Fenibut - Phenibutum

Phenibut (γ-amino-β-phenylbutyric acid) is an anxiolytic and nootropic agent, a β-phenyl derivative of the γ-aminobutyric acid neurotransmitter.

Trade names: Bifren, Noobut, Noofen, Fenibut, Anvifen

Phenibut was synthesized in the Leningrad Pedagogical Institute. Herzen Professor V. V. Perekalin. The study of clinical and pharmacological properties of phenibut was carried out in the laboratory of psychopharmacology of the Leningrad Scientific Research Institute. VM Bekhtereva senior researcher R. A. Khaunina.

At one time, Phenibut was among the medicines, which are necessarily included in the cosmonaut's first-aid kit. Conventional tranquilizers badly lowered the high level of astronaut stress, because in addition to calming effect, they also had a relaxing effect. With the reception of the Phenibut, the cosmonauts' working capacity remained at the same level.

In 1975, the phenybut preparation was included in the first aid kit of cosmonauts participating in the experimental flight "Soyuz" - "Apollo".

By chemical structure, phenobut can be regarded as a phenyl derivative of GABA, and also as a derivative of phenylethylamine.

Phenibut has elements of nootropic activity, has a tranquilizing effect, reduces tension, anxiety, improves sleep; prolongs and intensifies the effect of sleeping pills, narcotic, neuroleptic substances and psychostimulants.

Apply Phenibutum in asthenic and anxiety-neurotic states, anxiety, anxiety, fear, insomnia, and also as a sedative before surgical interventions.

Assign also with Meniere's disease, dizziness associated with dysfunction of the vestibular apparatus, for the prevention of motion sickness.

Children are prescribed for stuttering and tics.

There is evidence of an increase in the effect of antiparkinsonian drugs (due to the presence of a dopaminopositive component) under the influence of Phenibutum.

With the use of phenibut in children under 10 years of age who suffer from stuttering, speech impairment can occur, and a change in the picture of the electroencephalogram, including the appearance of sharp wave peaks, is possible. This drug should be given to children with extreme caution.

Indications:
Asthenic and anxiety-neurotic states, anxiety, anxiety, fears, insomnia, and also as a sedative before surgical intervention. A distinctive feature is the pronounced effect in the treatment of dizziness.

A direct effect on GABA-ergic receptors facilitates GABA-mediated transmission of nerve impulses in the CNS. Improves the functional state of the brain due to the normalization of tissue metabolism and the influence on cerebral circulation (increases the volume and linear speed of the cerebral blood flow, reduces the resistance of the cerebral vessels, improves microcirculation, has antiaggregant effect), also has a tranquilizing, psychostimulating, antiaggregant and antioxidant effect. Helps reduce or disappear feelings of anxiety, tension, anxiety and fear, normalize sleep, does not have an anticonvulsant effect, but enhances the effect of anticonvulsant drugs. Does not affect cholino- and adrenergic receptors. It prolongs the latent period and shortens the duration and severity of nystagmus. Reduces the manifestations of asthenia and vasovegetative symptoms (including headache, a feeling of heaviness in the head, sleep disturbance, irritability, emotional lability), increases mental performance. It improves psychological indicators (attention, memory, speed and accuracy of sensory-motor reactions). At the course reception increases physical and mental efficiency, improves memory, normalizes sleep; improves the condition of patients with motor and speech disorders. In patients with asthenia, from the first days of therapy, feeling better, increasing interest and initiative (motivation of activity) without sedation or arousal. In the appointment after severe craniocerebral trauma increases the number of mitochondria in the perifocal areas and improves the course of bioenergetic processes in the brain. With neurogenic lesions of the heart and stomach normalizes the processes of lipid peroxidation. In elderly people does not cause congestion and excessive lethargy, a relaxing aftereffect is most often absent. Improves microcirculation in the tissues of the eye, reduces the inhibitory effect of ethanol on the central nervous system. The drug is low-toxic, does not cause allergic action, does not have teratogenic, embryotoxic and carcinogenic properties.

Metabolized in the liver - 80-95%, metabolites are not pharmacologically active. Do not cumulate. After 3 hours begins to be secreted by the kidneys, while the concentration in the brain tissue does not decrease and it is found in the brain for another 6 hours. About 5% is excreted by the kidneys unchanged, partly with bile.

Side effects:
Usually well tolerated. At the first reception possible drowsiness, with an overdose - pronounced drowsiness, nausea, vomiting; increased irritability, agitation, anxiety, dizziness, allergic reactions.
With prolonged use, it is necessary to monitor the liver function and the peripheral blood picture. It is necessary to refrain from potentially dangerous activities requiring increased attention. It is not effective at the expressed phenomena of motion sickness ("indomitable" vomiting, dizziness, etc.).

