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Adamantyl bromophenylamine- trade name Ladasten

02 Apr 2018

A drug, a psychostimulant, an anxiolytic, an immunotropic drug.

Pharmachologic effect

- Enhanced synthesis and Ca2 + -dependent processes of dopamine release. The ability of the drug to enhance the synthesis of dopamine de novo fundamentally differentiates the drug from typical psychostimulants. Due to the increased synthesis of dopamine, with the treatment with adamantyl bromophenylamine there is no depletion of the neuronal reserves of catecholamines.

- Restoration of stress-depleted GABA-receptors and a decrease in the expression of the gene encoding the GABA GAT-3 carrier protein synthesis. GAT-3 is one of the isoforms of the GABA transfer protein, which reuptakes GABA from the synaptic cleft. By reducing the expression of the gene that codes for the synthesis of this protein, the GABA content in the synaptic cleft is increased, which increases the GABA-transmission and is a factor in increasing the binding of the ligands to the GABA-benzodiazepine-chloronophore complex.

- Antiradical action: reduces the activity of excessively elevated processes of lipid peroxidation, contributes to the preservation of the integrity and barrier function of cellular and mitochondrial membranes.

Indications

Asthenic conditions of various genesis, including somatic diseases and after the transferred infectious diseases.

Neurasthenia.

From the side of the central nervous system: there can be signs of excessive activation and a disorder of falling asleep.

From the cardiovascular system: development or aggravation of heart failure, orthostatic hypotension; hypertension, rarely - arrhythmia, tachycardia.

Other: allergic reactions (with increased individual sensitivity to the drug).

Adamantyl bromophenylamine belongs to the group of so-called actoprotectors - drugs of different groups, which increase the body's defenses. Adamantibromphenylamine was developed by Soviet military physicians as a means of increasing overall immunity, endurance of a person. It was found that the drug also has a psychostimulating effect. In addition, he disguises the use of steroids: all standard doping procedures that the IOC practiced turned out to be ineffective against adamantyl bromophenylamine. 


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Cogitum France and Cogitum Portugal. Are these different medications?

30 Mar 2018

It is often possible to meet the question: the French Ñogitum of the firm Sanofi and the Portuguese Cogitum company Korangi are different things?

Let's compare the compositions and understand - whether only the names of the preparations are consonant or indeed it is a question of the same drug with the same active substance.

Composition of the Portuguese Coguitum

175 mg of N-acetylaminosuccinic acid (250 mg of potassium salt),

1000 mg of levulose *,

15 mg of methyl parahydroxybenzoate *,

7 mg of banana flavor *

10 ml of purified water q.s.

DDR not set

Composition of the French Cogitum:

Sanofi company

Name of the product Trade name: Kogitum.

Chemical name: potassium N-acetylaminosuccinate

Dosage form Solution for oral administration.

The composition of 10 ml of the solution contains:

active substance: potassium acetylaminosuccinate 250 mg;

Excipients:

fructose 1000 mg,

methylparahydroxybenzoate 15 mg,

flavoring banana 7 mg,

water purified to 10 ml.

Pharmacotherapeutic group: tonic.

ATX Code: N06BX.

Description Transparent light yellow solution with the smell of a banana.

Let's compare the active substances. In Portuguese: N-acetylaminosuccinic acid (250 mg potassium salt) is the main component.

French: 250mg of potassium acetylamino succinate is the main component.

Acetylaminosuccinic acid (the dicalcium salt of N-acetylaminosuccinate) is a synthetic analog of aspartic acid (a non-essential amino acid); as a result, their chemical properties, as well as the mechanisms of biological action, do not differ. Moreover, aspartic acid, rather than acetylaminosuccinate (N-acetylaminosuccinic acid) was previously indicated as the active substance of the drug.

Acetylaminosuccinic acid (Cogitum, Sanofi Aventis, France) is not a food additive, does not refer to biologically active additives or "orthomolecular" complexes. Acetylamino-succinic acid is officially registered in Russia as a prescription drug. This drug belongs to the pharmacological group "Toning agents and adaptogenes", which allows you to extrapolate to the described drug the basic general characteristics of these drugs. In accordance with the existing definition, these are "herbal preparations (native or in the form of pure active substances) that have a low specific generalizing effect on the functions of the central nervous system, endocrine regulation, metabolic processes and increasing the adaptation of the organism to unfavorable conditions".

As a result, we can put an equal sign between the terms used: both here and there it is said about the N-acetylaminosuccinic acid contained in the two-potassium salt in the same volumes on the ampoule.

