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Active ingredients
Disulfiram
Release form
Pills
Composition
In 1 tablet: Disulfiram 500 mg. Excipients: polyvidone K30, carmellose sodium, magnesium stearate, microcrystalline cellulose.
Pharmacological effect
Drug for the treatment of alcoholism. The action of disulfiram is based on the blockade of acetaldehyde hydrogenase, which is involved in the metabolism of ethanol. This leads to an increase in the concentration of the ethanol metabolite - acetaldehyde, which causes negative sensations (including flushing, nausea, vomiting, tachycardia, a decrease in blood pressure), which make alcohol use extremely unpleasant after taking the drug. This leads to a conditioned reflex aversion to the taste and smell of alcoholic beverages .; The maximum therapeutic effect is achieved 12 hours after taking the drug inside and can last for 10-14 days after stopping treatment.
Pharmacokinetics
After oral administration, the absorption of disulfiram from the gastrointestinal tract is from 70 to 90%. It is rapidly metabolized, recovering to dithiocarbamate, which itself is excreted in the form of a glucuron conjugate or converted into diethylamine and carbon sulphide, part of which (4–53%) is excreted through the lungs.
Indications
treatment and prevention of recurrence of chronic alcoholism .; Additionally, the drug is used as a detoxification agent for chronic nickel poisoning.
Contraindications
Absolute: - severe liver failure; - diabetes; - epilepsy and convulsive syndrome of any genesis; - mental illness; - pregnancy; - lactation period; - hypersensitivity to the components of the drug .; Relative: - renal failure; - hypothyroidism.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation (breastfeeding).
Dosage and administration
Before starting treatment, the patient should be carefully examined and warned of the consequences and complications .; The drug is administered orally in a dose of 500 mg 1 time / day in the morning with meals according to an individual scheme, gradually reducing the dose to 250 mg (1/2 tablet) or 125 mg (1/4 tablet) per day. Depending on the patient's response to treatment, the dose can be increased or decreased .; After 7-10 days a teturam-alcohol test is carried out: 20-30 ml of 40% ethanol (vodka) after taking the drug at a dose of 500 mg; with a weak reaction, the dose of alcohol is increased by 10-20 ml (the maximum dose of vodka is 100-120 ml).The sample is repeated after 1-2 days in the hospital and after 3-5 days on an outpatient basis, with the correction of doses of alcohol and / or the drug, if necessary. In the future, the drug can be used in a maintenance dose of 150-200 mg / day for 1-3 years.
Side effects
Due to the properties of disulfiram: metallic taste in the mouth, unpleasant smell in patients with colostomy (associated with carbon sulphide); rarely - hepatitis, sometimes found in patients with nickel eczema, not suffering from alcoholism, lower limb polyneuritis, optic neuritis, memory loss, confusion, asthenia, headaches, skin allergic reactions .; Disulfiram-ethanol combination: cases of respiratory failure, collapse, cardiac arrhythmia or acute angina, sometimes myocardial infarction, as well as neurological disorders, brain edema are described .; Complications with prolonged use: psychoses, reminiscent of alcohol, hepatitis, gastritis; thrombosis of cerebral vessels is possible in patients with cardiovascular diseases, therefore, with complaints of paresthesias in the extremities and face, the drug should be immediately discontinued; exacerbation of polyneuritis .; When taking doses of alcohol over 50-80 ml (in terms of 40% ethanol) on the background of taking the drug develop severe violations of the cardiovascular and respiratory systems, edema, convulsions. In this case, detoxification therapy is urgently carried out, analeptics are administered, and symptomatic treatment is carried out.
Overdose
Symptoms: the combination of disulfiram-ethanol causes depression of consciousness up to coma, cardiovascular collapse, neurological complications .; Treatment: symptomatic treatment.
Interaction with other drugs
The combinations are contraindicated: While taking the drug Esperal; and ethanol develops an intolerance reaction (flushing, erythema, vomiting, tachycardia) .; Combinations are not recommended: When used simultaneously with isoniazid - behavioral and coordination disorders .; With simultaneous use with derivatives of 5-nitroimidazole (metronidazole, ornidazole, secnidazole, tinidazole) delirious disorders, confusion of consciousness develop; With simultaneous use with phenytoin, a significant and rapid increase in plasma concentration of phenytoin is observed with the development of toxic symptoms (due to inhibition of phenytoin metabolism). If combinations cannot be avoided, then plasma monitoring of plasma phenytoin should be carried out during and after treatment with disulfiram .;
special instructions
During the period of treatment, alcohol and drugs containing ethanol should be avoided.