Antabusum

Antabusum – the drug causing the following negative effects in combination with alcohol: nausea, vomiting, "inflows" of blood to the person, tachycardia, hypotonia, etc.; alcohol intake after its reception is extremely unpleasant that creates conditioned-reflex disgust for a smell and taste of alcoholic drinks.

Form of release and structure

Dosage form of Antabusum – a tablet sparkling: almost white or white color, round, flat, with slanted edges:

• dose of 0,2 g: one of the parties is divided risky with marking by "CD" | on each side "With" (on 100 pieces in containers from polyethylene of high density / bottles of dark glass with a polyethylene cover, 1 container/bottle in a cardboard pack);
• dose of 0,4 g: on one of the parties crosswise risk, dividing a tablet into four equal parts, and marking of "CJ" (on 50 pieces in containers from polyethylene of high density / bottles of dark glass with a polyethylene cover, 1 container/bottle in a cardboard pack).

Sparkling contain in 1 tablet:

• active ingredient: Disulfiramum – 0,2 g or 0,4 g;
• auxiliary components: povidone, starch corn, tartaric acid, talc, magnesium stearate, Natrii hydrocarbonas, silicon dioxide colloid, cellulose microcrystallic.

Indications to use

Drug is shown for therapy and prevention of a recurrence of an alcoholism.

Contraindications

Absolute:

• heavy pathologies of cardiovascular system, including noncompensated heart failure and disturbances of coronary circulation, such as arterial hypertension, coronary heart disease;
• crushing organic lesions of a brain, anamnestic data on the had stroke;
• renal failure of heavy degree;
• psychological frustration, including psychoses, risks of suicide attempts, severe forms of the pathologies relating to frustration of the personality;
• heavy abnormal liver functions with exceeding of the upper bound of standard of activity of microsomal liver enzymes by 3 times and more, data in the anamnesis on side reactions from a liver at the previous therapy by Disulfiramum;
• drunkenness or the use of the medicines or drinks containing ethanol for 24 hours before administration of drug;
• syndrome of medicinal dependence;
• the period of pregnancy and lactation (there are not enough data on safety and efficiency of use of Antabusum for this category of patients);
• children's and teenage age up to 18 years (there are no data on safety and efficiency of use);
• hypersensitivity to Disulfiramum or auxiliary components of drug.

Relative: Antabusum is applied with care at a diabetes mellitus, a hypothyroidism, signs of an irreversible damage of a brain, a renal failure, diseases of respiratory system or a liver, epilepsy or a convulsive syndrome of any genesis (the probability Disulfiramum - ethanol reaction in heavier degree), peripheral neuropathy, a peptic ulcer of a stomach and a 12-perstny gut, an optic neuritis, and also at advanced age (after 60 years is increased).

Route of administration and dosage

The sparkling pill Antabusum is taken inside, previously having dissolved in water (^1/2 glasses).

Drug is used only under observation of the doctor. Therapy is appointed after careful clinical inspection of the patient and the warning of abstention from alcohol intake for the period of treatment, and also possible complications and effects.

Drug is accepted according to the individual scheme determined by the attending physician at the rate of 0,2-0,5 g by 1-2 times a day.

7-10 days later from the beginning of therapy it is necessary to carry out Disulfiramum - alcoholic test. For this purpose the patient is given 20-30 ml of vodka after reception of 0,5 g of drug if reaction weak, the dose of alcohol is increased to 30-50 ml (the most admissible dose of vodka – 100-120 ml). In 1-2 days test is repeated in the conditions of a hospital, after 3-5 days – it is out-patient, as necessary adjust doses of alcohol and/or drug. Further Antabusum is allowed to use in a maintenance dose 0,15-0,2 g/days for 1-3 years.

Side effects

Nonspecific side effects, the most often observable at reception of Antabusum which, including, can be connected with a basic disease: a headache, drowsiness, reactions from the digestive tract (DT). At their manifestation, perhaps, it will be required to reduce a drug dose.

Frequency of undesirable reactions from bodies and systems (according to the following classification –> 1/10 – it is very frequent,> 1/100-<1/10 – often,> 1/1000-<1/100 – infrequently,> 1/10 000-<1/1000 – seldom, <1/10 000, including isolated cases – it is very rare, frequency is unknown):

