ABOUT NALMEFENE HCl
Nalmefene HCl: Another tool in your opioid overdose reversal toolbox.
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This site is intended for healthcare professionals only.
Duration of Action
Nalmefene hcl has a duration of action as long as most opioids1
While Nalmefene Hydrochloride injection has a longer duration of action than naloxone in fully reversing doses, the physician should be aware that a recurrence of respiratory depression is possible, even after an apparently adequate initial response to Nalmefene Hydrochloride injection treatment.
Patients treated with Nalmefene Hydrochloride injection should be observed until, in the opinion of the physician, there is no reasonable risk of recurrent respiratory depression.
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>80% of opioid receptors blocked within 5 minutes1
Following a 1 mg parenteral dose, nalmefene was rapidly distributed. In a pharmacology study of brain receptor occupancy, a 1 mg dose of nalmefene blocked more than 80% of brain opioid receptors within 5 minutes after administration.
10.8-Hour Mean Terminal Elimination Half-Life1
Nalmefene elimination half-life is based on pharmacokinetic data. The mean terminal elimination half-life is 10.8 hours and 9.4 hours in younger (19 to 32 years) and elderly (62 to 80 years) healthy male subjects, respectively, following a Nalmefene HCl 1 mg IV dose.
Safety and Tolerability Similar to Naloxone1
IV=intravenous.
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Demonstrated Efficacy With Strength That Lasts
Nalmefene Is The Longest-Acting Opioid Antagonist Approved For Opioid Overdose Reversal1,2
Fully reversing doses (1 mg/70 kg) that last hours1
- In a randomized, double-blind phase 3 trial (n=176), patients were evaluated for up to 4 hours3
- In experimental and other clinical studies, subjects were evaluated for 4 to 8 hours4-6
Approved for opioid overdose reversal in 1995 under the brand name Revex®. Withdrawn from the US market in 2008 by its manufacturer for reasons other than safety and effectiveness.7 Made available again in February 2022 to help address the specific needs of today’s opioid overdose crisis1
4 clinical trials* were done. Studied in 284 patients presumed to have taken an opioid overdose1
Effectively reversed respiratory depression at doses of 0.5 mg to 1 mg.1,3 Dose range in clinical trials was 0.5 mg to 2 mg1
IV injection shows effect within 2 to 5 minutes in most patients. Based on a pharmacokinetic study, a single 1-mg IM or SC dose should be effective within 5 to 15 minutes1
*The trials are based on studies conducted with Revex.
Known Safety Profile and Tolerability
SAFETY AND TOLERABILITY SIMILAR TO NALOXONE1
- In a clinical study with healthy volunteers, no serious toxicity was observed, even at 15x the highest recommended dose
- As with other narcotic antagonist drugs, higher-than-recommended doses of Nalmefene HCl resulted in symptoms suggestive of reversal of endogenous opioids, including nausea, chills, myalgia, dysphoria, abdominal cramps, and joint pain
- Symptoms were transient and usually occurred at very low frequency
Relative Frequencies of Common Adverse Reactions(incidences >1%, all clinical settings)1
ADVERSE EVENT | NALMEFENE (n=1127) | NALOXONE (n=369) | PLACEBO (n=77) |
|---|---|---|---|
Nausea | 18% | 18% | 6% |
Vomiting | 9% | 7% | 4% |
Tachycardia | 5% | 8% | – |
Hypertension | 5% | 7% | – |
Postoperative pain | 4% | 4% | N/A |
Fever | 3% | 4% | – |
Dizziness | 3% | 4% | 1% |
Headache | 1% | 1% | 4% |
Chills | 1% | 1% | – |
Hypotension | 1% | 1% | – |
Vasodilation | 1% | 1% | – |
Adverse events were observed in both 152 healthy volunteers and 1127 patients who were treated for opioid overdose or for postoperative opioid reversal.1
Nalmefene HCl Essentials
HELP TAKE CONTROL OF OPIOID OVERDOSE UNKNOWNS WITH NALMEFENE HCl
IM=intramuscular; IV=intravenous; SC=subcutaneous.
†
Studied in 284 patients presumed to have taken an opioid overdose. Effectively reversed respiratory depression at doses of 0.5 mg to 1 mg. Dose range in clinical trials was 0.5 mg to 2 mg.1,3
‡
Nalmefene elimination half-life is based on pharmacokinetic data. The mean terminal elimination half-life is 10.8 hours and 9.4 hours in younger (19 to 32 years) and elderly (62 to 80 years) healthy male subjects, respectively, following a Nalmefene HCl 1 mg IV dose.1
