Azafen is a psychotropic drug, a tricyclic antidepressant. It has a sedative and calming effect aimed at balancing certain elements of the brain that are responsible for the state of depression. Azafen reduces feelings of anxiety and excitement. The drug is an old-format antidepressant; it was developed and received permission for use back in 1970. However, its high effectiveness is still confirmed by positive reviews from patients and numerous studies of the drug. One of the latest studies was conducted in 2005, for a month and a half, people with depression were given Azafen. As a result, 53% experienced a complete recovery, while the rest remained with minor symptoms of the disease. First of all, the drug relieves anxiety, lethargy, and improves mood.
The main advantage of Azafen compared to other tricyclic antidepressants is that this drug has a low toxic effect on the body, including the heart, and it does not block cholinergic receptors and does not change the activity of monoamine oxidase. The maximum concentration in the blood is reached 1-2 hours after taking the drug. Absorbed in the gastrointestinal tract, metabolism occurs in the liver, and Azafen is excreted by the kidneys.
Pharmacodynamics and pharmacokinetics
Azafen is a tricyclic antidepressant and belongs to a group of drugs that indiscriminately inhibit (suppress) the neuronal uptake of monoamines . The antidepressant effectiveness of the active ingredient of the drug, pipofezin, is manifested due to its ability to non-selectively inhibit the neuronal reuptake of norepinephrine and serotonin , which leads to an increase in their levels in the central nervous system. In the drug Azafen, thymoleptic (improving mental state and mood) activity is combined with sedative (calming) effects and anxiolytic (anti-anxiety) effect.
Pipofezin has virtually no m-anticholinergic effects and does not affect the activity of the enzyme monoamine oxidase (MAO). Also, this drug is not characterized by cardiotoxic effects.
Oral administration of pipofezin leads to rapid and complete absorption from the gastrointestinal tract. The bioavailability of the drug is approximately 80%. Binding to plasma proteins occurs by 90%. With a single oral dose of 25 mg, the Cmax of pipofezin after 60-120 minutes is 24.5 ng/ml.
Metabolic transformations take place in the liver with the help of the CYP1A2 isoenzyme and the release of inactive metabolic products.
Pipofezin from the bloodstream quite quickly, T1/2 of the drug is 4.3 hours. Excretion is carried out primarily by the kidneys.
Release form and composition
Azafen belongs to the group of tricyclic antidepressants. Has sedative properties.
Available in the form of tablets containing 25 mg of the active substance - pipofezin dihydrochloride monohydrate, located in a carrier matrix.
Excipients:
- Potato starch;
- Colloidal silicon dioxide (aerosil);
- Microcrystalline cellulose;
- Lactose monohydrate;
- Povidone (low molecular weight medical polyvinylpyrrolidone);
- Magnesium stearate.
Contraindications
Therapy with Azafen is absolutely contraindicated in the following cases:
- severe liver and/or kidney pathologies;
- breastfeeding;
- concurrent use of MAO inhibitors ;
- personal hypersensitivity to pipofezin or other auxiliary ingredients of tablets;
- pregnancy.
Patients suffering from:
- chronic heart failure;
- infectious diseases;
- myocardial infarction;
- diabetes mellitus;
- coronary heart disease;
- cerebrovascular accidents (including post-stroke conditions).
Also, pediatric patients require a particularly careful approach to prescribing Azafen.
Side effects of Azafen
Some patients experienced side effects while using Azafen, such as headaches , nausea , dizziness and vomiting . Also, if the patient is sensitive to the active or auxiliary ingredients of the tablets, allergic reactions .
Indications for use
The effectiveness of pipofezin is based on the relief of symptoms of depression, therefore indications for the use of Azafen are depression of various origins, including:
- Endogenous;
- Exogenous;
- Alcohol;
- Senile.
In addition, the drug is used to treat the following conditions:
- Depression due to chronic somatic diseases;
- Anxiety and depressive syndromes;
- Depressive phase in manic-depressive syndrome;
- Astheno-neurotic syndromes.
First of all, after the start of treatment, an improvement in mood occurs, followed by the disappearance of anxiety and lethargy.
Azafen, instructions for use (Method and dosage)
Instructions for use of Azafen involve a course of prescription of the drug tablets for up to 1 year (the minimum therapeutic course is 1-1.5 months).
As a rule, Azafen is initially prescribed in a daily dose of 25-50 mg (1-2 tablets) taken twice a day (morning and afternoon). In case of good tolerability of the drug and adequate response of the patient to the treatment, a gradual increase in the daily dosage is practiced to 150-200 mg (6-8 tablets), sometimes up to 400 mg (16 tablets), with its 3-4-fold dose in 24 hours (last dose taken before bedtime). The optimal therapeutic dosage is considered to be a daily dose of 150-200 mg (6-8 tablets). It is permissible to take 500 mg (20 tablets) of the drug within a maximum of 24 hours. After achieving the desired positive effect of therapy, the patient is transferred to maintenance dosages varying in the range of 25-75 mg (1-3 tablets) per day.
