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Disulfiram information from DrugsUpdate  

See Available Brands of Disulfiram in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Disulfiram is a drug used to support the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Trade names for disulfiram in different countries are Antabuse and Antabus manufactured by Odyssey Pharmaceuticals. Disulfiram is also being studied as a treatment for cocaine dependence, as it prevents the breakdown of dopamine (a neurotransmitter whose release is stimulated by cocaine); the excess dopamine results in increased anxiety, higher blood pressure, restlessness and other unpleasant symptoms. Several studies have reported that it has anti-protozoal activity as well.Research for possible disulfiram use in cancer therapy has been announced.

Pharmacodynamics

Pharmacokinetics

Disulfiram inhibits aldehyde dehydrogenase, the oxidative enzyme of acetaldehyde, a metabolite of alcohol. The latter is accumulated in the blood, thus producing unpleasant symptoms of disulfiram-alcohol reaction when a patient has taken small amounts of alcohol.
Onset: 12 hrs.
Duration: 1-2 wk after last dose.
Absorption: Rapidly absorbed from the GIT; peak plasma concentrations after 8-10 hrs (oral).
Metabolism: Reduction to diethyldithiocarbamate by the glutathione reductase system in the erythrocytes.
Excretion: Urine (as metabolites); exhaled gas (carbon disulphide).

Disulfiram Indications / Disulfiram Uses

Information Not Available

Disulfiram Adverse Reactions / Disulfiram Side Effects

Drowsiness, fatigue, lassitude, psychotic reactions, peripheral and optic neuropathies, hepatotoxicity, garlic-like or metallic after-taste, GI upset, body odour, bad breath, headache, impotence.
Potentially Fatal: Respiratory depression, CV collapse, arrhythmias, myocardial infarction, acute CHF, convulsions, sudden death.

Precautions

Patients with a history of rubber contact dermatitis should be evaluated for hypersensitivity to thiuram derivatives before receiving Disulfiram.
It is suggested that every patient under treatment carry an Identification Card stating that he is receiving Disulfiram and describing the symptoms most likely to occur as a result of the Disulfiram-alcohol reaction. In addition, this card should indicate the physician or institution to be contacted in an emergency.
Alcoholism may accompany or be followed by dependence on narcotics or sedatives. Barbiturates and Disulfiram have been administered concurrently without untoward effects; the possibility of initiating a new abuse should be considered.
Hepatic toxicity including hepatic failure resulting in transplantation or death have been reported. Severe and sometimes fatal hepatitis associated with Disulfiram therapy may develop even after many months of therapy. Hepatic toxicity has occurred in patients with or without prior history of abnormal liver function. Patients should be advised to immediately notify their physician of any early symptoms of hepatitis, such as fatigue, weakness, malaise, anorexia, nausea, vomiting, jaundice, or dark urine.
Baseline and follow-up liver function tests (10 – 14 days) are suggested to detect any hepatic dysfunction that may result with Disulfiram therapy. In addition, a complete blood count and serum chemistries, including liver function tests, should be monitored.
Patients taking Disulfiram tablets should not be exposed to ethylene dibromide or its vapors. This precaution is based on preliminary results of animal research currently in progress that suggest a toxic interaction between inhaled ethylene dibromide and ingested Disulfiram resulting in a higher incidence of tumors and mortality in rats. A correlation between this finding and humans, however, has not been demonstrated.

Special Precautions

Diabetes, epilepsy, hepatic/renal impairment, hypothyroidism, cerebral damage, elderly. Liver function and blood tests should be monitored regularly. Pregnancy and lactation.

Other Drug Interactions

Inhibits hepatic enzymes thus interferes with metabolism of other drugs; enhances anticoagulant effects of phenytoin and coumarin. Adverse CNS effects may be precipitated with concurrent metronidazole, INH or MAOI therapy. Tricyclic antidepressants exacerbate symptoms of disulfiram alcohol reaction.
Potentially Fatal: Disulfiram alcohol interaction: Intense flushing of neck and face accompanied by heat and sweating, tachycardia, palpitation, dyspnoea, dizziness, headache, HTN initially and then hypotension; GI disturbances, exhaustion, convulsions and cardiopulmonary arrest.

Other Interactions

Information Not Available

Dosage

Oral
Adjunct to treatment of chronic alcoholism
Adult: 800 mg as a single dose on the 1st day of treatment, reduce dose by 200 mg daily. Maintenance: 100-200 mg daily.

Food(before/after)

May be taken with or without food

List of Contraindications

Disulfiram and Pregnancy

Caution when used during pregnancy.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Disulfiram and Lactation

Caution when used during lactation

Disulfiram and Children

Information Not Available

Disulfiram and Geriatic

Information Not Available

Disulfiram and Other Contraindications

Hypersensitivity, CVS diseases; peripheral neuropathy, psychosis. Not to be used in patients with alcohol intoxication.

Storage

Oral: Store at 15-30°C

Lab interference

Oral: Store at 15-30°C

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