THERAPEUTICS

Class

  • Neuroscience-based Nomenclature: opioid receptor antagonist (O-RAn)
  • Alcohol dependence treatment; mu and delta opioid receptor antagonist and kappa opioid receptor partial agonist

NALMEFENE commonly prescribed for

(Bold for FDA approved)

• Reduction of alcohol consumption in patients with alcohol dependence who have a high drinking risk level

How NALMEFENE works

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

• Blockade of mu opioid receptors prevents the pleasurable effects of alcohol, whereas modulation of the kappa opioid receptors may reduce dysphoria associated with alcohol withdrawal

How long until NALMEFENE works

• Can begin working immediately and can be used as needed

SIDE EFFECTS

Notable Side Effects

• Nausea, vomiting

• Dizziness, insomnia, headache

Life Threatening Side Effects

• Confusion, rare hallucinations

weight gain

unusual

unusual

sedation

not usual

not usual

What to do about NALMEFENE side effects

• Wait

• Switch to another agent

DOSING AND USE

usual dosage range

• 18 mg/day as needed

Dosage Forms

• Tablet 18 mg

long term use

• Has been evaluated in trials for up to 1 year

habit forming

• No

SPECIAL POPULATIONS

Renal Impairment

• Dose adjustment not necessary for mild to moderate impairment

• Not recommended for use in severe impairment

Hepatic Impairment

• Dose adjustment not necessary for mild to moderate impairment

• Not recommended for use in severe impairment

Cardiac Impairment

• Not studied

Elderly

• Limited data available

Children and Adolescents

• Safety and efficacy have not been established

Pregnancy

• 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 nalmefene 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