Phenibut should not be combined with alcohol.

Duloxetine - Duloxetinum

Trade names: "Simbalta", "Intriv"

Duloxetine - Duloxetinum - an antidepressant from the group of selective serotonin and noradrenaline reuptake inhibitors (SIOSCs), also slightly suppresses dopamine uptake. The drug is approved by the FDA for the treatment of major depressive disorder, fibromyalgia and chronic neuropathic pain. Has antidepressant, anti-anxiety, analgesic properties, relatively balanced stimulating and sedative effects.

Duloxetine is contraindicated in case of individual intolerance, glaucoma. It should not be combined with MAO inhibitors. Caution should be exercised when using drugs that have a similar mechanism to duloxetine, in the presence of convulsive seizures in the past, in case of impaired liver, kidney, heart failure, arterial hypertension.

The use of duloxetine can provoke suicidal behavior or the transition of depression to a manic state. Side effects also include general weakness, dizziness, headache, dyspeptic phenomena, drowsiness, insomnia, disturbances in the accommodation of vision.

Neurotransmitter Acetylcholine

The neurotransmitter acetylcholine improves memory and concentration of attention.

Acetylcholine can be considered the most important neurotransmitter involved in the process of remembering information. This highly chemically active substance is an ester of choline and acetic acid. It contributes to the fact that information is quickly and unhindered transmitted from the senses to the main control center - the brain.

Unfortunately, with age, less acetylcholine is synthesized in the human brain. As a result of this, scientists believe, forgetfulness, problems with concentration of attention, difficulties in the selection of necessary words.

Meclofenoxate and choline serve as a basis for good brain activity. In order to improve memory in a short time and keep it clear for a long time, the famous researcher of brain activity, professor of the University of Hyssin, Wilfried Dimpfel, recommends that the concentration of the main neurotransmitter, acetylcholine, be purposefully stabilized. This can be achieved by taking choline preparations. Choline is a natural building block for the synthesis of acetylcholine molecules.

It is even better to build your own food in such a way as to ensure sufficient natural intake of choline in the body with natural food. A large amount of choline contains cabbage (especially cauliflower and broccoli), eggs, peanuts, fish, meat, hard cheese varieties, liver, milk and wheat sprouts. In addition to choline for the synthesis of acetylcholine, vitamins such as pantothenic acid (vitamin B3), folic acid, vitamins B12 and B1 are needed. Just in the elderly, as well as in people suffering from bowel disease, there is a shortage of B vitamins.

The scientists also place great hopes on deanol (meclofenoxate) - in a scientific environment known as dimethylaminoethanol (Dimethylaminoethanol) or abbreviated DMAE. With a lack of acetylcholine in the body, it can be re-synthesized in the required amount from deanol. Some medical research has proved the positive effect of this substance on brain function.

In one experiment, conducted over a period of 3 months, a group of people with memory problems and concentration of attention took medications containing deanol and choline. At the end of the experiment, problems with concentration disappeared in 84% of the subjects, memory improved in 75% of the participants in the experiment.

In addition, supplying your body with all the necessary substances for building neurotransmitter molecules by substances, do not forget that the synthesis of acetylcholine (and hence memory improvement) will occur only if the brain is actively involved, receiving sufficient information for thought and memorization. Do not be lazy to load your memory, giving it food for thought.

And one more aspect of the problem of memorization. For intensive activity, brain cells require continuous intake of energy and nutrients, which is ensured by the flow of blood. Poor blood supply leads to rapid fatigue, headache and drowsiness. So do not be lazy at least 30 minutes a day to devote to intense physical training. Only all three factors - proper nutrition, physical and intellectual loads, - in aggregate will help to significantly improve memory and keep it to a very old age.

Tablets for memory

Memory is one of the higher functions of the brain, which is influenced from outside. The main varieties of this integrative brain activity are immediate, short-term (part of the operational) and long-term memory. Memory disorders can occur both in cases of vascular pathologies in conditions of chronic oxygen starvation of the cortex, and in bacterial or viral infections, parasitic invasions, under the influence of anesthesia, hypnotics, with various intoxications, including nakrokoticheskih, alcohol and tobacco. Separately there are traumatic brain injuries, tumors and epilepsy, in which memory is disturbed significantly. Memory loss can concern both events that occurred before a certain moment (trauma), and capture the present period of time. There is also a violation, in which there is a good memory for the old facts, and the fallout concerns fresh information (this type is typical for vascular dementia in the elderly). Often, memory impairments are of a non-structured nature and relate to the difficulties of memorization.

