonin reuptake inhibitors (such as fluoxetine, paroxetine, or sertraline) inhibit CYP2D6, other preparations of this group (e.g. fluvoxamine) also inhibit CYP1A2, CYP2C19, which may lead to an increase in the plasma concentration of clomipramine and development of relevant adverse effects. There was a 4-fold increase in the equilibrium concentration of clomipramine during coadministration with fluvoxamine (the concentration of N-dezmethylclomipramine decreased 2-fold).

The combined use of neuroleptics (eg phenothiazines) may increase the plasma concentrations of tricyclic antidepressants reduce seizure threshold and cause seizures. Combination with thioridazine may lead to the development of severe cardiac arrhythmias.

Combined use of histamine H2-receptor cimetidine (which is an inhibitor of some cytochromeP–450, including CYP2D6 and CYP3A4) may result in increased plasma concentrations of tricyclic antidepressants, and therefore requires a dose reduction of the latter.

There are no data confirming interaction between of Anafranil (25 mg/day) and oral contraceptives (15 or 30 mg of ethinyl estradiol/day) at constant reception latter. There is no evidence that estrogens are inhibitors of CYP2D6 - the main isoenzyme involved in the elimination of clomipramine, so there is no reason to expect their interaction. Although concomitant use of tricyclic antidepressant imipramine and estrogen in high doses (50 mg/d) in some cases reported worsening of side effects and enhancing the therapeutic effect of an antidepressant. It is not known whether these findings are significant in relation to the simultaneous use of clomipramine and estrogen in low doses. In joint use of tricyclic antidepressants and high doses of estrogen (50 mg/day) recommended monitoring therapeutic effect of antidepressants and, if necessary, correction mode.

Methylphenidate may promote increased concentrations of tricyclic antidepressants, possibly by inhibiting their metabolism. In a joint application of these drugs may increase the concentration of tricyclic antidepressants in the blood plasma, while you may need to decrease the dose of the latter.

Some tricyclic antidepressants may increase the anticoagulant effect of coumarins (eg, warfarin), possibly by inhibiting their metabolism (CYP2C9). There is no evidence to prove the ability to inhibit the metabolism of clomipramine anticoagulants (warfarin). However, when using this class of drugs is recommended monitoring plasma concentration of prothrombin.

Co-administration with drugs Anafranil - inducers of cytochromeP–450, especially CYP3A4, CYP2C19 and/or CYP1A2 may increase the metabolism and reduce the effectiveness of Anafranil.

Co-administration with drugs Anafranil - inducers of CYP3A and CYP2C, such as rifampicin or anticonvulsants (eg, barbiturates, carbamazepine, phenobarbital and phenytoin), may lead to a decrease in the concentration of clomipramine in plasma.

Known inducers of CYP1A2 (for example, nicotine/other components of cigarette smoke) lower concentrations of tricyclic antidepressants in the blood plasma. The equilibrium concentration of clomipramine cigarette smokers persons 2 times lower than that of non-smokers (the concentration of N-dezmethylclomipramine not changed).

Clomipramine, as in vivo, or in vitro, inhibits CYP2D6 (sparteine oxidation). Thus, clomipramine may increase the concentration of both of the drugs metabolized mainly involving CYP2D6, in patients with extensive metabolizer phenotype.

Pregnancy and lactation

Experience of using Anafranil in pregnancy is limited. Since there are anecdotal reports of a possible association between tricyclic antidepressants and impaired fetal growth, Anafranil should be avoided during pregnancy, except in cases where the expected effect of treatment of the mother clearly outweighs the potential risk to the fetus.

In cases where the tricyclic antidepressants used during pregnancy up until the birth, the newborn during the first few hours or days of developing the syndrome, which is manifested by shortness of breath, lethargy, colic, irritability, hypotension or hypertension, tremors, spastic phenomena or convulsions. To avoid the development of this syndrome Anafranil should be possible to gradually canceled at least 7 weeks prior to delivery.

Since the active ingredient of the drug is excreted in breast milk, you should either stop breastfeeding or gradually abolish Anafranil.

Anafranil Side effects

Adverse reactions are listed by frequency, beginning with the most common: occur very often (≥10%); often (≥1%, but <10%); sometimes (≥0.1%, but <1%); rarely (≥0.01%, but <0.1%); very rarely (<0.01%, including isolated cases).

CNS and peripheral nervous system. Mental status: very often - drowsiness, fatigue, restlessness, increased appetite; often - confusion, disorientation, hallucinations (especially in elderly patients and in patients with Parkinson’s disease), anxiety, agitation, insomnia, mania, hypomania state, aggression, memory impairment, depersonalization, increased depression, impaired concentration, insomnia, nightmares, yawning; sometimes - activation of psychotic symptoms. Neurological status: very often - dizziness, tremor, headache, myoclonus; often - delirium, speech disturbances, paresthesia, muscle weakness, increased muscle tone; sometimes - convulsions, ataxia; very rare - EEG changes, increased body temperature.

Effects due to the anticholinergic activity: very often - dry mouth, increased sweating, constipation, accommodation disturbances, blurred vision (“blurred vision”), voiding; often - flushing, mydriasis; very rare - glaucoma, urinary retention.

Cardio-vascular system: often - sinus tachycardia, palpitations, orthostatic hypotension, clinically insignificant changes in the ECG (eg, ST interval or tooth T) in patients without heart disease; sometimes - arrhythmias, increased blood pressure; very rarely - violation of intracardiac conduction (eg, expansion of the complex QRS, lengthening the interval QT, change the interval PQ, block bundle-branch block, ventricular tachycardia bidirectional fusiform/ventricular arrhythmias such as “pirouette” /), especially in patients with hypokalemia).

From the digestive system: very often - nausea; often - vomiting, abdominal discomfort, diarrhea, anorexia, increased transaminase levels; rarely - hepatitis with jaundice or without it.

Dermatological reactions: often - allergic skin reactions (rash, urticaria), photosensitivity, pruritus; very rare - edema (local or general), hair loss.

Part of the endocrine system and metabolism: very often - an increase in body weight, disturbances of libido and potency; often - galactorrhea, increase in the mammary glands; very rarely - a syndrome of inappropriate secretion of antidiuretic hormone.

Hypersensitivity reactions: rarely - allergic alveolitis (pneumonitis) with or without eosinophilia, systemic anaphylactic/anaphylactoid reactions, including hypotension.

Hematopoietic system: rarely - leukopenia, agranulocytosis, eosinophilia, thrombocytopenia, purpura.

From the senses: common - a violation of taste, tinnitus.

Other: after abrupt withdrawal or rapid dose reduction Anafranil often experience the following symptoms: nausea, vomiting, abdominal pain, diarrhea, insomnia, headache, irritability, anxiety.

The observed adverse events were usually mild and transient, are in the continuation of treatment or after dose reduction Anafranil. They do not always correlate with the concentration of the active drug substance in the blood plasma or its dose. Some adverse events such as general weakness, sleep disturbances, agitation, anxiety, constipation, dry mouth, it is often difficult to distinguish from depression.

In case of serious side effects from the nervous system or mental status Anafranil should be abolished.

The elderly are particularly susceptible to the action of Anafranil on the nervous system, cardiovascular system, and the effect of the drug on mental status, as well as anticholinergic effects Anafranil. Metabolism and excretion of drugs in this age may slow down, which leads to higher drug concentrations in blood plasma, even when used in high therapeutic doses.

Indications

Adults

The treatment of depressive states of different etiology, occurring with varying symptoms as endogenous, reactive, neurotic, organic, masked, involutional forms of depression; depression in patients with schizophrenia and psychopathy; depressive syndromes that occur in old age due to chronic pain or chronic physical illness; depressive disorders mood reactive, neurotic or psychopathic nature;

Obsessive-compulsive syndromes;

Chronic pain syndrome;

Phobias and panic attacks;

Cataplexy, accompanying narcolepsy.

Children and adolescents

Obsessive-compulsive syndromes;

Nocturnal enuresis (only in patients over the age of 5 years and subject to the exclusion of organic causes of disease).

Prior to initiating therapy with Anafranil nocturnal enuresis in children and adolescents should assess the value of the potential benefits and risks for the patient. Should consider the possibility of alternative therapy.

Currently not received sufficient evidence of efficacy and safety of clomipramine in children and adolescents for the treatment of depressive states of various etiology, occurring with varying symptoms, phobias and panic attacks, cataplexy accompanying narcolepsy and chronic pain. Therefore the use of Anafranil in children and adolescents (0–17 years) for these indications is not recommended.

Contraindications

Hypersensitivity to clomipramine and other ingredients, cross-hypersensitivity to tricyclic antidepressants from the group dibenzazepine;

Simultaneous use of MAO inhibitors, and the period of less than 14 days before and after use;

Simultaneous use of selective inhibitors of MAO-A reversible actions (such as moclobemide);

Recent myocardial infarction;

Congenital syndrome prolongation of the interval QT.

Do not use the drug during pregnancy and breastfeeding.

The drug is not recommended for use in children under the age of 5 years. Cautions

It is known that tricyclic antidepressants reduce seizure threshold, so Anafranil should be used with extreme caution in patients with epilepsy, as well as the presence of other predisposing to seizures of factors, such as traumatic brain injury of any etiology, the simultaneous use of antipsychotics during the period of refusal alcohol or drug withdrawal, with anticonvulsant properties (eg, benzodiazepines). It is believed that the occurrence of seizures while taking Anafranil depends on the dose of the drug. In this regard, should not exceed the recommended daily dose Anafranil.

Special care should be given to patients with Anafranil cardiovascular diseases, especially cardiovascular insufficiency, intracardiac conduction disturbances (eg, AV-blockade of I-III degree) or arrhythmias. In these patients, as well as in elderly patients, it is necessary to regularly monitor the performance of the heart and ECG.

Before therapy of Anafranil recommended to measure blood pressure, as in patients with orthostatic hypotension or lability of the cardiovascular system may be a sharp decline in blood pressure.

Because the drug has anticholinergic properties, it should be used with extreme caution in patients with a history there is evidence of increased intraocular pressure, angle-closure glaucoma or urinary retention (eg, due to diseases of the prostate gland).

Because of the anticholinergic actions characteristic of tricyclic antidepressants may reduce tearing and accumulation of mucus secretion, which can result in damage to the corneal epithelium in patients who use contact lenses.

Caution is needed in the treatment of tricyclic antidepressants in patients with severe liver disease, and in patients with tumors of the adrenal medulla (eg, pheochromocytoma, neuroblastoma), t. To., In this case, these drugs can provoke the development of hypertensive crisis.

It is known that in patients with cyclic affective disorders receiving tricyclic antidepressants, during the depressive phase may develop manic or hypomanic state. In such cases it may be necessary to decrease the dose Anafranil or its cancellation and antipsychotic therapy. After the relief of these conditions, if there are indications, treatment of Anafranil in low doses may be resumed.

In predisposed patients and elderly patients, tricyclic antidepressants can provoke the development of drug delirious psychosis, mainly at night. After discontinuation these disorders resolve within a few days.

Caution should be exercised when treating patients with hyperthyroidism, or receiving thyroid hormone drugs, which may have cardiotoxic effects.

Although changes in the level of white blood cells during treatment of Anafranil reported only in individual cases, it is recommended periodic study of peripheral blood and attention to symptoms such as fever and sore throat, especially in the first months of therapy or long-term use of the drug.

Caution is needed when using Anafranil in patients with chronic constipation. Tricyclic antidepressants may cause paralytic ileus, mainly in elderly patients or in patients who have to comply with bed rest.

In the application of Anafranil at doses higher than average therapeutic, or if the concentration of clomipramine in plasma exceeds the average therapeutic, there is a risk of QTc and QT c occurrence of ventricular tachycardia bidirectional spindle (ventricular arrhythmias such as “pirouette”). This is observed in the case of co-administration with selective serotonin reuptake inhibitors or serotonin reuptake inhibitors and norepinephrine. In this regard, it is necessary to avoid sharing clomipramine and preparations causing its cumulation. You should also avoid co-administration with drugs that cause lengthening of the interval QT c. Diuretics can lead to hypokalemia. Established that hypokalaemia is a risk factor for QT c interval prolongation and the occurrence of ventricular tachycardia bidirectional spindle (ventricular arrhythmias such as “pirouette”). Therefore, hypokalemia should be corrected before initiating therapy of Anafranil. Anafranil should be used with caution in conjunction with selective serotonin reuptake inhibitors or serotonin reuptake inhibitors and norepinephrine, as well as a diuretic.

Due to the risk of serotonin toxicity should follow the recommended dose and increase the dose with caution if Anafranil is used in conjunction with serotonergic drugs.

With simultaneous use of Anafranil with serotonergic drugs such as selective serotonin reuptake inhibitors, serotonin reuptake inhibitors and norepinephrine, tricyclic antidepressants or lithium, may develop serotonin syndrome with symptoms such as fever, myoclonus, agitation, convulsions, delirium, and coma. The appointment of fluoxetine, it is recommended to do a two-week break between the use of Anafranil and fluoxetine.

Many patients with panic disorder at baseline of Anafranil enhanced anxiety. Such a paradoxical increased anxiety is most pronounced in the first days of therapy and usually subsides within two weeks.

In patients with schizophrenia receiving tricyclic antidepressants, sometimes marked activation of psychosis.

In patients with liver disease is recommended periodic monitoring of liver enzymes.

Anafranil, as well as other tricyclic antidepressants administered in combination with electroconvulsive therapy only with careful medical supervision.

Severe depression peculiar risk of suicidal acts, which may persist until remission reliable. Patients with depression in adults and children, there may be increased depression and/or suicidal behavior or other psychiatric symptoms, regardless of whether they receive antidepressant medication or not. Antidepressants increased the risk of suicidal thoughts and suicidal behavior in short-term studies in children and adolescents with depression and other psychiatric disorders.

All patients taking Anafranil on any of the readings should be evaluated for clinical worsening, suicidal behavior and other psychiatric symptoms, especially in the initial phase of therapy or when changing the dose. These patients should be considered the possibility of changing therapy, including the possible removal of the drug, especially if such changes pronounced, appeared suddenly or have not been observed in patients initially.

Families and caregivers of patients (both children and adults) who take antidepressants for psychiatric or non-psychiatric indications, should be alerted about the need to monitor patients because of the risk of other psychiatric symptoms, including and suicidal behavior, and immediately report such symptoms to physicians.

When prescribing Anafranil should specify the minimum number of tablets to reduce the risk of overdose. It is necessary to observe adequate regimen.

There is evidence that in patients receiving Anafranil had fewer deaths due to overdose, than in patients receiving other tricyclic antidepressants.

Prior to the general or local anesthesia, the anesthetist should be warned that the patient is taking Anafranil.

Reported an increase in the incidence of dental caries in long-term treatment with tricyclic antidepressants. Therefore, in the case of long-term therapy of Anafranil recommended regular inspection of the patient’s dentist.

Diuretics can lead to hypokalaemia, in which the risk of QTc and QT c fusiform appearance bidirectional ventricular tachycardia (type “pirouette”). Prior to initiating therapy of Anafranil should be the correction of hypokalemia.

Avoid abrupt withdrawal Anafranil since This may lead to side reactions. If you decide to discontinue treatment, medication should be withdrawn gradually, as soon as it allows the clinical situation. Please keep in mind that the abrupt withdrawal of the drug may lead to the development of certain symptoms.

Film-coated tablets, 25 mg contain lactose and sucrose. Patients with rare hereditary diseases, such as galactose and fructose intolerance, severe lactase deficiency, sucrase-izomaltaznaya deficiency or glucose-galactose malabsorption should not take Anafranil tablets, coated tablets.

Keep in mind that alcohol may enhance the adverse effects of the CNS, such as blurred vision, drowsiness.

Use in Pediatrics

Experience with Anafranil in children under the age of 5 years are not available, it is not recommended to use the drug in children of this age group.

Effects on ability to drive vehicles and management mechanisms

Patients who during treatment with Anafranil arise drowsiness and other CNS side effects (including blurred vision), you should not drive a car, operate machinery, or engage in other activities that require attention and fast reaction.

Anafranil Review

Most excellent antidepressant, Anafranil inexpensive (packing - 30 tablets). I am a second time, "I go" to this drug, the first time "enough" for three years plus get rid of panic attacks (PA). I take three tablets at night (started with a ten-day course of injections).
From Side effects - tachycardia heart rate of 100-120 beats / min, blood pressure fluctuations (100-135 / 60-90). The first "approach" has been gaining weight (10 kg for 3 months), now weight gain absolutely not.

Anafranil decreased anxiety, a desire to do something, and all this after the third week of admission in tablet form, excluding the ten-day course of injections. I know people who for several years, "sit" on Anafranil and feel great.

Familiarity with Anafranil occurred in the hospital Alekseeva, where I got my horrible panic attacks. The first appointment was with no side effects, I am very easy on him, "the village" and as he became a great help. A year has passed without a panic attack treatment Anafranil was six months, in addition to him were antipsychotics, tranquilizers and correctors naturally. full nabor.all inclusive so to speak. When aggravation happened, I again began to take Anafranil. but something went wrong. the first tablet I started sausage as if I used some powerful drug. appearance corresponded to that feeling. Huge pupils, trembling hands, a lot of energy from a well, too bad, you do not know where to go, a terrible panic, tachycardia, and a state of the week for sure! A week side effects go and begins to act Anafranil. a month of reception you can feel the effect of this ancient antidepressant. good mood, there is no fear, a lot of positive energy, a lot of strength, up early, good night's sleep, a great performance. The drug actually helps, but to sustain these side effecrs during the week, or even two (I saw it once 5 courses and side effects was not only the first time, other times - horrible) is very difficult. That is, how did I- week at home, in bed, on half a tablet a day, then you can get out of bed. a week later on the whole, and then the doctor ordered, I drank 2 tablets per day. This is the only antidepressant that helped me (a lot of different generations of antidepressants has been tried), but had to abandon it, strength to endure the first week no longer.

