Open Access Articles- Top Results for Levallorphan


Systematic (IUPAC) name
Clinical data
AHFS/ International Drug Names
  • (Prescription only)
152-02-3 7pxY
PubChem CID 5359371
DrugBank DB00504 7pxN
ChemSpider 4514267 7pxY
UNII 353613BU4U 7pxY
ChEMBL CHEMBL1254682 7pxN
Chemical data
Formula C19H25NO
283.4079 g/mol
 14pxN (what is this?)  (verify)

Levallorphan (Lorfan, Naloxiphan) is a drug of the morphinan family used as an opioid modulator and antidote.[1] It acts as an antagonist on μ-opioid receptor and agonist on kappa receptor,[2] and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine or endogenous β-endorphin.[3]

Levallorphan was formerly widely used in general anaesthesia, mainly to reverse the respiratory depression produced by the opioid analgesics and barbiturates used for induction of surgical anaesthesia while maintaining a degree of analgesia (via kappa opioid receptor agonization) although it is now less common as the newer drug naloxone tends to be used, instead.

It was also used in combination with opioids to reduce their side effects, mainly in obstetrics, and a very small dose of levallorphan used alongside an opioid full agonist can produce greater analgesia than when the agonist is used by itself.[4] The combination of levallorphan with pethidine (meperidine) was indeed used so frequently, a standardized formulation was made available, known as Pethilorfan.[5]


Same method as for Racemorphan except different N-alkyl subsitutent.[6]

See also


  1. ^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 3-88763-075-0. 
  2. ^ Goodman & Gilman. The Pharmacological Basis of Therapeutics (10th ed.). McGraw Hill Medical Publishing. p. 602. ISBN 978-0-07-135469-1. 
  3. ^ Codd, E. E.; Shank, R. P.; Schupsky, J. J.; Raffa, R. B. (September 1995). "Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception". The Journal of Pharmacology and Experimental Therapeutics 274 (3): 1263–1270. PMID 7562497. 
  4. ^ Bullough, J. (1959). "Use of premixed pethidine and antagonists in obstetrical analgesia; with special reference to cases in which levallorphan was used" (PDF). British Medical Journal 2 (5156): 859–862. PMC 1990381. PMID 13805887. doi:10.1136/bmj.2.5156.859. 
  5. ^ Williams, G.; Cope, I. (1962). "An evaluation of a combination of pethidine and levallorphan ("pethilorfan") in labour". The Medical Journal of Australia 49 (2): 499–503. PMID 14000851. 
  6. ^ Hellerbach, J.; Gr�Ssner, A.; Schnider, O. (1956). "Hydroxy-morphinane. 7. Mitteilung. (?)-3-Hydroxy-N-allyl-morphinan und verwandte Verbindungen". Helvetica Chimica Acta 39 (2): 429. doi:10.1002/hlca.19560390212.  edit