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Other names for this medication:
Alcophobin, Anticol, Aversan, Diabuse, Disulfiramo, Disulfiramum, Disulphiram, Esperal, Etabus, Etiltox, Refusal, Tenutex.
.Active Ingredient: Disulfiram
Composition
In 1 tablet of disulfiram 200 mg (400 mg).
Corn starch, povidone, sodium bicarbonate, talc, silicon dioxide, tartaric acid, magnesium stearate, MCC, – as auxiliary substances.
Pharmachologic effect
Antialcoholic.
Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Inhibits acetaldehyde dehydrogenase, which is involved in the metabolism of ethyl alcohol. The delay in the oxidation of ethyl alcohol at the stage of acetaldehyde causes its accumulation and the development of intoxication – a disulfiram-alcohol reaction, which is accompanied by severe sensations and violent vegetative reactions: pulsating headache, noise in the head, tachycardia, a decrease in blood pressure, heartbeat, blurred vision, nausea, vomiting .
Discomfort associated with alcohol intake, lead to the conditioned reflex aversion of alcoholic beverages.
Pharmacokinetics
Absorbed 70–90% after ingestion. It is well soluble in lipids and accumulates in fat depots. It is rapidly metabolized, and as a result, during a series of transformations, it is converted into an active metabolite, methyl diethylthiocarbamic acid ester (methyl-DTC). The maximum concentration of which in the blood is determined after 4 hours, however, activity with respect to acetaldehyde dehydrogenase is noted after 3 days of regular administration.
T1 / 2 methyl-DTC – 10 h, but the activity with respect to aldehyde dehydrogenase lasts longer. Therefore, after the abolition of the drug effect will remain 7-14 days. Metabolites are excreted in the urine, partly in exhaled air, and 20% of unchanged disulfiram through the intestine.
Indications for use
Antabuse is used to prevent relapse in the treatment of chronic alcoholism and alcohol dependence.
Contraindications
Absolute contraindications:
– neuritis of the auditory and optic nerve;
– diseases of the cardiovascular system (marked cardiosclerosis, post-infarction conditions, cerebral arteriosclerosis, aortic aneurysm, hypertension);
– polyneuritis of any origin;
– glaucoma;
– emphysema, bronchial asthma;
– pulmonary tuberculosis;
– mental illness, epilepsy and epileptiform syndrome;
– diabetes;
– severe hepatic and renal failure;
– thyrotoxicosis;
– diseases of the blood-forming organs;
– aggravation of peptic ulcer disease;
– malignant tumors;
– pregnancy;
– hypersensitivity.
Other cardiovascular diseases, over 60 years of age, peptic ulcer in remission, consequences of strokes with residual effects, and Antabuse psychosis in history, are relative contraindications.
Side effects
Antabus can cause the following reactions due to the action of disulfiram:
– hepatitis;
– metallic taste in the mouth;
– polyneuritis of the lower extremities;
– memory loss, headaches;
– asthenia;
– optic neuritis;
– skin manifestations.
Reactions due to co-administration of disulfiram and alcohol:
– respiratory failure;
– heart rhythm disorders;
– myocardial infarction, angina;
– cardiovascular collapse;
– swelling of the brain;
– thrombosis of cerebral vessels;
– psychosis.
Instructions for use Antabuse (method and dosage)
Tablets are taken orally, dissolved in 0.5 cups of water. Take 200–500 mg 1–2 times a day, prescribed by a doctor. A week later, a disulfiram-alcohol sample is taken – in parallel with taking 500 mg of Antabuse, the patient drinks 20–30 ml of vodka. Observe the reaction of the body, and with a weak reaction, the dose of alcohol is increased by 20 ml. The sample is repeated several times, while adjusting the dose of alcohol and the drug. In the future, apply a maintenance dose of 200 mg / sutot 1 year to 3 years.
Instructions for use Antabuse contains warnings that the drug is prescribed after the examination and the mandatory amazon metformin. warning of the patient about complications. With prolonged therapy may develop psychosis, thrombosis of cerebral vessels, exacerbation of polyneuritis.
Overdose
An overdose of disulfiram increases the severity of reactions and leads to depression of the nervous system (coma), the development of neurological and cardiovascular complications. Symptomatic therapy is carried out.
Interaction
An unacceptable combination is the intake of alcoholic beverages, alcohol-containing drugs and products, since an intolerance reaction occurs.
Metronidazole, Tinidazole, Ordinazole, Secnidazole, while taking it with Antabuse, cause delirious disorders and disorders of consciousness.
When taken with phenytoin, a significant rise in its plasma level occurs with the development of toxic symptoms.
The anti-TB drug Isoniazid can cause poor coordination.
Antabuse increases the effect of oral anticoagulants (warfarin), and therefore there is a risk of bleeding.
Disulfiram inhibits the metabolism of Theophylline, so its dose should be reduced.
Potentiates the sedative effect of benzodiazepines (Chlordiazepoxide and Diazepam), the dosage of which should be reduced.
Storage conditions
At a temperature not exceeding 30 ° C.
Shelf life
5 years.
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