Anafranil (Clomipramine) ampoules - Instructions for Use, Dosage, Side Effects, Reviews

Synonyms: Anafranil, Atenual, Ausentron, Clomip, Clomipramin, Clonil, Depnil, Ocifril, Ocifril-XR, Praminex, Syconil, Anafranil, Anafranil retard, Anafranil SR, Anafril, Apo-Clomipramine, Chemmart Clomipramine, Clofranil, Clomi, Clomicalm (veterinary use), Clomidep, Clomine, Clomipramin-CT, Clomipramine (chlorhydrate) Mylan, Clomipramine HCl Actavis, Clomipramine HCl CF, Clomipramine HCl Mylan, Clomipramine HCl PCH, Clomipramine HCl ratiopharm, Clomipramine HCl Sandoz, Clomipramine Hydrochloride, Clomipramine Mylan, Clomipramine Sandoz, Clomipramine Teva, Clomipramine, Clomipraminhydrochlorid 2care4, Clomipramin-neuraxpharm, Clomipramin-neuraxpharm retard, Clomipramin-ratiopharm, Clopran, Clowin, CO Clomipramine, Cosinic, Equinorm, For-You, GenRX Clomipramine, Gromin, Hydiphen, Klomipramin Merck NM, Klomipramin Mylan, Klomipramin, Maronil, Pashin, Placil, Promil, Terry White Chemists Clomipramine, Trianil.

Active substance: Clomipramine.

What is clomipramine?

Clomipramine is a tricyclic antidepressant. It affects chemicals in the brain that may be unbalanced.

Clomipramine is used to treat symptoms of obsessive-compulsive disorder (OCD) such as recurrent thoughts or feelings and repetitive actions.

What is the most important information I should know about clomipramine?

Do not use this medicine if you have used an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine.

Some young people have thoughts about suicide when first taking an antidepressant. Stay alert to changes in your mood or symptoms.

ATC - N06AA04 clomipramine

Pharmacological group - Antidepressants.

Nosological classification (ICD–10)

F32 Depressive episode;

F40.0 Agoraphobia;

F42 Obsessive-compulsive disorder;

F44 Dissociative [conversion] disorders;

G47.4 Narcolepsy and cataplexy;

R32 Urinary incontinence, unspecified;

R52.2 Other constant pain.

Pharmacological action

Anafranil is a tricyclic antidepressant, inhibits the reuptake of norepinephrine and serotonin (a non-selective monoamine reuptake inhibitors). It is believed that the action is carried Anafranil due to its ability to inhibit neuronal noradrenaline (NA) and serotonin (5-HT) released into the synaptic cleft, and the most important is the inhibition of serotonin reuptake.

Anafranil furthermore inherent in a wide variety of other pharmacological activities: alpha 1-adrenolytic, anticholinergic, antihistaminic and anti-serotoninergic (blockade of 5-HT-receptors).

Anafranil works on the depressive syndrome as a whole, including its typical manifestations as psychomotor retardation, depressed mood and anxiety. The clinical effect is usually observed after 2–3 weeks of treatment.

In addition, Anafranil has a specific (different from his antidepressive effect) effect in obsessive-compulsive disorders and chronic pain syndromes.

Pharmacokinetics

Absorption

After the IM clomipramine absorbed completely. When you repeat the IM or IM introduction of Anafranil at a dose of 50–150 mg/day. equilibrium concentration is reached on the second week of treatment. The values of the equilibrium concentration of clomipramine ranges from less than 15 to 447 ng/ml, and the active metabolite N-desmmethylomipramine - from less than 15 to 669 ng/ml.

Distribution

Communication with clomipramine plasma proteins is 97.6%. The apparent Vd is about 12–17 L/kg of body weight. Clomipramine concentration in the cerebrospinal fluid are about 2% of its concentration in blood plasma. Clomipramine penetrates into breast milk, where it is determined at concentrations similar to the concentrations in the blood plasma.

Metabolism

Clomipramine is metabolized mainly by demethylation to the active metabolite N-decmetilklomipramina. In this reaction involves several cytochromeP–450 isozymes, but mainly CYP3A4, CYP2C19 and CYP1A2. Clomipramine and N-dezmethylclomipramine hydroxylated to 8 hydroxyclomipramine and 8-hydroxy-N-dezmethylclomipramine. Activity of hydroxy-metabolite in vivo is not defined. Clomipramine also hydroxylated in position 2; N-dezmethylclomipramine can be further demethylated to dezmethylclomipramine. 2 and 8-hydroxy metabolites are excreted predominantly in the urine as glucuronides. The elimination of the two active components - clomipramine and N-dezmethylclomipramine by forming 2 and 8 hydroxyclomipramine catalyzed CYP2D6.

Excretion

After the IM and IV the final T 1/2 Anafranil clomipramine is an average of 25 hours (range of variation from 20 to 40 h) and 18 h, respectively.

Approximately 2/3 of a single dose of clomipramine is output as the water-soluble conjugates in urine and approximately one third dose - feces. Unchanged in the urine output of about 2% of the dose of clomipramine and about 0.5% dezmethylclomipramine.

Pharmacokinetics in selected patients

In elderly patients, due to the reduction of metabolic rate in the plasma concentration of clomipramine higher than in younger patients, regardless of the dose used Anafranil. Data on the effect of functional disorders of the liver and kidneys on the pharmacokinetic parameters of clomipramine has not yet been received.

Anafranil clomipramine Dosage

Dosing regimen and route of administration of the drug is determined individually, taking into account the patient’s condition. Care should be taken when increasing the dose in elderly patients and adolescents, which are generally more sensitive to Anafranil than those of intermediate age groups.

IM injection

Begin treatment with the administration of 25–50 mg (1–2 ampoules content), and then increase the daily dose by 25 mg (1 vial) until the daily dose of 100–150 mg (4–6 capsules). After be noted improvement by injection is gradually reduced by substituting their supportive care with oral drug forms.

IV Infusion

Treatment starts with IV drip 50–75 mg (2–3 ampoules content) 1 time per day. To prepare the infusion solution using 250–500 ml isotonic sodium chloride or glucose solution; infusion duration of 1.5–3 h. During infusion, careful observation of the patient for early detection of possible adverse reactions. Particular attention should be given to control blood pressure, as can develop orthostatic hypotension. Upon reaching a distinct improvement Anafranil introduced IV for an additional 3–5 days. Then, to maintain the achieved effect on the admission of the drug inside; 2 tablets of 25 mg is usually equivalent Anafranil 1 ampoule containing 25 mg. With a view to the gradual transition from fluid therapy to the supporting oral admission of the drug may be first to transfer the patient to the IM introduction. The maximum therapeutic dose is 150 mg per day.

Anafranil Overdose

No cases of overdose Anafranil in the form of a solution for injections have been reported. Below is information about overdose Anafranil if swallowed. Symptoms developing in overdose Anafranil, are similar to those described in cases of overdose of other tricyclic antidepressants. The main complications are disorders of the heart and neurological disorders. Children casual acceptance of any dose of the drug inside should be regarded as a very serious and threatening fatal event.

Symptoms

Symptoms usually appear within 4 hours after administration and reaches a maximum expression after 24 hours. Due depot (anticholinergic drug action), a prolonged half-life and hepato-enteric recycling of active substance, the time period during which the patient remains in the “risk zone” is 4–6 days.

Following symptoms may occur.

The central nervous system: drowsiness, stupor, coma, ataxia, restlessness, agitation, increased reflexes, muscle rigidity, horeoatetoidnye movement, convulsions. In addition, there may be manifestations of serotonin syndrome (fever, myoclonus, delirium, coma).

Cardio-vascular system: marked reduction in blood pressure, tachycardia, prolongation of QTc-interval (interval corrected QT), arrhythmia (including “torsade de points”) violations of intracardiac conduction, shock, heart failure; in very rare cases - cardiac arrest. In addition, possible respiratory depression, cyanosis, vomiting, fever, mydriasis, sweating, oliguria or anuria.

Treatment

No specific antidote, treatment is primarily symptomatic and supportive. If you suspect an overdose of Anafranil, especially in the casual taking the drug in children, the patient should be hospitalized and closely monitored for a minimum of 72 hours.

In case of accidental ingestion of a solution for IV and IM, if the patient is conscious, you should as soon as possible to gastric lavage or induce vomiting. If the patient is unconscious, before the start of gastric lavage should be for the prevention of aspiration spend intubation using a tube with a cuff; vomiting in this case do not cause. These measures are recommended even if since overdosing passed 12 hours or more, as anticholinergic effects Anafranil can slow gastric emptying. To reduce the absorption of the drug useful for the use of activated carbon.

Treatment is based on the application of modern methods of intensive therapy with constant monitoring of cardiac functions, gas composition, and blood electrolytes, as well as on the application, if necessary urgent measures such as anticonvulsant therapy, mechanical ventilation and resuscitation techniques. Since then, as it was reported that physostigmine may cause severe bradycardia, asystole, and seizures, use of this drug for the treatment of overdose Anafranil is not recommended. Hemodialysis and peritoneal dialysis are not effective since concentrations in plasma clomipramine low.

Anafranil (clomipramine) Drug Interactions

Pharmacodynamic interaction type

Adrenergic blockers of neuronal transmission. Anafranil may reduce or completely eliminate the antihypertensive effects of guanethidine, betanidina, reserpine, clonidine and alfametildopy. Therefore, in cases where both the reception Anafranil requires treatment of hypertension, it is necessary to use other classes of drugs (e.g., vasodilators and beta blockers).

Anticholinergics. Tricyclic antidepressants may increase the effects of anticholinergic agents (eg, phenothiazines, antiparkinson drugs, atropine, biperiden, aitigistaminnyh drugs) on the organ of vision, central nervous system, intestines and bladder.

CNS depressants. Tricyclic antidepressants may increase the effects of alcohol and other agents having a depressing effect on the central nervous system (eg, barbiturates, benzodiazepines or anesthetic drugs). Keep in mind that alcohol may enhance the adverse effects of the CNS, such as blurred vision, drowsiness, and others.

MAO inhibitors. Anafranil should not be prescribed for at least 2 weeks after discontinuation of MAO inhibitors because of the risk of such severe symptoms and conditions such as hypertensive crisis, increased body temperature, as well as the symptoms of serotonin syndrome: myoclonus, agitation, seizures, delirium and coma. The same rule should be followed in the event that an MAO inhibitor is administered after previous treatment of Anafranil. In any of these cases, the initial dose or Anafranil MAO inhibitors should be low, they should increase gradually under constant drug effects.

The existing experience shows that Anafranil may be appointed not earlier than 24 hours after discontinuation of MAO inhibitors-A reversible action, such as moclobemide. However, if MAO-B inhibitor A reversible after discontinuation of Anafranil is assigned, the duration of the break should be at least 2 weeks.

Selective serotonin reuptake inhibitors. Combined use Anafranil with these funds may lead to increased action on the serotonin system.

Serotonergic agents. Anafranil With simultaneous use with selective serotonin reuptake inhibitors or serotonin reuptake inhibitors and norepinephrine, tricyclic antidepressants and lithium therapy may develop serotonin syndrome with symptoms such as fever, myoclonus, agitation, convulsions, delirium, and coma.

The appointment of fluoxetine is recommended to do a two-week break between the use of Anafranil and fluoxetine - finish fluoxetine to 2–3 weeks prior to initiation of therapy with Anafranil or assign fluoxetine 2–3 weeks after completion of treatment of Anafranil.

Sympathomimetic agents. Anafranil may potentiate the cardiovascular system of epinephrine, norepinephrine, isoprenaline, phenylephrine and ephedrine (including when these substances are part of local anesthetics).

Pharmacokinetic interaction type

The active ingredient of the drug Anafranil - clomipramine - mainly excreted as metabolites. The main metabolic pathway - demethylation to the active metabolite N-desmmethylomipramine followed by hydroxylation and conjugation of N-desmmethylomipramine with clomipramine. In demethylation involves several isoforms of cytochrome P450, mainly CYP3A4, CYP2C19 and CYP1A2. The elimination of two active components by hydroxylation is catalyzed by CYP2D6.

Co-administration with inhibitors of CYP2D6 isoform may lead to increased concentrations of both active ingredients to three times the value of the phenotype in patients with rapid acetylator debrisoquine/sparteine. In this case, the metabolism in these patients is reduced to the level typical for people with slow acetylators phenotype. It is assumed that co-administration with inhibitors of the isoforms CYP1A2, CYP2C19 and CYP3A4 may lead to increased concentrations of clomipramine and lower concentrations of N-desmmethylomipramine.

MAO inhibitors (such as moclobemide) contraindicated in clomipramine, as in vivo, they are potent inhibitors of CYP2D6.

Antiarrhythmics (e.g. quinidine and propafenone) should not be used in conjunction with tricyclic antidepressants, since they are potent inhibitors of CYP2D6.

Selective serotonin reuptake inhibitors (such as fluoxetine, paroxetine, or sertraline) inhibit CYP2D6, other preparations of this group (e.g. fluvoxamine) also inhibit CYP1A2, CYP2C19, which may lead to an increase in the plasma concentration of clomipramine and development of relevant adverse effects. There was a 4-fold increase in the equilibrium concentration of clomipramine during coadministration with fluvoxamine (the concentration of N-desmmethylomipramine decreased 2-fold).

The combined use of neuroleptics (eg phenothiazines) may increase the plasma concentrations of tricyclic antidepressants reduce seizure threshold and cause seizures. Combination with thioridazine may lead to the development of severe cardiac arrhythmias.

Combined use of histamine (H2) receptor cimetidine (which is an inhibitor of certain isoforms of cytochrome P450, including CYP2D6 and CYP3A4) can lead to increased plasma concentrations of tricyclic antidepressants in connection with what is required a dose reduction of the latter.

There is evidence supporting the interaction between Anafranil (at a dose of 25 mg per day.) And oral contraceptives (15 or 30 mcg ethinyl estradiol d.) At constant reception latter. There is no evidence that estrogens are inhibitors of CYP2D6 - the main enzyme involved in the elimination of clomipramine, so there is no reason to expect their interaction. Although, while applying the tricyclic antidepressant imipramine and estrogens at high doses (50 mcg day.), In some cases reported worsening of side effects and enhancing the therapeutic effect of the antidepressant. It is not known whether these findings are significant in relation to the simultaneous use of clomipramine and estrogen in low doses. In joint use of tricyclic antidepressans and estrogens at high doses (50 ug per day). Recommended to monitor therapeutic effect of antidepressants, and if necessary, correction mode.

Methylphenidate (Ritalin) may contribute to increased concentrations of tricyclic antidepressants, possibly through inhibition of their metabolism. In a joint application of these drugs may increase the concentration of tricyclic antidepressants in the blood plasma, while it may be necessary to reduce the dose of the latter.

Some tricyclic antidepressants may increase the anticoagulant effect of coumarins (eg, warfarin), possibly by inhibiting their metabolism (CYP2C9). There is no evidence to prove the ability to inhibit the metabolism of clomipramine anticoagulants (warfarin). However, when using this class of drugs is recommended monitoring plasma concentration of prothrombin.

Co-administration with drugs Anafranil - inducers of cytochrome P450, especially CYP3A4, CYP2C19 and/or CYP1A2 may increase the metabolism and reduce the effectiveness of Anafranil.

Co-administration with drugs Anafranil - inducers CYP3Ai CYP2C, such as rifampicin or anticonvulsants drugs (such as barbiturates, carbamazepine, phenobarbital and phenytoin), may lead to a decrease in the concentration of clomipramine in plasma.

Known inducers CYP1A2 (for example, nicotine/other components of cigarette smoke) lower concentrations of tricyclic antidepressants in the blood plasma. The equilibrium concentration of clomipramine cigarette smokers persons 2 times lower than that of non-smokers (the concentration of N-desmmethylomipramine not changed).

Clomipramine is in vivo, or in vitro (Ki = 2.2 microM) inhibits CYP2D6 (sparteine oxidation). Thus, clomipramine may increase the concentration of the drugs at the same time, metabolized mainly involving CYP2D6, in patients with rapid acetylator phenotype.

Pharmaceutical incompatibility. Injection incompatible with sodium Voltaren (diclofenac sodium) injection.

Pregnancy and lactation

Experience of using Anafranil in pregnancy is limited. Since there are anecdotal reports of a possible association between tricyclic antidepressants and impaired fetal growth, Anafranil should be avoided during pregnancy, unless the expected benefit to the mother clearly outweighs the potential risk to the fetus.

In cases where the mother was taking tricyclic antidepressants during pregnancy up until the birth, the newborn during the first few hours or days of life developed the syndrome, which is manifested by shortness of breath, lethargy, intestinal colic, increased nervous excitability, a marked increase or a marked reduction in blood pressure, tremor, spastic phenomena or convulsions. To avoid the development of this syndrome, Anafranil should, if possible, gradually cancel at least 7 weeks prior to delivery.

Since the active ingredient of the drug passes into breast milk, you should either stop breastfeeding or gradually abolish Anafranil.

Anafranil (clomipramine) Side effects

The observed adverse events were usually mild and transient, are in the continuation of treatment or after dose reduction Anafranil. They do not always correlate with the concentration of the active substance in blood plasma or a dose of the drug. Some adverse effects such as fatigue, sleep disturbances, agitation, anxiety, constipation, dry mouth, it is often difficult to distinguish from depression. In the case of serious reactions in the nervous system or mental status Anafranil should be abolished.

