Esperal, tablets 500 mg 20 pcs

The action of disulfiram is based on the blockade of acetaldehydrogenase, which is involved in the metabolism of ethyl alcohol.

This leads to an increase in the concentration of the metabolite of ethyl alcohol – acetaldehyde, which causes negative feelings (rushes of blood to the face, nausea, vomiting, tachycardia, decreased blood pressure, etc.), which make it extremely unpleasant to drink alcohol after taking the drug.

This leads to a conditioned reflex aversion to the taste and smell of alcoholic beverages.

The maximum therapeutic effect is reached 12 hours after oral administration and may continue for 10-14 days after stopping treatment.

Indications

Prevention and treatment of relapses in chronic alcoholism.

In additionally, the drug is used as a detoxifying agent in chronic nickel poisoning.

Active ingredient

Composition

1 tablet contains:

disulfiram – 0.5 g.

Auxiliary substances:

Polividone K 30,

sodium carmellose,

magnesium stearate,

microcrystalline cellulose,

purified water.

How to take, the dosage

The treatment is prescribed after careful examination of the patient and warning about the consequences and complications.

The drug is taken orally at 0.5 g once a day in the morning with meals according to an individual schedule, gradually reducing the dose to 1/2 or 1/4 tablet a day.

The dose can be changed up or down depending on the response of the patient.

Tetramalcohol test (20-30 ml of 40% ethanol (vodka) after taking 0.5 g of the drug) should be carried out in 7-10 days, in case of weak reaction the alcohol dose should be increased by 10-20 ml (maximum dose of vodka is 100-120 ml).

The test is repeated in 1-2 days in the hospital and in 3-5 days on an outpatient basis, with correction of the dose of alcohol and/or the drug as necessary.

A maintenance dose of 0.15-0.2 g per day for 1-3 years may be used thereafter.

Interaction

Contraindicated combinations:

Alcohol: intolerance reaction (flushes, erythema, vomiting, tachycardia). Alcohol and medicinal products containing alcohol should be avoided. Undesirable combinations.

Isoniazid: behavioral and coordination disorders.

Nitro-5-imidazoles (metronidazole, ornidazole, secnidazole, tinidazole): delirium disorders, confusion.

Phenytoin: significant and rapid increase in plasma concentrations of phenytoin with toxic symptoms (suppression of its metabolism).

If the combination cannot be avoided, clinical monitoring and control of plasma concentrations of the drug during and after treatment with disulfiram should be performed.

Combinations requiring caution:

Warfarin (and other oral anticoagulants): increased effect of oral anticoagulants and risk of bleeding (decreased metabolism of warfarin in the liver). More frequent monitoring of blood prothrombin levels and adjustment of anticoagulant dose within 8 days after disulfiram withdrawal is recommended.

Theophylline: Disulfiram inhibits theophylline metabolism. As a result, the dose of theophylline should be adjusted (reduced dosage), depending on clinical symptoms and plasma concentrations of the drug.

Benzodiazepines: Disulfiram may increase the sedative effect of benzodiazepines by inhibiting their oxidative metabolism (especially chlordiazepoxide and diazepam). Benzodiazepine dosage should be adjusted according to clinical manifestations.

Tricyclic antidepressants: aggravation of alcohol intolerance reaction (if patients who received disulfiram take alcoholic beverages).

Special Instructions

In case of concomitant administration with warfarin or other oral anticoagulants, prothrombin levels should be monitored more frequently and doses of anticoagulants should be adjusted, which is associated with an increased risk of bleeding.

Contraindications

– Severe hepatic insufficiency.
– Diabetes mellitus.
– Epilepsy and seizure syndrome of any genesis.
– Mental disorders.
– Pregnancy.
– Period of lactation.
– Increased individual sensitivity to the drug.

With caution:
– Renal insufficiency.
– Hypothyroidism.

Side effects

Side effects caused by disulfiram:
– metallic taste in the mouth;
– unpleasant odor (caused by sulfur-carbon) in patients with a functioning colostomy;
– rarely – hepatitis (noted both in patients with chronic alcoholism, and in some patients treated for eczema on nickel);
– Polyneuritis of the lower extremities;
– neuropsychiatric disorders, memory loss, disorientation in time and space, asthenia;
– headache;
– skin allergic reactions;

Side effects caused by disulfiram-ethanol association:
– collapse, heart rhythm disorders, angina attacks, myocardial infarction;
– brain edema, cerebral hemorrhage.

Overdose

The disulfiram-ethanol combination causes depression of consciousness, up to coma, cardiovascular collapse, neurological complications.

The treatment is symptomatic.

Pregnancy use

The use is contraindicated in pregnancy and lactation.

Similarities