Aphobazol Retard, 30 mg 20 pcs.

Pharmacotherapeutic group: anxiolytic medicine (tranquilizer).

ATX code: N05BX.

PHARMACODINAMICS.

Aphobazol® Retard is a selective non-benzodiazepine anxiolytic.

Acting on sigma-1 receptors in nerve cells in the brain, Aphobazol® Retard stabilizes GABA/ benzodiazepine receptors and restores their sensitivity to endogenous mediators of inhibition. Aphobazol® Retard also increases the bioenergetic potential of neurons and has a neuroprotective effect: it restores and protects nerve cells.

The action of the drug is mainly realized as a combination of anxiolytic (anti-anxiety) and mild stimulant (activation) effects.

Afobazol® Retard decreases or eliminates anxiety (anxiety, misgivings, apprehension), irritability, tension (jitteriness, tearfulness, anxiety, inability to relax, insomnia, fear), depressed mood, somatic anxiety manifestations (muscular, sensory, cardiovascular, respiratory, gastrointestinal symptoms), autonomic disturbances (dry mouth, sweating, dizziness), cognitive disturbances (difficulty concentrating, impaired memory), including those resulting from stressors.including those arising from stress disorders (adaptation disorders). The drug is especially indicated for people with predominantly asthenic personality traits such as anxious mistrustfulness, uncertainty, increased vulnerability and emotional lability, propensity to emotional stress reactions.

Aphobazole® Retard does not cause muscle weakness or drowsiness and has no negative effect on concentration and memory. Its use is not addictive, does not cause drug dependence and does not lead to withdrawal syndrome.

Pharmacokinetics

Aphobazole® Retard is well and quickly absorbed from the gastrointestinal tract after oral administration. Food intake has no effect on the drug absorption and pharmacokinetic parameters.

The maximum concentration of the drug in plasma (Cmax) after a single dose is 47.740+43.252 ng/ml, after multiple dosing – 27.668+13.770 ng/ml; time to reach maximum concentration (Tmax) is 2.1+1.1 and 2.6+1.0 hours after single and multiple dosing, respectively.

Metabolism: Afobazol® Retard undergoes a “first pass effect” through the liver; the main directions of metabolism are hydroxylation by the aromatic ring of the benzimidazole cycle and oxidation by the morpholine fragment.

Aphobazole® Retard is intensively distributed to well vascularized organs and is characterized by rapid transfer from the central pool (blood plasma) to the peripheral pool (highly vascularized organs and tissues).

The elimination half-life of Aphobazol® Retard when administered orally is 8.41+5.01 hours after a single dose and 6.05+3.54 hours after multiple doses. The drug is excreted mainly as metabolites and partially unchanged by the kidneys and through the intestine.

Indications

Active ingredient

How to take, the dosage

It is administered orally.

1 tablet once a day, in the morning, regardless of meals.

The duration of course of application of the drug is 2-4 weeks.

If after treatment, there is no improvement, or if symptoms get worse or new symptoms develop, you should talk to your doctor.

To use the drug only according to the indication, route of administration, and dosage listed in the directions.

Interaction

Aphobazole® Retard does not interact with ethanol and has no effect on the hypnotic effect of thiopental. It enhances the anticonvulsant effect of carbamazepine. Causes increase in the anxiolytic effect of diazepam.

If you are using the above or other drugs (including over-the-counter medications), please consult your physician before using Aphobazol® Retard.

Special Instructions

The drug has no adverse effect on driving and performing potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

Contraindications

If you have any of the above conditions, you should consult your doctor before using the drug.

Side effects

Unwanted effects that may develop during treatment with Aphobazol® Retard are classified according to the following frequency of occurrence:

Very common (> 1/10), common (> 1/100 to < 1/10), infrequent (> 1/1,000 to < 1/100), rare (> 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency unknown (cannot be determined from available data).

Immune system disorders: frequency unknown – allergic reactions.

Nervous system disorders: rarely – headache, which usually resolves on its own and does not require withdrawal of the drug.

If you experience or worsen the side effects listed in the instructions, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms. In case of significant overdose and intoxication, development of sedation and increased somnolence without myorelaxation manifestations is possible. Treatment. As an emergency treatment caffeine 20 % solution is used in 1.0 ml ampoules 2-3 times a day subcutaneously.

In case of symptoms of overdose, discontinue the drug and consult a physician immediately.

Pregnancy use

The use of the drug Aphobazol® Retard is contraindicated in pregnancy.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Please consult your physician before using Aphobazol® Retard if you are pregnant or suspect that you may be pregnant or are planning to become pregnant.