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disulfiram

(dye sul' fi ram)


Antabuse

Pregnancy Category C

Drug classes
Antialcoholic drug
Enzyme inhibitor

Therapeutic actions
Inhibits the enzyme aldehyde dehydrogenase, blocking oxidation of alcohol and allowing
acetaldehyde to accumulate to concentrations in the blood 5–10 times higher than
normally achieved during alcohol metabolism; accumulation of acetaldehyde produces
the highly unpleasant reaction described below that deters consumption of alcohol.

Indication
• Aids in the management of selected chronic alcoholics who want to remain in a
state of enforced sobriety

Contraindications and cautions


• Contraindicated with allergy to disulfiram or other thiuram derivatives used in
pesticides and rubber vulcanization, severe myocardial disease or coronary
occlusion; psychoses, current or recent treatment with metronidazole,
paraldehyde, alcohol, alcohol-containing preparations (eg, cough syrups, tonics),
pregnancy.
• Use cautiously with diabetes mellitus, hypothyroidism, epilepsy, cerebral damage,
chronic and acute nephritis, hepatic cirrhosis or dysfunction.

Available forms
Tablets—250, 500 mg.

Dosages
Never administer to an intoxicated patient or without patient's knowledge. Do not
administer until patient has abstained from alcohol for at least 12 hr.
ADULTS
• Initial dosage: Administer maximum of 500 mg/day PO in a single dose for 1–2
wk. If a sedative effect occurs, administer at bedtime or decrease dosage.
• Maintenance regimen: 125–500 mg/day PO. Do not exceed 500 mg/day. Continue
use until patient is fully recovered socially and a basis for permanent self-control
is established.
• Trial with alcohol (do not administer to anyone > 50 yr): After 1–2 wk of therapy
with 500 mg/day PO, a drink of 15 mL of 100 proof whiskey or its equivalent is
taken slowly. Dose may be repeated once, if patient is hospitalized and supportive
facilities are available.
Pharmacokinetics
Route Onset Peak Duration
Oral Slow 12 hr 1–2 wk

Metabolism: Hepatic; T1/2: unclear


Distribution: Crosses placenta; enters breast milk
Excretion: Feces, lungs

Adverse effects
Disulfiram with alcohol
• Flushing, throbbing in head and neck, throbbing headaches, respiratory difficulty,
nausea, copious vomiting, sweating, thirst, chest pain, palpitations, dyspnea,
hyperventilation, tachycardia, hypotension, syncope, weakness, vertigo, blurred
vision, confusion; severe reactions may include arrhythmias, CV collapse, acute
CHF, unconsciousness, seizures, MI, death
Disulfiram alone
• CNS: Drowsiness, fatigability, headache, restlessness, peripheral neuropathy,
optic or retrobulbar neuritis
• Dermatologic: Skin eruptions, acneiform eruptions, allergic dermatitis
• GI: Metallic or garliclike aftertaste, hepatotoxicity

Interactions
Drug-drug
• Increased serum levels and risk of toxicity of phenytoin and its congeners,
diazepam, chlordiazepoxide
• Increased therapeutic and toxic effects of theophyllines
• Increased PT caused by disulfiram may lead to a need to adjust dosage of oral
anticoagulants
• Severe alcohol-intolerance reactions with any alcohol-containing liquid
medications (eg, elixirs, tinctures)
• Acute toxic psychosis with metronidazole

Nursing considerations
Assessment
• History: Allergy to disulfiram or other thiuram derivatives; severe myocardial
disease or coronary occlusion; psychoses; current or recent treatment with
metronidazole, paraldehyde, alcohol, alcohol-containing preparations (eg, cough
syrups, tonics); diabetes mellitus, hypothyroidism, epilepsy, cerebral damage,
chronic and acute nephritis, hepatic cirrhosis or dysfunction; pregnancy
• Physical: Skin color, lesions; thyroid palpation; orientation, affect, reflexes; P,
auscultation, BP; R, adventitious sounds; liver evaluation; renal and liver function
tests, CBC, SMA-12

Interventions
• Do not administer until patient has abstained from alcohol for at least 12 hr.
• Administer orally; tablets may be crushed and mixed with liquid beverages.
• Monitor liver function tests before, in 10–14 days, and every 6 mo during therapy
to evaluate for hepatic dysfunction.
• Monitor CBC, SMA-12 before and every 6 mo during therapy.
• Inform patient of the seriousness of disulfiram-alcohol reaction and the potential
consequences of alcohol use. Disulfiram should not be taken for at least 12 hr
after alcohol ingestion, and a reaction may occur up to 2 wk after disulfiram
therapy is stopped; all forms of alcohol must be avoided.
• Arrange for treatment with antihistamines if skin reaction occurs.

Teaching points
• Take drug daily; if drug makes you dizzy or tired, take it at bedtime. Tablets may
be crushed and mixed with liquid.
• Abstain from forms of alcohol (beer, wine, liquor, vinegars, cough mixtures,
sauces, aftershave lotions, liniments, colognes). Taking alcohol while using this
drug can cause severe, unpleasant reactions—flushing, copious vomiting,
throbbing headache, difficulty breathing, even death.
• Wear or carry a medical ID while you are using this drug to alert any medical
emergency personnel that you are using this drug.
• Have periodic blood tests while using drug to evaluate its effects on the liver.
• These side effects may occur: Drowsiness, headache, fatigue, restlessness, blurred
vision (use caution driving or performing tasks that require alertness); metallic
aftertaste (transient).
• Report unusual bleeding or bruising, yellowing of skin or eyes, chest pain,
difficulty breathing, ingestion of any alcohol.

Adverse effects in Italic are most common; those in Bold are life-threatening.

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