Nalmefene

Information about Nalmefene

Nalmefene is an opiate receptor antagonist which is used to treat acute opioid overdose and in the management of alcohol dependence and addictive behaviors.

Liver safety of Nalmefene

Nalmefene has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.

Mechanism of action of Nalmefene

Nalmefene (nal’ me feen) is a semisynthetic opiate receptor antagonist which is similar structurally to naltrexone and oxymorphone. Nalmefene is distinctive in having antagonist activity against all three types of opiate receptors – μ, κ and δ. When given intravenously or intramuscularly, nalmefene causes rapid onset of withdrawal symptoms in opioid dependent persons and has been used successfully to treat acute opioid overdose. It is also used to reverse opioid actions in the postoperative period. It has a longer duration of action than naloxone and better oral availability.

FDA approval information for Nalmefene

Nalmefene was approved for use in the United States in 1995 as a therapy of opioid overdose. Oral formulations, which have been used to treat alcohol dependence and other addictive behaviors, have not been approved for this use in the United States. Nalmefene is available in solutions for injection in concentrations of 100 μg/mL (for postoperative use) and 1 mg/mL (for management of known of suspected opioid overdose) under the trade name Revex.

Side effects of Nalmefene

Side effects of parenterally administered nalmefene in opioid dependent patients include mood changes, sweating, anxiety, restlessness, trembling, dizziness, flushing, headache, nausea, vomiting, cardiac tachyarrhythmias, seizures, chest pain and acute pulmonary edema—symptoms of acute opioid withdrawal. In persons not taking opioids, nalmefene has minimal effects. Nalmefene is not a controlled substance, but its use is sometimes restricted to medical staff trained in emergency medicine or anesthesia.

Full and partial opiod agonists:

• Alfentanil
• Butorphanol
• Codeine
• Diphenoxylate
• Fentanyl
• Heroin
• Hydrocodone
• Hydromorphone
• Levorphanol
• Loperamide
• Meperidine
• Methadone
• Morphine
• Opium
• Oxycodone
• Oxymorphone
• Pentazocine
• Remifentanil
• Sufentanil
• Tramadol

Opiate antagonists:

• Nalmefene
• Naloxegol
• Naloxone
• Naltrexone

• Dailymed label info on Nalmefene
• FDA Nalmefene