Tricyclic antidepressant. Reverse blocking presynaptic neuronal uptake of monoamines membranes increases their content in the synaptic cleft, which leads to a relief of the symptoms of depression. Timolepticheskoe effect of the drug combined with sedative activity, and anxiolytic effect. Unlike tricyclic antidepressants has no anticholinergic properties, it has no effect on MAO activity, lacking cardiotoxic action.
Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability – 80%. Tmaxposle reception of tablets – 2 hours.
In tablets Azafen MB active substance enclosed in a special matrix carrier that provides a gradual release in the gastrointestinal tract pipofezine. Pipofezine liberated rapidly and almost completely absorbed from the gastrointestinal tract. In single ingestion tablets azafen CF 150 mg Cmax pipofezine blood achieved after 3-4 hours and is 111 ng / ml.
Distribution and metabolism
Binding to plasma proteins – 90%.
Largely biotransformation in the liver to inactive metabolites.
The in vitro study demonstrated that pipofezine not a substrate isoenzymes CYP2C9, CYP2C19, CYP2D6 and CYP3A4, and is metabolized mainly influenced by CYP1A2.
T1 / 2 after taking the tablets – 16 hours, T1 / 2, after receiving a modified release tablets -. 9 hours Write excreted mainly by the kidneys.
The residence time of the drug in the organism (MRT) – average 13.4 hours (10 to 20 hours). Repeated receptions fluctuations in plasma concentrations of drug in the interval between the two doses are smoothed. Excreted mainly by the kidneys.
Makiz Pharma, Russia
Adults are prescribed by a doctor
Active ingredient: pipofezine dihydrochloride monogidrat25 mgvspomogatelnye material: potato starch – 4 mg; colloidal silicon dioxide (Aerosil) – 1.75 mg; MCC – 45 mg; lactose monohydrate – 22 mg; Povidone (PVP low molecular Medical) – 1.25 mg; Magnesium stearate – 1 mg
Depressive episodes of mild to moderate severity (including chronic somatic diseases).
Hypersensitivity to main and / or auxiliary components of the drug; severe degree of hepatic and / or renal failure; simultaneous MAO inhibitors; pregnancy; lactation; Children up to age 18 years (experience of medical use in children is limited).
Rare hereditary problems of lactose intolerance, lactase deficiency, glucose-galactose malabsorption (drug contains lactose).
Chronic heart failure, myocardial infarction, ischemic heart disease, post-stroke, infectious diseases, diabetes mellitus (due to the lack of safety data).
Headache, dizziness, nausea, vomiting, allergic reactions.
At the beginning of therapy may cause weakness, drowsiness, impaired concentration, dry mouth, which leveled without additional treatment.
How to accept, acceptance rate and dosage
The initial dose for adults is 25-50 mg in 2 divided doses (morning and afternoon). With good endurance gradually increase the dose to 150-200 mg / day (3-4 hours, the last intake before bedtime), in some cases – up to 400 mg / day. The optimal daily dose – 150-200 mg with a maximum daily dose – 400-500 mg. When the desired effect on the moving support dose – 25-75 mg / day. The course of treatment – up to 1 year (at least 1-1.5 months).
After establishing the optimal daily dose using Azafen tablets of 25 mg, administered Azafen MB (modified-release tablets) of 150 mg of 1 times (morning) or 2 times (morning and evening) with the efficacy and tolerability.
List B. Store in a dry, dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Enhances effects of ethanol, antihistamines and others. CNS depressants, anticoagulants.
Reduces the effectiveness of antiepileptic drugs.
The in vitro study demonstrated that Azafen not an inhibitor or inducer isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, is therefore unlikely azafen interaction with drugs that are substrates of these isoenzymes.
Fluvoxamine, propafenone, mexiletine, ciprofloxacin (inhibitors isoenzyme CYP1A2) azafen can increase the concentration in plasma.
After transfer therapy with MAO inhibitors on Azafen required interval in 1-2 weeks.
During the period of treatment should refrain from drinking alcohol. Any depressive disorder in itself increases the risk of suicide. Therefore, during treatment of patients should be monitored for early detection of faults or changes in behavior and suicidal tendencies.
Impact on the performance of potentially hazardous activities that require attention and quickness of psychomotor reactions
In connection with a possible decrease in concentration during the period of treatment should refrain from activities potentially hazardous activities that require increased attention and psychomotor speed reactions (vehicle control, work with moving machinery, the work manager and the operator and others.).
No data available.