The elderly are particularly susceptible to the action of Anafranil on the nervous system, cardiovascular system, and the effect of the drug on mental status, as well as anticholinergic effects Anafranil. Metabolism and excretion of drugs in this age may slow down, resulting in increased drug concentration in blood plasma when using therapeutic doses.

Adverse reactions are listed by frequency, beginning with the most common: occur “very often” - = 10.1, “often” - = 1/100 to <1/10, “sometimes” - = 1/1000 to <1/100, “rarely” - = 1/10000- <1/1000, “very rare” - <1/10000, including individual cases.

Mental disorders: very often - drowsiness, fatigue, restlessness, increased appetite; often -sputannost of consciousness, disorientation, hallucinations (especially in elderly patients and in patients with Parkinson’s disease), anxiety until agitation, sleep disorders, compulsive disorders, aggression, memory impairment, depersonalization, depressed mood, impaired concentration, insomnia, night nightmares, yawning, delirium; sometimes - activation of psychotic symptoms.

Of the central and peripheral nervous system: very often - dizziness, tremor, headache, myoclonus; often - a speech disorder, paresthesia, muscle weakness, increased muscle tone; sometimes - convulsions, ataxia; very rare - changes in the electroencephalogram, increased body temperature, and neuroleptic malignant syndrome.

Anticholinergic effects: very often - dry mouth, increased sweating, constipation, accommodation disturbances, blurred vision (“blurred vision”), voiding; often - flushing, mydriasis; very rare - glaucoma, urinary retention.

Cardio-vascular system: often - sinus tachycardia, palpitations, orthostatic hypotension, clinically insignificant changes in the ECG (eg, ST interval or T wave) in patients without heart disease; sometimes - arrhythmias, increased blood pressure; very rarely - violation of intracardiac conduction (eg, expansion of the complex QRS, lengthening the interval QT, change the interval PQ, block bundle-branch block, ventricular tachycardia of “feasting» (”torsade des pointes"), especially in patients with hypokalemia).

From the digestive system: very often - nausea; often - vomiting, abdominal discomfort, diarrhea, anorexia.

On the part of the hepatobiliary system: often - transaminase elevation; rarely - hepatitis with jaundice or without it.

Dermatological reactions: often allergic skin reactions (rash, urticaria), photosensitivity, pruritus; very rare - edema (local or general), hair loss, local reactions at/in the introduction (thrombophlebitis, lymphangitis, burning sensation, allergic skin reactions).

Part of the endocrine system and metabolism: very often - an increase in body weight, disturbances of libido and potency; often - galactorrhea, increase in the mammary glands; very rarely - a syndrome of inappropriate secretion of antidiuretic hormone.

Hypersensitivity reactions: rarely - allergic alveolitis (pneumonitis) with or without eosinophilia, systemic anaphylactic/anaphylactoid reactions, including hypotension.

Hematopoietic system: rarely - leukopenia, agranulocytosis, eosinophilia, thrombocytopenia, purpura.

From the senses: common - a violation of taste, tinnitus.

Withdrawal syndrome: after the sudden cancellation or rapid dose reduction Anafranil often experience the following symptoms: nausea, vomiting, abdominal pain, diarrhea, insomnia, headache, irritability, anxiety.

Indications

Treatment of depressive states of various etiologies that occur with different symptoms:

Endogenous, reactive, neurotic, organic, masked, involutional forms of depression;

Depression in patients with schizophrenia and psychopathy;

Depressive syndromes that occur in old age due to chronic pain or chronic physical illness;

Depressive mood disorders reactive, neurotic or psychopathic nature.

Obsessive-compulsive syndromes.

Phobia.

Cataplexy, accompanying narcolepsy.

Chronic pain syndromes.

Contraindications

Increased sensitivity to clomipramine or any other ingredients of the formulation, the cross-hypersensitivity to tricyclic antidepressants from the dibenzazepine group.

Simultaneous use of inhibitors of monoamine oxidase (MAO) as well as the period at least 14 days before and after their application. Contraindicated as concurrent use of selective inhibitors of MAO-A reversible action, such as moclobemide.

Recent myocardial infarction.

Congenital syndrome prolongation QT-interval.

Do not use the drug during pregnancy and breastfeeding. The drug is not recommended for use in children and adolescents.

Precautions

It is known that tricyclic antidepressants reduce seizure threshold, so Anafranil should be used with extreme caution in patients with epilepsy, as well as the presence of other predisposing to seizures factors, such as traumatic brain injury of various etiologies, the simultaneous use of antipsychotics during the period of refusal alcohol or drug withdrawal, with anticonvulsant properties (eg, benzodiazepines). It is believed that the occurrence of seizures against application Anafranil dose-dependent. In this regard, should not exceed the recommended daily dose Anafranil. Special care should be given to patients with Anafranil cardiovascular diseases, especially cardiovascular insufficiency, intracardiac conduction disturbances (eg, atrioventricular block I-III degree) or arrhythmias. In these patients, as well as in elderly patients, it is necessary to regularly monitor the performance of the heart and ECG.

Before therapy of Anafranil recommended to measure blood pressure, as in patients with orthostatic hypotension or lability of the cardiovascular system may be a sharp decline in blood pressure.

Because the drug has anticholinergic properties, it should be used with extreme caution in patients with a history there is evidence of increased intraocular pressure, angle-closure glaucoma or urinary retention (eg, due to diseases of the prostate gland).

Because of the anticholinergic actions characteristic of tricyclic antidepressants may reduce tearing and accumulation of mucus secretion, which can result in damage to the corneal epithelium in patients who use contact lenses.

Caution is needed in the treatment of tricyclic antidepressants in patients with severe liver disease, and in patients with tumors of the adrenal medulla (eg, pheochromocytoma, neuroblastoma), as in this case, these drugs can provoke the development of hypertensive crisis. It is known that in patients with cyclic affective disorders receiving tricyclic antidepressants, during the depressive phase of manic disorders may develop. In such cases it may be necessary to decrease the dose Anafranil or its cancellation and antipsychotic therapy. After the relief of these conditions, if there are indications, treatment of Anafranil in low doses may be resumed.

When parenteral administration Anafranil reported some cases of anaphylactic shock. Therefore, by intravenous administration of the drug, caution is necessary.

Caution should be exercised when treating patients with hyperthyroidism, or receiving thyroid hormone drugs, which may have cardiotoxic effects.

Although changes in the level of white blood cells during treatment of Anafranil reported only in individual cases, it is recommended periodic study of peripheral blood and attention to symptoms such as fever and sore throat, especially in the first months of therapy or long-term use of the drug.

Caution is needed when using Anafranil in patients with chronic constipation. Tricyclic antidepressants may cause paralytic ileus, mainly in elderly patients or in patients who have to comply with bed rest.

Cautions

Before the start of drug therapy should be eliminated hypokalemia. When applying Anafranil at doses exceeding the therapeutic medium, or if the plasma concentration of clomipramine than average therapeutic, there is a risk of elongation QTc-interval and the occurrence of ventricular tachycardia type “piruet» (”torsade des pointes“). This is observed in the case of co-administration with selective serotonin reuptake inhibitors or serotonin reuptake inhibitors and norepinephrine. In this regard, it is necessary to avoid coadministration klomiiramina and preparations causing its cumulation. You should also avoid co-administration with drugs that cause QTc-interval prolongation. Established that hypokalaemia is a risk factor for QTc-interval prolongation and the occurrence of ventricular tachycardia of the ”feast“ (”torsade des pointes"). Therefore, hypokalemia should be corrected before initiating therapy of Anafranil.

Because of the risk of QTc prolongation and development of serotonin syndrome should follow the recommended dose and increase the dose with caution when coadministered with drugs that prolong the interval QT, and serotonergic drugs. With simultaneous use of Anafranil with serotonergic drugs such as selective serotonin reuptake inhibitors, serotonin reuptake inhibitors and norepinephrine, tricyclic antidepressants or lithium, may develop serotonin syndrome with symptoms such as fever, myoclonus, agitation, convulsions, delirium and coma. The appointment of fluoxetine, it is recommended to do a two-week break between the use of Anafranil and fluoxetine.

Many patients with panic disorder at baseline of Anafranil enhanced anxiety. Such a paradoxical increased anxiety is most pronounced in the first days of therapy and usually subsides within two weeks.

In patients with liver disease is recommended periodic monitoring of liver enzymes.

Anafranil, as well as other tricyclic antidepressants administered in combination with electroconvulsive therapy only with careful medical supervision.

In predisposed patients and elderly patients, tricyclic antidepressants can provoke the development of drug delirious psychosis, mainly at night. After discontinuation these disorders resolve within a few days.

When use of tricyclic antidepressants in patients with schizophrenia sometimes marked activation of psychosis. Severe depression peculiar risk of suicidal acts, which may persist until remission reliable. Patients with depression in adults and children, there may be increased depression and/or suicidal behavior or other psychiatric syndromes, regardless of whether they receive antidepressant medication or not. Antidepressants increased the risk of suicidal thoughts and suicidal behavior in short-term studies in children and adolescents with depression and other mental illnesses. All patients taking Anafranil on any of the readings should be evaluated for clinical worsening, suicidal behavior and other psychiatric syndromes, especially in the initial phase of therapy or when changing dose. These patients should be considered the possibility of changing therapy, including the possible removal of the drug, especially if such changes pronounced, appeared suddenly and were not observed in the patient’s baseline.

Families and caregivers of patients (both children and adults) who take antidepressants for mental or nepsihicheskim indications, should be alerted about the need to monitor patients because of the risk of other psychiatric syndromes, including suicidal behavior, and immediately report such symptoms of the attending physicians. There is evidence that in patients receiving Anafranil had fewer deaths due to overdose, than in patients receiving other tricyclic antidepressants.

Prior to the general or local anesthesia, the anesthetist should be warned that the patient is taking Anafranil. Reported an increase in the incidence of dental caries in long-term treatment with tricyclic antidepressants. Therefore, in the case of long-term therapy of Anafranil recommended regular inspection of the patient’s dentist.

Diuretics can lead to hypokalaemia, in which an increased risk of QTc-interval prolongation and the occurrence of ventricular tachycardia of the “feast» (”torsade des pointes"). Prior to initiating therapy of Anafranil correction must be made hy.

Avoid abrupt withdrawal Anafranil, as it may lead to side reactions. If you decide to discontinue treatment, medication should be withdrawn gradually, as soon as it allows the clinical situation. Please keep in mind that the abrupt withdrawal of the drug may lead to the development of certain withdrawal symptoms.

Data on the effect of long-term treatment of Anafranil on growth, development, cognitive function and behavior in children and adolescents younger than 18 years is not.

Effects on ability to drive vehicles and/or work with machinery. If you experience during treatment with Anafranil drowsiness, blurred vision and other disorders of the nervous system, patients should relinquish control of vehicles and operate machinery, as well as to perform other activities that require greater attention and quick response.

Anafranil (clomipramine) Reviews

I want to share my impressions from taking this drug. Anafranil - tricyclic antidepressant, the active ingredient Clomipramine; I was appointed in connection with the panic attacks and anxiety-depressive disorder. I note that the attacks were very strong emotionally, and then they always remained an unpleasant aftertaste in the form of causeless anxiety and fear. In general, life was impossible, even from home could not get out. Yes, and the house could not be safely, because fear and foreboding that now something terrible happens, do not let go for a minute.
As a result, I had to take this drug. Looking at the instructions in it, I immediately drew attention to the huge number of side effects. And many of them appeared immediately in the first days of admission. I describe what exactly was I:
- The instructions stated that at Pa while taking Anafranil anxiety for the first time can be enhanced - and it was, but only for the first day.
- In a couple of weeks appetite. Even thinner per kg, although I did not need.
- Month 4 forgot about sexual desires.
- Month been low blood pressure, tachycardia
- Dilated pupils (mydriasis), too, a certain number of weeks.
More than anything unpleasant from side effects with me did not happen, despite the fact that, according to the instructions of Anafranil can almost throw the skates.
Now for the therapeutic effect. For me personally, it is very, very good. I must say - not manifested at once (one week approximately) and gradually. Gradually it went anxiety, improved mood, and very significantly increased efficiency. There was a feeling that I am re-learning to have fun and enjoy life. And, most importantly, panic attacks were no more. At all. Not for the reception, or after, or now, and I hope that there will be more! Of course, I mentally customizable and soothed, trying to convince himself that the panic attack is a simple reaction of the body, and that's okay with me is not going to happen. Still a major role in facilitating my condition is played Anafranil. At the moment, already 1-1,5g not take anything, I feel good.

This drug pulled me out of the grave condition. When life was just hell. Without much hope began to take 1 tablet. As a result, the dose reached 3 tablets, and only then felt the effect. Fear, panic and depression is gone. Wait effect accounted for about two months. Prior to this, only aggravation and side effects. But in the end Anafranil grateful for the help. The drug is an old, 70-ies. Lots of side effects and carries uneasy. It may give weight gain. Having moved to the effect and one tablet which is easier tolerated. A dose of 75 mg is very heavy. If you want to take this drug, tune in long-term treatment, at least a month.

For family reasons I have for a long time remained under stress. When applied to the doctors, I already had a deep depression. The doctor took me very well Anafranil and the dose of application. After 10 droppers turned me on pills. I accept for a long time and feel great.

Amitriptyline - Instructions for Use, Dosage, Side Effects, Reviews

International Nonproprietary Name (INN): Amitriptyline

Pharmaceutic group: Antidepressants

Chemical Name: 3- (10,11-dihydro-5H-dibenz [a, d] cyclohepten-5-ylidene) -N, N-dimethylpropan-1-amine hydrochloride

Presentation: Amitriptyline Tablets 10 mg n50 or 25 mg n50.

Synonyms: ADTzimaia, Amiline, Amiplin, Amitone, Amitrac, Amitrac-CZ (Amitriptyline and Chlordiazepoxide), Amitrip, Amitriptilina Andromaco, Amitriptilina Cevallos, Amitriptilina L.CH., Amitriptilina La Santé, Amitriptilina Luar, Amitriptilina MK, Amitriptilina, Amitriptiline, Amitriptyline GM, Amitriptyline Remedica, Amitriptyline, Amitriptyline-Grindeks, Amitriptyline-IKA, Amypres, Amypres-C (Amitriptyline and Chlordiazepoxide), Amyzol, Apo-Amitriptyline, Axeptyl (Amitriptyline and Chlordiazepoxide), Conmitrip, Cuait-D (Amitriptyline and Trifluoperazine), Dapaz Compuesto (Amitriptyline and Chlordiazepoxide), Emotrip (Amitriptyline and Chlordiazepoxide), Fiorda, Kamitrin, Latilin, Limbival Forte (Amitriptyline and Chlordiazepoxide), Limbritol (Amitriptyline and Chlordiazepoxide), Maxitrip, Mitryp, Mitryp Forte (Amitriptyline and Chlordiazepoxide), Odep, Tadamit, Tiperin (Amitriptyline and Chlordiazepoxide), Trepiline, Tryptanol, Adepril, ADT, Amilavil, Amilin, Amineurin, Amineurin retard, Amiplin, Amirol, Amit, Amitin, Amitrip, Amitriptilin R. Desitin, Amitriptilina Clorhidrato Mintlab, Amitriptilinã, Amitriptilino, Amitriptylin beta, Amitriptylin beta retard, Amitriptylin Dak, Amitriptylin Desitin, Amitriptylin Leciva, Amitriptylin Nycomed, Amitriptylin Slovakofarma, Amitriptylin Valeant, Amitriptylin, Amitriptylin-CT, Amitriptylin-dura, Amitriptyline Changzhou Siyao, Amitriptyline Chen Ho, Amitriptyline Glaxo, Amitriptyline HCl Actavis, Amitriptyline HCl Apotex, Amitriptyline HCl CF, Amitriptyline HCl Mylan, Amitriptyline HCl PCH, Amitriptyline HCl ratiopharm, Amitriptyline HCl Sandoz, Amitriptyline HCl Teva, Amitriptyline Hydrochloride Caraco, Amitriptyline Hydrochloride Medopharm, Amitriptyline Hydrochloride Mutual, Amitriptyline Hydrochloride Mylan, Amitriptyline Hydrochloride Sandoz, Amitriptyline Hydrochloride Vintage, Amitriptyline Hydrochloride, Amitriptyline Jinup, Amitriptyline Nycomed, Amitriptyline Update, Amitriptyline, Amitriptyline-Grindeks, Amitriptylin-neuraxpharm, Amitriptylin-neuraxpharm retard, Amitriptylin-Sandoz, Amitriptylinum ICN Polfa, Amitriptylinum, Amitriptylinum VP, Amitriptylin-Zentiva, Amitryp, Amixide (Amitriptyline and Chlordiazepoxide), Amixide H (Amitriptyline and Chlordiazepoxide), Amotrip, Amyline, Amytril, Amyzol, Anapsique, Antalin (Amitriptyline and Chlordiazepoxide), Apo-Amitriptyline, Chlordiazepoxide and Amitriptyline Hydrochloride Mylan (Amitriptyline and Chlordiazepoxide), Deprelio, Diapatol (Amitriptyline and Chlordiazepoxide), Elatrol, Elatrolet, Elavil, Endep, Klotriptyl (Amitriptyline and Chlordiazepoxide), Laroxyl, Libotryp-XL (Amitriptyline and Chlordiazepoxide), Limbitrol (Amitriptyline and Chlordiazepoxide), Limbitrol-H (Amitriptyline and Chlordiazepoxide), Limbitryl (Amitriptyline and Chlordiazepoxide), Limbival (Amitriptyline and Chlordiazepoxide), Maxitrip-CZ (Amitriptyline and Chlordiazepoxide), Maxivalet, Minitran (Amitriptyline and Perphenazine), Modup, Morelin (Amitriptyline and Chlordiazepoxide), Mutabase (Amitriptyline and Perphenazine), Mutabon (Amitriptyline and Perphenazine), Neo Amitriptilin, Neuragon (Amitriptyline and Perphenazine), Nobritol Forte (Amitriptyline and Medazepam), Nobritol (Amitriptyline and Medazepam), Normaln, Perphenazine and Amitriptyline Hydrochloride Mylan (Amitriptyline and Perphenazine), Pertriptyl (Amitriptyline and Perphenazine), Pinsaun, Polybon (Amitriptyline and Perphenazine), Polytanol, Protanol, Qualitriptine, Redomex, Sandoz Amitriptyline, Saroten, Saroten Retard, Sarotex, Sarotex Retard, Sedans (Amitriptyline and Chlordiazepoxide), Stelminal, Syneudon, Teperin, Thymontil, Trip, Tripta, Triptafen (Amitriptyline and Perphenazine), Triptilin, Triptizol, Triptyl, Triptyline, Tripyline, Trynol, Tryptanol, Tryptin, Tryptizol, Uxen Retard.

