2010/09/21

Antabus

Composition, structure and packing

Effervescent tablets are white or almost white, round, flat, beveled edges, scored and marked with "CD" on the one hand the risks and "C" on the other hand the risks.

1 tab. Disulfiram 200 mg.

Excipients: corn starch, povidone, tartaric acid, sodium bicarbonate, talc, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose.

Effervescent tablets are white or almost white, round, flat, beveled edges, with a Phillips scored, dividing the tablet into four parts, and marking "CJ" on one side.

1 tab. Disulfiram 400 mg.

Excipients: corn starch, povidone, tartaric acid, sodium bicarbonate, talc, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose.

Clinico-pharmacological group: Drug for treatment of alcohol dependence.

Pharmacological action

The drugs are based on the blockade atsetaldegiddegidrogenazy, which is involved in the metabolism of ethanol. This leads to increased concentrations of metabolites of ethanol - acetaldehyde, which causes negative feelings (facial flush, nausea, vomiting, tachycardia, lowering blood pressure, etc.) that make it extremely unpleasant alcohol after taking Antabusa. This leads to a conditioned reflex aversion to the taste and odor of alcoholic beverages. Antialcoholic.

Pharmacokinetics

Following oral intake of disulfiram from the gastrointestinal tract ranges from 70 to 90% and is rapidly metabolized, reducing to diethyldithiocarbamate, which is itself presented as glyukuron-conjugated or converted to diethylamine and carbon sulfide, some of which (4-53%) is derived through the lungs.

Statement
treatment and prevention of relapse of chronic

Dosage regimen

Ext. Effervescent tablets dissolved in water in sufficient quantity to dissolve the drug (half a cup).

Treatment is prescribed after a thorough examination of the patient and the prevention of the consequences and complications.

Accepted by 200-500 mg 1-2 times a day on an individual scheme. After 7-10 days spend disulfiram-alcohol test (20-30 ml of vodka after taking 500 mg of the drug), with a weak reaction dose of alcohol increased by 10-20 ml (maximum dose of vodka 100-120 ml). The sample is repeated after 1-2 days in hospital and after 3-5 days of outpatient adjusted doses of alcohol and / or medication if necessary. In the future, you can use supporting dose 150-200 mg / day for 1-3 years.

Side effect

Conditional properties of disulfiram: - metallic taste in the mouth - an unpleasant smell in patients with colostoma (associated with carbon sulfide) - rare cases of hepatitis B (similar to sometimes occur in patients with nickel eczema is not suffering from alcoholism) - polyneuritis of lower limbs, optic neuritis - memory loss, confusion, asthenia - headaches - skin allergic manifestations. Linked with a combination of disulfiram-ethanol: describes cases of respiratory failure, cardiovascular collapse, cardiac arrhythmias, angina, sometimes - myocardial infarction, and neurological disorders, cerebral edema. Complications of chronic administration: rarely - psychoses resembling alcoholic, hepatitis, gastritis, in patients suffering from cardiovascular diseases and possible thrombosis of the brain, so when complaints of paresthesias in the extremities and face should immediately remove the drug, worsening polyneuritis. When you receive a dose of alcohol than 50-80 ml of vodka on a background of reception of disulfiram may develop severe disorders of the cardiovascular and respiratory systems, edema, convulsions. In this case urgently conduct detoxication therapy, introducing analeptics, spend symptomatic treatment. The combination of disulfiram-ethanol may cause depression of consciousness, even coma, cardiovascular collapse, neurological complications.

Contraindications
absolute:
severe diseases of the cardiovascular system,
Hearing (neuritis of the auditory nerve) and the eye (glaucoma, optic neuritis);
bronchial asthma, emphysema, pulmonary tuberculosis;
severe hepatic insufficiency,
disease-forming organs;
diabetes;
thyrotoxicosis;
epilepsy and convulsions of any origin;
mental illness;
aggravation of peptic ulcer;
Usable kidneys
Malignant tumor;
polyneuritis any etiology;
Pregnancy
breastfeeding;
individual hypersensitivity to the drug.
Relative:
cardiovascular disease in the stage of compensation;
advanced age (over 60);
stomach ulcer and duodenal ulcer in remission;
residual effects after ischemic;
previously deferred disulfiramnye (antabusnye) psychoses.

Cautions

Patients should warn of the dangers of intolerance reactions of alcoholic beverages. In case of simultaneous appointment with oral anticoagulants should exercise more frequent monitoring of the content of prothrombin and correction doses of anticoagulants, which is associated with increased risk of bleeding. Antabus should be taken with caution in patients with renal insufficiency or hypothyroidism, especially when the risk of a possible combination with alcohol.

Overdose

Treatment: symptomatic.

Drug Interactions

Reaction to ethanol reduces the ascorbic acid. Contraindicated combination

Alcohol. Hypersensitive reaction (flushing, erythema, vomiting, tachycardia). Avoid taking alcoholic drinks and medicines containing alcohol.

Undesirable combinations

Isoniazid. Violations of the conduct and coordination.

Nitro-5-imidazole (metronidazole, ordinazol, seknidazol, tinidazole). Delirious disorder, confusion.

Phenytoin. A significant and rapid rise in plasma levels of phenytoin with toxic symptoms (suppression of its metabolism).

If the combination can not be avoided, should be clinical observation and monitoring of drug concentration in plasma during and after treatment with disulfiram.

Combinations that require caution

Warfarin (and other oral anticoagulants). Increased effect of oral anticoagulants and the risk of bleeding (decrease in the collapse of warfarin in the liver). We recommend more frequent monitoring of the concentration of warfarin and adjusted doses of anticoagulants within 8 days after discontinuation Antabusa.

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

Benzodiazepines. Disulfiram may potentiate the sedative effects of benzodiazepines by inhibiting their oxidative metabolism (especially chlordiazepoxide and diazepam). Benzodiazepine dosage should be adjusted in accordance with the clinical manifestations. Possible intensification of the reaction of intolerance of alcohol, if patients on intake of disulfiram take alcoholic drinks.

Terms and Conditions of storage

Store at temperatures not above 30 ° C. Shelf life 5 years