There are electoral defects. For example, the inability to memorize dates or persons. Such deviations are hardly noticeable to others, but they can bring a lot of inconveniences in everyday life to those who suffer from them.

Since there is a wide range of diseases and functional conditions for memory disorders, it makes sense to consult a doctor in all cases when memory disorders are fixed by the patient himself or his relatives. This will make it possible to understand in due time the true causes of what is happening and not to miss the conditions that threaten not only complete loss of memory, but also life.

To diagnose memory disorders, patients undergo special testing from a neurologist or psychiatrist.

Tablets used to treat memory disorders, the so-called, mnemotropic drugs.

• 1.Cholinesterase blockers. Donezyl hydrochloride (aricept), galantamine (dilated), rivastigmine (exelon). Drugs interfere with the cleavage of acetylcholine, which facilitates the transmission of a nerve impulse in the brain cells, improves memory.
• 2.. Pyrrolidine derivatives or ratsetamy: phenylpyrazetam (phenotropil), pyracetam (nootropil, lucetam, vinpcetin, oikamide, pyrabene), aloracetam, brivaracetam, aniracetam (draganol), dupracetam, dorracetam, dimiracetam, imaracetam, nebrasetam, noopept, nefiracetam, fazoracetam, pramiracetam, rolziratsetam, rolipram, seletracetam. Activates glutamate receptors that are adjacent to acetylcholine and potentiate their action.
• 3. Derivatives of precursors of acetylcholine (dimethylaminoethanol) -aclumate deanol (noctolin, clerel, deanol), meclofenoxate (anilux, lucidryl, cerutil, acephene). Increase the content of acetylcholine, responsible for improving nerve conduction.
• 4. Group B vitamins. Pyridoxine derivatives (pyrithinol, encephabol, energibol, pyriditol). Thiamin (B1) potentiates memory, smooths out the effects of anesthesia. Niacin, nicotinic acid (B3) increases the efficiency of the brain. Cyanocobalamin (B12) improves neuromuscular transmission, prevents the development of Alzheimer's disease (milgamma).
• 5. Gamma-aminobutyric acid (aminalon), its derivatives and analogues: gamma-amine-beta-phenylbutyric acid hydrochloride (phenibut), nicotinoyl-gamma-aminobutyric acid (picamylon), gapontenic acid (pantokalcin, pantogam). It provides removal of unnecessary excitation in the brain, increases the resistance of neurocytes to hypoxia, regulates the transportation and utilization of sugar, enhances protein synthesis, acting as a protector for cells.
• 6. Neuropeptides with analogues: semax, vasopressin, selank, oxytocin, tiroliberin, noopept. Memories are influenced by individual parts of the molecules of neuropeptides, changing the postsynaptic effect of acetylcholine and increasing the activation of nerve cells.
• 7. Cerebrovascular drugs (tanakan).
• 8. Amino acids: biotreidine, glycine, glutamic acid, picamilon, gopantenic acid. Mediators that excite the central nervous system.
• 9. Polypeptides: cerebrolysin, cortexin, celebrex, cerebramine. These are chains of amino acids that work similarly to them. Simultaneously improve the blood supply to the brain.
• 10.. Antioxidants: vitamin C (ascorbic acid), alpha-tocopherol (Vitamin C), mexidol (oxymethylethylpyridine succinate). Decrease the level of lipid peroxidation, stabilize the membranes of neurocytes.
• 11. Adamantane derivatives: mefexamid (timodine, perineuron, mefexadin), adamantin bromophenylamine (memantine, inertast, bromantine), adrafine (olimpone), tonibral, ciprodenate (actebral), bifimelan, pyrisudanol (mentis, nanox), deminol, linopyridine. These drugs increase the content of choline in the brain (in synapses), accelerating the transmission of the nerve impulse, the synthesis of phospholipids in the brain. Also, under the influence of drugs, the content of lipofuscin, which is the pigment of aging, decreases in the brain cells.
• 12. Combined preparations. Combine the mnemotropic properties of its components. Melatonin-apic (pyridoxine plus melatonin), inotropin (melatonin plus aminalon), pituitary (aminalon plus pyracetam), fesam (cinnarizine plus pyracetam), orocetam (oric acid plus pyracetam), thiocetam (tiotriazoline plus pyracetam).

