|
Pronunciation |
|
(dye
SUL fi
ram) |
|
|
U.S. Brand
Names |
|
Antabuse® |
|
|
Generic
Available |
|
Yes |
|
|
Pharmacological Index |
|
Aldehyde Dehydrogenase Inhibitor |
|
|
Use |
|
Management of chronic alcoholism |
|
|
Pregnancy Risk
Factor |
|
C |
|
|
Contraindications |
|
Severe myocardial disease and coronary occlusion; psychoses; hypersensitivity
to disulfiram and related compounds or any component; patients receiving or
using alcohol, metronidazole, paraldehyde, or alcohol-containing preparations
like cough syrup or tonics |
|
|
Warnings/Precautions |
|
Use with caution in patients with diabetes, hypothyroidism, seizure
disorders, nephritis (acute or chronic); hepatic cirrhosis or insufficiency;
should never be administered to a patient when he/she is in a state of alcohol
intoxication, or without his/her knowledge. Patient must receive appropriate
counseling, including information on "disguised" forms of alcohol (tonics,
mouthwashes, etc) and the duration of the drug's activity (up to 14
days). |
|
|
Adverse
Reactions |
|
Central nervous system: Drowsiness, headache, fatigue, psychosis
Dermatologic: Rash, acneiform eruptions, allergic dermatitis
Gastrointestinal: Metallic or garlic-like aftertaste
Genitourinary: Impotence
Hepatic: Hepatitis
Neuromuscular & skeletal: Peripheral neuritis, polyneuritis, peripheral
neuropathy
Ocular: Optic neuritis |
|
|
Overdosage/Toxicology |
|
Management of disulfiram reaction: Institute support measures to restore
blood pressure (pressors and fluids); monitor for
hypokalemia |
|
|
Drug
Interactions |
|
CYP2C9 and 2E1 enzyme inhibitor, both disulfiram and diethyldithiocarbamate
(disulfiram metabolite) are CYP3A3/4 enzyme inhibitors
Disulfiram increases phenytoin and theophylline serum concentrations;
toxicity may occur
Disulfiram inhibits the metabolism of warfarin resulting in an increased
hypoprothombinemic response
Disulfiram results in severe ethanol intolerance
(Antabuse® reaction) secondary to disulfiram's ability to
inhibit aldehyde dehydrogenase; this combination should be avoided
Combined use with isoniazid, metronidazole, or MAOIs may result in adverse
CNS effects; this combination should be avoided
Intravenous trimethoprim-sulfamethoxazole contains 10% ethanol as a
solubilizing agent and may interact with disulfiram; monitor for
Antabuse® reaction |
|
|
Mechanism of
Action |
|
Disulfiram is a thiuram derivative which interferes with aldehyde
dehydrogenase. When taken concomitantly with alcohol, there is an increase in
serum acetaldehyde levels. High acetaldehyde causes uncomfortable symptoms
including flushing, nausea, thirst, palpitations, chest pain, vertigo, and
hypotension. This reaction is the basis for disulfiram use in postwithdrawal
long-term care of alcoholism. |
|
|
Pharmacodynamics/Kinetics |
|
Onset of action: Full effect: 12 hours
Duration: May persist for 1-2 weeks after last dose
Absorption: Rapid from GI tract
Full effect: 12 hours
Metabolism: To diethylthiocarbamate |
|
|
Usual Dosage |
|
Adults: Oral: Do not administer until the patient has abstained from alcohol
for at least 12 hours
Average maintenance dose: 250 mg/day; range: 125-500 mg; duration of therapy
is to continue until the patient is fully recovered socially and a basis for
permanent self control has been established; maintenance therapy may be required
for months or even years |
|
|
Dietary
Considerations |
|
Alcohol: Avoid use, including alcohol-containing
products |
|
|
Mental Health: Effects
on Mental Status |
|
Psychotic reactions have been noted |
|
|
Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
|
No information available to require special precautions |
|
|
Dental Health:
Effects on Dental Treatment |
|
No effects or complications reported |
|
|
Patient
Information |
|
Tablets can be crushed or mixed with water or juice. Metallic aftertaste may
occur; this will go away. Do not drink any alcohol, including products
containing alcohol (cough and cold syrups), or use alcohol-containing skin
products for at least 3 days and preferably 14 days after stopping this
medication or while taking this medication. Drowsiness, tiredness, or visual
changes may occur. Use care when driving or engaging in tasks requiring
alertness until response to drug is known. Report yellow color in eyes or skin
and any respiratory difficulty. Pregnancy/breast-feeding precautions:
Inform prescriber if you are or intend to be pregnant. Consult prescriber if
breast-feeding. |
|
|
Nursing
Implications |
|
Administration of any medications containing alcohol including topicals is
contraindicated |
|
|
Dosage Forms |
|
Tablet: 250 mg, 500 mg |
|
|
References |
|
Motte S, Vincent JL, and Gillet JB,
"Refractory Hyperdynamic Shock Associated With Alcohol and Disulfiram," Am J
Emerg Med, 1986, 4(4):323-5.
Pompidou A, Delsaux MC, Telvi L, et al,
"Isoprinosine and Imuthiol, Two Potentially Active Compounds in Patients With AIDS-Related Complex Symptoms,"
Cancer Res, 1985, 45(9 Suppl):4671S-4673S.
|
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
|