brands

Class

• Neuroscience-based Nomenclature: opioid receptor antagonist (O-RAn)
• Alcohol dependence treatment; mu opioid receptor antagonist

NALTREXONE commonly prescribed for

(Bold for FDA approved)

How NALTREXONE works

• Blocks mu opioid receptors, preventing exogenous opioids from binding there and thus preventing the pleasurable effects of opioid consumption

• Reduces alcohol consumption through modulation of opioid systems, thereby reducing the reinforcing effects of alcohol

How long until NALTREXONE works

• Can begin working within a few days but maximum effects may not be seen for a few weeks

Notable Side Effects

• Nausea, vomiting, decreased appetite

• Dizziness, dysphoria, anxiety

• Injection site reactions (pain, tenderness, pruritis, induration, swelling, erythema, or bruising); in some cases injection site reactions may be very severe

Life Threatening Side Effects

• Eosinophilic pneumonia

• Hepatocellular injury (at excessive doses)

• Severe injection site reactions requiring surgery

weight gain

unusual

sedation

not usual

What to do about NALTREXONE side effects

• Wait

• Adjust dose

• If side effects persist, discontinue use

usual dosage range

• Oral: 50 to 150 mg/day

• Injection: 380 mg every 4 weeks

Dosage Forms

• Tablet 25 mg, 50 mg, 100 mg

• Intramuscular formulation 380 mg/vial

long term use

• Has been studied in trials up to 1 year

habit forming

• No

Renal Impairment

• Dose adjustment not generally necessary for mild impairment

• Not studied in moderate to severe renal impairment

Hepatic Impairment

• Has the potential to cause hepatocellular injury when given in excessive doses

• Dose adjustment not generally necessary for mild impairment

• Not studied in severe hepatic impairment

• Contraindicated in acute hepatitis or liver failure

Cardiac Impairment

• Limited available data

Elderly

• Safety and efficacy have not been established

• Some patients may tolerate lower doses better

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• Controlled studies have not been conducted in pregnant women

• 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

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or bottle feed