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disulfiram (Antabuse)
Tradename: Antabuse.
Indications:
-> management of alcoholics who want enforced sobriety
Contraindications:
-> use with caution in the elderly {potential cardiac toxicity} [5]
Dosage: Sobriety: 250-500 mg PO QD.
Tabs: 250 & 500 mg.
Pharmacokinetics:
1) rapidly absorbed after oral administration
2) metabolized by liver to:
a) diethyldithiocarbamate (t1/2 of 15 hours)
b) carbon disulfide (t1/2 of 9 hours)
3) t1/2 of 7 hours
4) 20% of the drug remains in the body 1 week after administration
5) patients may be alcohol sensitive 1-2 weeks after the last dose taken
Monitor:
- liver function tests at baseline, 10-14 days after initiation, then periodically [7]
Adverse effects:
1) drowsiness (common, > 10%)
2) fatigue
3) peripheral neuritis
4) blurred vision
5) skin eruptions
6) metallic or garlic taste
7) hepatotoxicity
8) mood changes
9) encephalopathy (uncommon, < 1%)
10) cardiac toxicity [5]
Drug interactions:
1) alcohol: produces intolerance reaction
2) disulfiram inhibits warfarin metabolism
3) disulfiram increased phenytoin levels
4) may result in psychosis/behavioral changes when used in combination with metronidazole or INH
5) may result in organic brain syndrome when used in combination with tricyclic antidepressants (TCA)
Laboratory:
1) specimen: plasma; analyze promptly
2) methods: GLC, HPLC
Mechanism of action:
1) inhibits aldehyde dehydrogenase resulting in accumulation of acetaldehyde
2) metabolites:
a) diethyldithiocarbamate
b) carbon disulfide
2) reaction with alcohol (intolerance reaction)
a) flushing
b) throbbing headache
c) nausea/vomiting
d) hypotension
e) palpitations
f) chest pain
g) blurred vision
h) confusion
General
miscellaneous pharmacologic agent
Properties
MISC-INFO: elimination route LIVER
1/2life 7 HOURS
therapeutic-range 75-300 NG/ML
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM cid=3117
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Geriatrics Review Syllabus, American Geriatrics Society,
5th edition, 2002-2004
- Department of Veterans Affairs, VA National Formulary
- Prescriber's Letter 17(7): 2010
Recommended Lab Monitoring for Common Medications
Liver Function Test Scheduling
Detail-Document#: 260704
(subscription needed) http://www.prescribersletter.com