The drugs of the above groups should be prescribed according to strict indications after a detailed examination by a specialist.

To date, a huge number of different studies have been conducted, during which it has been proved that the mnemotropic medications do not affect the healthy brain so that the memory improves significantly. Therefore, it is not advisable to use the drugs of this group for students and students, as well as adult able-bodied population, in order to increase the concentration of attention and increase the assimilation of new material without the presence of neurological deficit symptoms.

Medications are appropriate during recovery from cerebral hemorrhages, craniocerebral trauma, in the treatment of chronic cerebrovascular disorders and Alzheimer's disease, and other senile dementias.

#pharmacology #psychiatry #memory #dementia #nootropics

Phentermine

White crystalline powder, similar in its effect to amphetamine, psychostimulant and sympathomimetic, is mainly used to suppress appetite. Phentermine, in contrast to amphetamine, does not cause a strong sense of euphoria and is, for this reason, allowed in some countries as a drug for obesity therapy. Phentermine is realized in both high-speed form (Adipex®) and in the form of resins with prolonged action (Ionamin, Duromin in Australia and New Zealand).

Dosage forms: Adipex, Ionamin, Duromine

Listed in List II of the list of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation.

Indications: Exogenous obesity.

Assign 1 capsule, 2 hours after breakfast. During the treatment it is not possible to increase the dose of phentermine above the recommended dose. In the case of addiction, the drug should be discontinued.

With the abuse of phentermine, the development of physical dependence is possible. Patients taking phentermine should refrain from driving a motor vehicle and any other activity requiring increased attention.

Side effect on the NS and the psyche: sleep disorders, tremor, nervousness, increased excitability, dizziness, euphoria, dysphoria, psychotic episodes.
On CAS: increased blood pressure, tachycardia.
On the PS: dryness, unpleasant taste in the mouth, diarrhea, constipation.
On the reproductive system: impotence, change of libido.

Contraindications:
Atherosclerosis; diseases SSS, including arterial hypertension; hyperthyroidism; glaucoma; simultaneous use of MAO inhibitors; the state of agitation; children's age till 12 years; hypersensitivity to sympathomimetic amines.

Overdose:
Symptoms: anxiety, tremor, tachypnea, hyperreflexia, confusion, aggression, hallucinations, phobias, fatigue, depression, heart rhythm disorder, AH or hypotension, collapse, nausea, vomiting, diarrhea, abdominal pain. In severe cases - the development of coma.

Treatment. It is necessary to remove the drug from the stomach, causing vomiting or rinsing the stomach. It is necessary to monitor the vital functions of the body in a hospital.

#phentermine #psychostimulants #obesity #amphetamine

Sulpiride

Trade names: Sulpirid, Modal, Betamax, Depral, Dogmatil, Noneston, Prosulpin, Eglek, Eglonil.

Atypical neuroleptic with "regulating" effect on the central nervous system. Moderate antipsychotic effects in him combined with a weak antidepressant and even psychostimulating effect.

According to its chemical structure, sulpiride is a substituted benzamide. The same group includes tiaprid and some other psychotropic drugs. By its structure and some pharmacological properties, sulpiride is also close to metoclopramide. All these agents to some extent block dopamine D2 receptors. The blockade of these receptors is associated with the antipsychotic effect of sulpiride, and its antiemetic effect (as in other neuroleptics).

In psychiatric practice, sulpiride is most often used in combination with other antipsychotics and antidepressants in cases of lethargy, inhibition, anergy, including hallucinatory-delusional and affective (mainly depressive) disorders, as well as alcoholic psychoses.

As an activator is used to treat neurotic disorders in schizotypic disorder. As an antidepressant it is used for monotherapy of depressions of various origin.

Sulpiride has a high level of evidentiary efficacy mainly in relation to psychotic disorders.

In addition, it is used in the treatment of migraine, - for the prevention of atypical and complicated forms of vegetative dysfunction.

Antipsychotic effect of sulpiride is manifested in doses of more than 600 mg / day, in smaller doses (up to 600 mg / day) the stimulating and antidepressant effect prevails. Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine, and GABA receptors.

Sulpiride has some properties common to antipsychotics: it has moderate antiserotonin and cataleptogenic action, weakens the stimulating effects of phenamine. It also enhances the effects of opioid analgesics, barbiturates, tranquilizers, neuroleptics, tricyclic antidepressants, antihypertensives [10], antihistamines, clonidine alcohol. The effects of sulpiride and levodopa are mutually weakened. Antacids reduce its bioavailability by 20-40%.

