Dosing and uses of Antabuse (disulfiram)
Adult dosage forms and strengths
tablet
- 250mg
- 500mg
Alcoholism
Only administer after the patient has abstained from ethanol for at least 12 hr
Use ONLY as adjunct to supportive & psychotherapeutic treatment; in motivated patient
500 mg PO qDay initially for 1-2 weeks; not to exceed 500 mg/day
Maintenance: 250 mg PO qDay (125-500 mg range); continue therapy until a bases for self-control has been established; patient may continue to take drug therapy for months or even years
Glioblastoma Multiforme (Orphan)
Combination of disulfiram and copper gluconate
Orphan designation for treatment of glioblastoma multiforme
Sponsor
- Cantex Pharmaceuticals, Inc; 1792 Bell Tower Lane; Weston, Florida 33326
Pediatric dosage forms and strengths
Safety and efficacy not established
Antabuse (disulfiram) adverse (side) effects
Frequency not defined
Fatigue
Headache
Impotence
Metallic aftertaste
Acneiform eruptions
Polyneuritis
Rash
Hepatitis
Peripheral neuropathy
Optic neuritis
Psychotic disorder
Warnings
Black box warnings
Never administer to a patient in a state of alcohol intoxication or without patient's full knowledge
Instruct patient's relatives accordingly
Contraindications
Ethanol, metronidazole, paraldehyde, any alcohol-containing products (e.g., some mouthwashes)
Severe cardiac disease
Coronary occlusion
Psychosis
Hypersensitivity
Cautions
When EtOH ingested by patient taking disulfiram: flushing, throbbing HA, N/V, diaphoresis, thirst, SOB, syncope, vertigo, blurred vision, confusion; respiratory depression, cardiac arrhythmias, MI or liver failure may occur
Use caution in diabetes, hypothyroidism, seizures, nephritis, hepatic impairment
Severe hepatitis and/or hepatic failure has been associated with therapy even in patients without prior history of abnormal hepatic function
Pregnancy and lactation
Pregnancy category: C
Lactation: excretion in milk unknown/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Antabuse (disulfiram)
Mechanism of action
Produces sensitivity to EtOH via blocking its oxidation at acetaldehyde stage, resulting in unpleasant reactions including palpitations, hypotension, chest pain, nausea, vertigo, thirst, flushing, and nausea
Absorption
Peak plasma time: 4 hr
Peak plasma concentration: 2.4 mcg/mL
Duration: up to 2 wk
Onset: 2-12 hr
Metabolism
Hepatic 80-90%
Metabolites: Diethyldithiocarbamate
Enzymes inhibited: hepatic CYP2C9, CYP2E1
Elimination
Excretion: Feces and exhaled gases