Active substance: Amitriptyline.

Amitriptyline is a tricyclic antidepressant (TCA). It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs according to a study from early 2001. As well as reducing depressive symptoms, these types of tricyclics also ease migraines, tension headaches, anxiety attacks and some schizophrenic symptoms.

Amitriptyline acts primarily as a serotonin-norepinephrine reuptake inhibitor, with strong actions on the serotonin transporter and moderate effects on the norepinephrine transporter. It has negligible influence on the dopamine transporter and therefore does not affect dopamine reuptake, being nearly 1,000 times weaker on it than on serotonin.

Amitriptyline additionally functions as a 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, α1-adrenergic, H1, H2, H4, and mACh receptor antagonist, and σ1 receptor agonist. It has also been shown to be a relatively weak NMDA receptor negative allosteric modulator at the same binding site as phencyclidine. Amitriptyline inhibits sodium channels, L-type calcium channels, and Kv1.1, Kv7.2, and Kv7.3 voltage-gated potassium channels, and therefore acts as a sodium, calcium, and potassium channel blocker as well.

Recently, amitriptyline has been demonstrated to act as an agonist of the TrkA and TrkB receptors. It promotes the heterodimerization of these proteins in the absence of NGF and has potent neurotrophic activity both in-vivo and in-vitro in mouse models. These are the same receptors BDNF activate, an endogenous neurotrophin with powerful antidepressant effects, and as such this property may contribute significantly to its therapeutic efficacy against depression. Amitriptyline does also act as FIASMA (functional inhibitor of acid sphingomyelinase).

Amitriptyline is used for a number of medical conditions including: depressive disorders, anxiety disorders, attention deficit hyperactivity disorder, migraine prophylaxis, eating disorders, bipolar disorder, post-herpetic neuralgia, and insomnia.

Amitriptyline is used in ankylosing spondylitis for pain relief. It is also used as a preventive for patients with recurring biliary dyskinesia (sphincter of Oddi dysfunction).

Amitriptyline is also used in the treatment of nocturnal enuresis in children.

Amitriptyline may be prescribed for other conditions such as, post-traumatic stress disorder (PTSD), chronic pain, carpal tunnel syndrome (CTS), fibromyalgia, vulvodynia, interstitial cystitis, male chronic pelvic pain syndrome, irritable bowel syndrome (IBS), diabetic peripheral neuropathy, neurological pain, laryngeal sensory neuropathy, chronic fatigue syndrome and painful paresthesias related to multiple sclerosis. Typically lower dosages are required for pain modification of 10 to 50 mg daily.

Amitriptyline USUAL ADULT DOSE FOR DEPRESSION.

Oral:

Initial dose: 25 to 100 mg per day in 3 to 4 divided doses or 50 to 100 mg at bedtime.

Maintenance dose: 25 to 150 mg per day in single or 3 to 4 divided doses. 25 mg per day at bedtime has been used for premenstrual depression. Dose increases should be made gradually. A small number of hospitalized patients may need as much as 300 mg per day.

Patients with major depressive disorder (MDD), both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications, and this risk may persist until significant remission occurs. Suicide is a known risk of depression and certain other psychiatric disorders, and these disorders themselves are the strongest predictors of suicide. There has been a long-standing concern, however, that antidepressants may have a role in inducing worsening of depression and the emergence of suicidality in certain patients during the early phases of treatment. Pooled analyses of short-term placebo-controlled trials of antidepressant drugs (SSRIs and others) showed that these drugs increase the risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (ages 18-24) with major depressive disorder (MDD) and other psychiatric disorders. Short -term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction with antidepressants compared to placebo in adults aged 65 and older.

Ingredients: One tablet contains:

active ingredient: amitriptyline hydrochloride - 11.32 mg and 28.30 mg, or 10 mg and 25 mg of amitriptyline;

Other ingredients: microcrystalline cellulose - 40/100 mg, lactose monohydrate (milk sugar) - 40/100 mg, pregelatinised starch - 25.88 / 64.70 mg colloidal silicon dioxide (Aerosil) - 0.4 / 1 mg, talc - 1.2 / 3 mg magnesium stearate - 1.2 / 3 mg.

Pharmacotherapeutic group: anti-depressant

ATX Code: [N06AA09]

pharmacological properties

pharmacodynamics

Antidepressants (tricyclic antidepressant). Has also some analgesic (central origin) antiserotoninovoe action helps to eliminate bedwetting and reduces appetite.

It has a strong peripheral and central anticholinergic effect due to a high affinity to the nicotinic acetylcholine receptor m; strong sedative effect connected with affinity of H1-histamine receptors, and alpha-adrenoceptor blocking action. It has the properties of anti-arrhythmic drug (PM) the IA class, like quinidine in therapeutic doses slows ventricular conduction (in overdose can cause severe intraventricular block).

The mechanism of antidepressant action is associated with increasing concentrations of norepinephrine and / or serotonin in the central nervous system (CNS) (reducing their reabsorption). The accumulation of these neurotransmitters occurs as a result of inhibition of the reverse capture presynaptic neuronal membrane. With prolonged use reduces the functional activity of beta-adrenergic and serotonin receptors of the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, impaired in depressive states. When anxiety and depressive states reduces anxiety, agitation and depressive symptoms.

The mechanism of action of anti-ulcer due to the ability to provide sedation and m-anticholinergic action.

Efficacy in bedwetting due, apparently, anticholinergic activity, resulting in an increased ability of the bladder to stretch direct beta-adrenergic stimulation, the activity of alpha-adrenergic agonists, accompanied by increased sphincter tone, and central serotonin reuptake blockade.

It has a central analgesic action, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and effects on endogenous opioid system.

The mechanism of action for bulimia nervosa is unclear (perhaps similar to that in depression). It shows a clear effect of the drug in patients with bulimia as a non-depressed, and if available, with the reduction of bulimia can be observed without a concomitant weakening of the most depressed.

When general anesthesia reduces blood pressure (BP) and body temperature. It does not inhibit monoamine oxidase (MAO).

The antidepressant effect develops within 2-3 weeks after the start of the application.

Pharmacokinetics
Absorption - high. Bioavailability 30-60% amitriptyline, nortriptyline its active metabolite - 46-70%. The time to maximum concentration (Tmax) after ingestion 2,0-7,7 hours. The volume of distribution of 5.10 l / kg. Effective therapeutic blood concentration for amitriptyline - 50-250 ng / ml, nortriptyline 50-150 ng / ml. The maximum plasma concentration (Cmax) 0,04-0,16 g / ml. Passes (including nortriptyline) histohematogenous barriers, including the blood-brain barrier, placental barrier, enters the breast milk. Relationship to plasma proteins - 96%.

It is metabolized in the liver with isozymes CYP2C19, CYP2D6, has the effect of "first pass" (by demethylation, hydroxylation) to form active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and active metabolites. The half-life of plasma (T1 / 2) - 10-26 hours for 18-44 hours amitriptyline and nortriptyline. Excreted by the kidneys (mainly as metabolites) - 80% for 2 weeks, partly with bile.

Indications
Depression (especially anxiety, agitation and sleep disorders, including childhood, endogenous, involutional, reactive, neurotic, drug, with organic brain lesions).

In the combined therapy is used with mixed emotional disorders, psychoses, schizophrenia, alcohol withdrawal, disorders of behavior (activity and attention), nocturnal enuresis (except in patients with hypotension bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical facial pain, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other. peripheral neuropathy), headache, migraine (prevention), gastric ulcer and 12 duodenal ulcer.

Contraindications
Hypersensitivity, use together with MAO inhibitors and 2 weeks before starting treatment, myocardial infarction (acute and subacute periods), acute alcohol intoxication, acute intoxication with hypnotics, analgesic and psychoactive drugs, angle-closure glaucoma, severe violations of AV and intraventricular conduction (blockade beam legs branch block, AV block II st.), lactation, children under 6 years.

Due to the content of the tablets of lactose monohydrate (milk sugar), the drug should not be taken by patients with rare hereditary disorders such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully
Amitriptyline should be used with caution in patients with alcoholism, bronchial asthma, schizophrenia (possible activation of psychosis), bipolar disorder, epilepsy, the oppression of bone marrow hematopoiesis, diseases of the cardiovascular system (CVS) (angina, arrhythmias, heart block, chronic heart failure, myocardial infarction, hypertension), ocular hypertension, stroke, decreased motor function of the gastrointestinal tract (GIT) (risk of paralytic ileus), liver and / or kidney failure, hyperthyroidism, prostatic hyperplasia, urinary retention, hypotension bladder, pregnancy (especially I trimester), in old age.

Amitriptyline Dosing and Administration
Assign the inside, without chewing, immediately after a meal (to reduce irritation of the gastric mucosa).

Adults
Adults with depression initial dose - 25-50 mg at night, then gradually the dose may be increased based on efficacy and tolerability up to a maximum
300 mg / day in 3 divided doses (the largest part of the dose is taken at night). When the therapeutic effect of the dose can be gradually reduced to the minimum effective depending on the condition of the patient. The duration of treatment is determined by the condition of the patient, efficacy and tolerability of the therapy, and can range from a few months to 1 year, and if necessary more.

In old age with lung disorders, as well as bulimia nervosa, in the complex therapy of mixed emotional disorders and behavioral disorders, psychosis, schizophrenia, and alcohol withdrawal is prescribed in doses of 25-100 mg / day (at night), after reaching the therapeutic effect of pass at the minimum effective dose - 10-50 mg / day.

For the prevention of migraine, chronic pain syndrome of neurogenic nature (including long-term headaches), as well as in the treatment of gastric ulcer and 12 duodenal ulcer - from 10-12,5-25 to 100 mg / day (maximum of the dose is taken at night).

Children
Babies as an antidepressant: from 6 to 12 years - 10-30 mg / day or 05/01 mg / kg / day fractionally, as a teenager - to 100 mg / day.

If nocturnal enuresis in children 6-10 years - 10-20 mg / day for the night of 11-16 years - up to 50 mg / day.

Amitriptyline Side effects
Related anticholinergic effect of the drug: blurred vision, paralysis of accommodation, mydriasis, increased intraocular pressure (only in persons with local anatomical predisposition - narrow angle of anterior chamber), tachycardia, dry mouth, confusion (delirium or hallucinations), constipation, paralytic intestinal obstruction, difficulty urinating.

CNS: drowsiness, fainting, fatigue, irritability, anxiety, disorientation, hallucinations (particularly in elderly patients and in patients with Parkinson's disease), anxiety, agitation psychomotor, mania, hypomania, impaired memory, reduced ability to concentrate, insomnia, "nightmarish" dream, asthenia; headache; dysarthria, tremor of small muscles, especially arms, hands, head and tongue, peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus; ataxia, extrapyramidal syndrome, acceleration and intensification of seizures; changes in the electroencephalogram (EEG).

From the CCC: tachycardia, palpitations, dizziness, orthostatic hypotension, non-specific changes in the electrocardiogram (ECG) (range S-T or T-wave) in patients without heart disease; arrhythmia, labile blood pressure (decrease or increase in blood pressure), violation of intraventricular conduction (extension of the QRS complex, changing the interval P-Q, bundle branch block blockade).

On the part of the digestive tract: nausea, heartburn, gastralgia, hepatitis (including altered liver function and cholestatic jaundice), vomiting, increased appetite and weight gain or loss of appetite and weight loss, stomatitis, taste change, diarrhea, darkening of the tongue.

From endocrine system: an increase in size (swelling) of the testicles, gynecomastia; an increase in the size of the breast, galactorrhea; decreased or increased libido, reduced potency, hypo- or hyperglycemia, hyponatremia (decreased production of vasopressin), antidiuretic hormone syndrome of inappropriate secretion (ADH).

Allergic reactions: skin rash, pruritus, photosensitivity, angioedema, urticaria.

Other: hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, urinary retention, pollakiuria.

With prolonged treatment, especially in high doses, when it stopped suddenly may develop withdrawal symptoms: nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual excitement; while phasing out after long-term treatment - irritability, restlessness, insomnia, abnormal dreams.

Amitriptyline Overdose
Symptoms. CNS: drowsiness, stupor, coma, ataxia, hallucinations, anxiety, agitation, decreased ability to concentrate, disorientation, confusion, dysarthria, hyperreflexia, muscle rigidity, choreoathetosis, epileptic syndrome.

From the CCC: lowering blood pressure, tachycardia, arrhythmia, violation of intracardiac conduction, characteristic of tricyclic antidepressants poisoning ECG changes (particularly QRS), shock, heart failure; in very rare cases - cardiac arrest.

Others: respiratory depression, dyspnea, cyanosis, vomiting, hyperthermia, mydriasis, increased sweating, oliguria or anuria.

Symptoms develop within 4 hours after the overdose, peak within 24 hours and lasts 4-6 days. If you suspect an overdose, especially in children, the patient should be hospitalized.

Treatment: orally: gastric lavage, activated charcoal; symptomatic and supportive therapy; in severe anticholinergic effects (lowering of blood pressure, arrhythmias, coma, myoclonic seizures) - the introduction of a cholinesterase inhibitor (physostigmine use is not recommended due to an increased risk of seizures); maintenance of blood pressure and fluid and electrolyte balance. Showing CCC control functions (including ECG) for 5 days (a relapse can occur after 48 hours and later), anticonvulsant therapy, artificial lung ventilation (ALV), and others. Resuscitation. Hemodialysis and forced diuresis are not effective.

Amitriptyline Interaction with other drugs

In a joint application of ethanol and drugs which depress the central nervous system (including the others. Antidepressants, barbiturates, benzadiazepinov and general anesthetics) may significantly increased inhibitory action on CNS, respiratory depression and hypotensive effect.

Increases sensitivity to drinks containing ethanol.

Increases anticholinergic effect of drugs with anticholinergic activity (eg, phenothiazine derivatives, antiparkinsonian drugs, amantadine, atropine, biperiden, antihistamine drugs), which increases the risk of side effects (CNS, vision, bowel and bladder). In a joint application with holinoblokatorami, phenothiazine derivatives and benzodiazepines - mutual enhancement of the sedative and central anticholinergic effects and increased risk of seizures (lowering the threshold for seizure activity); phenothiazine derivatives, may further increase the risk of neuroleptic malignant syndrome.

In a joint application with antiepileptic drugs may increase depressant effects on the central nervous system, lowering the threshold for seizure activity (when used in high doses) and a decrease in the efficiency of the latter.

In a joint application with antihistamine drugs, clonidine - increased inhibitory action on the central nervous system; with atropine - increases the risk of paralytic ileus; with drugs that cause extrapyramidal reactions - increased severity and frequency of extrapyramidal effects.

With simultaneous use of amitriptyline and indirect anticoagulants (coumarin derivatives or indadiona) may increase the anticoagulant activity of the latter.

Amitriptyline may enhance the depression caused by glucocorticosteroids (GCS).

Drugs for the treatment of hyperthyroidism increases the risk of agranulocytosis.

Reduces the effectiveness of phenytoin and alpha-blockers.

Inhibitors of microsomal oxidation (cimetidine), extend T1 / 2, increase the risk of toxic effects of amitriptyline (may require dose reduction of 20-30%), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce the concentration in the plasma and reduce the effectiveness of amitriptyline.

The combined use of disulfiram and others. Atsetaldegidrogenazy inhibitors provokes delirium.

Fluoxetine and fluvoxamine increase in plasma concentration of amitriptyline (may require amitriptyline dose reduction by 50%).

Oral contraceptive drugs and estrogens may increase the bioavailability of amitriptyline.

In an application amitriptyline with clonidine, guanethidine, betanidinom, reserpine and methyldopa - decrease the hypotensive effect of the latter; with cocaine - the risk of cardiac arrhythmias.

Antiarrhythmic drugs (such as quinidine) increase the risk of arrhythmias (possibly slowing metabolism of amitriptyline).

Pimozide probucol and can enhance cardiac arrhythmia, which is manifested in the extension of Q-T interval on the ECG.

It enhances the effect of the SCA epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine (including when these drugs are part of the local anesthetics), and increases the risk of cardiac arrhythmias, tachycardia, severe hypertension.

When coadministered with alpha-adrenergic agonists for intranasal administration, or for use in ophthalmology (with significant systemic absorption) can be amplified vasoconstrictor action of the latter.

In a joint reception with thyroid hormones - the mutual reinforcement of therapeutic effects and toxic effect (include heart arrhythmia and a stimulating effect on the central nervous system).

M-holinoblocators and antipsychotic drugs (neuroleptics) increase the risk of hyperpyrexia (especially in hot weather).