Contrary to the widespread view of sulpiride as an easily tolerated drug, it often (with a risk only slightly lower than haloperidol, but higher than risperidone) causes extrapyramidal disorders; In addition, among all the typical neuroleptics, the risk of hyperprolactinaemia is the most associated with the intake of sulpiride.

Amdoal, Zilaxera, Abilifay - Aripiprazolum

Trade names: Amdoal, Zilaxera, Abilifay

A relatively new (admitted by the FDA in 2002) drug of the class of atypical antipsychotics (antipsychotics), introduced into the world pharmaceutical market following clozapine, risperidone, olanzapine, quetiapine and ziprasidone.

Aripiprazole displays antagonism typical of "neuroleptics" for dopamine receptors of the D2 subtype in the mesolimbic path, while possessing the unique property of partial agonism to the same receptors in the mesocortical pathway. Like other "atypical" antipsychotics, aripiprazole displays a strong antagonism to the serotonin 5-HT2A receptor subtype and, like ziprasidone, agonism to 5-HT1A receptors. If to speak more correctly, aripiprazole is a partial agonist (mixed agonist-antagonist) of 5HT1 and D2 receptors, that is, it excites the receptor in the absence of a neurotransmitter and blocks it in excess. The drug has the lowest affinity among all atypical antipsychotic agents for adrenergic (α1), histamine (H1), and muscarinic (m1) receptors. Such a pharmacodynamic spectrum explains the high therapeutic efficacy of aripiprazole in schizophrenia and bipolar disorders and at the same time the low frequency and severity of the observed side effects, including weight gain and motor disorders. The latter is of exceptional importance in long-term psychosis therapy. The ability of aripiprazole to reduce the levels of prolactin, glucose and lipid injection is noted; The significance of these changes requires further research. An important positive feature of the action of aripiprazole is its ability to reduce the QT interval of the electrocardiogram, which may indicate a higher cardiovascular safety of treatment with this drug.

Aripiprazole should be taken 1 time per day. The drug is well tolerated by patients. In clinical trials, there has never been a need to titrate the dose of this drug.

Indications

- Schizophrenia, with acute attacks and for maintenance therapy (including adolescents from 13 years of age)

- acute manic attacks of type I with bipolar disorder (including children from 10 years of age)

- Supportive therapy for bipolar affective disorder type I, after a manic or mixed episode of a single manic episode as an adjunct to antidepressants

- in the treatment of major depressive disorder

Bristol-Myers Squibb is considering the possibility of using aripiprazole in the treatment of alcoholism.

It is shown that in cases of exacerbation of chronic schizophrenia aripiprazole is much more effective than placebo. It can be clarified that the drug at a dose of 30 mg / day has an advantage in comparison with placebo, but this is not observed at doses of 2 or 10 mg / day. At the same time, the authors noted a clinical improvement in symptoms in all patients receiving aripiprazole. It was also found that the drug in doses of 15 or 30 mg / day is significantly more effective than placebo in exacerbating schizophrenia. In a study by Carson, Pigott, Saha et al. aripiprazole at a dosage of 30 mg / day compared with haloperidol (10 mg / day) in the treatment of patients with exacerbation of schizophrenia. In comparison with haloperidol, a much larger number of patients responded positively to therapy (reduction of symptomatology by PANSS score more than 30%, stable condition for 1 month). In addition, the authors showed that the reduction of negative and depressive symptoms in patients treated with aripiprazole was significantly greater than with haloperidol. Thus, the results of a number of short-term studies have convincingly shown that aripiprazole is effective in treating positive and negative symptoms in the structure of schizophrenia.

In long-term studies, it has been demonstrated that aripiprazole is effective in the prevention of exacerbations of chronic schizophrenia. Patients treated with aripiprazole reported a significantly lower risk of exacerbations and a better improvement in their condition compared to those receiving placebo.

A significant improvement in secondary verbal memory in patients treated with aripiprazole compared with olanzapine (p <0.05) was shown when comparing the neurocognitive effect in the treatment of aripiprazole and olanzapine in chronic schizophrenia.

Sertralinum

Sertralinum - an antidepressant from the group of selective serotonin reuptake inhibitors (SSRIs).

Trade names of "Asentra", "Deprespolt", "Zoloft", "Emoton", "Seralin", "Serenata", "Sulfleft", "Stimuloton", "Torin", "Adjuvin", "Misol".

