Азафен®

General characteristics. Structure:

Active agent: Pipofezinum of dihydrochloride of monohydrate of 25 mg;
Excipients
Potato starch, silicon dioxide colloid (aerosil), cellulose microcrystallic, lactoses monohydrate, povidone (polyvinylpirrolidone low-molecular medical), magnesium stearate.
Description: Tablets ploskotsilindrichesky with a facet, yellowish-greenish color. Existence of a mramornost is allowed.

Pharmacological properties:

Pharmacodynamics. Tricyclic antidepressant from group of not selective inhibitors of neyronalny capture of monoamines.

The mechanism of antidepressive action is connected with not selective inhibition of the return neyronalny serotonin reuptake and noradrenaline that leads to increase in their concentration in TsNS. Timoleptichesky effect of drug is combined with sedative activity and anxiolytic effect.

Practically the m-holinoblokiruyushchey has no activity, does not influence activity of monoamine oxidase (MAO). Has no cardiotoxic effect.

Pharmacokinetics. It is quickly and completely soaked up in digestive tract. Bioavailability - about 80%. After oral administration of a single dose of 25 mg of Azaphenum the maximum concentration makes 24,5 ng/ml and is defined 1-2 hours later. Communication with proteins of plasma - 90%.

It is metabolized in a liver with formation of inactive metabolites. In the research in vitro it is shown that Pipofezinum is not substrate of isoenzymes CYP2C9, CYP2C19, CYP2D6 and CYP3A4, and it is preferential metabolized under the influence of CYP1A2 isoenzyme.

Drug is quickly enough removed from a blood channel, the elimination half-life makes 4,3 hours. It is brought out of an organism preferential by kidneys.

Indications to use:

Depressive episodes easy and moderate severity (including at chronic somatopathies).

Route of administration and doses:

Inside.
Initial dose for adults - 25-50 mg, in 2 receptions (in the morning and during the lunchtime). At good tolerance the dose is gradually increased to 150-200 mg/days (in 3-4 receptions, the last reception before going to bed), and in certain cases - to 400 mg/days. An optimum daily dose - 150-200 mg, maximum - 400-500 mg. At achievement of desirable effect pass to maintenance doses: 25-75 mg/days. A course of treatment - till 1 year (not less than 1-1,5 months).

Features of use:

After transfer from therapy by MAO inhibitors on Azaphenum the interval of 1-2 weeks is necessary.

During treatment it is necessary to abstain from alcohol intake. Any depressive frustration in itself increases risk of a suicide. Therefore during treatment for patients observation for the purpose of early identification of disturbances or changes of behavior, and also suicide bents has to be established.
Influence on performance of potentially dangerous types of activity requiring special attention and speed of psychomotor reactions

Due to the possible decrease in concentration of attention during treatment it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions (control of vehicles, work with moving mechanisms, work of the dispatcher and operator, etc.).

Side effects:

Headache, dizziness, nausea, vomiting, allergic reactions.

At the beginning of therapy emergence of weakness, drowsiness, disturbance of concentration of attention, dryness in a mouth which are leveled without additional treatment is possible.

Interaction with other medicines:

Strengthens effects of ethanol, antihistaminic drugs, etc. means, the oppressing TsNS, anticoagulants.

Reduces efficiency of antiepileptic drugs.

In the research in vitro it is shown that Azaphenum is not inhibitor or the inductor of isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 therefore interaction of Azaphenum with the medicines which are substrates of these isoenzymes is improbable.

Fluvoksamin, пропафенон, мексилетин, ciprofloxacin (CYP1A2 isoenzyme inhibitors) can increase concentration of Azaphenum in a blood plasma.

Contraindications:

Hypersensitivity to the basic and/or auxiliary components of drug; heavy degree of a liver and/or renal failure; concomitant use of MAO inhibitors; pregnancy; lactation period; children's age up to 18 years (experience of a medical use at children is limited).

Rare hereditary problems of a lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption (drug contains lactose).

Overdose:

Strengthening of side effects. Symptomatic treatment.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 25 mg. On 10 or 14 tablets in a blister strip packaging.

On 100, 200, 250, 300 tablets in banks polymeric, corked by covers.

To bank of polymeric or 3, 4, 5 blister strip packagings on 10 tablets or 1, 2, 3, 4 blister strip packagings on 14 tablets together with the application instruction place in a pack from a cardboard.