Incompatible with MAO inhibitors (possible increase in the frequency of periods hyperpyrexia, severe convulsions, hypertensive crises, and death of the patient).

Special instructions
Before treatment is necessary to monitor blood pressure (in patients with low or labile blood pressure, it may be reduced even more); during treatment - control peripheral blood (in some cases may develop agranulocytosis, and therefore it is recommended to monitor blood picture, especially with an increase in body temperature, the development of influenza-like symptoms and a sore throat), long-term therapy - control functions SSA and the liver. In the elderly and patients with CVD is shown control of heart rate (HR), blood pressure, ECG. The ECG may appear clinically insignificant changes (smoothing of the T wave, depression S-T segment, the expansion of the QRS complex).

Care should be taken with a sharp transition to the upright position of "lying" or "sitting".

The treatment should be to exclude the use of ethanol.

Assign no earlier than 14 days after discontinuation of MAO inhibitors, starting with low doses.

With the sudden discontinuation after long-term treatment may develop the syndrome of "cancellation".

Amitriptyline at a dose higher than 150 mg / day decreases the threshold for seizure activity (note the risk of epileptic attacks in susceptible patients, and also in the presence of others. Predisposing to seizures of factors, such as brain damage of any etiology, the simultaneous use of antipsychotic drugs (neuroleptics) , during the non-ethanol or cancel drugs with anticonvulsant properties, such as benzodiazepines).

Major depression is peculiar risk of suicidal actions, which may persist until significant remission. In this regard, at the beginning of the treatment with a combination of drugs from the group of benzodiazepines or neuroleptic drugs and the constant medical supervision (charging proxies storage and issuing of drugs) may be indicated.

In children, adolescents and young adults (under 24 years) with depression and others. Mental disorders antidepressants compared to placebo, increased the risk of suicidal thoughts or suicidal behavior. Therefore, the appointment of amitriptyline or any other. Antidepressants in these patients should be related to the risk of suicide and the benefits from their use. In short-term studies in people older than 24 years, the risk of suicide did not increase, and in people over 65 years is somewhat reduced. During antidepressant treatment all patients should be monitored for early detection of suicidal tendencies.

In patients with cyclic affective disorders during the depressive phase of manic or hypomanic state may develop during therapy (requires dose reduction or withdrawal of the drug and the appointment of antipsychotic drugs). After the relief of these conditions, if there is evidence of low doses in the treatment can be resumed.

Due to the potential cardiotoxic effects need to be careful in the treatment of patients with hyperthyroidism or patients receiving thyroid hormone drugs.

In conjunction with electroconvulsive therapy is prescribed only with careful medical supervision.

In predisposed patients and elderly patients may provoke the development of drug psychoses, especially at night (after discontinuation of the drug tested within a few days).

It may cause paralytic ileus, especially in patients with chronic constipation, the elderly or patients who are forced to comply with bed rest.

Before the general or local anesthesia, the anesthesiologist should be warned that the patient is taking amitriptyline.

Because of the anticholinergic action of lacrimation may decrease and increase the relative amount of mucus in the tear fluid which may cause damage to the corneal epithelium in patients who use contact lenses.

With prolonged use, an increase in the incidence of dental caries. It may be increased need for riboflavin.

The study of reproduction in animals showed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not performed. Pregnant women should use the drug only if the expected benefit to the mother outweighs the potential risk to the fetus.

It penetrates into breast milk and may cause drowsiness in infants.

In order to avoid the syndrome of "cancellation" in neonates (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous irritability, increased or decreased blood pressure, tremor or spastic phenomena) receiving amitriptyline gradually canceled at least 7 weeks before the expected birth.

Children are more sensitive to acute overdose, which should be considered dangerous and potentially fatal for them.

During the period of treatment must be careful when driving and other lesson. Potentially hazardous activities that require high concentration and quick.

Amitriptyline Reviews

Amitriptyline is a very good anti-depressant and copes with its task, reduces anxiety, and normal sleep. The most interesting is that it does not affect the normal sleep rhythms, that is not disturbed natural process of falling asleep. One of its drawbacks is essential that it is very greatly reduces the pressure that can cause fainting and loss of consciousness.
And generally tolerated and perfectly fulfills its function antidepressant.
Recently I learned that oncologists prescribe this drug for chronic pain syndrome caused by the cancer. Such people often change the mentality and comes anxiety and depression, which helps to cope with amitriptyline.

Amitriptyline tablets are really good. And where it is not very expensive to sell. One time I saw them. Appoint a physician 1/4 tablet one dose. Not only that, they are very effective because besides still very strong, probably therefore administered a small dose. It is best to take them when you have nowhere in particular to work. They are very relaxing and in no event shall sit behind the wheel of the car, because the body's reaction is inhibited and reduced reaction. I know for sure that often take a long time they can not otherwise be highly addictive. If you have severe problems then you better choose these pills.

A few years ago because of the constant lack of sleep and fatigue, work-related, began insomnia and constant depression. Familiar doctor advised me to drink a vial Amitriptyline. A few days later depression and anxiety went after his admission, finally began to sleep. The only thing that is important to note when using these tablets, so it is getting used to the device, which quickly arise in humans. Before you use this antidepressant, see your doctor and be sure to consult on this matter with him. As for my case, the drug was effective.

Adepress (Paroxetine) tablets - Instructions for Use, Dosage, Side Effects, Reviews

Synonyms: Actaparoxetine, Adco-Paroxetine, Apodepi, APT-Paroxetine, Arketis, Aropax, Axepat, CO Paroxetine, Deparoc, Deproxyl, Deprozel, Deroxat, Divarius, Doc Paroxetine, Dropax, Eugine, Humoxat, Melev, Moxetin, Neurotrox, Olane, Oxat, Oxitine-PR, Pacex, Paluxetil, Pamax, Pamoxet, Panex, Parax, Parexat, Parexis, Pari, Pari CR, Parocetan, Parogen, ParoGen, Paroksetin Actavis, Paroksetin Aurobindo, Paroksetin Teva, Parotin, Paroxat, Paroxet, Paroxetin Actavis, Paroxetin Hexal, Paroxetin Teva, Paroxetina Bluepharma, Paroxetina Germed, Paroxetina La Santé, Paroxetina, Paroxetine Aurobindo, Paroxetine EG, Paroxetine ratiopharm, Paroxetine Teva, Paroxetine-GA, Paroxetin-ratiopharm, Paroxil, Paxan, Paxera, Paxetin, Paxil, Paxotin, Petin-CR, Pharmapar, Plisil, Raxit, Rexetin, Sarolife, Serestill, Serrapress, Sumiko, Traviata, Xilanic, Afenexil, Allenopar, Anziatina, Apo-Parox, Apo-Paroxetine, Arapaxel, Arketis, Aropax, Arotin, Aroxat, Bectam, Benepax, Caremod, Casbol, Cebrilin, Chemmart Paroxetine, Datevan, Denerval, Deroxat, Doc Paroxetine, Dropaxin, Eutimil, Extine, Frosinor, Gen-Paroxetine, GenRX Paroxetine, Le You, Loxamine, Meplar, Moratus, Motivan, Noprilex, Novo-Paroxetine, Ocampina, Optipar, Paluxon, Paretin, Parexel, Parocetan, Parogen, Parolex, Paromerck, Paronex, Parosat, Parosenin, Paroser, Parotin, Parox, Paroxalon, Paroxat Hexal, Paroxat, Paroxe, Paroxedura, Paroxetin - 1 A Pharma, Paroxetin +pharma, Paroxetin 1A Farma, Paroxetin 1A Pharma, Paroxetin 2care4, Paroxetin AbZ, Paroxetin Actavis, Paroxetin AL, Paroxetin Arcana, Paroxetin Aurobindo, Paroxetin beta, Paroxetin Easypharm, Paroxetin Genericon, Paroxetin Helvepharm, Paroxetin Hexal, Paroxetin HEXAL, Paroxetin Interpharm, Paroxetin Nycomed, Paroxetin Orifarm, Paroxetin Orion, Paroxetin PCD, Paroxetin Pfizer, Paroxetin ratiopharm, Paroxetin Sandoz, Paroxetin STADA, Paroxetin Teva, Paroxetina Acost, Paroxetina Actavis, Paroxetina Almus, Paroxetina Alter, Paroxetina Aphar, Paroxetina Apotex, Paroxetina Arafarma Group, Paroxetina Bexal, Paroxetina Cinfa, Paroxetina Combix, Paroxetina Cuve, Paroxetina Davur, Paroxetina Decrox, Paroxetina Doc, Paroxetina Edigen, Paroxetina EG, Paroxetina Farmalid, Paroxetina Germed, Paroxetina Hexal, Paroxetina Jaba, Paroxetina Kern Pharma, Paroxetina Labesfal, Paroxetina Mabo, Paroxetina Mepha, Paroxetina MK, Paroxetina Mundogen, Paroxetina Mylan, Paroxetina Normon, Paroxetina Paxpar, Paroxetina Pensa, Paroxetina Pharmagenus, Paroxetina Qualigen, Paroxetina Ranbaxy, Paroxetina Ratiopharm, Paroxetina Rimafar, Paroxetina Sandoz, Paroxetina Stada, Paroxetina Tarbis, Paroxetina Teva, Paroxetina Tevagen, Paroxetina Ur, Paroxetina Uxa, Paroxetina Winthrop, Paroxetina, Paroxetin-CT, Paroxetine Actavis, Paroxétine Actavis, Paroxétine Alter, Paroxetine Apotex, Paroxétine Arrow, Paroxetine Aurobindo, Paroxétine Biogaran, Paroxetine CF, Paroxétine CristerS, Paroxetine EG, Paroxétine EG, Paroxétine Evolugen, Paroxetine Generics, Paroxetine GenRx, Paroxetine Hydrochloride Actavis, Paroxetine Hydrochloride Alphapharm, Paroxetine Hydrochloride Apotex, Paroxetine Hydrochloride Aurobindo, Paroxetine Hydrochloride Caraco, Paroxetine Hydrochloride Mylan, Paroxetine Hydrochloride Teva, Paroxetine Hydrochloride Zydus, Paroxetine I.C.C., Paroxétine Isomed, Paroxetine Mylan, Paroxétine Mylan, Paroxetine Orion, Paroxetine PCH, Paroxetine Pharma, Paroxetine ratiopharm, Paroxétine Ratiopharm, Paroxétine RPG, Paroxetine Sandoz, Paroxétine Sandoz, Paroxetine Teva, Paroxetine Winthrop, Paroxétine Zydus, Paroxetine, Paroxetin-Hormosan, Paroxetin-neuraxpharm, Paroxetin-ratiopharm, Paroxia, Paroxiflex, Paroxin, Paxeratio, Paxetil, Paxetin, Paxil CR, Paxil, Paxil CR, Paxtin, Paxtine, Paxxet, Pharmacor Paroxetine, PMS-Paroxetine, Pondera, Posivyl, Prexat, Prexor, Psicoasten, ratio-Paroxetine, Remood, Rexetin, Roxetin, Sandoz Paroxetine, Seretran, Seroxat, Seroxat CR, Setine, Sicotral, Solben, Stiliden, Taberil, Terry White Chemists Paroxetine, Teva-Paroxetine, Tiarix, Traviata, Xerenex, Xet, Xetanor, Xetin, Xetine-P, Zyparox, Aipratex (Paroxetine and Alprazolam), Cronadyn, Depoxat, Deprozel, Paroksetin Pfizer, Paroksetin PharmaS, Paroten, Paroxat, Paroxetin Orifarm, Paroxetin Orion, Paroxetin Pfizer, Paroxetin Spirig, Paroxetin Teva, Paroxetine A, Paroxetine Aurobindo, Paroxetine GSK, Paroxetine Orion, Paroxétine Pfizer, Paroxétine PHR Lab, Paroxétine Teva, Paroxétine Zentiva, Paroxetine, Paroxetin-hemihydrat-Teva, Paroxetin-Mepha, Paroxetin-ratiopharm, Paroxetin-Teva, Paxil, Remood, Rexetin, Riedilex, Roxepar, Serestill, Sereupin, Seroxat, Stiliden, Traviata XR, Daparox, Divarius, Ennos, Paroxetin Avansor, Paroxetine Generichealth, Paroxetine Genthon, Paroxetine Kiron, Pexeva, Plisil.

Active substance: Paroxetine.

What is paroxetine?

Paroxetine is an antidepressant in a group of drugs called selective serotonin reuptake inhibitors (SSRIs). Paroxetine affects chemicals in the brain that may be unbalanced in people with depression, anxiety, or other disorders.

Paroxetine is used to treat depression, obsessive-compulsive disorder, anxiety disorders, post-traumatic stress disorder (PTSD), and premenstrual dysphoric disorder (PMDD).

Paroxetine may also be used for purposes not listed in this medication guide.

What should I discuss with my healthcare provider before taking paroxetine?

You should not use this medicine if you are allergic to paroxetine, or if:

you are also taking pimozide or thioridazine; or

you are being treated with methylene blue injection.

Do not use an MAO inhibitor within 14 days before or after you take paroxetine. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, and tranylcypromine. After you stop taking paroxetine you must wait at least 14 days before you start taking an MAO inhibitor.

ATC - N06AB05 Paroxetine

Pharmacological group - Antidepressants.

Nosological classification (ICD–10)

F10.2 alcohol dependence syndrome;

F31.9 Bipolar affective disorder, unspecified;

F32 Depressive episode;

F34.1 Dysthymia;

F41.0 Panic disorder [episodic paroxysmal anxiety];

F42.9 Obsessive-compulsive disorder, unspecified.

Composition, structure and packing

Film-coated tablets are white or nearly white, round, biconvex.

Other ingredients: calcium hydrogen phosphate (calcium phosphate dibasic), corn starch, sodium carboxymethyl starch (Primogel), magnesium stearate.

Cover structure: Opadry II (hypromellose, lactose monohydrate, macrogol/polyethylene glycol 3350, polyethylene glycol 4000 /, titanium dioxide).

Pharmacological action

Antidepressant. Is a selective inhibitor of the reuptake of serotonin (5-hydroxytryptamine, 5-HT) neurons in the brain, which determines its antidepressant action and effectiveness in the treatment of obsessive-compulsive (OCD) and panic disorder.

Paroxetine has low affinity for m-cholinergic receptors (has weak anticholinergic action), α1 -, α2 - and β-adrenergic receptors, as well as dopamine (D2), 5HT1 -like, 5HT2 -like and histamine H1 - receptors. Paroxetine does not violate the psychomotor function and does not potentiate the inhibitory effect of ethanol on them. You can buy Adepress.

According to the study of behavior and EEG of paroxetine detected weak activating properties when it is administered at doses higher than those required for the inhibition of serotonin reuptake. In healthy volunteers, it does not cause a significant change in blood pressure, heart rate and EEG.

Pharmacokinetics

Absorption

After oral administration of paroxetine is well absorbed from the gastrointestinal tract. Simultaneous ingestion does not affect the absorption and pharmacokinetics of paroxetine.

Distribution

The equilibrium state is reached after 7–14 days after initiation of therapy, further pharmacokinetics during long-term therapy is not changed. Clinical effects of paroxetine (adverse effects and effectiveness) are not correlated to its concentration in plasma.

Since paroxetine exposed the effect of “first pass” through the liver, the amount determined in the systemic circulation is less than that which is absorbed from the gastrointestinal tract. With increasing doses of paroxetine or with repeated dosing of a partial absorption of the effect of “first pass” through the liver and reduced plasma clearance of paroxetine. As a result, this may increase the concentration of Paroxetine in the plasma pharmacokinetic parameters and vibrations that can occur only in those patients taking the drug at a low dose of paroxetine achieved low levels in plasma.

Paroxetine is extensively distributed in the tissues and pharmacokinetic calculations indicate that only 1% of it is present in the plasma, and in therapeutic concentrations, 95% bound to plasma proteins.

Metabolism

The major metabolites of paroxetine are polar and conjugated products of oxidation and methylation, which are rapidly cleared from the body, have a weak pharmacological activity and do not affect its therapeutic effect.

Excretion of metabolites of paroxetine biphasic, first as a result of “first pass” through the liver, and then it is controlled by systemic elimination.

Excretion

T 1/2 paroxetine is in the range of from 6 to 71 h, but the average was 24 hours. About 64% of the paroxetine is excreted with urine (2% - unchanged, 64% - as metabolites); approximately 36% is excreted in the bile through the intestines, mostly in the form of metabolites, less than 1% - unchanged.

Pharmacokinetics in special clinical situations

The concentration of paroxetine in plasma increases with abnormal liver function and kidney function, as well as in the elderly, and the range of plasma concentrations of almost coincides with the range of concentrations in healthy adult volunteers.

Adepress (Paroxetine) Dosage

Tablets should be taken 1 time/day, in the morning, during a meal, without chewing, drinking water.

The dose is adjusted individually for the first 2–3 weeks after initiation of therapy and subsequently adjusted if necessary. The effect is, in most cases develops gradually.

In depression the recommended dose is 20 mg 1 time/day. If necessary, gradually increase the dose by 10 mg at intervals of 1 week to achieve a therapeutic effect, the maximum daily dose should not exceed 50 mg/day.

In obsessive-compulsive disorders initial therapeutic dose is 20 mg/day, followed by weekly increases of 10 mg to achieve a therapeutic response. Recommended average therapeutic dose - 40 mg/day, if necessary, the dose may be increased to 60 mg/day.

When panic disorder initial dose - 10 mg/day (in order to reduce the possible risk of acute panic symptoms), followed by weekly increases of 10 mg. The average therapeutic dose - 40 mg/day. The maximum daily dose should not exceed 60 mg/day.

