Azafen, pills 25mg, 50pcs

Composition

Active ingredient:  

pipofesin dihydrochloride monohydrate 25 mg

excipients:

potato starch-4 mg;

colloidal silicon dioxide (aerosil) – 1.75 mg;

MCC-45 mg;

lactose monohydrate-22 mg;

povidone (low-molecular-weight medical PVP) – 1.25 mg;

magnesium stearate-1 mg

Pharmacological action

Tricyclic antidepressant. Blocking the reverse neuronal uptake of monoamines by presynaptic membranes increases their content in the synaptic cleft, which leads to relief of symptoms of depression. The thymoleptic effect of the drug is combined with sedative activity and anxiolytic effect. Unlike tricyclic antidepressants, it does not have holinoblocking properties, does not affect the activity of MAO, and does not have a cardiotoxic effect.

Pharmacokinetics

Suction

It is quickly and completely absorbed from the gastrointestinal tract. Bioavailability is about 80%. Tmax After taking tablets – 2 hours.

In Azafen MB tablets, the Active ingredient is contained in a special matrix carrier that provides a gradual release of pipofesin in the gastrointestinal tract. Released pipofesin is rapidly and almost completely absorbed from the gastrointestinal tract. With a single oral dose of Azafen MB 150 mg tablet, the Cmax of pipofesin in the blood is reached in 3-4 hours and is 111 ng / ml.

Distribution and metabolism

Binding to plasma proteins is 90%.

It is largely biotransformed in the liver with the formation of inactive metabolites.

An in vitro study showed that pipofesin is not a substrate of the isoenzymes CYP2C9, CYP2C19, CYP2D6 and CYP3A4, but is mainly metabolized under the influence of CYP1A2.

Elimination

T1 / 2 after taking tablets – 16 hours, T1 / 2 after taking tablets with modified release – 9 hours. It is excreted from the body mainly by the kidneys.

Drug retention time in the body (MRT) is an average of 13.4 hours (from 10 to 20 hours). With repeated doses, fluctuations in the concentration of the drug in blood plasma in the interval between two doses are smoothed out. It is excreted from the body mainly by the kidneys.

Indications

Depressive episodes of mild and moderate severity (including those with chronic somatic diseases).

Contraindications

Hypersensitivity to the main and / or auxiliary components of the drug; severe hepatic and/or renal insufficiency; concomitant use of MAO inhibitors; pregnancy; lactation; children under 18 years of age (limited experience of medical use in children). Rare hereditary problems of lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the drug contains lactose). With caution, chronic heart failure, myocardial infarction, ischemic heart disease, post-stroke conditions, infectious diseases, diabetes mellitus (due to insufficient safety data).

Side effects

Headache, dizziness, nausea, vomiting, allergic reactions.

At the beginning of therapy, weakness, drowsiness, impaired concentration of attention, dry mouth may appear, which are leveled without additional treatment.

Interaction

Enhances the effects of ethanol, antihistamines, and other CNS depressants, anticoagulants.

Reduces the effectiveness of antiepileptic drugs.

An in vitro study showed that Azafen is not an inhibitor or inducer of the isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, so it is unlikely that Azafen interacts with drugs that are substrates of these isoenzymes.

Fluvoxamine, propafenone, mexiletine, ciprofloxacin (inhibitors of the CYP1A2 isoenzyme) can increase the concentration of Azafen in blood plasma.

How to take, course of use and dosage

The initial dose for adults is 25-50 mg in 2 divided doses (in the morning and at lunch). With good tolerability, the dose is gradually increased to 150-200 mg / day (in 3-4 doses, the last dose before bedtime), in some cases – up to 400 mg/day. The optimal daily dose is 150-200 mg, the maximum daily dose is 400-500 mg. When the desired effect is achieved, they switch to maintenance doses of 25-75 mg / day. The course of treatment is up to 1 year (at least 1-1.5 months).

After establishing the optimal daily dose using 25 mg Azafen tablets, Azafen MB (modified release tablets) is prescribed 150 mg 1 time (morning) or 2 times (morning and evening), taking into account the effectiveness and tolerability.

Overdose

There is no information available.

Special instructions

After switching from MAO inhibitor therapy to Azafen, an interval of 1-2 weeks is required.

During the treatment period, you should refrain from taking alcohol. Any depressive disorder itself increases the risk of suicide. Therefore, during treatment, patients should be monitored for early detection of behavioral disorders or changes, as well as suicidal tendencies.

Influence on the performance of potentially dangerous activities that require special attention and speed of psychomotor reactions

Due to a possible decrease in concentration during treatment, you should refrain from engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions (driving vehicles, working with moving mechanisms, working as a dispatcher and operator, etc. ).

Form of production

Tablets of 25 mg. 10 or 14 tablets in a contour cell package. 100,200,250,300 tablets in polymer cans, sealed with lids. A polymer jar or 3,4,5 contour cell packs of 10 tablets or 1,2,3,4 contour cell packs of 14 tablets together with the instructions for use is placed in a cardboard pack.

Storage conditions

List B. Store in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 5 years.

Active ingredient

Pipofezin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

Adults as prescribed by a doctor

Indications

Depression