THERAPEUTICS

brands

Class

  • Alcohol dependence treatment

DISULFIRAM commonly prescribed for

(Bold for FDA approved)

• Maintenance of alcohol abstinence

How DISULFIRAM works

• Irreversibly inhibits aldehyde dehydrogenase, the enzyme involved in second-stage metabolism of alcohol</br>

• Alcohol is metabolized to acetaldehyde, which in turn is metabolized by aldehyde dehydrogenase; thus, disulfiram blocks this second-stage metabolism</br>

• If alcohol is consumed by a patient taking disulfiram, toxic levels of acetaldehyde build up, causing unpleasant side effects</br>

• This aversive experience ideally leads to negative conditioning, in which patients abstain from alcohol in order to avoid the unpleasant effects

How long until DISULFIRAM works

• Disulfiram’s effects are immediate; patients should not take disulfiram until at least 12 hours after drinking

SIDE EFFECTS

Notable Side Effects

• Metallic taste, dermatitis, sedation

• Flushing, headache, tachycardia, nausea, vomiting (if alcohol is consumed)

Life Threatening Side Effects

• Hepatotoxicity

• Myocardial infarction, congestive heart failure, respiratory depression, other signs of alcohol toxicity (if alcohol is consumed)

weight gain

unusual

unusual

sedation

not usual

not usual

What to do about DISULFIRAM side effects

• Wait

• Reduce dose

• Take at night to reduce sedation

DOSING AND USE

usual dosage range

• 250–500 mg/day; 1-year duration

Dosage Forms

• Tablet 250 mg, 500 mg scored

long term use

• Maintenance treatment should be continued until the patient is recovered

habit forming

• No

SPECIAL POPULATIONS

Renal Impairment

• Not recommended for patients with chronic renal failure

Hepatic Impairment

• Not recommended

Cardiac Impairment

• Contraindicated

Elderly

• Not generally recommended for patients older than age 60

• Some patients may tolerate lower doses better

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• Some animal studies have shown adverse effects

• Pregnant women needing to stop drinking may consider behavioral therapy before pharmacotherapy

• Not generally recommended for use during pregnancy, especially during first trimester

Breast Feeding

• Unknown if disulfiram is secreted in human breast milk, but all psychotropics are assumed to be secreted in breast milk

• Recommended either to discontinue drug or bottle feed