Zurnai (Purdue), an autoinjector formulation of the opioid antagonist nalmefene, has been approved by the FDA for intramuscular (IM) or subcutaneous (SC) emergency treatment of known or suspected opioid overdose in persons ≥12 years old. Naloxone, another opioid antagonist, has been available in single-use syringes for years. Both nalmefene and naloxone are also available in nasal sprays; some naloxone nasal sprays (Narcan, and others) are available over the counter.

Opioid use disorder is a chronic, relapsing disease with physical and psychiatric components. It is associated with economic hardship, social isolation, incarceration, increased rates of blood-borne infections such as HIV and viral hepatitis, adverse pregnancy outcomes, and increased mortality. According to the NIH, there were 80,411 deaths involving an opioid in the US in 2021, more than in any previous year. Several guidelines on the management of opioid use disorder are available; all recommend maintenance pharmacotherapy as the standard of care.

The FDA has approved a generic injectable formulation of the opioid antagonist nalmefene (Purdue) for the management of known or suspected opioid overdose. Revex, the reference product, was withdrawn from the market in 2008 for commercial reasons.

Nalmefene (Revex - Ohmeda), an i methylene analog of naltrexone (Trexan), is a long-acting opioid antagonist that has been approved by the US Food and Drug Administration for reversal of postoperative opioid drug effects, including respiratory depression, sedation and hypotension and for management of known or suspected opioid overdose in the emergency department. The only other opioid antagonists available in the USA are naloxone (Narcan), which is also injectable but has a short duration of action, and naltrexone, which has a long duration of action but is marketed only for oral...

In our article on abuse-deterrent opioids (Med Lett Drugs Ther 2017; 59:95), the information on Targiniq ER in Table 1 is incorrect. The drug, which is not available in the US, is a combination of oxycodone ER and naloxone, not naltrexone, and naloxone is dispersed throughout the tablet, not sequestered. Targiniq ER will be deleted from the table in the article as it appears on our website.

The FDA has approved subdermal implants of the partial opioid agonist buprenorphine (Probuphine – Titan) for maintenance treatment of opioid dependence in patients stabilized on low to moderate doses of transmucosal buprenorphine. Probuphine was designed to provide continuous low levels of buprenorphine for 6 months and to safeguard against illicit use of the drug.

Since the publication of our articles entitled Drugs for Opioid Use Disorder and In Brief: Over-the-Counter Narcan Nasal Spray earlier this year, Narcan (Emergent), a nasal spray that delivers 4 mg of the opioid antagonist naloxone, has become available for sale over the counter (OTC). According to the manufacturer, the retail price for a box containing 2 doses is $44.99. Some insurance companies have announced plans to cover OTC purchase of the drug for their members.

View Expanded Table: Some Drugs for Management of Opioid Withdrawal Symptoms

Healthcare providers are often asked if drugs can be used past their expiration date. Because of legal restrictions and liability concerns, manufacturers do not sanction such use and usually do not comment on the safety or effectiveness of their products beyond the date on the label. Since our last article on this subject, more data have become available.

The FDA has approved a subcutaneously injected, extended-release formulation of the mu-opioid receptor partial agonist and kappa-opioid receptor antagonist buprenorphine (Brixadi – Braeburn) for once-weekly or once-monthly treatment of moderate to severe opioid use disorder. Brixadi is the second subcutaneously injected buprenorphine formulation to be approved in the US; Sublocade, which is administered once monthly, was the first. Buprenorphine is also available for treatment of opioid use disorder in sublingual formulations with and without the opioid antagonist...