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Active Ingredient: Disulfiram.
Other names for this medication:
Alcophobin, Anticol, Aversan, Diabuse, Disulfiramo, Disulfiramum, Disulphiram, Esperal, Etabus, Etiltox, Refusal, Tenutex.
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.
Pharmacodynamics and pharmacokinetics
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 a conditioned reflex aversion of alcoholic beverages.
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 DTK). The maximum concentration of which in the blood is determined after 4 hours, however, activity towards 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 drug withdrawal, the effect will remain 7-14 days. Metabolites are excreted in the urine, partly with exhaled air, and 20% of unchanged disulfiram through the intestine.
Indications for use
Antabuse is used to prevent recurrence in the treatment of chronic alcoholism and alcohol dependence.
– 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;
– emphysema, bronchial asthma;
– mental illness, epilepsy and epileptiform syndrome;
– severe hepatic and renal failure;
– diseases of the blood-forming organs;
– aggravation of peptic ulcer disease;
– malignant tumors;
Other cardiovascular diseases, over 60 years of age, peptic ulcer in remission, consequences of strokes with residual effects, history of antabuse psychoses, are relative contraindications.
Antabuse can cause the following reactions due to the action of disulfiram:
– metallic taste in the mouth;
– polyneuritis of the lower extremities;
– memory loss, headaches;
– optic neuritis;
– skin manifestations.
Reactions due to the joint intake of disulfiram and alcohol:
– respiratory failure;
– heart rhythm disorders;
– myocardial infarction, angina;
– cardiovascular collapse;
– swelling of the brain;
– thrombosis of cerebral vessels;
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 warning of the patient about complications. With prolonged therapy may develop psychosis, thrombosis of cerebral vessels, acute polyneuritis.
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.
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-tuberculosis drug Isoniazid may 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.
At a temperature not exceeding 30 ° C.
Anti-recurrent and supportive treatment of alcoholism is carried out by drugs: Disulfiram, Naltrexone and Acamprosate. The innovative form of disulfiram is “effervescent” Antabus tablets, which dissolve in water, have no taste or smell. When taken together with alcohol, the drug causes unpleasant (aversive), painful sensations: fear of death, shortness of breath, feeling of lack of air and so on. The fear of death – the main manifestation of the action of disulfiram – forces the alcoholic to stop drinking alcohol.
Reviews of doctors boil down to a warning about serious complications of disulfiram-alcohol reaction. Given this and a large number of contraindications, the drug is prescribed only by a doctor, and the treatment should be under the supervision of a narcologist. It is impossible to carry out treatment independently in secret from the patient, since the phenomena caused by the preparation can be so pronounced that reanimation measures will be required. The patient should be informed that drinking a small dose of alcohol while taking Antabuse can be fatal. Before the appointment of the drug to conduct an examination and the patient must confirm that he wants to get rid of alcoholism.
Doctors remind that, unfortunately, there are no sufficiently effective medicines that suppress the craving for ethyl alcohol. And this method is not a treatment, but a “prohibitive method”, so that the patient does not have a path to retreat, and has the opportunity to achieve stable remission. Treatment of alcoholism should be comprehensive (psychological assistance, acupuncture, sedatives and a great desire to stop drinking). And reviews about the Antabuse – proof of this. Many patients took it for several years, but the craving for alcohol persisted, and only the fear of physical pain and death restrained them.
“I took it 5 years ago under the control of a narcologist and a psychologist. I was torn off several times, but now I can control myself – the psychologist helps ”
“There was always a craving for alcohol, but Antabus always restrained me and stopped me.”