Nalmefene

Nalmefene
Clinical data
Trade namesRevex, others
Other namesNalmetrene; 6-Desoxy-6-methylenenaltrexone; CPH-101; JF-1; Lu AA36143; NIH-10365; ORF-11676
AHFS/Drugs.comMonograph
MedlinePlusa605043
License data
Routes of
administration		By mouth, intranasal, intramuscular, intravenous, subcutaneous
Drug classOpioid antagonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability40–50% (orally)[7]
Protein binding45%
MetabolismLiver
Elimination half-life10.8 ± 5.2 hours
ExcretionKidney
Identifiers
  • 17-Cyclopropylmethyl-4,5α-epoxy-6-methylenemorphinan-3,14-diol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.164.948 Edit this at Wikidata
Chemical and physical data
FormulaC21H25NO3
Molar mass339.435 g·mol−1
3D model (JSmol)
  • OC(C1=C2[C@@]34[C@H]5O1)=CC=C2C[C@@H](N(CC4)CC6CC6)[C@]3(O)CCC5=C
  • InChI=1S/C21H25NO3/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13/h4-5,13,16,19,23-24H,1-3,6-11H2/t16-,19+,20+,21-/m1/s1 checkY
  • Key:WJBLNOPPDWQMCH-MBPVOVBZSA-N checkY
  (verify)

Nalmefene, sold under the brand name Revex among others, is a medication that is used in the treatment of opioid overdose and alcohol dependence.[2][3] Nalmefene belongs to the class of opioid antagonists and can be taken by mouth, administered by injection, or delivered through nasal administration.[8]

In terms of its chemical structure and biological activity, nalmefene is similar to another opioid antagonist called naltrexone, as they are both derivatives of opiates. However, nalmefene offers certain advantages over naltrexone. These include a longer elimination half-life, which means it stays in the body for a longer duration, improved absorption when taken by mouth, and no observed liver toxicity that is dependent on the dosage.[9]

Nalmefene is available as a generic medication.[10]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2015". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. Retrieved 10 April 2023.
  2. ^ a b Cite error: The named reference UKlabel was invoked but never defined (see the help page).
  3. ^ a b "Revex- nalmefene hydrochloride injection, solution". DailyMed. Archived from the original on 21 January 2022. Retrieved 11 February 2022.
  4. ^ "Opvee- nalmefene hydrochloride spray". DailyMed. 19 June 2023. Archived from the original on 8 August 2024. Retrieved 25 June 2023.
  5. ^ https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/218590s000lbl.pdf
  6. ^ "Selincro EPAR". European Medicines Agency. 13 March 2013. Archived from the original on 11 February 2022. Retrieved 11 February 2022.
  7. ^ Kyhl LE, Li S, Faerch KU, Soegaard B, Larsen F, Areberg J (February 2016). "Population pharmacokinetics of nalmefene in healthy subjects and its relation to μ-opioid receptor occupancy". British Journal of Clinical Pharmacology. 81 (2). Wiley: 290–300. doi:10.1111/bcp.12805. PMC 4833148. PMID 26483076.
  8. ^ "FDA Approves Prescription Nasal Spray to Reverse Opioid Overdose". U.S. Food and Drug Administration (FDA) (Press release). 23 May 2023. Archived from the original on 1 June 2023. Retrieved 1 June 2023.
  9. ^ "Nalmefene". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Library of Medicine. 24 March 2020. PMID 31643618. Bookshelf ID: NBK548295. Archived from the original on 13 November 2021. Retrieved 12 February 2022.
  10. ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 11 February 2022. Archived from the original on 12 February 2022. Retrieved 11 February 2022.