Disulfiram

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Antabus; Belgium: Antabuse; Czech Republic: Antabus; Denmark: Antabus; Finland: Antabus; France: Esperal; Germany: Antabus; Hungary: Antabus, Antaethyl; Ireland: Antabuse; Italy: Antabuse, Etiltox; Luxembourg: Antabuse; Malta: Antabuse; Netherlands: Antabus, Refusal; Poland: Anticol, Disulfiram, Esperal; Portugal: Tetradin; Romania: Antalcol; Spain: Antabus; Sweden: Antabus, Mekostest, Tenutex; UK: Antabuse.

North America

USA: Antabuse.

Latin America

Argentina: Disulfix; Brazil: Antietanol, Sarcoton; Mexico: Etabus.

Asia

Japan: Nocbin.

Drug combinations

Chemistry

Disulfiram: C~10~H~20~N~2~S~4~. Mw: 296.54. (1) Thioperoxydicarbonic diamide [(H~2~N)C(S)]~2~S~2~, tetraethyl-; (2) Bis(diethylthiocarbamoyl) disulfide. CAS-97-77-8.

Pharmacologic Category

Alcohol Deterrents; Aldehyde Dehydrogenase Inhibitor. (ATC-Code: N07BB01; P03AA04).

Mechanism of action

Thiuram derivative which interferes with aldehyde dehydrogenase. When taken concomitantly with alcohol, there is an increase in serum acetaldehyde levels.

Therapeutic use

Management of chronic alcoholism. The drug is not a cure for alcohol dependence.

Pregnancy and lactiation implications

The drug should be administered during pregnancy only when potential benefits justify possible risks to the fetus. Use with caution during lactation.

Unlabeled use

Contraindications

Hypersensitivity to disulfiram and related compounds or any component of the formulation. Patients receiving or using ethanol, metronidazole, paraldehyde, or ethanol-containing preparations like cough syrup or tonics. Psychosis. Severe myocardial disease and coronary occlusion.

Warnings and precautions

Severe and sometimes fatal hepatitis or hepatic failure associated with therapy may develop and may occur with or without prior history of abnormal hepatic function. In individuals who ingest alcohol while receiving disulfiram, the drug produces an adverse disulfiram-alcohol reaction which may persist for 30 minutes to several hours, or as long as alcohol remains in the blood. Adverse nervous system effects have been produced by low doses of disulfiram in patients with no previous history of neurologic illness (e.g. vertigo, irritability, insomnia, abnormal gait, slurred speech, disorientation, confusion, personality changes, tonic-clonic (Grand mal) seizures, peripheral neuropathy, polyneuritis, optic neuritis, delirium, bizarre behavior, drowsiness, and psychoses). Sudden withdrawal from alcohol itself may disclose a preexisting neurologic disorder. Disulfiram may aggravate preexisting EEG abnormalities. Disulfiram itself may produce adverse effects in the absence of alcohol, especially during the first 2 weeks of therapy (e.g. fatigue, impotence, headache, acneiform or allergic dermatitis, and a metallic or garlic-like aftertaste may occur), but usually disappear with continued therapy or temporary dosage reduction. The drug has rarely caused blood dyscrasias. Patients receiving disulfiram should be warned to avoid other preparations which contain alcohol (may produce a disulfiram-alcohol reaction). Hepatic toxicity, including hepatic failure resulting in transplantation or death, and blood dyscrasias reported. Disulfiram should be given with caution, if at all, to patients with diabetes mellitus, hypothyroidism, seizure disorders, cerebral damage, chronic or acute nephritis, hepatic cirrhosis or insufficiency, abnormal EEG results, or multiple drug dependence. Disulfiram is contraindicated in alcohol intoxication, cardiovascular disease, or psychoses. Disulfiram is also contraindicated in individuals hypersensitive to the drug or other thiuram derivatives such as those used in pesticides or rubber vulcanization. Administration of any medications containing alcohol, including topicals, is contraindicated. Disulfiram administration should be avoided if ethanol has been consumed within the prior 12 hours.

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