• GIT: often – pain in epigastriums, nausea, vomiting, diarrhea, metal smack in a mouth, an unpleasant smell from a mouth; frequency is unknown – the unpleasant smell at patients with colostomy caused by availability of carbon sulfide;
• gepatobiliarny system: often – increase in activity of liver enzymes (gamma глутамилтрансферазы and transaminases); seldom – jaundice; very seldom – clinical symptoms of a hepatotoxic, defeat of cells of a liver, hepatitis, fulminantny hepatitis owing to an extensive necrosis of a liver which result can become a liver failure a hepatic coma and a lethal outcome (these side effects usually arise within the first 8 weeks of therapy and are not dozozavisimy);
• immune system: infrequently – allergic reactions;
• data of laboratory and tool researches: seldom – deviations of results of functional tests of a liver from normal indicators, in t. h increase in blood of concentration of bilirubin and growth of activity of aspartate aminotransferase (nuclear heating plant) and alaninaminotranspherase (ALT);
• nervous system: often – a food faddism, drowsiness, a headache; seldom – polyneuropathy, peripheral neuropathy, an optic neuritis (smokers are most predisposed to its development), a tremor, encephalopathy; very seldom – confusion of consciousness, a spasm, neurologic disturbances (most likely dozozavisima, arise usually several months later from an initiation of treatment, are slowly reversible);
• mentality: often – manias, a depression; seldom – psychotic reactions (schizophrenia, paranoia) (such frustration arise preferential at patients with schizophrenia or a depression in the anamnesis, they are connected probably with increase in level of a dopamine as a result of inhibition допамин-β-гидроксилазы Disulfiramum); very seldom – an acute organic brain syndrome, behavior disorders;
• generative organs and mammary gland: infrequently – sexual dysfunction, decrease in a libido;
• skin and hypodermic cellulose: infrequently – allergic dermatitis, an acne, a skin itch, rash;
• other reactions: often – a subjective sensation of discomfort, a somnolence, fatigue.

The side reactions which are possibly arising owing to combined use of Disulfiramum and ethanol:

• cardiovascular system: heart consciousness, tachycardia, short wind, arrhythmias, dizziness, faint;
• GIT: vomiting;
• musculoskeletal system: muscular spasm;
• nervous system: headache, drowsiness, lack of coordination, loss of consciousness;
• mentality: apathy;
• skin and hypodermic cellulose: a hyperhidrosis, "inflows" of blood to the person;
• vessels: hypotonia, cardiovascular collapse;
• other reactions: fatigue.

Result of overdose of a combination ethanol Disulfiramum can be a cardiovascular collapse, consciousness oppression (up to a coma), neurologic complications. In such situation symptomatic therapy is carried out.

Special instructions

Patients are required to be warned about danger of reaction of intolerance of alcoholic beverages.

At co-administration of Antabusum with peroral anticoagulants more frequent control of maintenance of a prothrombin and correction of doses of anticoagulants is necessary, it is connected with the increased probability of development of bleeding.

Patients with a hypothyroidism or a renal failure take Disulfiramum with caution, especially at risk of its possible combination to alcohol.

The side reactions caused by reception of Disulfiramum (including fatigue and drowsiness), exert impact on speed of psychomotor reactions and ability to concentration of attention. In case of such states during therapy by the drug Antabusum from control of difficult mechanisms and vehicles, including the car, it is required to abstain.

Medicinal interaction

Ascorbic acid reduces reaction of Disulfiramum to ethanol.

Contraindicated combined use of Antabusum and alcohol (the alcoholic drinks and medicines containing alcohol) as it can cause the reactions of intolerance which are followed by blood "inflows", an erythema, vomiting, tachycardia.

Others the undesirable and demanding care combinations with Disulfiramum:

• isoniazid – the lack of coordination and behavior is possible;
• орнидазол, секнидазол, metronidazole, Tinidazolum (nitro-5-imidazoles) – can cause confusion of consciousness and delirious frustration;
• Phenytoinum – Disulfiramum suppresses his metabolism thereof there is a bystry and considerable rise in level of Phenytoinum in plasma which is followed by toxic symptoms;
• peroral anticoagulants (including warfarin) – their effect and danger of bleeding as a result of reduction of disintegration in a liver amplifies (it is required to carry out more frequent control of concentration and dose adjustment of anticoagulants, including for 8 days after cancellation of Disulfiramum);
• theophylline – correction of its dose towards decrease depending on concentration in plasma and clinical symptoms is necessary (because of inhibition theophylline metabolism Disulfiramum);
• benzodiazepines – Antabusum is capable to exponentiate their sedation by inhibition of oxidizing metabolism (in particular diazepam and chlordiazepoxide) that demands correction of a dosage according to a clinical picture;
• tricyclic antidepressants – there is a probability of strengthening of reaction of intolerance of ethanol, especially at the patients accepting alcohol against the background of therapy by Disulfiramum.

When above-mentioned combinations cannot be avoided, in the course of therapy and after treatment by Antabusum control of concentration of drug in plasma and regular clinical observation of patients is necessary.

Terms and storage conditions

To store at a temperature not above 30 °C. To protect from children.

Period of validity – 5 years.