Azafen® (Azaphen)
Manufacturer: NIZHFARM OJSC (Russia)
tab. 25 mg: 14, 28, 30, 40, 42, 50, 56, 100, 200, 250 or 300 pcs. Reg. No.: LS-000325
Clinical and pharmacological group:
Antidepressant
Release form, composition and packaging
Pills
yellowish-greenish color, flat-cylindrical, chamfered; Marbling is allowed.
| 1 tab. | |
| pipofezin | 25 mg |
Excipients:
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) - 1.25 mg, magnesium stearate - 1 mg.
10 pieces. — cellular contour packages (3) — cardboard packs. 10 pieces. — contour cell packaging (4) — cardboard packs. 10 pieces. — contour cell packaging (5) — cardboard packs. 14 pcs. — cellular contour packages (1) — cardboard packs. 14 pcs. — contour cell packaging (2) — cardboard packs. 14 pcs. — cellular contour packages (3) — cardboard packs. 14 pcs. — contour cell packaging (4) — cardboard packs. 100 pieces. — polymer jars (1) — cardboard packs. 200 pcs. — polymer jars (1) — cardboard packs. 250 pcs. — polymer jars (1) — cardboard packs. 300 pcs. — polymer jars (1) — cardboard packs.
Description of the active components of the drug "Azafen®"
pharmachologic effect
Tricyclic antidepressant. By blocking the reverse neuronal uptake of monoamines by presynaptic membranes, it increases their content in the synaptic cleft, which leads to relief of symptoms of depression. The thymoleptic effect of the drug is combined with sedative activity and anxiolytic effect. Unlike tricyclic antidepressants, it does not have anticholinergic properties, does not affect the activity of MAO, and does not have a cardiotoxic effect.
Indications
- depressive disorders of mild and moderate severity (including depressive states in chronic somatic diseases).
Dosage regimen
Initial dose for adults
is 25-50 mg in 2 doses (morning and lunch). 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 - 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 using Azafen® 25 mg tablets, Azafen® MB (modified-release tablets) 150 mg is prescribed 1 time (morning) or 2 times (morning and evening), taking into account effectiveness 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 liver and/or kidney failure;
- simultaneous use of MAO inhibitors;
- pregnancy;
- lactation period (breastfeeding);
- hypersensitivity to the drug.
Carefully _
the drug should be prescribed for chronic heart failure, myocardial infarction, ischemic heart disease, a condition after an acute cerebrovascular accident, infectious diseases, diabetes mellitus, in childhood (there is insufficient data on the safety of use).
Pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
Use for liver dysfunction
The drug is contraindicated in severe renal failure.
Use for renal impairment
The drug is contraindicated in severe renal failure.
Application for children
Carefully _
the drug should be prescribed in childhood (there is insufficient data on the safety of use).
special instructions
After transferring from therapy with MAO inhibitors to Azafen®, an interval of 2 weeks is required.
Periodic monitoring of liver and kidney functions is necessary.
During the treatment period, alcohol consumption is prohibited.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, patients should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions, for example, driving.
Overdose
There is no information about overdose.
Drug interactions
When used simultaneously, Azafen® potentiates the effects of ethanol and other central nervous system depressants, antihistamines and anticoagulants.
Reduces the effectiveness of anticonvulsant therapy.
An in vitro study showed that pipofezin is not an inhibitor or inducer of the isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, therefore it is unlikely that Azafen® will interact with drugs that are substrates of these isoenzymes. Fluvoxamine, propafenone, mexiletine, ciprofloxacin, being inhibitors of CYP1A2, can increase the concentration of pipofezine in the blood plasma.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
List B. The drug should be stored in a dry place, protected from light, out of reach of children, at a temperature not exceeding 25°C. The shelf life of tablets is 5 years, modified-release tablets are 3 years.
Drug interactions
When used simultaneously, Azafen® potentiates the effects of ethanol and other central nervous system depressants, antihistamines and anticoagulants.
Reduces the effectiveness of anticonvulsant therapy.
An in vitro study showed that pipofezin is not an inhibitor or inducer of the isoenzymes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, therefore it is unlikely that Azafen® will interact with drugs that are substrates of these isoenzymes. Fluvoxamine, propafenone, mexiletine, ciprofloxacin, being inhibitors of CYP1A2, can increase the concentration of pipofezine in the blood plasma.
Interaction
While taking Azafen, there is a decrease in the effectiveness of concurrent anticonvulsant therapy .
The combined use of pipofezin with anticoagulants , antihistamines , ethanol-containing and other central nervous system depressants potentiates their effectiveness and, as a result, toxicity .
