Antabuse, Cronetal, Ro-sulfiram
Classifications: enzyme inhibitor; antialcohol agent; Therapeutic: alcohol abuse deterrant
Pregnancy Category: B
250 mg, 500 mg tablets
Acts as a deterrent to alcohol ingestion by inhibiting the enzyme acetaldehyde dehydrogenase, which normally metabolizes
alcohol in the body.
When a small amount of alcohol is ingested, a complex of highly unpleasant symptoms known as the disulfiram reaction occurs,
which serves as a deterrent to further drinking.
Adjunct in treatment of the patient with chronic alcoholism who sincerely wants to maintain sobriety.
Severe myocardial disease; cardiac disease; psychosis; patients who have recently ingested alcohol, metronidazole, paraldehyde;
multiple drug dependence.
Diabetes mellitus; epilepsy; seizure disorders; hypothyroidism; coronary artery disease, cerebral damage; chronic and acute
nephritis; renal disease; hepatic cirrhosis or insufficiency; abnormal EEG; pregnancy (category B), lactation.
Route & Dosage
Adult: PO 500 mg/d for 12 wk, then 125500 mg/d (max: 500 mg/d)
- Give daily dose in the morning when the resolve not to drink may be strongest.
- Give at bedtime to minimize sedative effect of the drug. Decrease in dose may also reduce sedative effect.
- Make sure patient has abstained from alcohol and alcohol-containing preparations for at least 12 h and preferably 48 h before
- Determine compliance periodically. Maintenance therapy may be required for months or even years.
- Store at 15°30° C (59°86° F) unless otherwise directed. Protect tablets from light.
Adverse Effects (≥1%)Reaction with alcohol ingestion:
Flushing of face, chest, arms, pulsating headache, nausea, violent vomiting, thirst, sweating, marked uneasiness, confusion,
weakness, vertigo, blurred vision, pruritic skin rash, hyperventilation, abnormal gait, slurred speech, disorientation,
confusion, personality changes, bizarre behavior, psychoses, tachycardia, palpitation, chest pain, hypotension to shock level arrhythmias, acute congestive failure. Severe reactions: Marked respiratory depression, unconsciousness, convulsions, sudden death. Body as a Whole:
Hypersensitivity (allergic or acneiform dermatitis; urticaria, fixed-drug eruption). CNS:
, restlessness, headache, tremor, psychoses (usually with high doses), polyneuritis
, peripheral neuropathy
Mild GI disturbances, garlic-like or metallic taste, hepatotoxicity,
Diagnostic Test Interference
Disulfiram can reduce uptake of I131; or decreases PBI test results (rare).
Interactions Drug: Alcohol
(including in liquid OTC drugs, IV nitroglycerin, IV cotrimoxazole
), metronidazole, paraldehyde
will produce disulfiram reaction; isoniazid
can produce neurological symptoms
; may increase blood levels and toxicity
of warfarin, paraldehyde, barbiturates
Readily absorbed from GI tract. Onset:
Up to 12 h. Duration:
Up to 2 wk. Distribution:
Initially deposited in fat. Metabolism:
Metabolized slowly in liver. Elimination:
520% excreted in feces; 20% remains in body for 12 wk; some may be excreted in breath as carbon disulfide.
Assessment & Drug Effects
- Do a complete physical examination and careful drug history prior to initiation of therapy.
- Lab tests: Baseline and follow-up transaminase studies every 1014 d to detect hepatic dysfunction, and perform CBC
and sequential multiple analysis (SMA-12) tests every 6 mo.
- Note: Disulfiram reaction occurs within 510 min following ingestion of alcohol and may last 30 min to several hours. Intensity
of reaction varies with each individual, but is generally proportional to the amount of alcohol ingested.
- Treat patient with severe disulfiram reaction as though in shock. Monitor potassium levels, especially if patient has diabetes
Patient & Family Education
- Understand fully the possible dangers if alcohol is ingested during disulfiram treatment before consenting to therapy.
- Report promptly to physician the onset of nausea with right upper quadrant pain or discomfort, itching, jaundiced sclerae
or skin, dark urine, clay-colored stools. Withhold drug pending liver function tests.
- Note: Ingestion of even small amounts of alcohol or use of external applications that contain alcohol may be sufficient to produce
a reaction. Read all labels and avoid use of anything containing alcohol.
- Prolonged administration of disulfiram does not produce tolerance; the longer the therapy, the higher the sensitivity to
- Alcohol sensitivity may last as long as 2 wk after disulfiram has been discontinued.
- Note: Adverse effects of drug are often experienced during first 2 wk of therapy; symptoms usually disappear with continued therapy
or with dose reduction.
- Carry an identification card stating you are on disulfiram therapy and describing the symptoms of disulfiram reaction. Also
provide the name of the physician or institution to contact in an emergency.
- Do not drive or engage in other potentially hazardous activities until response to drug is known.