When social anxiety disorder/social phobia, the initial dose is 20 mg/day, with no effect for a minimum of 2 weeks may increase the dose to a maximum of 50 mg/day. Dose should be increased to 10 mg at intervals of not less than a week in accordance with the clinical effect.

In PTSD, for most patients the initial and therapeutic dose is 20 mg/day. In some cases it is recommended to increase the maximum dose of 50 mg/day. Dose should be increased by 10 mg every week in accordance with the clinical effect.

In generalized anxiety disorders and the initial therapeutic dose is 20 mg/day.

When renal and/or hepatic insufficiency the recommended dose is 20 mg/day.

For Older patients the daily dose should not exceed 40 mg.

To prevent a recurrence necessary supportive therapy. Once the symptoms of depression this course may be 4–6 months, while obsessive and panic disorders - more than 4–6 months.

Avoid abrupt withdrawal of the drug. In order to prevent the development of withdrawal discontinuation of the drug should be gradual.

Adepress (Paroxetine) Overdose

Symptoms: nausea, dilated pupils, fever, changes in blood pressure, headache, involuntary muscle contractions, agitation, anxiety, tachycardia. In very rare cases, when taken with other psychotropic drugs and/or ethanol (alcohol), possible changes in the EKG, coma.

Treatment: gastric lavage, administration of activated charcoal. If necessary, symptomatic therapy. No specific antidote.

Adepress (Paroxetine) Drug Interactions

Simultaneous treatment with antacids does not affect the absorption and pharmacokinetic parameters of Adepress.

Due to the inhibition of cytochrome P–450 with paroxetine may increase the effect of barbiturates, phenytoin, anticoagulants, tricyclic antidepressants, phenothiazine neuroleptics and antiarrhythmics class 1C, metoprolol, and increased risk of side effects, while the appointment of these medicines.

When concomitant administration with drugs that inhibit liver enzymes, may require dose reduction of Adepress.

Between paroxetine and warfarin is expected pharmacodynamic interaction (with unchanged prothrombin time marked by increased bleeding).

While appointing of Adepress with atypical antipsychotics, tricyclic antidepressants, drugs phenothiazine series, aspirin, NSAIDs may impair the process of blood clotting.

Simultaneous with the appointment of Adepress with serotonergic drugs (tramadol, sumatriptan) may lead to increased serotonin effect.

Observed synergy among the tryptophan drugs lithium and paroxetine.

While appointing of Adepress phenytoin and other anticonvulsants may decrease the concentration of paroxetine in plasma and increased frequency of side effects.

Paroxetine much weaker suppresses guanethidine antihypertensive effects in comparison with antidepressants which inhibit noradrenaline.

Adepress (Paroxetine) Side effects

CNS and peripheral nervous system: often - drowsiness or insomnia, tremor, fatigue, dizziness, anxiety; sometimes - confusion, hallucinations, extrapyramidal disorders, paresthesias, decreased ability to concentrate; rarely - seizures, mania; very rare - serotonin syndrome (agitation, hyperreflexia, diarrhea), panic disorder.

On the part of the organ of vision: in some cases - blurred vision, mydriasis.

On the part of the musculoskeletal system: rarely - myasthenia gravis, myoclonus, arthralgia, myalgia.

Urinary system: frequent urination; rarely - urinary retention.

Part of the reproductive system: ejaculation disorders, disorders of libido; rarely - hyperprolactinaemia/galactorrhoea, anorgasmia.

From the digestive system: loss of appetite, nausea, vomiting, dry mouth; sometimes - constipation or diarrhea; in some cases - hepatitis.

Cardio-vascular system: orthostatic hypotension.

Allergic reactions: seldom - rash, urticaria, ecchymosis, pruritus, angioedema.

Other: increased sweating; in rare cases - hyponatremia, inappropriate secretion of antidiuretic hormone.

Adepress (Paroxetine) Indications

Depression of all types, including reactive, endogenous depression and severe depression accompanied by anxiety;

Obsessive-compulsive disorder (OCD);

Panic disorder, including with the fear of staying in the crowd (agoraphobia);

Social anxiety disorder/social phobia;

Generalized anxiety disorder;

Post-traumatic stress disorder.

Contraindications

Concomitant use of monoamine oxidase inhibitors and a period of 14 days after their cancellation;

Unstable epilepsy;

Pregnancy;

Lactation (breastfeeding);

Hypersensitivity to the drug.

Precautions should be prescribed the drug for hepatic failure, renal failure, closed-angle glaucoma, prostatic hyperplasia, mania, heart disease, epilepsy, convulsive states, while the appointment of cardioversion, simultaneous administration of drugs that increase the risk of bleeding, the presence of risk factors for bleeding disorders and diseases increase the risk of bleeding, as well as elderly patients.

Cautions

In order to avoid the development of neuroleptic malignant syndrome should be given with caution Adepress patients taking neuroleptics.

Treatment by Adepress appoint 2 weeks after discontinuation of MAO inhibitors.

In elderly patients, in patients receiving of Adepress possible hyponatremia.

In some cases, dosage adjustment is simultaneously applied insulin and/or oral hypoglycemic drugs.

With the development of seizures treatment by Adepress is stopped.

At the first sign of mania should be discontinued therapy of Adepress.

During the first few weeks of therapy of Adepress should carefully monitor the condition of the patient in relation to possible suicide attempts.

During therapy of Adepress should abstain from alcohol in connection with the enhancement of its toxicity.

Use in Pediatrics

Application of Adepress children not recommended as its safety and efficacy in this group of patients have not been established.

Effects on ability to drive vehicles and management mechanisms

Despite the fact that paroxetine does not impair cognitive and psychomotor performance, patients should refrain or exercise extreme caution when driving and when engaging in other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Renal impairment

Precautions should be prescribed the drug for renal failure. In renal insufficiency, the recommended dose is 20 mg/day.

In hepatic dysfunction

Precautions should be prescribed the drug for liver failure. In hepatic impairment the recommended dose is 20 mg/day.

Adepress (Paroxetine) Reviews

Doctors Reviews about Adepress

Adepress (Paroxetine) - A good analogy of the famous Paxil. Among the notable advantages of the drug, it may be noted a good clinical effect in the medium and heavy anxiety and depressive disorders. OCD, panic attacks, in the rehabilitation of gambling addiction and dependence on cannabis. When the duration of a course of therapy 5 months, the results are quite good.

Adepress - A good generic Rexetine / paroxetine, respectively, the price is not bad, as the onset of action of all serotonin antidepressants 10-14 days. Operates well in generalized anxiety, anxiety-depressive states, panic attacks. + This technique once a day.

I am quite often in my clinical practice using Adepress and its analogs. Adepress very effective in depressive disorders of varying severity, with anxiety and depressive disorders, as well as generalized anxiety disorder, accompanied by panic attacks. The effect begins to appear after 10-14 days from the start of the reception. The most common side effect from my experience primeneriya Adepressa is nausea, which can be avoided by taking the drug with a gradual increase in dosage. Also gradually should pursue the abolition of the drug to avoid withdrawal symptoms. Price matches the quality of the drug.

Patient Review about Adepress

Adepress really helps during stress. Well, I have these moments do not happen often, so do not regularly use this drug and can not say about its side factors, if any. But for a single exposure - very effective.

Read reviews of real people about Adepress and not be afraid to ask your doctor about these medications! Yes, it lifted me nervous tension almost immediately, but after three days of reception I realized that I had already become dependent on him. Action from it stronger, somnolence and fatigue, it is due to this and passes the feeling of anxiety and nervousness. There are medications and much better with a softer effect.

Adepress Good medicine, but I do not advise to take without a prescription. Yes, over the counter without a prescription, and you do not sell. The first time was a strange sensation, lethargy, some after starting. Then nothing, the body has adapted, it lasted a week. Now, after the full course of the drug I feel great. Alert left me, headaches and underwent a great mood. We can say now I live a full life, and relations with household adjusted.

Riboxine (Inosine) ampoules - Instructions for Use, Dosage, Side Effects, Reviews

Pharmacological group: Anabolics.

Synonyms: An Jie Di Lin, An Qi Mi Rui, Ba Quan, Bioxin, Catacol, Correctol, Dan Ze, De Yi Mei, Di Li, En Li Ke, Fu Li Ding, Fu Li Xin, Gan Ke, Gan Quan, Hu Yue, Inosie F, Inosine Towa, Inosine-Hua Nan Pharm, Lai Mei Kang, Lan Xu, Li Fu - Binhu Shuanghe Pharm, PiDi Gan, Pu Fu, Qi Fang Neng, Quan Zhu, Riboxins, Riboxin, Riboxine, Riboxine-Darnitsa, Tonarsyl (veterinary use), WeiMeiJia, Xin Feng, Yan Luo Qi, Yi Rong Xin, Ying Di Te (Inosine and Citicoline), Yong Rui Neng, Ze Bei, Zhu Lu, Zuo He, Antikataraktikum N, Catacol, Correctol, Lumiclar.

Active substance: Inosine.

Inosine is a nucleoside that is formed when hypoxanthine is attached to a ribose ring (also known as a ribofuranose) via a β-N9-glycosidic bond.

Inosine is commonly found in tRNAs and is essential for proper translation of the genetic code in wobble base pairs.

Knowledge of inosine metabolism has led to advances in immunotherapy in recent decades. Inosine monophosphate is oxidised by the enzyme inosine monophosphate dehydrogenase, yielding xanthosine monophosphate, a key precursor in purine metabolism. Mycophenolate mofetil is an anti-metabolite, anti-proliferative drug that acts as an inhibitor of inosine monophosphate dehydrogenase. It is used in the treatment of a variety of autoimmune diseases including granulomatosis with polyangiitis because the uptake of purine by actively dividing B cells can exceed 8 times that of normal body cells, and, therefore, this set of white cells (which cannot operate purine salvage pathways) is selectively targeted by the purine deficiency resulting from inherited metabolic diseases (IMD) inhibition.

Inosine Reactions

Adenine is converted to adenosine or inosine monophosphate (IMP), either of which, in turn, is converted into inosine (I), which pairs with adenine (A), cytosine (C), and uracil (U).

Purine nucleoside phosphorylase intraconverts inosine and hypoxanthine.

Inosine is also an intermediate in a chain of purine nucleotides reactions required for muscle movements.

Inosine was tried in the 1970s in Eastern countries for improving athletic performance. Nevertheless, the clinical trials for this purpose showed no improvement.It has been shown that inosine has neuroprotective properties. It has been proposed for spinal cord injury; because it improves axonal rewiring, and for administration after stroke, because observation has shown that axonal rewiring is encouraged. You can buy Riboxin.

After ingestion, inosine produces uric acid that is suggested to be a natural antioxidant and a peroxynitrite scavenger with potential benefits to patients with multiple sclerosis (MS). Peroxynitrite has been correlated with axon degeneration. In 2003, a study was initiated at the University of Pennsylvania MS Center to determine whether raising the levels of uric acid by the administration of inosine would slow the progression of MS. The study was completed in 2006 but the results were not reported to NIH. A subsequent publication hinted at potential benefits but the sample size (16 patients) was too small for a definitive conclusion. In addition, the side effect of the treatment was the development of kidney stones in four of 16 patients. Thus, additional studies are necessary to prove the treatment's efficacy.

Inosine (Riboxin) is classified as an antiviral.

Riboxin (Inosine ) at Fitness

Despite lack of clinical evidence that it improves muscle development, inosine remains an ingredient in some fitness supplements.

Feeding Stimulant

Inosine has also been found to be an important feed stimulant by itself or in combination with certain amino acids in some species of farmed fish. For example, inosine and inosine-5-monophosphate have been reported as specific feeding stimulants for turbot fry, (Scophthalmus maximus) and Japanese amberjack, (Seriola quinqueradiata). The main problem of using inosine and/or inosine-5-monophosphate as feeding attractants is their high cost. However, their use may be economically justified within larval feeds for marine fish larvae during the early weaning period, since the total quantity of feed consumed is relatively low.

Inosine monophosphate dehydrogenase (IMP)

IMP dehydrogenase (Inosine-5'-monophosphate dehydrogenase) (Inosinic acid dehydrogenaseis) (IMPDH) an enzyme that converts inosine monophosphate to xanthosine monophosphate:

inosine 5'-phosphate + NAD+ + H2O ⇌ {\displaystyle \rightleftharpoons } \rightleftharpoons xanthosine 5'-phosphate + NADH + H+

Inosine monophosphate dehydrogenase catalyzes the rate-limiting reaction of de novo GTP biosynthesis.

IMP dehydrogenase is associated with cell proliferation and is a possible target for cancer chemotherapy. Mammalian and bacterial IMPDHs are tetramers of identical chains. There are two IMP dehydrogenase isozymes in humans. IMP dehydrogenase nearly always contains a long insertion that has two CBS domains within it.

The structure of this enzyme is composed of a TIM barrel domain with two CBS domains inserted within a loop.

It is inhibited by Mycophenolic acid, ribavirin, and 6TGMP (6-thioguanine monophosphate). 6TGMP inhibition prevents purine interconversion and thus the synthesis of purine nucleotides.

ATC C01EB Drugs for treatment of other diseases of the heart.

Nosological classification (ICD–10)

E80 Disorders of porphyrin and bilirubin;

I20 Angina [ angina ];

I21 Acute myocardial infarction;

I25 Chronic ischemic heart disease;

I42 Cardiomyopathy;

I49.9 Heart rhythm disturbances, unspecified;

K73 Chronic hepatitis, not elsewhere classified;

K74 Fibrosis and cirrhosis;

R07.2 Pain in the Heart;

T46.0 Poisoning by cardiac glycosides and drugs of similar action.

Pharmacological action

Riboxinum - derivative (nucleoside) purine - predecessor. Adenosine triphosphate (ATP). Refers to a group of drugs that stimulate the metabolic processes.

Riboxin has antihypoxia and antiarrhythmic effect. Increases the energy balance of the myocardium, improves coronary circulation, prevents the effects of intraoperative renal ischemia. Directly involved in the metabolism of glucose and promotes activation of metabolism in hypoxic conditions and in the absence of ATP. Activates the metabolism of pyruvic acid necessary to ensure the normal process of cell respiration and promotes activation of xanthine dehydrogenase. Stimulates the synthesis of nucleotides, enhances the activity of certain enzymes of the Krebs cycle. Penetrating into cells, has a positive effect on metabolism in the myocardium increases the force of heart contractions and promotes more complete relaxation of the myocardium in diastole, resulting in increased stroke volume. The mechanism of antiarrhythmic action until the end is unclear. Reduces platelet aggregation, activates the regeneration of tissues (particularly infarction and gastrointestinal mucosa).

Pharmacokinetics

Metabolized in the liver to form glucuronic acid and its subsequent oxidation. In small amounts excreted through the kidneys.

Riboxin Dosage

The drug is used IV jet slowly drip (40–60 drops/min). Treatment is initiated by introducing 200 mg (10 ml solution of 20 mg/ml), 1 time/day, and then, if tolerated, the dose was increased to 400 mg (20 ml solution of 20 mg/ml) 1–2 times/day. Duration of treatment - 10–15 days.

Bolus drug may acute when arrhythmias in a single dose of 200–400 mg (10–20 ml of 20 mg/ml).

In order to protect renal pharmacological subjected ischemia Riboxinum introducing IV single bolus dose of 1200 mg (60 ml solution of 20 mg/ml) for 5–15 min before the renal artery clamping, and then another 800 mg (40 ml solution of 20 mg/ml) immediately after the restoration of blood flow.

For IV drip a solution of 20 mg/ml diluted in 5% dextrose (glucose) solution or 0.9% sodium chloride (250 mL).

Riboxin Overdose

Currently, the cases of overdose have been reported.

Riboxin Drug Interactions

Reduce the effectiveness of immunosuppressants Riboxinum.

In a joint application with cardiac glycosides drug can prevent the occurrence of arrhythmias, amplify positive inotropic effect.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Riboxin (Inosine) Side effects

Allergic reactions: itching, redness of the skin (the drug should be discontinued.)

Rare: increased concentration of uric acid in the blood, increase gout (with prolonged use).

Indications for Riboxin

Comprehensive treatment of myocardial infarction, coronary heart disease, heart rhythm disorders associated with the use of cardiac glycosides, amid myocardiodystrophy after infectious diseases;

Liver disease (hepatitis, cirrhosis, fatty degeneration);

Operations in the isolated kidney (as a means of pharmacological protection when you turn off blood circulation).

Contraindications for Riboxin (Inosine)

Gout;

Hyperuricemia;

Pregnancy;

Lactation;

Age 18 (efficacy and safety have not been established);

Hypersensitivity to the drug.

Precautions: renal failure.

Cautions

Riboxinum not applicable for emergency correction of disorders of cardiac activity.

When the itching and redness of the skin drug treatment should be discontinued.

During prolonged treatment is desirable to control the concentration of uric acid in the blood and urine.

Riboxin Reviews

Riboxinum drug used in bodybuilding to support the heart muscle during the "dry", and for the anabolic properties. The latter, however, are greatly exaggerated - no 10 kg of muscle per course with him not to increase. In medicine, it is known as a means to increase coronary blood flow, and the treatment of various heart diseases.

Application Riboxinum bodybuilding
The effect of receiving Riboxinum Inositol used in sport as the iron in the form of conventional tablets and injections pharmacy, and as a component of some fat burners. There it is necessary to support the work of the heart, which is experiencing higher loads during the "drying". There are some drugs Riboxinum of sports nutrition lines, usually called Inosine.

The drug has anabolic properties and affects the metabolism, but the gain in muscle mass and strength can not be expected from him.

In the 70s of the last century Riboxinum widely used in bodybuilding and sports of force, it was later proven that his influence on the processes in the Krebs cycle and metabolism has nothing to do with the growth indicators of strength in athletes. Not reflected in its reception and the structure and muscle density.