Co-administration of ciprofloxacin , fluvoxamine , mexiletine , propafenone and other drugs that inhibit the CYP1A2 isoenzyme may cause an increase in the plasma concentration of pipofezin .
special instructions
depressive state itself is associated with a risk of suicidal tendencies , and therefore, during the treatment of such mental disorders patients should be monitored for early detection of changes in their behavioral sphere and the prevention of possible suicide attempts .
between courses of therapy using MAO inhibitors and Azafen.
At all stages of the therapeutic course, it is necessary to periodically check the functionality of the liver / kidneys .
While taking Azafen tablets, it is better for the patient to refrain from performing potentially life-threatening activities, including driving.
Analogs
Level 4 ATC code matches:
Pipofezin
Bethol
Incazan
Melitor
Miaser
Velafax
Mirtazonal
Venlaxor
Remeron
Venlafaxine
Lerivon
Mirtazapine
Cymbalta
Velaxin
Coaxil
Pyrazidol
Deprim
Gelarium Hypericum
Negrustin
Trittico
Analogues of Azafen are represented by medicinal drugs with a similar main effect:
- Alventa;
- Velaxin;
- Bethol;
- Venlaxor;
- Mirzaten;
- Deprim;
- Mirtazonal;
- Coaxil;
- Pyrazidol;
- Noxibel;
- Remeron;
- Trittico;
- Neuroplant;
- Ephevelon;
- Tetrindole , etc.
Reviews about Azafen
In the process of discussing the effectiveness and relative safety of using this antidepressant , positive reviews about Azafen are much more common than negative statements about it. Most patients who took this drug at one time managed to overcome their own depression , cope with feelings of anxiety and apathy , and significantly improve their mood and general mental state. Mentions of Azafen's side effects are quite rare and are mainly related to personal sensitivity to its ingredients.
However, it is worth recalling that the personal prescription and use of any antidepressant medications is unacceptable and can lead to serious negative consequences. Treatment of a person’s mental sphere, with individual selection of a medicinal drug and its dosage regimen, should be carried out exclusively by a psychotherapist with experience in conducting such therapy.
Azafen
Azafen (pipofezin) is a drug from the group of tricyclic antidepressants. Prescribed for mild to moderate depression. This is an original drug developed in the USSR in the 60s of the last century. Introduced into medical practice in 1970. In 1996, the drug was discontinued due to the lack of pharmaceutical raw materials for its production, but in 2005 Azafen reappeared on pharmacy shelves. The effect of the drug is based on its ability to increase the level of serotonin and norepinephrine in the central nervous system. Among other tricyclic antidepressants, the drug stands out due to its lack of toxic effect on the heart and anticholinergic activity. Azafen also has a moderate sedative effect. The effectiveness of the drug has been confirmed in several clinical trials. In patients with mild to moderate depression, Azafen showed a uniform reduction in the severity of symptoms of affective disorders. In half of the study participants, the symptoms were completely relieved; in the rest, the clinical picture was noticeably smoothed out. Experience with Azafen shows that when using the drug, mood improvement is observed most quickly, then anxiety symptoms (anxiolytic component) are eliminated, and lethargy is eliminated a little more slowly. Thus, the sedative and anxiolytic effects of the drug are somewhat ahead of its antidepressant effect. Complete elimination of inhibition of thinking and speech, as well as restoration of previous motor activity, is observed after a month of drug therapy. Azafen has demonstrated its effectiveness in depression of alcohol origin, both after abstinence and at the stage of remission.
The drug eliminates the craving for alcohol, reduces the risk of developing behavioral disorders, and improves mood. Azafen is also used for depression caused by somatic pathologies, incl. cardiovascular and gastrointestinal diseases, menopausal syndrome. Azafen has a favorable safety profile. Undesirable side reactions (weakness, drowsiness, absent-mindedness, slight increase in heart rate, hyposalivation, headache) are, as a rule, mild in severity and, when taking the drug in a daily dose of 100–200 mg, develop only in every fifth case. Pipofezin is quickly and completely absorbed from the gastrointestinal tract. Peak concentration in the blood is reached 2 hours after administration. Half-life is 16 hours. Excreted from the body mainly with urine. Azafen is contraindicated in persons with individual intolerance to pipofezin, severe liver and kidney diseases, during pregnancy and breastfeeding. The frequency of use of the drug is 2 times a day (after waking up in the morning and at lunchtime). If the drug is well tolerated, it is taken 3-4 times a day, with the last dose before going to bed. When control of the symptoms of the disease is achieved, the dose is reduced (so-called maintenance therapy). The duration of the medication course is at least one month. The maximum duration is up to one year. Taking Azafen is incompatible with drinking alcohol. During the medication course, you should refrain from engaging in potentially hazardous activities that require attention and concentration, incl. driving a car.