In a 2009 study comparing 12 new-generation antidepressants, sertraline along with mirtazapine, escitalopramome venlafaxine was found to be one of the best. Has a stimulating and sedative effect and is used to treat patients with depression, accompanied by both inhibition, hypersomnia, apathy and anguish, and with anxious depression, anxiety, bad sleep, irritability. He quickly suppresses both anxious and phobic component, and longing, although at the beginning of therapy can increase the manifestations of anxiety, which sometimes requires the appointment of tranquilizers.

In combination with cognitive-behavioral psychotherapy sertraline gives excellent results in the treatment of obsessive-compulsive disorder (ROC).

Sometimes reduces the sensitivity of the sexual act, which can persist for some time after stopping the drug. During the entire period of use, some patients developed the idea of suicide and / or aggression to others. There have also been cases of committing suicides and murders during and after the end of the drug use period, for example shooting in American schools, as well as committed suicides. Despite the final decision of the international pharmaceutical commission on the high effectiveness of the drug, the question of its controversial effectiveness and the absence of side effects is now being raised again.

History of creation
The drug was developed by the pharmaceutical company Pfizer. Initially, the work was carried out on the drug "tametrolin", which was an inhibitor of the re-uptake of catecholamines. Tamerlagen has not proven itself as an effective antidepressant, since it demonstrated the undesirable effects of prohibited psychostimulants.

Many years later, studies of tametrolin resumed, resulting in the creation of sertraline. Sertraline differs from tametalin by the presence of two chlorine atoms in the molecule. However, studies have shown that this substance is an extremely selective inhibitor of serotonin reuptake. At the time of the research Pfizer considered other drugs as an antidepressant put forward on the broad market. However, scientists working on sertraline without any motivation persistently offered their invention. As a result of these actions, sertraline was sold under the trade name Zoloft and Lustral and for some time was the most prescribed remedy against depressive conditions in the USA.

pharmachologic effect

Antidepressant, a specific inhibitor of serotonin reuptake, enhances its effects, has little effect on the re-uptake of norepinephrine and dopamine; in therapeutic doses blocks the seizure of serotonin in human platelets. Suppression of serotonin reuptake activity increases serotonergic transmission, which leads to a subsequent inhibition of adrenergic activity in the blue nucleus (locus ceruleus). Sertraline also inhibits the excitation of serotonin neurons in the seam region (median line of the medulla oblongata); which leads to an initial increase in the activity of the blue core, followed by a decrease in the activity of postsynaptic beta-adrenergic receptors and presynaptic alpha-2-adrenergic receptors.

Does not cause drug dependence, does not have psychostimulating, sedative, m-holinoblokiruyuschego and cardiotoxic effect, does not change psychomotor activity. Due to selective inhibition of seizure of serotonin does not increase the activity of the sympathetic nervous system. Has no affinity for m-cholino-, serotonin (5-HT1A, 5-HT1B, 5-HT2), dopamine, adreno-histamine, GABA- or benzodiazepine receptors; does not inhibit MAO. In contrast, tricyclic antidepressants in the treatment of depression or obsessive-compulsive disorder (obsessive-compulsive disorder) does not increase body weight. Unlike other representatives of SSRIs - to a lesser extent produces an inversion of phases from depression - in hypomaniacal and manic state. The initial effect develops by the end of the first week, to a greater extent after 2-4 weeks, the maximum therapeutic effect - after 3 months, from the beginning of the regular intake of the drug.

Indications for use

Depressive conditions (including those accompanied by a sense of anxiety); prevention of initial or chronic episodes of depression; obsessive-compulsive disorder; panic disorder, social phobia.

With poorly treatable depression, it is possible to use in combination with other drugs. Combine only drugs related to different groups of antidepressants. Sertraline can be combined, for example, with bupropion or mirtazapine.

Dosing and Administration
Inside, 50 mg, 1 time per day in the morning or evening, regardless of food intake. In the absence of effect, a gradual (for several weeks) increase in the dose to 200 mg / day (at 50 mg / week) is possible. Some clinicians recommend prescribing a dose of 25 mg / day for 1-2 days. Panic disorders: the initial dose is 25 mg / day, followed by an increase to 50 mg / day for 1 week. In the case of prolonged maintenance therapy, a minimum effective dose is prescribed, which is subsequently changed depending on the effect. Obsessive-compulsive disorders and social phobias: in children and adolescents 13-17 years, the initial dose is 50 mg / day, in children 6-12 years the initial dose is 25 mg / day, followed by an increase in 1 week to 50 mg / day . If the effect is insufficient, the dose can be increased stepwise at 50 mg / day to 200 mg / day, with an interval of at least 1 week. In elderly patients, the initial dose is 25 mg / day (morning or evening) followed by a gradual increase.