There is a belief that the drug affects the recovery of muscle tissue, and can be used in the process of weight loss, as the anti-catabolic. Indeed, such properties are not expressed in the preparation, and wishing to lose weight only take it to protect cardiac muscle overload, and further its power.

How to take Riboxinum bodybuilding
As riboksin bodybuilding answer to the question of how to take Riboxinum bodybuilding depends on indication for use. For the purpose of improving the performance of the cardiovascular bodibildera system applied dosage of 1.5 - 2.5 g of substance in the form of tablets, half an hour before meals, three times a day. Start using tablets with half the dosage - 0.6 grams 3 times per day. If well tolerated, the amount of the substance increases.

Need to track inositol as a component in sports foods, and adjust the dosage. The injectable form is considered less hepatotoxicity, but in the practice of body building is used little.
Side effects

Common side effects Riboxinum arising Propafenone - allergic reaction, possible aggravation of pre-existing gout. When poor tolerability noted bradycardia and flushing. Then the drug overturned. Contraindications: acute renal failure

Reviews Riboxinum
Analyzing feedback on Riboxinum in bodybuilding, it may be noted that the taking is not only wishing to gain muscle mass, but also slimming. And most of the information of such a plan comes from them. Of course, to lose 5-10 kg inositol without diet yet it failed anyone yet, because there is a certain amount of disappointment, however.

Not happy Riboxinum and striving for muscle gain, especially if the latter are engaged in too little. The drug is quite specific, and keep track of a healthy person is difficult to real work.

Semax Nasal Spray

Impaired memory and attention

Memory impairment - one of the earliest signs of age-related diseases or disorders caused by a variety of brain functions. The main cause of memory decline - irreversible death of nerve cells. The first to suffer short-term memory and memory quality, which has a bad effect on the quality of work and life. Treat such memory impairment may be using the drug "Semax 0,1%."

Save memory in the modern world
Impaired memory and attention
The rapid pace of today's world everyone is faced with huge amounts of information. Therefore, for anyone who wants to keep up, succeed and just feel comfortable, it is very important a good memory and ability to concentrate. However, the problem of reducing or disorders of attention and memory, almost all familiar - someone from school or college students, anyone - from 30-35 years. A memory improvement in older - is an urgent need of almost every after 50-55 years.
What causes impaired attention and memory problems?
The deterioration of the ability to memorize and reproduce information contribute to:

stresses, violation of work and rest;
increased mental and emotional stress;
diseases of the cardiovascular or nervous system;
unhealthy lifestyle and bad habits.

Who suffers from a short-term memory, so that people do not remember firmly and constantly forgets the events of the recent past and the long-term. Therefore, to preserve and improve the ability to memorize is recommended to follow a healthy lifestyle, to respect the sleep mode, as well as the time to pass diagnosis and treatment of diseases. However, this may not be enough to remedy the situation and is taking medication to improve memory and attention. To understand how effective the medication must act to improve memory, you need to know the mechanism of learning new information.

How does our memory work?

The mechanism of memory formation consists of three stages:

Initial processing of the information;
the transition from short-term memory to long-term;
information retrieval or playback.

N Acetyl Semax - Means to improve memory
For the full and meaningful effect of drugs to improve memory should affect all three of the described stage - but many affect only the first two phases of the memory trace formation.

The unique mechanism of action Semax 0,1% provides the effect of the drug on all three stages of the formation of the memory trace, allowing you to achieve effectively improve memory and attention. This comprehensive "triple" action is a practical and convenient solution that allows to achieve the best possible result.

Nootropic Nasal Spray Protection against loss of memory
Prevention is preferable to treatment of memory disorders, but even the early detection of problems and timely initiation of medication to improve memory will significantly slow down or stop the pathological process. In the absence of treatment of the initial disturbances are moving into a more severe form, which ultimately may result in total or partial loss of memory.
"Semax 0,1%" - a unique neurotrophic agent to improve memory and treat memory impairment - prevents the build-up of a critical mass of pathological changes in the brain tissue and contributes to the speedy restoration of the disturbed functions of the brain:

It creates optimal conditions for protein synthesis in neurons;
New interneuron forms a connection that allows the normally functioning cells to increase efficiency;
increases neuronal survival, with cerebrovascular insufficiency, which is present;
restores cognitive function;
It normalizes the autonomic centers.

Interneuronal communication - process of transferring information between neurons - the cells of the nervous system.

Cognitive function - brain functions, with the aid of which the process of understanding the world. These include memory, attention, psychomotor coordination, speech, account, thinking, orientation, planning and control of higher mental activity.

Autonomic centers - centers of the nervous system, regulating the function of internal organs.

Buy Semax - Asthenic-neurotic disorders
Increased psychological and mental fatigue, irritability - the first signs of asthenic-neurotic disorders. Their treatment - a complex process that requires versatile effects on the body. Applying medication "Semax 0,1%", it is possible to organize the work of the brain centers responsible for performance, stress, and emotions.

Serious causes of a bad mood
Semax Effect – at Asthenic-neurotic disorders
Asthenoneurotic disorders are much more common pathology than is commonly believed. In varying degrees, they accompany all the most important human pathologies - so asthenic-neurotic syndrome may occur with the flu and other infectious diseases, with life difficulties and stressful situations, diseases of the cardiovascular, respiratory, nervous and digestive systems, cancer pathology, psychiatric disorders.

Warning signs
The symptoms of asthenic-neurotic disorders are typical, but depending on their cause vary in their strength and severity, from irritability, fatigue, weakness, early fatigue sets - for example, the flu, until complete exhaustion of mental and physical functions in conjunction with excessive excitability, with a sense of constant internal voltage with a decrease in performance, memory and attention, and severe sleep disturbances in neurasthenia, chronic fatigue syndrome, or a variety of brain lesions - after a traumatic brain injury, neuroinfections and so on. Neurotic disorders often occur in patients with cerebrovascular diseases and pathological circulatory disorders.

Unfortunately, many patients do not attach importance to danger signs, "drowning" them with various stimulants.

Rules of admission "Semax 0,1%"
The daily Semax dosage - Reception 14 days

Duration of reception Semax - 3 drops in each nostril, 3 times a day

The amount of the Semax Nasal Spray on the course - Course 4 bottles; 2-4 courses per year
vial contains 60 drops
Instill produce strictly to the nasal mucosa.

Complications of treatment asthenia
Treatment of asthenic-neurotic disorders is a complex problem, because at the same time you need to work on two divergent mental process - on the one hand, this is a decrease of weakness and drowsiness, and increase efficiency, on the other hand - reducing excessive irritability, anxiety and irritability. The only drug having anti-asthenic effect, increases memory efficiency, and on the background of normalization of mental activity - reduced excitability, anxiety, and irritability - is Semax. Complex action of this drug makes it one of the most effective drugs in asthenia.

The causes of fatigue:
prolonged severe stress on the nervous system;
chronic stress, mental tension, emotional stress;
too much work to be done by a certain date;
Chronic lack of sleep, lack of proper rest, and so on. etc .;
violations of metabolic processes in the brain;
lack of vitamins in the diet;
viral and bacterial infections that occur with neurotoxicosis;
hypoxia during labor and birth injuries;
craniocerebral trauma (even minor);
poisoning (including chronic: alcohol, nicotine and drug intoxication);
transferred inflammatory diseases of the central nervous system (encephalitis, meningitis);
chronic liver and kidney disease.

The combined effects of Semax Drop
Due to the positive influence on the work of nerve cells, Semax can successfully improve resistance to stress and stimulate psycho-emotional processes. Admission Semax drop - effective nootropic new generation - provides a quick recovery of the nervous system, normalization of the regulatory systems of the brain, and the violation of which causes a lot of emotional problems.

The positive effect of N Acetyl Semax Spray in the treatment of asthenia:
optimization of activity emotional centers of the brain;
performance return;
improved concentration;
increase resistance to stress, especially when changing the environment community;
normalization of sleep;
memory recovery due to the influence of all three phases of its formation;
normalization of the vegetative centers, prevents mental exhaustion.

Semax shows high efficacy in the treatment of asthenic-neurotic disorders of various origins, and returns the joy of life.

Nasal Drops Semax - Instruction, Dosage, Side Effects, Review

Pharmacological group: Nootropics.

Synonyms: Minisem.

Active substance: Methionyl-glutamyl-histidyl-phenylalanyl-prolyl-glycyl-proline.

Indications for Semax

- Intellectual and mental disorders in vascular brain lesions, post-traumatic brain injury, brain surgery and anesthesia;

- Encephalopathy, transient ischemic attacks (TIAs) and neurotic disorders of various origins, including after ionizing radiation, the recovery period after a stroke;

- To increase the adaptive capacity of the human body in extreme situations;

- Prevention of mental fatigue when the monotone operator activity in the most intense periods of work in a stressful environment.

In ophthalmology: Semax used in optic nerve atrophy, neuritis, inflammatory, toxic and allergic etiology.

In pediatrics: as nootropic agents in children aged 7 years in the treatment of minimal brain dysfunctions (including ADHD - Attention Deficit Hyperactivity Disorder).

Semax dosage

Semax applied intranasally using a bottle, a sealed plastic cap-pipette.

One drop of the standard solution contains 50 mg of active substance. Pipette the solution of the drug in an amount of not more than 2-3 drops administered in each nostril. If necessary, increase the dosage administration is carried out in several stages with intervals of 10-15 minutes.

When intellectual-mental disorders, vascular brain lesions, encephalopathy, transient ischemic attack single dose of 200 - 2000 mg (per 3 - 30 mleg / kg).

The daily dose of 800-8000 mg (calculated 7-70 mcg / kg).

The drug is prescribed for 2-3 drops in each nostril four times a day for 10 -14 days, repeat the treatment if necessary.

After a traumatic brain injury, brain surgery and anesthesia single dose of 1400 - 3500 g (40-50 mg / kg) 3 times a day for 3-5 days. If necessary, treatment is extended up to 14 days.

To increase the adaptive capacities of the human body and the prevention of mental fatigue 3-5 days 2-3 drops in each nostril 2-3 times in the first half of the day. The daily dose of 400-900 mg / day. repeat the treatment if necessary.

In diseases of the optic nerve drug instill 2-3 drops in each nostril 2-3 times a day. The daily dose of 600-900 mg / day. The course of treatment 7-10 days. Furthermore, the drug can be administered by intranasal electrophoresis drug is injected from the anode. The current strength of 1 mA, duration of exposure 8.12.15 minutes.
The daily dose of 400-600 mg / day. The course of treatment 7-10 days.
In pediatrics:
Children from 7 years old. With minimal brain dysfunction: 1-2 drops in each nostril (the rate of 5-6 mg / kg) 2 times a day (morning and afternoon). The daily dose of 200-400 mg / day. The course of treatment for 30 days.

Semax Side effect
Prolonged use may slight irritation of the nasal mucosa.

Semax Drug interactions
Pharmaceutical
Based on the chemical structure of the drug presence of chemically incompatible combinations are not supposed to: the drug quickly breaks down and does not enter the digestive tract.

Pharmacokinetic
Given the chemical structure of the drug (heptapeptide - a synthetic analogue of adrenocorticotropic hormone, completely devoid of hormonal activity), the speed of absorption and the rate of admission into the bloodstream, as well as intraiazalny route of administration, the effect of other drugs on the pharmacokinetic parameters of Semax nasal drops 0.1% is expected. Given the route of administration Semax nasal drops 0.1% (intranasal) administration desirable agents possessing local vasoconstrictor activity when administered intranasally.

Semax for children
Combination with other neuroprotective drugs
Q - Is it possible to combine with a course of reception Semax nootropil? Cogitum?
Answer - Semax important feature - the lack of interaction with other drugs. Semax does not violate the actions of other medicines, so used in any combination therapy.
Combine with Semax nootropil (piracetam) does not make sense, because Semax surpasses it in nootropic effect; other effects have no piracetam.
With Cogitum can be mutual reinforcement of clinical activity, since drugs in the CNS have a different point of application, but the effect is the same direction. However, it is desirable to use drugs in a child up to 16.00, as possible sleep disorder (present at Cogitum stimulating effect, which may overlap antiastenic effect Semax).

Semax for child two years, safety

Question - Doctors prescribe Semax children, and in the instructions contraindications age - up to 7 years. For some reason, there is a contraindication? What happens to the baby?

Answer - Semax has a normalizing effect on the neurons of the brain and, consequently, on brain function. Moreover, the more depressed brain function (eg, voice), the drug will be more active. Semax therapeutic effect appears in all CNS: it increases the synthesis of neurotrophins brain that enhances neuronal plasticity of the brain and their functions are normalized.

With regard to instruction. Currently, there are instructions, which stated that Semax prescribed to children from 7 years. Where appropriate, the application of the drug issues not addressed instruction of the Ministry of Health standards for the treatment of a separate decree.

The clinic of Pediatrics Medical University conducted a study in which, Semax administered to children, starting from 3-6 months, with good clinical results and without significant side effects. Based on these studies, the Ministry of Health of the Russian Federation included in treatment standards Semax retinopathy of prematurity. While a change in the instructions are not made, the need for Semax children determined by the attending physician.

Statistics show that more than half of all medicines used in pediatric practice, not shown in children and their use in children regulates doctor the relevant specialty. Semax is one of the safest drugs currently available on the pharmaceutical market, not only in Russia but also in the world, in spite of 17 years of clinical experience of its use did not report any serious adverse disorders or symptoms of overdose, including in children's practice.

Most of the drugs used in medicine, children and adults can cause ambiguous effects, for example, in children is more pronounced side effects of drugs. First of all, this is due to the immaturity of the systems of neutralization of drugs in the liver. The action of Semax on children and adults equally. Equally high for them and the safety of the drug. Especially that Semax metabolism is not associated with liver enzymes, and is carried out by tissue enzyme systems responsible for the degradation of endogenous proteins and forming in utero development.

Semax at ADHD
Question - child 7 years old, diagnosed with hyperactivity, attention deficit, before school pediatrician recommends 0.1% Semax help at ADHD?
Answer - "Semax 0,1%" has been used successfully for the treatment of ADHD. Due to its effects, the drug helps to reduce the symptoms of ADHD, helps the child to adapt to a new school and mental stresses, increases perseverance, positive effect on memorizing new material, reduces emotional lability.

Semax with delayed mental and speech development (CRA)
Question - A child 10 years old diagnosed with mental and speech development delay, have a problem in correctional school (impaired attention and consideration, distraction) which better concentration of drug use 0.1% or 1%?
Answer - Semax solution of 1%.
The course is 1 drop in each nostril 2 times a day. From the practice of the pediatricians at CRA assignment - 21 days.

Semax at TBI
Semax and Recovering from a traumatic brain injury
Q - What can help Semax after a head injury?
The answer Semax prevents and reduces the effects of TBI. It stimulates the regeneration of damaged shock or injury when cells stop damaging chain of changes in the brain. It helps in restoring the memory, speech and movement, prevent and reduce the long-term effects of head trauma, such as reduced vision, memory disorders, and others.

How can help Semaks drop in head injury?
Question - Do Semax really speed up recovery after TBI?
Answer - Semax unique product created just for restoration of disturbed functions of the CNS. It prevents the destruction of damaged neurons, promoting their rehabilitation and inclusion in the work, allowing the surviving trauma cells take over the function of the victims.
Semax intranasally injected: in this case, during the preparation of the olfactory nerves directly penetrates into the brain and rapidly exerts its therapeutic effect, thereby accelerating the recovery. Therefore, "Semax 0,1%" recommended for TBI to prevent complications.

Semax and Anesthesia
Question - How can Semax reduce the effects of anesthesia?
Answer - "Semax" protects nerve cells from oxygen starvation and caused them damage which is adverse reaction to anesthetic agents. To expedite and facilitate the way out of the anesthesia, as well as to restore the normal functioning of nerve cells after it.

It is recommended to use "Semax 0,1%" for 3-6 days before the operation and another 3-6 days after her 3 drops in each nostril 2 times a day.

In the future, repeat courses "Semax 0,1%" will help reduce the effects of the old general anesthesia on the nervous system.

Restore memory after anesthesia
Question - Can Semax shorten the recovery of memory due to its deterioration after anesthesia?
Answer - Applications Semax able to restore memory (especially short-term) and to enhance attention. It restores the functional activity of neurons impaired due to exposure to harmful factors (in this case, means for anesthesia), thus reducing the time of recovery of memory.

Semax at Stroke
You can enable Semax by the complex in the treatment of stroke?
Q - Is it possible to drip Semax stroke simultaneously with other medications?
Answer - Adding to the "1% Semax" comprehensive treatment of the drug, and possibly justified - it is beneficial and does not disturb the action of other drugs. "Semax" absorbed into the bloodstream through the nasal mucosa and the olfactory nerves and blood flow quickly and freely passes directly into the nervous tissue of the brain, eliminating unwanted drug interactions with other medications applied.

Semax at Recovering lost brain function after an ischemic stroke
Question - Is Effective Semax as secondary prevention of ischemic stroke?
A - Currently Semax 1% is one of the most effective drugs used to restore the lost functions of the brain after a stroke. Semax has a pronounced clinical benefit in the treatment, and in recovery from stroke.
However, you must remember, the sooner treatment is started, the more relevant the results will be obtained.

