Azafen, tablets 25 mg 50 pcs

Tricyclic antidepressant. By blocking reverse neuronal uptake of monoamines by presynaptic membranes, it increases their content in the synaptic cleft, which leads to relief of depression symptoms. The tholeptic action of the drug is combined with sedative activity and anxiolytic effect. Unlike tricyclic antidepressants it does not have choline-blocking properties, does not affect the activity of MAOIs, does not have cardiotoxic effect.

Pharmacokinetics

Intake

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

The active substance in tablets Azafen MB is contained in a special carrier matrix allowing gradual release of pipofesine in the gastrointestinal tract. Released pipofesine is quickly and almost completely absorbed from the gastrointestinal tract. When single oral administration of Azafen MB 150 mg tablet Cmax in blood is reached after 3-4 hours and is 111 ng/ml.

Distribution and metabolism

The binding to plasma proteins is 90%.

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

In in vitro study it was shown that pipofezine is not a substrate of CYP2C9, CYP2C19, CYP2D6 and CYP3A4 isoenzymes, but is predominantly metabolized under the influence of CYP1A2.

The T1/2 after taking the tablets is 16 h, the T1/2 after taking the tablets with modified release is 9 h. It is excreted mainly by the kidneys.

The drug retention time in the body (MRT) is on the average 13.4 hours (from 10 to 20 hours). When repeated administration of the drug in plasma concentration fluctuations between two doses are smoothed out. It is eliminated from the body mainly by the kidneys.

Indications

Depressive episodes of mild to moderate severity (including chronic somatic diseases).

Active ingredient

Composition

Active ingredient:

propofezine dihydrochloride monohydrate 25 mg

Her excipients:

Potato starch, 4 mg;

Colloidal silicon dioxide (aerosil) – 1.75 mg;

MCC – 45 mg;

Lactose monoclase – 25 mg.

Lactose monohydrate – 22 mg;

Povidone (low molecular weight medical PVC) – 1.25 mg;

Magnesium stearate – 1 mg

How to take, the dosage

The initial dose for adults is 25-50 mg in 2 doses (in the morning and at lunchtime). If well tolerated, 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, 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 with Azafen 25 mg tablets, Azafen MB (tablets with modified release) is prescribed 150 mg once (in the morning) or twice (morning and evening), taking into account efficacy and tolerability.

Interaction

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

Decreases the effectiveness of antiepileptic drugs.

In vitro study showed that AZAPHEN is not an inhibitor or inducer of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 isozymes, so there is unlikely interaction of AZAPHEN with drugs which are substrates of these isozymes.

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

Special Instructions

A 1-2 week interval is necessary after switching from MAO inhibitor therapy to Azafen.

Alcohol should be avoided during treatment. Any depressive disorder itself increases the risk of suicide. Therefore, patients should be monitored during treatment for early detection of disturbances or behavioral changes, as well as suicidal tendencies.

Influence on performance of potentially hazardous activities requiring increased attention and psychomotor responsiveness

Due to the possible decrease in concentration during treatment, one should refrain from performing potentially hazardous activities requiring increased attention and psychomotor responsiveness (driving vehicles, working with moving machinery, work of dispatcher and operator, etc.).

Contraindications

Side effects

Headache, dizziness, nausea, vomiting, allergic reactions.

In the beginning of therapy, weakness, drowsiness, impaired concentration, dry mouth may occur, which are leveled out without additional treatment.