Antabuse - a drug that causes, in combination with ethyl alcohol, the following negative effects: nausea, vomiting, flushing of the face, tachycardia, hypotension, etc .
The use of alcohol after its reception is extremely unpleasant, which forms a conditioned reflex aversion to the smell and taste of alcoholic beverages.
Form of release and composition Drug form Antabuse - tablets effervescent: almost white or white, round, flat, with beveled edges:
0.2 g dose: one side is divided by a risk labeled on the sides "CD" | "C" (100 pieces each in high density polyethylene containers / dark glass bottles with a polyethylene lid, 1 container / bottle in a cardboard bundle);
0.4 g dose: on one side there is a cross-shaped risk separating the tablet into four equal parts and the "CJ" marking (50 pieces in high density polyethylene containers / dark glass bottles with a polyethylene lid, 1 container / vial in a cardboard container Pack).
In 1 effervescent tablet contains:
active substance: disulfiram - 0.2 g or 0.4 g;
Auxiliary components: povidone, corn starch, tartaric acid, talc, magnesium stearate, sodium hydrogen carbonate, silicon dioxide colloid, microcrystalline cellulose.
Indications for use
The drug is indicated for the therapy and prevention of recurrences of chronic alcoholism.
Absolute: severe cardiovascular pathologies, including uncompensated heart failure and coronary artery disorders, such as hypertension, ischemic heart disease;
Severe organic lesions of the brain, anamnestic data on a stroke;
Severe renal failure;
Neuropsychiatric disorders, including psychoses, risks of suicidal attempts, severe forms of pathologies related to personality disorder;
Severe liver function abnormalities exceeding the upper limit of the norm of activity of microsomal hepatic enzymes by 3 times or more, the history of adverse reactions from the liver with previous disulfiram therapy;
Alcohol intoxication or use of ethanol-containing drugs or beverages for 24 hours before taking the drug;
Drug dependence syndrome;
Period of pregnancy and lactation (insufficient data on the safety and effectiveness of Antabuse in this category of patients);
Children and adolescents under 18 years of age (no data on safety and efficacy of use);
Hypersensitivity to disulfiram or auxiliary components of the drug.
Relative: Antibuse is used with caution in diabetes mellitus, hypothyroidism, signs of irreversible brain damage, kidney failure, respiratory or liver diseases, epilepsy or seizure syndrome of any genesis (increased probability of disulfiram-ethanol reaction to a more severe degree), peripheral neuropathy, ulcerative
Diseases of the stomach and duodenum, neuritis of the optic nerve, and also in the elderly (after 60 years).
Method of application and dosage
Effervescent tablet Antabuse taken inside, previously dissolved in water (1/2 cup).
The drug is used only under the supervision of a doctor. Therapy is prescribed after a thorough clinical examination of the patient and a warning about abstinence from drinking during treatment, as well as possible complications and consequences.
The drug is taken according to an individual scheme, determined by the attending physician, at the rate of 0.2-0.5 g 1-2 times a day.
After 7-10 days from the start of therapy, it is necessary to conduct a disulfiram-alcohol test.
For this, the patient is given 20-30 ml of vodka after taking 0.5 g of the drug, if the reaction is weak, the dose of alcohol is increased to 30-50 ml (the maximum permissible dose of vodka is 100-120 ml).
After 1-2 days, the sample is repeated in a hospital, after 3-5 days - on an outpatient basis, if necessary, adjust the dose of alcohol and / or drug.
In the future Antabuse can be used in a maintenance dose of 0.15-0.2 g / day for 1-3 years.
Nonspecific side effects, most often observed with Antabuse taking, which, among other things, can be associated with the underlying disease: headache, drowsiness, reactions from the gastrointestinal tract (GI tract).
