Azafen (pipofesin) - return to clinical practice

Mixing alcoholic beverages with any medications is extremely dangerous, since the consequences can be very unpredictable. It is especially dangerous to combine alcohol with antidepressants. As a result of such experiments, the therapeutic effect of sedatives is completely neutralized, but the toxic effect increases by 2–3 times.

Read in the article:
• What are antidepressants?
• Effect of drugs
• Main groups of antidepressants
• Consequences of combining antidepressants and alcohol
• Antidepressants and beer
• Azafen and alcohol
• Zoloft and alcohol
• Cipralex and alcohol
• Deprim and alcohol
• Pyrazidol with alcohol
• Persen and alcohol
• Novopassit and alcohol
• Xanax and alcohol
• Tranquilizers with alcohol
• Neuroleptics and alcohol: possible lethal outcome?
• Antidepressant after alcohol
• Signs of poisoning with antidepressants and alcohol
• Help with detoxification in drug treatment

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.

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As a result, the load on internal organs sharply increases, which can lead to:

• A sharp jump in blood pressure,
• Tachycardia,
• Shortness of breath.

In severe cases, a hypertensive crisis may occur.

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.

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Antidepressants and beer

Beer itself has a pronounced sedative effect; after drinking it, a person relaxes and becomes lethargic. When combined with antidepressants, excessive depression of the central nervous system is possible, resulting in:

• A sharp drop in blood pressure is possible, leading to critical conditions and death;
• Movements and speech will become inhibited, the person will not be able to adequately think and perceive what is happening;
• Excessive depression of the central nervous system can cause an effect similar to an overdose of sleeping pills - a person will plunge into a deep and prolonged sleep, from which he may not recover at all.

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 .

Help with detoxification in drug treatment

If such a situation occurs and a person experiences negative symptoms due to taking a sedative with alcohol, it is necessary to urgently consult a neurologist for a detoxification procedure.

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Specialists can detoxify the body using a drip both in the clinic and at home. In severe cases, a resuscitation team arrives on call, and hardware techniques are used for detoxification.

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.

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 .

Signs of poisoning with antidepressants and alcohol

When drinking alcohol together with sedatives, acute intoxication of the body can occur, which manifests itself in the following symptoms:

• vomiting and nausea,
• severe headaches,
• increased body temperature,
• hyperemia of the skin of the face, hands, neck,
• tachycardia,
• cramps in the limbs.

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.

Effect of drugs

Antidepressants have a stimulating psycho-energizing effect) on the central nervous system, resulting in:

• increasing initiative,
• activation of thinking, normal daily activities,
• reduction of physical fatigue;
• reducing anxiety;
• normalization of sleep.

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.

Use of the drug for alcoholism

If alcohol is constantly in a person’s blood, taking the drug is contraindicated. This is due to the sedative effect. There is a high probability of mutual reinforcement of this effect - the person will fall asleep for several days or fall into a coma. There is also a high risk of death.

Moreover, both substances negatively affect the liver, overloading it. Systematic combined use will lead to the destruction of its cells. Therefore, taking antidepressants for alcoholism is contraindicated.

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.

Consequences of combining antidepressants and alcohol

• Increased symptoms of depression and anxiety . Alcohol consumption negates the use of antidepressants, which complicates drug treatment. Alcohol may seem to improve your mood temporarily, but its overall effect will only increase symptoms of anxiety and depression.
• Increased side effects from both medications and alcohol . Sedatives have a toxic effect, which is greatly enhanced when the body is poisoned by ethanol particles. As a result, hangover symptoms and negative effects on the body increase significantly.
• When taken together with certain types of alcoholic drinks and foods, antidepressants , called IMAOs, can cause a dangerous spike in blood pressure. If you are taking IMAOs, make sure what foods and drinks you can take with these medications.
• Weakened concentration, coordination and memory . The combination of sedatives and alcohol affects thinking, coordination, motor skills and reaction time more than just the intoxication of alcohol. This can impair the ability to perform tasks requiring high concentration and can be life-threatening.
• Increased sedation . The sedative effect of sleeping pills can be increased several times. Or, conversely, you can reduce the effectiveness of the sleeping pills, resulting in insomnia.
• The combined use of two psychoactive substances (substances that act at the level of the central nervous system) can lead to hallucinosis, a mental disorder that leads to impaired consciousness, memory and attention disorders.

When can you take the drug, after how long

It is allowed to begin therapy with antidepressants only after complete removal of ethyl alcohol and its breakdown products from the blood and body. This usually takes 24 to 48 hours. But doctors recommend starting to take medications 2-3 days after the last drink.

This time is needed so that all toxins have time to be neutralized. Following this rule will minimize the occurrence of adverse reactions and increase the effectiveness of treatment.

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.