What is Disulfiram?
Disulfiram is a drug used for the treatment of alcohol dependence (alcoholism).
The brand name of Disulfiram in the United States is Antabuse.
Disulfiram Mechanism of Action (MOA)
Disulfiram produces an irreversible inhibition of the enzyme aldehyde dehydrogenase (ALDH).
The accumulation of acetaldehyde in the blood contributes to the reaction following alcohol intake in patients treated with disulfiram.
Therapeutic Indications, Uses and Benefits of Disulfiram
Treatment of alcohol dependence (chronic alcoholism), as an adjunct to integrated programmes to stop drug abuse.
Dosage of Disulfiram
Oral.
Adults:
Do not start treatment until at least 24 hours have elapsed since the last alcohol intake.
Start with 250-500 mg/day, single dose, 1 or 2 weeks Maintenance: 250 mg/day.
Max. dose: 500 mg/day.
Mode of administration
Oral. To be taken when waking up, although in patients with sedative effects it can be taken at bedtime. Alternatively, to minimize the sedative effect, the initial dose may be reduced.
Contraindications of Disulfiram
- Hypersensitivity to this active ingredient, severe myocardial disease or coronary occlusion, psychotic states, alcohol intake, concomitant with alcohol preparations, current or recent treatment with: metronidazole, or paraldehyde.
- Severe liver failure.
- Severe kidney failure.
- Addicted to opiates or being treated with opiates such as morphine, heroin or codeine; addicted to cocaine and alcohol; pregnancy.
Disulfiram Warnings and Precautions
- Diabetes mellitus, hypothyroidism, epilepsy, concomitant with phenytoin (risk of intoxication), cerebrovascular diseases, acute and chronic nephritis or renal insufficiency, cirrhosis or hepatic insufficiency.
- Recommended monitoring of liver function before and during treatment, periodic hematological and biochemical counts.
- Contact dermatitis, assess hypersensitivity to this active ingredient compounds prior to treatment.
- Children, no data available.
Liver failure
Contraindicated in severe liver failure.
Caution in hepatic insufficiency.
Renal Insufficiency
Contraindicated in severe renal failure.
Caution in renal insufficiency.
Interactions with Disulfiram
- Increases plasma concentration and toxicity of: propylene glycol, hydantoins, phenytoin, oxidative metabolism benzodiazepines (e.g. diazepam, chlordiazepoxide), theophylline.
- Prolongs the prothrombin time of oral anticoagulants. Evaluate a dose adjustment of the anticoagulant.
- Synergistic effect with: metronidazole.
- Increases the antipsychotic efficacy of clozapine as a result of disulfiram inhibition of clozapine metabolism, on the other hand, this interaction results in blocking the psychotic effects of disulfiram.
- Enhanced toxicity with: isoniazid
- Concomitant administration of antacids containing divalent cations may decrease absorption. Similarly, high doses of ferrous salts block absorption.
- Blocks oxidation and renal excretion of rifampicin.
- May potentiate the toxicity of tranylcypromide (MAOI) with some delusional pictures described due to inhibition of tranylcypromide metabolism.
- Confused and psychotic pictures have been described with the concomitant use of amitriptyline and disulfiram.
- Increases intestinal absorption of nickel.
- Lob: may increase urinary concentrations of homovanilic acid.
Pregnancy and Disulfiram
Contraindicated.
Breastfeeding
Avoid. It is not known whether it is excreted.
Adverse reactions and side effects of Disulfiram
Depression, mania; drowsiness, headache, peripheral neuritis, optic neuritis, polyneuritis; nausea, vomiting, diarrhea.
Alterations in hepatic function determinations with
increased transaminases and bilirubin.
Numbness, fatigue, general malaise, halitosis, abdominal pain, loss of taste, metallic or garlic taste.
⭐⭐⭐⭐⭐ VIDEO OF DISULFIRAM/ANTABUSE (DRUG)
Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).
In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.
Resources:
UNII: C10H20N2S4
ChemIDplus
DrugPortal
PubChem CID: 3117
NCI Thesaurus: C447