If they manifest, you may need to reduce the dose of the drug. The frequency of unwanted reactions from organs and systems (according to the following classification 1/10 - very often, 1/100 - 1/10 - often, 1/1000 - 1/100 - infrequently, 1/10 000 - 1/1000 - rarely, 1/10 000, including single cases - very rarely, frequency unknown):
Gastrointestinal: often epigastric pain, nausea, vomiting, diarrhea, metallic taste in the mouth, Bad breath;
Frequency unknown - unpleasant odor in patients with colostomy due to the presence of carbon sulphide;
Hepatobiliary system: often - increased activity of hepatic enzymes (gamma-glutamyltransferase and transaminase);
Rarely - jaundice;
Very rarely - clinical signs of hepatotoxicity, liver cell damage, hepatitis, fulminant hepatitis due to extensive liver necrosis, which may result in hepatic insufficiency, hepatic coma and death (these side effects usually occur during the first 8 weeks of therapy and are not dose-dependent);
Immune system: infrequently - allergic reactions;
Data from laboratory and instrumental studies:
rarely - deviations in the results of functional liver tests from normal parameters, including a rise in blood levels of bilirubin and an increase in activity of aspartate aminotransferase (AST) and alanine aminotransferase (ALT);
Nervous system: often - perversion of taste, drowsiness, headache;
Rarely - polyneuropathy, peripheral neuropathy, optic neuritis (the smokers are most prone to develop it), tremor, encephalopathy;
Very rarely - confusion, convulsions, neurological disorders (most likely dose-dependent, usually after a few months from the start of treatment, slowly reversible);
Psyche: often - mania, depression; Rarely psychotic reactions (schizophrenia, paranoia) (such disorders occur primarily in patients with schizophrenia or a history of depression, they are probably associated with an increase in dopamine levels due to inhibition of dopamine-β-hydroxylase by disulfiram); Very rarely - acute organic brain syndrome, behavioral disorders;
Genital organs and mammary gland: infrequently - sexual dysfunction, decreased libido;
Skin and subcutaneous tissue: infrequently - allergic dermatitis, acne, itching, rash;
Other reactions: often - a subjective feeling of discomfort, drowsiness, fatigue.
Adverse reactions likely due to the combined use of disulfiram and ethanol:
cardiovascular system: palpitations, tachycardia, dyspnea, arrhythmias, dizziness, fainting;
GASTROINTESTINAL TRACT: vomiting;
Musculoskeletal system: muscular spasm;
Nervous system: headache, drowsiness, impaired coordination, loss of consciousness;
Skin and subcutaneous fat: hyperhidrosis, flushes of blood to the face;
Vessels: hypotension, cardiovascular collapse;
Other reactions: fatigue.
The result of an overdose of a combination of ethanol-disulfiram can be cardiovascular collapse, depression of consciousness (up to coma), neurological complications. In this situation, symptomatic therapy is performed.
Specific guidance Patients need to be warned about the dangers of the reaction of intolerance to alcoholic beverages. With the simultaneous administration of Antabuse with oral anticoagulants, more frequent monitoring of prothrombin content and correction of anticoagulant doses is required, this is associated with an increased likelihood of bleeding.
Patients with hypothyroidism or renal failure disulfiram are taken with caution, especially at the risk of its possible combination with alcohol. Adverse reactions caused by taking disulfiram (including fatigue and drowsiness) affect the speed of psychomotor reactions and the ability to concentrate.
In the case of the emergence of such conditions during the therapy with Antabuse, the control of complex mechanisms and vehicles, including a car, is required to abstain.
Ascorbic acid reduces the reaction of disulfiram to ethanol. Contraindicated the joint use of Antabuse and alcohol (alcoholic beverages and medications containing alcohol), as this can cause reactions of intolerance, accompanied by hot flushes, erythema, vomiting, tachycardia.
Other undesirable and prudent combinations with disulfiram:
isoniazid - coordination and behavior may be impaired;
Ornidazole, secnidazole, metronidazole, tinidazole (nitro-5-imidazoles) - can cause confusion and delirious disorders;
Phenytoin - disulfiram inhibits its metabolism, as a result of which there is a rapid and significant increase in the level of phenytoin in the plasma, accompanied by toxic symptoms;
Oral anticoagulants (including warfarin) - their effect and the risk of bleeding are increased as a result of a decrease in the disintegration in the liver (more frequent control of concentration and correction of the dose of anticoagulants, including during 8 days after disulfiram cancellation);
Theophylline - it is necessary to correct its dose in the direction of decrease depending on the concentration in the plasma and clinical symptoms (due to the inhibition of theophylline metabolism by disulfiram);
Benzodiazepines - The antabuse is able to potentiate their sedative effect by inhibiting oxidative metabolism (especially diazepam and chlordiazepoxide), which requires dosage adjustment in accordance with the clinical picture;
Tricyclic antidepressants - there is a possibility of increasing the reaction of intolerance to ethanol, especially in patients taking alcohol against disulfiram therapy. When the above combinations can not be avoided, in the course of therapy and after treatment with Antabus, control of plasma concentrations in the plasma and regular clinical monitoring of patients are necessary.