| Drug Name |
ZURNAI™ (nalmefene) |
| Active Ingredient |
nalmefene |
| Date of Approval |
August 07, 2024 |
| Manufacturer |
Purdue Pharma L.P. |
| Approval Pathways and Indications |
Approval Pathway: NDA
Indication: ZURNAI™ is an opioid antagonist used for the emergency treatment of opioid overdose in individuals aged 12 and older, addressing respiratory and/or central nervous system depression caused by natural or synthetic opioids. It is meant for immediate administration in settings where opioids are present but is not a substitute for emergency medical care. |
| Therapeutic Class |
Opiod Antagonist |
| Formulation |
Injection: 1.5 mg nalmefene base/0.5 mL in a prefilled, single-dose autoinjector |
| MoA |
ZURNAI™ is an antagonist at opioid receptors. |
| Dosing and Administration |
Route: Intramuscular or subcutaneous injection into the anterolateral thigh. Can be administered through clothing if needed.
Initial Dose: 1.5 mg for adults and pediatric patients aged 12 years and older, using a single-use auto-injector.
Follow-Up: Seek emergency medical assistance immediately after the first dose.
Additional Doses: If there is no response or if respiratory depression recurs within 2 to 5 minutes, administer additional doses every 2 to 5 minutes with a new auto-injector until help arrives.
Special Cases: For overdoses involving partial agonists or mixed agonist/antagonists (e.g., buprenorphine), repeated doses may be necessary due to incomplete reversal of respiratory depression. |
| Administered by self or by HCP |
Administered by Self |
| Place in Therapy |
ZURNAI™ is the first and only auto-injector containing nalmefene, the longest-acting opioid antagonist approved for reversing opioid overdoses. It offers an additional option for overdoses caused by both prescription opioids and illicit synthetic opioids, effectively reversing respiratory depression, sedation, and hypotension.
ZURNAI™ does not cause respiratory depression, psychotomimetic effects, or pupillary constriction, and shows no pharmacological activity without opioid agonists. It has not been shown to cause tolerance, physical dependence, or abuse potential. However, it can induce acute withdrawal symptoms in opioid-dependent individuals. |
| Expected Market Launch Date |
2025 |
| New Molecular Entity (NME) or Existing Formulation |
Existing Formulation |
| Expected Cost |
Data Unavailable |
| Product Discontinuation |
N/A |
| Clinical Trials |
The effect of ZURNAI™ was studied in an experimental clinical opioid-induced respiratory depression (OIRD) model involving 24 opioid-experienced, non-opioid dependent subjects (NAL1004). This study evaluated changes in minute ventilation (MV) during a 3-step intravenous fentanyl infusion. Initially, fentanyl was infused until MV nadir, defined as a 50% reduction from baseline, was achieved. After reaching MV nadir, the fentanyl infusion rate was reduced to maintain fentanyl concentrations. ZURNAI™ was administered 10 minutes post-MV nadir, with the onset of reversal of respiratory depression occurring between 2.5 to 5 minutes. At 5 minutes, the mean MV change from nadir was 4.42 L/min, with full recovery of respiratory drive noted between 5 and 15 minutes after ZURNAI™ administration.
The safety of ZURNAI™ is supported by pharmacokinetic and pharmacodynamic studies. From a pharmacokinetic study (NAL1005) of 21 healthy adult volunteers and from a pharmacodynamic study (NAL1004), involving 23 healthy adult volunteers, the most common adverse reactions that occurred in >5% of subjects were: feeling hot, nausea, headache, dizziness, chills, allodynia, vomiting, palpitations, tinnitus, ear discomfort, feeling abnormal, burning sensation, irritability, and hot flush. |
| Sources |
FDA Grants Nalmefene Injection Approval for Emergency Treatment of Opioid Overdose. Pharmacy Times. Published August 7, 2024. Accessed August 8, 2024. https://www.pharmacytimes.com/view/
fda-grants-nalmefene-injection-approval-for-emergency-treatment-of-opioid-overdose
FDA Approves ZURNAI (Nalmefene) Injection Auto-Injector for the Emergency Treatment of Known or Suspected Opioid Overdose Induced by Natural or Synthetic Opioids in Adults and Pediatric Patients 12 Years and Older. Morningstar. Published August 7, 2024. Accessed August 8, 2024. https://www.morningstar.com/news/
business-wire/20240807347421/
fda-approves-zurnai-nalmefene-injection
-auto-injector-for-the-emergency-treatment
-of-known-or-suspected-opioid-overdose-
induced-by-natural-or-synthetic-opioids-in-
adults-and-pediatric-patients-12-years-and-older
ZURNAI (nalmefene) injection, for intramuscular or subcutaneous use. U.S. Food and Drug Administration. Published 2024. Accessed August 8, 2024. https://www.accessdata.fda.gov/
drugsatfda_docs/label/2024/
218590s000lbl.pdf |