Instruction for use: Afobazol

Trade name of the drug – Afobazol

The chemical rational name: 5-ethoxy-2- [2- (morpholino) ethylthio] benzimidazole dihydrochloride.
Dosage Form: pills

Composition:
Each tablet contains:
Active ingredient: afobazol (on dry substance) - 5 mg or 10 mg.
Excipients: potato starch, microcrystalline cellulose, milk sugar (lactose), povidone, magnesium stearate.

Description:
Tablets white or white with a color shade.

Pharmacotherapeutic group: anxiolytic.

ATX Code N05BX.

Pharmacological Properties
Pharmacodynamics.
Afobazol - a derivative of 2-mercaptobenzimidazole, selective anxiolytic, not belonging to the class of benzodiazepine receptor agonists. It prevents the development of membrane-dependent changes in the GABA receptor.
Afobazol possesses anxiolytic effects with an activating component, are not accompanied by hypnotic-sedative effects (sedation detected in AFOBAZOL at doses 40-50 times higher than the ED50 for the anxiolytic effect). There are no muscle relaxant properties of the drug, a negative impact on memory and attention indicators. If its application is not formed drug dependence and withdrawal symptoms do not develop. The drugs are sold mainly in the form of a combination of anxiolytic (antianxiety) and easily stimulating (activating) effects.
Reducing or eliminating anxiety (concern, foreboding, fear, irritability), strength (fearfulness, tearfulness, anxiety, inability to relax, insomnia, fear), and thus somatic (muscular, sensory, cardiovascular, respiratory, gastrointestinal symptoms ), autonomic (dry mouth, sweating, dizziness), cognitive (difficulty concentrating, impaired memory) violations observed at 5-7 days of treatment AFOBAZOL . The maximum effect is achieved by the end of 4 weeks of treatment and stored in post-therapeutic average period of 1-2 weeks. Especially shows the use of the drug in patients with predominantly asthenic personality traits as alarming suspiciousness, insecurity, increased vulnerability and emotional lability, tendency to emotional stress hazardous reactions. Afobazol toxic (LD50 in rats is 1.1 g at ED50 0,001 g).
Pharmacokinetics.
The half-life of Afobazol ingestion is 0.82 hours, the mean maximum concentration (Cmax) - 0,130 ± 0,073 g / ml; mean residence time of the drug in the organism (MRT) - 1,60 ± 0,86 h. Afobazol distributed extensively on well vascularized organs.

Indications
Afobazol is used in adults with anxiety: generalized anxiety disorder, neurasthenia, adjustment disorder, in patients with various medical conditions (asthma, irritable bowel syndrome, systemic lupus erythematosus, ischemic heart disease, hypertension, arrhythmias), dermatological, oncological and al. diseases. In the treatment of sleep disorders associated with anxiety, neuro dystonia, premenstrual syndrome, alcohol withdrawal syndrome, to facilitate withdrawal for smoking cessation.

Contraindications
Pregnancy, lactation. Individual intolerance to the drug. Children under 18 years old.

Dosing and Administration
Administered orally, after meals. The optimal single dose - 10 mg daily - 30 mg, distributed into 3 doses during the day. The duration of a course of the drug is 2-4 weeks. If necessary, the daily dose can be increased to 60 mg, and the duration of the treatment and 3 months.
Side effect
Individual hypersensitivity, allergic reactions are possible.

Overdose
If a large overdose and intoxication may develop sedation and increased sleepiness without manifestations of muscle relaxation. As used emergency caffeine sodium benzoate 20% solution in vials of 1.0 ml 2-3 times a day subcutaneously.
Interaction with other medicinal products.
Afobazol has no effect on the narcotic effect of ethanol, and the hypnotic effect of thiopental. Potentiates the anticonvulsant effect of carbamazepine. It is strengthening the anxiolytic effect of diazepam.
Release Form10 tablets or 25 tablets in blisters of PVC film and aluminum foil.

At 30.50, or 100 tablets in a polymer jar complete with lids. Each bank or 3, 5 or 10 contour packs of 10 tablets, or 2 or 4-outline package 25 tablets together with instructions for use in a stack of cardboard.
Shelf life
2 years. Do not use after the date printed on the packaging.
Storage conditions
List B in a dry, dark place, out of reach of children, at a temperature no higher than 25 °

Conditions of supply of pharmacies
Without a doctor's prescription.