Pipofesin

Azafen was developed in the USSR at the Sergo Ordzhonikidze All-Union Scientific-Research Chemical-Pharmaceutical Institute (now OJSC TsKhLS-VNIHFI ). Azafen is approved for medical use by order of the Ministry of Health of the USSR dated 06.06.1970 No. 356. By order of the Ministry of Health of Russia dated 01.23.1998 No. 17 is included in the List of Essential and Essential Medicines . In the new edition of the List , approved by order of the Government of Russia dated March 29, 2007 No. 376-r, azafen is present under the international non-proprietary name pipofesin. In 2007, the registration certificate of Roszdravnadzor for a new prolonged-release dosage form, “Azafen MV” modified-release tablets, was obtained.

The crystalline powder is yellowish-green in color. Easily soluble in water, practically insoluble in alcohol, pH 1.25% solution 2.5-3.0.

It has antidepressant (timoleptic) and sedative effects. The mechanism of action is associated with indiscriminate inhibition of the reverse neuronal uptake of serotonin and norepinephrine , which leads to an increase in their concentrations and relief of symptoms of depression. By pharmacological properties, it is close to imipramine , weakens the depriminating effects of reserpine , enhances the effects of phenamine and 5-hydroxytryptophan, but unlike imipramine (and amitriptyline ) does not have anticholinergic activity. It has no inhibitory effect on MAO . It has no cardiotoxic effect.

Quickly and completely absorbed in the digestive tract . Bioavailability - about 80%, T _max - 2 hours, C _max - 3-4 hours (111 ng / ml). Communication with plasma proteins - 90%. It is metabolized in the liver with the formation of inactive metabolites. T _1/2 - 16 hours. It is excreted mainly by the kidneys .

Pipofesin is widely used in the treatment of various depression. It is prescribed for asthenic and anxiety-depressive states, the depressive phase of bipolar affective disorder , involutional depression, depressions of organic origin, somatogenically caused depressions, reactive depressions, depressive states that develop with prolonged treatment with antipsychotics, as well as with asthenodepressive states of a neurotic nature. It can be used as a “healing” remedy after treatment with other, more powerful drugs.

The drug is especially effective for mild and moderate depression; for deep depression can be used in combination with other tricyclic antidepressants. Pipofesin, if necessary, can be prescribed in combination with antipsychotics.

Due to its good tolerance, sufficiently strong antidepressant activity and sedative effect, pipofesin is widely used in diseases accompanied by depressive and neurotic conditions. There is evidence of the effectiveness of pipofesin for the treatment of depressive states in patients with coronary heart disease.

Pipofesin has been successfully used to treat shallow alcoholic depressions, which occur both with anxiety and with lethargy.

Hypersensitivity, hepatic and / or renal failure , chronic heart failure , myocardial infarction , coronary heart disease , condition after stroke , infectious diseases , diabetes mellitus , first trimester of pregnancy and lactation ^[1] , while taking MAO inhibitors . There is no information on the use of pipofesin in children ^[1] .

Azafen tablets are prescribed orally (after eating) at a dose of 0.025-0.05 g (25-50 mg) in 2 doses (in the morning after breakfast and in the afternoon after lunch). Then the dose is gradually increased by 25-50 mg per day (in 3-4 doses). Typically, the therapeutic dose is 0.15-0.2 g (150-200 mg) per day. If necessary, increase the daily dose to 0.4 g (400 mg). The course of treatment lasts up to 1 year, but at least 1-1.5 months. Upon reaching the therapeutic effect, the doses are gradually reduced and switched to maintenance therapy (25-75 mg per day).

After the optimal daily dose has been established using 25 mg azafen tablets, Azafen MB modified release tablets are prescribed 150 mg 1 time (morning) or 2 times (morning and evening), taking into account their effectiveness and tolerance.

Pipofesin is usually well tolerated. Unlike imipramine, it does not cause exacerbation of psychotic symptoms in patients with schizophrenia (delirium, hallucinations), and does not increase anxiety and fear. The drug does not cause sleep disturbances, and patients can take it in the evening; Pipofesin generally improves sleep. The drug does not have cardiotoxic properties. The absence of pronounced side effects allows you to prescribe the drug to patients with somatic diseases and the elderly.

Due to its good tolerance, pipofesin is more convenient than more powerful tricyclic antidepressants - imipramine , clomipramine and amitriptyline , for use in outpatient practice. Due to the almost complete absence of the anticholinergic action, azafen can be prescribed for patients with glaucoma and other diseases in which the use of drugs with anticholinergic activity, including imipramine and amitriptyline, is contraindicated .

When taking pipofesin, dizziness, nausea, vomiting, and allergic reactions are possible (rarely) ^[1] . After reducing the dose, these phenomena quickly pass. Rarely - mainly at the beginning of therapy or at high doses - there are most often mild side effects such as weakness, fatigue, drowsiness, impaired attention, tachycardia , headache, dry mouth, tremor , dizziness, decreased sex drive ^{[2] [3]} . Has a sedative effect ; cholinolytic and cardiotoxic side effects characteristic of other tricyclic antidepressants are absent ^[4] . In rare cases, an increase in body weight is possible ^[1] .

Enhances the effects of anticoagulants , ethanol , antihistamines , barbiturates ^[1] and other drugs that depress the central nervous system . Reduces the effectiveness of antiepileptic drugs ^[5] . Asafen, like other tricyclic antidepressants, should not be prescribed together with irreversible MAO inhibitors and with reserpine ^[1] . After the use of irreversible MAO inhibitors, pipofesin can be prescribed after 1-2 weeks.

Storage: List B. In a dry, dark place.

Since 1970, azafen was produced at the association of Moskhimpharmpreparat them. N.A. Semashko . In the mid-90s, due to a lack of raw materials, the drug was not developed. Since 2005, under the exclusive license of OJSC “ TsKHLS-VNIHFI ”, azafen is again produced by ZAO “Makiz-Pharma” at an enterprise in Moscow, since 2007 it has been part of the STADA CIS holding (STADA CIS).

• Description of the drug on the manufacturer's website