Universal reference book for medicines
Name of the drug: AZAPHEN ® (AZAPHEN)

Active substance: pipofezine
Type: Antidepressant
Manufacturer: NIZHFARM (Russia) manufactured by MAKIZ-PHARMA (Russia)
Composition, form of production and packaging
Azafen ®
Tablets are yellowish-greenish, flat-cylindrical, with a facet; the presence of marble is allowed.
1 tab.
Pipofezin 25 mg
Auxiliary substances: potato starch - 4 mg, silicon dioxide colloid (aerosil) - 1.75 mg, microcrystalline cellulose - 45 mg, lactose monohydrate - 22 mg, povidone (polyvinylpyrrolidone low molecular weight medical) - 1.25 mg, magnesium stearate - 1 mg.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
14 pcs. - packings of cellular contour (1) - packs cardboard.
14 pcs. - packings cellular planimetric (2) - packs cardboard.
14 pcs. - packings cellular planimetric (3) - packs cardboard.
14 pcs. - packings cellular planimetric (4) - packs cardboard.
100 pieces. - polymer cans (1) - packs of cardboard.
200 pcs. - polymer cans (1) - packs of cardboard.
250 pcs. - polymer cans (1) - packs of cardboard.
300 pcs. - polymer cans (1) - packs of cardboard.
Azafen® MB
Tablets with modified release of a yellowish-greenish color, round, biconvex; the presence of marble is allowed.
1 tab.
Pipofezin 150 mg
Auxiliary substances: hypromellose (methocel K4M Premium) - 90.7 mg, povidone (collidon 25) - 5.6 mg, cellulose microcrystalline - 102.0-98.7 mg, silicon colloidal dioxide (aerosil) - 5.5 mg, magnesium hydrosilicate (talc) - 7.1 mg, magnesium stearate - 3.7 mg.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
14 pcs. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Tricyclic antidepressant. Blocking the reverse neuronal capture of monoamines by presynaptic membranes, increases their content in the synaptic cleft, which leads to relief of the symptoms of depression. Timoleptic action of the drug is combined with sedative activity and anxiolytic effect. In contrast to tricyclic antidepressants it does not possess anticholinergic properties, does not affect the activity of MAO, does not have cardiotoxic effect.
PHARMACOKINETICS
Suction
Quickly and completely absorbed from the digestive tract. Bioavailability is about 80%. T max after taking the tablets - 2 h.
In tablets of Azafen ® MB, the active substance is enclosed in a special carrier matrix, which ensures the gradual release of pipophazine in the digestive tract. The released pypofezin quickly and almost completely absorbed from the digestive tract. With a single ingestion of Azafen 150 mg C max pipofezin in the blood, blood is achieved after 3-4 hours and is 111 ng / ml.
Distribution and Metabolism
Binding to plasma proteins - 90%.
To a large extent, it undergoes biotransformation in the liver with the formation of inactive metabolites.
An in vitro study showed that pipophezin is not a substrate for the isoenzymes CYP2C9, CYP2C19, CYP2D6 and CYP3A4, but is mainly metabolized by CYP1A2.
Excretion
T 1/2 after taking the tablets - 16 h, T 1/2 after taking the modified-release tablets - 9 h. It is excreted mainly by the kidneys.
Time of the drug in the body (MRT) - an average of 13.4 hours (10 to 20 hours). At repeated receptions of fluctuation of concentration of a preparation in a blood plasma in an interval between two doses are smoothed out. It is excreted mainly by the kidneys.
INDICATIONS
- Depressive disorders of mild and moderate severity (including depressive states in chronic somatic diseases).
DOSING MODE
The initial dose for adults is 25-50 mg in 2 divided doses (morning and lunch). With good tolerability, the dose is gradually increased to 150-200 mg / day (3-4 doses, the last intake 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 pass to maintenance doses of 25-75 mg / day. The course of treatment is up to 1 year (not less than 1-1.5 months).
After setting the optimal daily dose using Azafen ® tablets of 25 mg, prescribe Azafen ® MB (modified-release tablets) 150 mg 1 time (morning) or 2 times (morning and evening), taking into account the efficacy and tolerability.
SIDE EFFECT
From the side of the central nervous system: headache, dizziness.
From the digestive system: nausea, vomiting.
Other: allergic reactions.
CONTRAINDICATIONS
- severe hepatic and / or renal insufficiency;
- simultaneous administration of MAO inhibitors;
- Pregnancy;
- lactation period (breastfeeding);
- Hypersensitivity to the drug.
With caution should prescribe the drug for chronic heart failure, myocardial infarction, with IHD, condition after acute cerebrovascular accident, infectious diseases, diabetes, in childhood (not enough data on safety of use).
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated in severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated in severe renal failure.
APPLICATION FOR CHILDREN
Caution should be given to the drug in childhood (not enough data on safety of use).
SPECIAL INSTRUCTIONS
After the transfer from therapy with MAO inhibitors to Azafen ® , an interval of 2 weeks is necessary.
Periodic monitoring of liver and kidney function is necessary.
During the period of treatment, alcohol is not allowed.
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, patients should refrain from engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions, for example, vehicle management.
OVERDOSE
There is no information about overdose.
DRUG INTERACTION
With the simultaneous use of Azafen ® potentiates the effects of ethanol and other drugs that depress the central nervous system, antihistamines and anticoagulants.
Reduces the effectiveness of anticonvulsant therapy.
An in vitro study showed that pipiphezin is not an inhibitor or inducer of the isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, so it is unlikely that the drug Azafen ® interacts with drugs that are substrates of these isoenzymes. Fluvoxamine, propafenone, mexiletine, ciprofloxacin, being inhibitors of CYP1A2, can increase the concentration of pipophezin in the blood plasma.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light, out of reach of children, at a temperature of no higher than 25 ° C. The shelf life of the tablets is 5 years, the modified release tablets are 3 years.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!