Nefopam

Nefopam
Clinical data
Trade namesnefopam medisol
AHFS/Drugs.comInternational Drug Names
Routes of
administration		intramuscular, intravenous
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
Pharmacokinetic data
BioavailabilityLow[1]
Protein binding70–75% (mean 73%)[1][2]
MetabolismLiver (N-demethylation, others)[1]
MetabolitesDesmethylnefopam, others[1]
Elimination half-lifeNefopam: 3–8 hours[1]
Desmethylnefopam: 10–15 hours[1]
ExcretionUrine: 79.3%[1]
Feces: 13.4%[1]
Identifiers
  • (RS)-5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxazocine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
ECHA InfoCard100.033.757 Edit this at Wikidata
Chemical and physical data
FormulaC17H19NO
Molar mass253.345 g·mol−1
3D model (JSmol)
  • CN1CCOC(C2=CC=CC=C2C1)C3=CC=CC=C3
  • InChI=1S/C17H19NO/c1-18-11-12-19-17(14-7-3-2-4-8-14)16-10-6-5-9-15(16)13-18/h2-10,17H,11-13H2,1H3 ☒N
  • Key:RGPDEAGGEXEMMM-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Nefopam, sold under the brand name Acupan among others, is a centrally acting, non-opioid painkilling medication, with central stimulant and sympathomimetic properties that is primarily used to treat moderate to severe pain.[3]

Nefopam acts in the brain and spinal cord to relieve pain via novel mechanisms: antinociceptive effects from triple monoamine reuptake inhibition, and antihyperalgesic activity through modulation of glutamatergic transmission.[4]

  1. ^ a b c d e f g h Sanga M, Banach J, Ledvina A, Modi NB, Mittur A (November 2016). "Pharmacokinetics, metabolism, and excretion of nefopam, a dual reuptake inhibitor in healthy male volunteers". Xenobiotica; the Fate of Foreign Compounds in Biological Systems. 46 (11): 1001–16. doi:10.3109/00498254.2015.1136989. PMID 26796604. S2CID 34603935.
  2. ^ Seyffart G (6 December 2012). Drug Dosage in Renal Insufficiency. Springer Science & Business Media. pp. 407–. ISBN 978-94-011-3804-8.
  3. ^ Brayfield A, ed. (27 October 2016). "Nefopam hydrochloride". MedicinesComplete. London, UK: Pharmaceutical Press. Retrieved 4 September 2017.
  4. ^ Cite error: The named reference RevPharm2016 was invoked but never defined (see the help page).