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Active ingredients
Pipofezin
Release form
Pills
Composition
1 tablet contains: pipofezin 25 mg. Auxiliary substances: potato starch - 4 mg, colloidal silicon dioxide (aerosil) - 1.75 mg, microcrystalline cellulose - 45 mg, lactose monohydrate - 22 mg, povidone (low molecular weight medical polyvinylpyrrolidone medical) - 1.25 mg, medical mg, 1.25 mg, honey, stearate - 1 mg.
Pharmacological 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 symptoms of depression. Thymoleptic effect of the drug is combined with sedative activity and anxiolytic effect. Unlike tricyclic antidepressants, it does not possess anticholinergic properties, does not affect the activity of MAO, and has no cardiotoxic effect.
Pharmacokinetics
Absorption: Quickly and completely absorbed from the digestive tract. Bioavailability is about 80%. Tmax after taking the pills - 2 hours. In the pills Asaphen MB, the active substance is enclosed in a special carrier matrix, which ensures the gradual release of pipofesin in the gastrointestinal tract. The released pipofezin is rapidly and almost completely absorbed from the gastrointestinal tract. With a single ingestion of Azafen MV tablet, 150 mg Cmax of pipofezin in the blood is reached in 3-4 hours and is 111 ng / ml. Distribution and metabolism: Plasma protein binding - 90%. Substantially undergoes biotransformation in the liver with the formation of inactive metabolites. An in vitro study has shown that pipofesin is not a substrate of CYP2C9, CYP2C19, CYP2D6, and CYP3A4 isoenzymes, but is primarily metabolized by CYP1A2. Withdrawal: T1 / 2 after taking the pills - 16 h, T1 / 2 after taking the pills with a modified release - 9 h. Excreted mainly by the kidneys. The residence time of the drug in the body (MRT) is on average 13.4 hours (from 10 to 20 hours). With repeated administration, fluctuations in the concentration of the drug in the blood plasma in the gap between the two doses are smoothed out. Excreted mainly by the kidneys.
Indications
Azafen is widely used in the treatment of various depressions (depressed state). Azafen is prescribed for asthenia anxiety-depressive states, the depressive stage of manic-depressive psychosis (psychosis with alternating arousal and depression of mood), involutionary melancholia (senile depression), and organic depression ), somatogenous depression, reactive depression, depressive states,developing with prolonged treatment with neuroleptics (drugs that have an inhibitory effect on the central nervous system and in usual doses do not cause a hypnotic effect), as well as in astheno-depressive states (weakness, depressed state) of a neurotic nature. It can be used as a “after-treatment” agent after treatment with other drugs. The drug is especially effective in depressions of mild to moderate severity. with deep depression can be used in combination with other tricyclic antidepressants. Azafen, if necessary, can be prescribed in combination with neuroleptics. Due to its good tolerance, a sufficiently strong antidepressant (improving mood) activity and sedative effect, azaphene is widely used in diseases accompanied by depressive and neurotic states. There is evidence of the effectiveness of azafen for the treatment of depressive states in patients with ischemic heart disease. With success, azafen has been used to treat shallow alcoholic depressions that occur with both anxiety and inhibition.
Contraindications
Azafen, like other tricyclic antidepressants, should not be prescribed together with MAO inhibitors. After applying these drugs, azaphene can be prescribed in 1-2 weeks.
Precautionary measures
From the side of the central nervous system: headache, dizziness. On the part of the digestive system: nausea, vomiting.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Dosage and administration
Azafen Inside. The initial dose for adults is 25–50 mg in 2 doses (in the morning and in the afternoon). With good tolerance, the dose is gradually increased to 150–200 mg / day (3–4 doses, the last dose before bedtime), and in some cases up to 400 mg / day. The optimal daily dose is 0.15–0.2 g, the maximum is 0.4–0.5 g. When the desired effect is achieved, they are transferred to maintenance doses: 25–75 mg / day. The course of treatment is up to 1 year (at least 1–1.5 months). Azafen MVVnutr. After establishing the optimal daily dose using 25 mg Azafen pills, Azafen MV is prescribed 150 mg 1 time (in the morning) or 2 times (in the morning and in the evening) taking into account effectiveness and tolerability.
Overdose
No information on overdose.
Interaction with other drugs
With the simultaneous use of Azaphen potentiates the effects of ethanol and other means of inhibiting the central nervous system, antihistamines and anticoagulants. Reduces the effectiveness of anticonvulsant therapy. The in vitro study showed that pipofesin is not an inhibitor or inducer of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 isoenzymes, therefore, the interaction of the drug Azaphen with drugs, which are substrates of these isoenzymes, is unlikely. Fluvoxamine, propafenone, meksiletin, ciprofloxacin, being CYP1A2 inhibitors, can increase the concentration of pipofezin in the blood plasma.
special instructions
After transferring from therapy with MAO inhibitors to Azafen, an interval of 2 weeks is required. Periodic monitoring of liver and kidney function is necessary. Alcohol is prohibited during treatment. Influence on the ability to drive vehicles and control mechanisms During the period of treatment, patients should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions, for example, driving.