Contraindications

Manic conditions, hypersensitivity, liver disease, alcohol poisoning, psychotropic drugs and other drugs, pregnancy, lactation, simultaneous administration of MAO inhibitors. C caution. Neurological disorders (including delayed mental development), epilepsy, hepatic and / or renal failure, weight loss, child age.

Treatment of obsessive-compulsive disorder with sertraline
Studies have shown that sertraline is slightly more effective in treating OCD than an antidepressant of the same class of SSRIs Fluoxetine (Prozac). With insufficient effect, increasing the dose above the recommended dose (50-200 mg) did not yield any results. Participants in the studies confirmed the positive effect of sertraline treatment and maintenance of this effect for a year or more of sertraline. The constant use of the drug is not required by everyone. However, when the drug was discontinued, OCD exacerbations were often observed, which were a consequence of side effects or withdrawal syndrome. 48% of patients who stopped using the drug felt the same as those who continued treatment. Sertralin is effective in the treatment of OCD in adults and children. It is known that setralin can be used in OCD with concomitant Tourette's syndrome, but it can cause an exacerbation of tics in the Tourette syndrome.

Side effects:
Anxiety, affect inversion (development of mania or hypomania), tremor, hyperhidrosis, allergic reactions, bleeding (including nasal), palpitations, dry mouth, decreased appetite. Rarely - increased appetite (possibly as a consequence of eliminating depression), nausea, vomiting, unstable stools, diarrhea, stomach or abdominal cramps, flatulence or pain, weight loss; headache, dizziness, insomnia, drowsiness, movement disorders (extrapyramidal symptoms, gait alteration), akathisia, convulsions, paresthesia, symptoms of depression, hallucinations, aggressiveness, agitation, anxiety, psychosis, skin hyperemia or "hot flushes" (including blurred vision), yawning, increased sweating, impaired sexual function (delay in ejaculation, priapism, decreased potency and / or libido, anorgasmia), dysmenorrhea, galactorrhea, hyponatremia (ADH) laktinemiya, withdrawal syndrome, erythema multiforme, skin rash and itching. In rare cases - serotonin syndrome.

Can lead to emotional and behavioral changes, including an increased risk of suicide.

Lamotrigine

Antiepileptic drug used in the treatment of epilepsy and bipolar disorders; has also normotime activity.

Trade names: Convulsan, Lamykal, Lamitor, Lamolep, Lamotrin, Seizar.

The mechanism of lamotrigine is not exactly known; the drug was developed as an antagonist of folic acid, but this effect was found to be weak. It is assumed that it stabilizes the neuronal membranes by affecting the sodium channels and blocks the excess release of excitatory amino acids (mainly glutamate) without reducing its normal release.

The drug is used for the following indications:

- Epilepsy (partial or generalized seizures, including tonic-clonic seizures, as well as seizures in Lennox-Gastaut syndrome in adults and children);
- bipolar disorder with predominantly depressive phases in patients aged 18 years and older.

Prolonged prophylactic monotherapy with lamotrigine in bipolar depression showed that this drug is equally effective in bipolar disorder type I and II.

The advantages of lamotrigine, allowing to justify its use at the stage of long-term prophylactic therapy, are the impact on the residual manifestations of depression, the absence of ricochetial withdrawal symptoms and the minimal presentation of side effects.

In epilepsy, lamotrigine is used in the therapy of partial epileptic seizures, primary and secondary tonic-clonic seizures and seizures associated with the Lennox-Gastaut syndrome. Can have an anticonvulsant effect when other antiepileptic drugs are ineffective.

Possible antidepressant activity of the drug is not confirmed, but it is recommended for the treatment and prevention of depressive episodes in the composition of bipolar affective disorder type I. It is suggested that in patients with depression in bipolar disorder monotherapy with antidepressants is undesirable because of a possible worsening of the course of bipolar disorder. Official recommendations published by the American Psychiatric Association recommend that from the very beginning, antidepressants should not be used as monotherapy at all in these patients; Instead of monotherapy with antidepressants, a one-stage appointment of at least combination therapy is suggested. Lamotrigine and lithium salts are recommended to be used as a "first line" at the stage of active therapy along with antidepressants.

Off-label lamotrigine is used for the treatment of depersonalization syndrome - derealization (in combination with selective serotonin reuptake inhibitors (SSRIs), schizoaffective disorder, borderline personality disorder, prolonged mental disorder caused by hallucinogens, resistant obsessive-compulsive disorder.