Other components: these are auxiliary elements (including sweeteners) that practically coincide in both compositions and do not affect the pharmacological effect.

You can safely say - both drugs are identical in composition and volume of ampoules. Only one insignificant difference: it is a 20 ampoule in the Portuguese cogitum instead of 30 ampoules in the French coguitum (now withdrawn from production or re-registered).


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Atomoxetinum (Atomoxetinum) - Strattera

26 Mar 2018

A drug intended for the treatment of attention deficit hyperactivity disorder (ADD, ADHD). By the mechanism of action, atomoxetine is an inhibitor of norepinephrine reuptake (indirect sympathomimetic of the central action).

Atomoxetine is approved by the US Food and Drug Administration for the treatment of attention deficit / hyperactivity disorder in children, adolescents and adults. Its effectiveness has not been investigated in children under 6 years. Unlike psychostimulants traditionally prescribed for ADHD, atomoxetine is not a narcotic and does not have the inherent potential for abuse. In clinical trials, it has been shown that atomoxetine is able to provide a stable 24-hour monitoring of ADHD symptoms in both adults and children.

Atomoxetine is also used to treat treatment-resistant depression as an independent remedy or as part of a comprehensive treatment with SSRIs or other drugs.

The therapeutic effects of atomoxetine develop gradually over at least one week. The duration of the course use of the drug should be 6-8 weeks before the decision on its level of effectiveness. Many patients with ADHD, whose disease can not be corrected by psychostimulants, respond to treatment with atomoxetine. Atomoxetine is also more preferred in patients with a variety of mental disorders, those who do not tolerate psychostimulants well, as well as patients with substance abuse in the anamnesis. Psychostimulants based on amphetamine (mixed salts of amphetamine and dextroamphetamine), pure dextroamphetamine, lisdexamphetamine, etc.) are not recommended for use in patients suffering from nervous disorders (such as facial tics, spasms, etc.). In such cases, atomoxetine is the best choice.

Atomoxetine potently and highly selectively inhibits the proteins of the presynaptic membrane carrying out the re-uptake of norepinephrine, serotonin and dopamine. The binding constants (Ki) are 5, 77 and 1451 nM, respectively. In studies of tissue microdialysis, it has been shown that atomoxetine triply increases levels of norepinephrine and dopamine in the prefrontal cortex, but does not alter the level of dopamine in the striatum and adjacent nucleus. Also, atomoxetine in therapeutic doses acts as an NMDA receptor antagonist. The role of such antagonism in the therapeutic profile of atomoxetine has yet to be clarified, however, fresh sources of literature imply that the dysfunction of the glutamatergic system may play a role in the etiology and pathogenesis of ADHD.

Atomoxetine does not have a clinically significant affinity for serotonin, acetylcholine and adrenergic receptors.

Side effects include dry mouth, fatigue, irritability, nausea, decreased appetite, constipation, dizziness, sweating, upset urination, sexual problems, decreased libido, urinary retention, weight changes, slower growth in children, increased heart rate and blood pressure, aggressiveness, mania, hypomania.

Atomoxetine was initially studied as a drug for the treatment of depression, but did not show a favorable risk / benefit ratio in clinical trials. Subsequently, the manufacturing company Eli Lilly and Company examined the atomomxetine for the treatment of ADHD. Many patients observe a pronounced antidepressant effect of atomoxetine (when used with other antidepressants).

The efficacy of atomoxetine in the treatment of psychogenic overeating was investigated. The average dose of atomoxetine was 106 mg / day. The study showed that "the use of atomoxetine was associated with a significantly higher rate of reduction in episodes of overeating, weight loss and BMI." The authors of the study concluded that atomoxetine can be effective in the short-term treatment of psychogenic overeating.


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Fenibut - Phenibutum

20 Mar 2018

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

Fenibut - Phenibutum buy online

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.


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Duloxetine - Duloxetinum

16 Mar 2018

Trade names: "Simbalta", "Intriv"

cymbalta, duloksetin

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.


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Neurotransmitter Acetylcholine

15 Mar 2018

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.


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Tablets for memory

14 Mar 2018

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.

Tablets for memory buy online

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.

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Phentermine

13 Mar 2018

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).

Phentermine buy online

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.

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Sulpiride

12 Mar 2018

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.

Sulpiride

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.


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Amdoal, Zilaxera, Abilifay - Aripiprazolum

07 Mar 2018

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.

Aripiprazolum

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.


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