Paralysis of arms and legs after stroke - how to restore motor function?
Question - Can help Semax after suffering a stroke five years ago with partial lesion of the right arm and a leg?
A - 5-7 years ago it was believed that post-stroke recovery lasts approximately one year, and then there is the stabilization of the state of progress. It has now been shown that the recovery processes can stimulate about at any one time.
Semax 1% is an effective drug nootropic group recommended for the treatment and recovery after stroke.
A great advantage of the drug is to prevent recurrent stroke: the likelihood of stroke in patients receiving Semax decreases 2.5-3 times.
The recommended dosage regimen: "Semax % 1" to 2 drops in each nostril 3 times a day, 14 days, can repeat the course in 3-6 months.
In the future, it is recommended for the prevention of the use of "Semax 0,1%," according to the scheme: 3 drops in each nostril 3 times a day, a course of 14 days, 2-4 courses per year.

Semax at Recovering from a stroke
Q - Sometimes doctors recommend Semax only in the acute phase, and then in rehabilitation applications Semax does not make sense, is it?
Answer - When stroke "Semax 1%" is highly effective not only in the acute phase, but also in early recovery. In the future, we recommend using "Semax 0,1%" for prevention and rehabilitation.

Semax creates optimal conditions for the survival of neurons by activating them in the metabolic and plastic processes. Saved cells take on the functions of the dead, and thus reduces the degree of disability of a sick person.
An important effect of Semax is its positive effect on cognitive function, especially when the defeat of stroke: use Semax accelerates and enhances memory recovery, focus, mental and physical performance.

Semax and Glaucoma
Why Semax is used in ophthalmology, such as glaucoma
Question - Why Semax is suitable for the eyes and for the nerves? How it can help with glaucoma?
Answer - Yes, "and for the eyes and for the nerves" is used one and the same drug - "Semax 0,1%."
Semax - neuropeptide assistant nerve cells, normalises and restores their work. The main cause of blindness in glaucoma - this is the death of optic nerve fibers under the influence of the chain of pathological processes running high intraocular pressure. Even if the pressure in the eye leads to the normal process of progressive damage to the optic nerve does not stop immediately, but continues for some time.
Preparation "Semax 0.1%" has no effect on the intraocular pressure, but helps to prevent or reduce damage to the optic nerve and interrupt circuit changes running high intraocular pressure. The maximum result from the use of "Semax 0,1%" will be received subject to prior normalization of pressure in the eye with the help of medication (drugs that reduce intraocular pressure) or surgical treatment.

Semax at glaucoma against the background of non-normalized IOP
Question - Is it necessary to stabilize the IOP in glaucoma and then drip Semax? Or Semaxs take after surgery?
Answer - Semax shows effect in the treatment of glaucoma only background normalized intraocular pressure (IOP).
Semax itself does not affect the level of IOP, but the recovery of retinal functions damaged by elevated IOP. If medications can not normalize the IOP, then surgery is needed, and after surgery - Semax.
Please note, if even after normalizing operation IOP, glaucoma development continues because of the running processes of death of retinal cells, the surgery is extremely important to use Semax to this process as much as possible to slow down or stop.

Glaucoma 3 stages. Optic atrophy
Question - Do Semax will be effective in the third stage of glaucoma disease, can be prevented atrophy of the optic nerve? And how to take the drug?
Answer - You're right, Semax - not a panacea and if the fibers of the optic nerve or visual retinal cells are lost, it will not help.

However Semax:
- Protects from destruction still alive fibers and cells;
- Restores the functional activity of a large part of the optic nerve and visual cells in the retina fibers that glaucoma are at parabiosis (still alive, but do not work). Due to these cells and nerve fibers, which were to be killed, but when taking Semax recovered and earned, is the eye functions increase, including the field of view. Semax shown at any stage of glaucoma and in the background of any of the treatment.

In glaucoma, the eye and optic nerve atrophy Semax applied from 2000's. To date, it was held on 3 placebo-controlled studies (1999, 2001 and 2011) with the total number of patients more than 300 people.

Intranasal application used "Semax 0,1%» 3 drops in each nostril, 3 times a day. Recommended courses of 14 days every 3-6 months.

Semax for Improving memory and attention

Focus on work assignments and to adequately cope with the usual work is becoming increasingly difficult? The brain simply refuses to memorize large amounts of information? Improve memory, you can use nootropic drops "Semax 0,1%", which normalize the operation and interaction of brain cells.

Semax - Effective means for the brain
Semax for Improved memory and attention
You want to concentrate better at work or to receive the information? Innovative nootropic drops in the nose "Semax 0,1%" can effectively stimulate the process of improving memory and more successfully cope with the tasks. "Semax 0,1%" has a specific effect on the integrative functions of the brain and increases its resistance to damaging factors - such as stress and fatigue. This is due to the interaction normalization of brain cells - neurons. As a result, healthy people using "Semax 0,1%", observed improvement of memory and the increased focus that contributes to the high intellectual activity throughout the day.

Nootropics - Medicinal products intended to influence the higher functions of the brain. Improves memory, stimulates mental activity, enhance and facilitate the learning process.

Chronic fatigue - Status loss of activity and the ability to pursue any of the activities. It affects the physical and intellectual abilities, reducing the quality of life.

How does this happen?
"Semax 0,1%" contributes to the improvement of human memory in all three phases of education:

information processing proceeds to step brain
Systematization of the data
Retrieving information from memory

This complex action makes "Semax 0,1%" unique representative of a class of nootropics - new generation nootropic.
High efficiency and safety of the drug was confirmed by authoritative research and clinical use since 1994.
Semax Course admission is only 10 days, and improved memory is stored up to 3-6 months.

The intense pace of life and "Semax 0,1%"
On the daily intellectual activity, attentiveness and discipline is largely influenced by factors such as stress, nervousness, high mental stress. Therefore, a person who wants to improve attention and memory, thus increasing their intellectual performance, can use the appropriate means. If you can not reduce the load, taking medication can help the body to cope successfully with all the challenges. "Semax 0,1%" - this drug to improve memory, has integrated nootropic, neurometabolic and neurotrophic effect.

Neuro-metabolic effect - The ability of drugs directly or indirectly to improve the metabolism of the central nervous system.

Neurotrophic action - ability of drugs to maintain the viability of nerve cells - neurons.

Drip drop, or swallow pills to improve memory?
Release Form "Semax 0,1%" - nasal drops, so the drug has such an advantage, such as high bioavailability and lack of drug-drug interactions. For example, taking a capsule or pill to improve memory, it should be remembered that the effectiveness of such dosage forms release below and possible adverse interactions with other medications taken due to the passage of the active ingredient through the gastrointestinal tract, liver and kidneys.

An additional advantage of intranasal administration - is to get the result as in the one-off admission and at course.

The effect of the exchange rate will be higher and persist longer, but also receive a one-time "Semax 0,1%" 30-60 minutes before an important event will allow a person to achieve improvement of attention, memory, and most focus on the task at hand.

Semax for Improving mental health

Permanent overload at work, challenges and problems, lack of sleep and lack of rest gradually lead to chronic nervous exhaustion and a noticeable decrease in mental performance.
Semax help to improve the situation and restore the lost brain activity can be in just 10 days.

Mental fatigue - the enemy of man
Improving mental health and stability of attention
Reduced mental capacity may be due to constant fatigue, lack of physical activity, violation of work and rest, chronic fatigue and the lack of a full annual holiday. When the brain gets tired and is in constant tension, do not force yourself to wait for memory impairment, loss of concentration and stability of attention, decreased performance.

Chronic fatigue - Status loss of activity and the ability to pursue any of the activities. It affects the physical and intellectual abilities, reducing the quality of life.
Innovative means "Semax 0,1%" enhances mental performance through increased brain activity and allows you to:

Increase the concentration and stability of attention; Remove mental fatigue; It is easier to process the information and will use it due to the influence on all stages of memory formation; Maintain fully operational and brain health, even under conditions of stress and fatigue; Restore the cycle sleep / wake; To reduce the impact on the nervous system hazards and stress.

"Semax 0,1%" - a simple and safe way to improve mental health and recovery of lost brain activity.

The hard life of the mind
Colossal incoming pressure of responsibility and challenges, "manager syndrome", in financial difficulties, disrupted daily routine, bad habits, unhealthy environment - all this is not the best way affects the human brain to the nerve cells and their interaction. In the brain and nerve pathways play a key role regulatory peptides, secreted by nerve cells. These agents regulate processes taking place in the brain. But the possibility of its own regulatory peptides are limited. Accumulating minor violations can lead to full-fledged serious diseases.

A coffee will not help?
Coffee, energy drinks and tonics, even if for a while and help to awaken the body, can cause serious damage in the future. And vitamins to improve memory efficiency, improve mental activity can be used as an addition to receiving the drug "Semax 0,1%."

Healthy lifestyle
Do not forget that "Semax 0,1%" promotes mental health, but it is no substitute for a healthy lifestyle, proper rest and proper nutrition - and this is an important step in the treatment of fatigue and related offenses.

Preservation of youth and brain health
Memory, attention, intellect - the higher brain functions. Healthy people are beginning to notice a decrease in their activity of approximately 35-40 years. Slow down or stop the deterioration of the brain age, correct sleep disorders, reduce mental fatigue helps "Semax 0,1%" - a drug that restores brain function.

Semax Nootropic - Creative engine
Improve memory and brain function
Saving mind clear and effective creative thinking available at any age, the elderly, and even in old age.

The preparation "Semax 0,1%" helps to improve brain function, preserving its young and active for many years at the expense of conservation and restoration of damaged relationships nerve cells in the brain, as well as their regeneration Tip. These nerve cells - neurons - are experiencing tremendous stress and need help. In his youth, it does not usually think, but in old age and old age, the administration of drugs for the brain becomes a vital necessity. With age, people need to purposefully strive for improving brain health in order to maintain their intellectual abilities into old age. After all, a healthy, fully functioning mind and the brain as a physical manifestation of his make us who we are.

Alarm bells come with age
The development of many age-related undesirable changes in the brain can be prevented - it is important not to miss the appearance of the first warning signs. The main symptoms of which began in the brain aging process are memory impairment, slight at first, scattering attention and problems with his concentration, blurred vision, hearing loss, fatigue, dizziness, frequent headaches, sleep disturbances, severe recovery after illness, and so on. All these manifestations - an occasion to reflect on the medication to improve brain function. Modern medicine offers a wide variety of products and forms of their release - as a tablet for the brain, and drugs in the form of injections, but there is a way to more modern and better.

Semax Spray - Intranasal - it is effective and convenient
The preparation "Semax Spray 0,1%" - a drop in the nose. This form has a number of advantages:

Lack of drug-drug interactions - the elderly and often taking different sets of tablets of the brain, heart and blood vessels, gastrointestinal tract, etc.
High bioavailability - 60-70%
The speed of onset of effect - treatment takes only 10 days

The older people get, the more we appreciate life and its joys. The years do not add health to us. After all, nothing so depressing as the feeling of being lost forgotten or something important and necessary. Therefore, not only to preserve but also to improve memory and brain function, it is possible to use the preparation " N acetyl Semax 0,1%."

Antidepressants General Information

Medications specifically relieving depression.

According to modern concepts in depressive states decrease serotonergic and noradrenergic synaptic transmission. Therefore, an important link in the mechanism of action of antidepressants caused their accumulation in the brain of serotonin and norepinephrine.

Common property of all antidepressants - their timoleptic action, ie, a positive impact on patient affective sphere, accompanied by improvements in mood and general mental state. Various antidepressants differ, however, the amount of the pharmacological properties. So some antidepressants combine timoleptic effect with stimulating, anxiolytic and sedative effects.

Antidepressants have been used not only in psychiatric practice, but also for the treatment of a number of neurovegetative and somatic disorders, chronic pain syndromes, etc.

Therapeutic effect of antidepressants, such as by oral or parenteral application with develops gradually and usually occurs in 3–10 days or more after the start of treatment. This is because the development of an antidepressant effect due to the accumulation and neurotransmitters in nerve endings, and the adaptive changes slowly appearing in the circuit of neurotransmitters and in the sensitivity of this receptor in the brain.

Adepress (Paroxetine) tablets 20, mg N30

Amitriptyline nycomed tablets

Amitriptyline tablets

Anafranil (Clomipramine) ampoules 25 mg, 2 ml N10

Anafranil (Clomipramine) tablets

Asentra (Sertraline) tablets 50 mg, N28

Azaphen (Pipofezine) tablets

Biotredin (Pyridoxine+Threonine) tablets

Cipralex (Escitalopram) tablets

Cipramil (Citalopram) tablets

Cymbalta (Duloxetine) pills

Deprim (St John's wort) tablets

Fevarin (Fluvoxamine) tablets

Fluoxetine pills

Heptor (Ademetionine) lyophilisate for solution vail 400 mg, N5

Heptor (Ademetionine) tablets

Heptral (Ademetionine) lyophilisate for solution vail 400 mg, N5

Heptral (Ademetionine) tablets 400 mg, N20

Ixel (Milnacipran) pills

Lerivon (Mianserin) tablets 30 mg, N20

Melipramin (Imipramine) dragee 25 mg, N50

Paxil (Paroxetine) tablets

Prozac (Fluoxetine) pills 20, N14

Pyrazidol (Pirlindole) tablets

Rexetin (Paroxetine) tablets

Asentra (Sertraline) tablets 50 mg, N28

Anafranil (Clomipramine) ampoules 25 mg, 2 ml N10

Velaxin (Venlafaxine) pills

Cipralex (Escitalopram) tablets

Cymbalta (Duloxetine) pills

Lerivon (Mianserin) tablets 30 mg, N20

Cipramil (Citalopram) tablets

Remeron (Mirtazapine) tablets

Heptor (Ademetionine) lyophilisate for solution vail 400 mg, N5

Why Semax removed from the ambulance first aid kit?

During the Christmas holidays the number of deaths is increasing exponentially. And most of the victims are people with disorders of the cardiovascular system. Many of these people could have been saved if the time came to the doctor with the right medications. But now, even if the ambulance and will reach in time – there are no essential drugs in its medicine kit anymore.

During the Christmas holidays the number of deaths is increasing exponentially. And most of the victims are people with disorders of the cardiovascular system. Scientists studied data on the health of more than 700,000 people who died in the New Year period from 1988 to 2013 and found that nearly 200,000 deaths occur as a result of cardiovascular disease. And if we talk for example about stroke in annualized terms, they occur more than 450,000 per year!

In our domestic reality mortality during the first month is 35%, and the survivors or die within a year after a stroke (usually due to repetitive), or remain disabled. Unfortunately, no more than 20% of patients return to a normal lifestyle.

Now there are over 1 million. People who have had a stroke, and more than 80% of them have a disability of varying degrees of severity. This bleak picture indeed caused by many factors, such as a doctor it is important to get in the first 3 hours after the onset of symptoms of the disease! Throw in the absence of appropriate treatment. For example, lists of regulated "Ambulance" mysteriously disappeared one of the drugs.

There is a drug called "Semax", developed back in the USSR commissioned by the Ministry of Defence. This drug, nootropic, neuroprotective, anti-oxidant action. Incidentally, Semax included in the list of vital and essential medicines, and its formulation is rather unusual for this kind of drugs - it is produced in the form of a solution of 0.1% and 1% for intranasal administration. Simply put, Semax is a conventional nasal drops.

It is important that Semax, for example, included in the standards of treatment of this terrible disease in Russia, as stroke. The fact that most of the drugs in this instance intravenously, but through an occluded vessel in stroke medicine is not able to penetrate to the affected area of the brain. Semax in the form of nose drops easily into the brain along the olfactory nerves. And he's a first aid help hospital before, in the first minutes and hours of the disease.

It is known that in stroke Semax solves questions drug delivery to brain cells (and treatment of ischemic and hemorrhagic stroke), resulting in the preservation of human life is ensured, and reduction of disability. Therefore it is better to have these drops are always in the home medicine cabinet, as well as to carry out preventive maintenance for your loved ones (but this is a separate issue, and 0.1% used for the prevention Semax).
In addition, the drug is widely used in sports medicine because it increases physical performance, speeds up the production of automatisms, increases resistance to hypoxia of the brain during intense workouts, reduces the recovery period after the competition, prevents the development of competitive stress and its complications.

Semax can appoint and to improve mental performance. By optimizing the higher functions of the brain, it improves thinking, coordination of movements, improves memory.

And now an interesting twist. Order of the Minister of EMERCOM of Russia ¹246 from 05.05.1997, the Semax included in the sets of search and rescue services of the Russian Emergencies Ministry. Order of the Health and Social Development of the Russian Federation from 5.09.2006 ¹643 Semax is included in the standard treatment of stroke by the SMP. Order of the Ministry of Health and Social Development of the Russian Federation of 27.05.2009 ¹276n Semax is included in the list of vital drugs. But N549n current order from 08.07.2013. In it we see:

1.27. Anti - hypoxants and nootropics.
1.27.1. N06BX. Psychostimulants and nootropics. Glycine, sublingual tablets.
1.27.2. N07XX. Drugs for treatment of nervous system diseases and other: inosine + nicotinamide + succinic acid + riboflavin (Citoflavin) - a solution for intravenous administration.

As can be seen, and a number of other drugs - Semax disappeared out mysteriously and left cytoflavin and glycine. I wonder why? Glycine use under the tongue, however, in the case of a stroke due to a violation of consciousness it becomes impossible, and little significant, to say the least. Citoflavin itself is pretty good, we have long and successfully use it in everyday work. However, Semax seems still more advantageous option. For example, cytoflavin administered intravenously at a rate of 60 drops per minute (0.5-1.5 hours and that - before the patient arrives in the hospital than at least half of the dose is administered). Semax is administered intranasally (through the nose) and can immediately deliver all the required dose. In cytoflavin maximum concentration occurs after about 40 minutes in the blood plasma, in Semax therapeutic effect appears after 3-5 minutes, at a stroke account goes on a minute! Both drugs have a pronounced anti-hypoxic effects, while semaks boasts more and anti-ischemic and neuroprotective.