Outside of psychiatry, the off-label drug is also used to treat peripheral neuropathy, trigeminal neuralgia, cluster headaches, migraine, and to reduce neuropathic pain.

The drug stabilizes the presynaptic membranes of neurons and their potential-dependent sodium channels, and also blocks the release of neurotransmitters (primarily glutamate and aspartate). Glutamate, being an exciting neurotransmitter of the brain, plays a major role in the occurrence of epileptic seizures.

After ingestion lamotrigine quickly and completely absorbed from the digestive tract. Cmax is reached after about 2.5 h.

Lamotrigine has a linear pharmacokinetic profile when taken in doses up to 450 mg. The time to reach Cmax increases slightly after ingestion, but the level of absorption remains unchanged.

Lamotrigine is metabolized by the enzyme glucuronyl transferase. Does not affect the pharmacokinetics of other antiepileptic drugs.

The special value of the drug is attached to the lack of the property of causing weight gain in long-term administration, which may justify the need to transfer to it from other drugs (including lithium) patients with a tendency to obesity.

The most significant side effect of lamotrigine is skin rash, observed in about 10% of cases of prescription. There are reports of rare cases of severe, potentially life-threatening skin lesions, including Stevens-Johnson syndrome, toxic epidermal necrolysis; the drug hypersensitivity syndrome, in addition to the rash, may be accompanied by impaired blood and internal organs.

For the drug, the risk of developing drug aseptic meningitis is noted.

Among the side effects often noted are headache, dizziness, double vision, blurred vision, nausea, diarrhea, irritability, tremor, drowsiness, insomnia.

Treatment of bipolar disorders with lamotrigine is associated with an increased risk of developing suicidal thoughts or behavior.

During the treatment period, care must be taken when driving vehicles and other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

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Glycine

Glycine (aminoacetic amphitaminic acid, aminoethanoic acid) - the simplest aliphatic amino acid, the only proteinogenic amino acid that does not have optical isomers. The name of the glycine is derived from other Greek. γλυκύς, glycys - sweet, because of the sweetish taste of the amino acid. It is used in medicine as a nootropic drug.

Biological role
Glycine is part of many proteins and biologically active compounds. From the glycine in living cells, porphyrins and purine bases are synthesized.

Glycine is also a neurotransmitter amino acid that exhibits a dual effect. Glycine receptors are found in many areas of the brain and spinal cord. By binding to receptors (encoded by the GLRA1, GLRA2, GLRA3 and GLRB genes), glycine causes a "retarding" effect on neurons, reduces the excretion of "exciting" amino acids, such as glutamic acid, from neurons and increases the release of GABA. Also, glycine binds to specific sites of NMDA receptors and, thus, facilitates the signal transmission from the excitatory neurotransmitters of glutamate and aspartate. In the spinal cord, glycine leads to inhibition of motoneurons, which allows the use of glycine in neurological practice to eliminate increased muscle tone.

In medicine

Manufacturers of glycine pharmacological agents claim that glycine has a sedative (sedative), mild tranquilizing (anti-anxiety) and mild antidepressant effect, reduces anxiety, fear, psychoemotional stress, reduces the severity of side effects of antipsychotics (antipsychotics), anxiolytics, antidepressants, hypnotics and anticonvulsants is included in a number of therapeutic practices to reduce alcohol, opiate and other types of abstinence, as an auxiliary Reparata, providing a weakly expressed sedative and tranquilizing effect. Has some nootropic properties, improves memory and associative processes.

Glycine is a regulator of metabolism, normalizes and activates the processes of protective inhibition in the central nervous system, reduces psychoemotional stress, increases mental performance.

Glycine is glycine- and GABA -ergic, alpha1-adrenoblocking, antioxidant, antitoxic; regulates the activity of glutamate (NMDA) receptors, due to which the drug is able to:

★ Reduce psycho-emotional stress, aggressiveness, conflict, improve social adaptation;
★ improve your mood;
★ ease falling asleep and normalize sleep;
★ Improve mental performance;
★ Reduce vegetative-vascular disorders (including in the climacteric period);
★ reduce the severity of cerebral disorders in ischemic stroke and head injury;
★ Reduce the toxic effects of alcohol and drugs depressing the functions of the central nervous system;
★ reduce the desire for sweets.

Glycine is present in significant amounts in cerebrolysin (1.65-1.80 mg / ml).

Glycine is a regulator of the processes of protective inhibition in the central nervous system, reducing psychoemotional stress.

In the pharmaceutical industry, glycine tablets can be potentiated with vitamins (eg vitamins B1, B6 or B12).