Antabusum

General characteristics. Structure:

Active agent - Disulfiramum of 200 mg or 400 mg;
excipients: starch corn, povidone, tartaric acid, Natrii hydrocarbonas, talc, silicon dioxide colloid, magnesium stearate, cellulose microcrystallic.

Description:

For a dosage of 200 mg: round flat tablets of white or almost white color with slanted edges, with risky and marking of "CD" on the one hand risks and "About" on the other hand risks.

For a dosage of 400 mg: round flat tablets of white or almost white color with slanted edges, with crosswise risky, dividing a tablet into four parts, and marking of "CJ" on the one hand.

Pharmacological properties:

Effect of drug is based on blockade of an atsetaldegiddegidrogenaza. which participates in alcohol metabolism. It leads to increase in concentration of a metabolite of alcohol - the acetic aldehyde causing negative feelings (rushes of blood to the person, nausea, vomiting, tachycardia, lowering of arterial pressure (ABP), etc.) which do extremely unpleasant alcohol intake after reception of Antabusum. It leads to conditioned-reflex disgust for taste and a smell of alcoholic drinks.

Pharmacokinetics. After oral administration absorbability of Disulfiramum makes from 70 to 90% of the digestive tract (DT), is quickly metabolized, being recovered to diethyldithiocarbamate which is removed in a look a glucloss conjugate or turns into diethyl amine and carbon sulfide which part (4-53%) is removed through lungs.

Indications to use:

Treatment and prevention of a recurrence of an alcoholism.

Route of administration and doses:

The sparkling tablet is dissolved in water in quantity sufficient for full dissolution of drug (half-glass). Treatment is appointed after careful inspection of the patient and the warning of effects and complications. Drug is accepted inside on 200-500 mg 1-2 times a day according to the individual scheme. In 7-10 days carry out disulfiramalkogolny test (20-30 ml of vodka after reception of 500 mg of drug), at weak reaction increase a dose of alcohol by 10-20 ml (the maximum dose of vodka of 100-120 ml). Test repeat in 1-2 days in a hospital and in 3-5 days out-patient clinic with correction of doses of alcohol and/or drug as necessary. Further it is possible to use a maintenance dose of 150-200 mg a day within 1-3 years.

Features of use:

Patients should be warned about danger of reaction of intolerance of alcoholic drinks. In case of co-administration with peroral anticoagulants it is necessary to exercise more frequent control of maintenance of a prothrombin and correction of doses of anticoagulants that is connected with the increased risk of development of bleeding.

Antabusum should be taken with caution at patients with a renal failure or a hypothyroidism, especially at risk of a possible combination to alcohol.

Side effects:

Caused by properties of Disulfiramum:

- Metal taste in a mouth.
- An unpleasant smell at patients with colostomy (connected with carbon sulfide).
- The exceptional cases of hepatitis which sometimes are found at the patients with nickel eczema who do not have alcoholism.
- Polyneuritis of the lower extremities, neuritis of an optical nerve.
- Memory loss, confusion of consciousness, adynamy.
- Headaches.
- Skin allergic manifestations.

Connected with a combination Disulfiramum - alcohol:

- Cases of respiratory insufficiency are described; cardiovascular collapse, disturbance of a heart rhythm, stenocardia, sometimes myocardial infarction, and also neurologic frustration; wet brain.

Complications at long reception: seldom the psychoses reminding alcoholic, hepatitis, gastritis; at the persons having cardiovascular diseases thrombosis of vessels of a brain, therefore at complaints of a pas of paresthesia in extremities and a face, it is necessary to cancel drug immediately is possible; polyneuritis aggravation.

At reception of doses of alcohol over 50-80 ml of vodka against the background of reception of Disulfiramum can develop heavy disturbances of cardiovascular and respiratory systems, hypostases, spasms. In this case carry urgently out disintoxication therapy, enter analeptics, carry out a symptomatic treatment.

Interaction with other medicines:

Reaction to ethanol is reduced by ascorbic acid.

Contraindicated combinations:

- Alcohol. Reaction of intolerance (rushes of blood, erythema, vomiting, tachycardia). To avoid reception of the alcoholic drinks and medicines containing alcohol.

Undesirable combinations:

- Isoniazid. Behavior disorder and coordination.
- Nitro-5-imidazoles (metronidazole, ординазол, секнидазол, Tinidazolum). Delirious frustration, confusion of consciousness.
- Phenytoinum. Essential and bystry rise in level of Phenytoinum in plasma with toxic symptoms (suppression of his metabolism).

If the combination cannot be avoided, it is necessary to make clinical observation and control of concentration of drug in plasma in the course and after treatment by Disulfiramum.

The combinations demanding care:

- Warfarin (and other peroral anticoagulants). The increased effect of peroral anticoagulants and danger of bleeding (decrease in disintegration of warfarin in a liver). More frequent control of concentration of warfarin and correction of a dose of anticoagulants within 8 days after cancellation of Antabusum is recommended.
- Theophylline. Disulfiramum inhibits theophylline metabolism. As result of it, a dose of theophylline it has to be corrected (a reduced dosage), depending on clinical symptoms and concentration of drug in plasma.
- Benzodiazepines. Disulfiramum can exponentiate sedation of benzodiazepines by inhibition of their oxidizing metabolism (especially chlordiazepoxide and diazepam). The dosage of benzodiazepine has to be corrected according to clinical manifestations.
- Tricyclic antidepressants. Strengthening of reaction of intolerance of alcohol, especially, is possible if patients against the background of reception of Disulfiramum take alcoholic drinks.

Contraindications:

Absolute: serious illness of cardiovascular system, acoustic organs (neuritis of an acoustical nerve) and eye (glaucoma, optic neuritis); bronchial asthma, emphysema of lungs; a pulmonary tuberculosis, a heavy liver failure, diseases of the hemopoietic bodies, a diabetes mellitus, a thyrotoxicosis, epilepsy and a convulsive syndrome of any genesis, mental diseases, an aggravation of a peptic ulcer, a disease of kidneys, malignant tumors, polyneurites of any etiology, pregnancy and the period of a lactation, the increased individual sensitivity to drug.

Relative: cardiovascular diseases in compensation stages, advanced age (60 years are more senior), a peptic ulcer of a stomach and a 12-perstny gut in remission stages, the residual phenomena after disturbance of cerebral circulation, earlier postponed disulfiramny (antabusny) psychoses.

Overdose:

The combination Disulfiramum ethanol can cause oppression of consciousness up to a coma, a cardiovascular collapse, neurologic complications. Symptomatic treatment.

Storage conditions:

At a temperature not above 30 °C. To store in the place, unavailable to children!

Period of validity of 5 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets sparkling 200 mg or 400 mg.

On 50 tablets (with a dosage of 400 mg) or 100 tablets (with a dosage of 200 mg) in a container from polyethylene of high density or in a bottle of dark glass with a cover from polyethylene. On 1 container with the application instruction in a cardboard pack.