Nalmefene

Nalmefene, a 6-methylene analogue of naltrexone, is an opioid receptor antagonist. It acts as an antagonist at the mu (μ)-opioid and delta (δ)-opioid receptors and a partial agonist at the kappa (κ)-opioid receptor.

In Europe, nalmefene oral tablets are used to reduce alcohol consumption in adults with alcohol dependence. Nalmefene was approved in the United States in 1995 as an antidote for opioid overdose. Nalmefene injection is used to manage known or suspected opioid overdose. It is used for complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. The nasal spray formulation of nalmefene was approved by the FDA in May 2023.

Nalmefene oral tablet is indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking risk level (DRL), without physical withdrawal symptoms and who do not require immediate detoxification. Nalmefene should only be prescribed in conjunction with continuous psychosocial support focused on treatment adherence and reducing alcohol consumption. Nalmefene should be initiated only in patients who continue to have a high DRL two weeks after the initial assessment.

Nalmefene injection and nasal spray are indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. They are also indicated in the management of known or suspected opioid overdose. Nalmefene injection can be used for postoperative opioid overdose reversal.