|Systematic (IUPAC) name|
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Levallorphan (Lorfan, Naloxiphan) is a drug of the morphinan family used as an opioid modulator and antidote. It acts as an antagonist on μ-opioid receptor and agonist on kappa receptor, and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine or endogenous β-endorphin.
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, 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. The combination of levallorphan with pethidine (meperidine) was indeed used so frequently, a standardized formulation was made available, known as Pethilorfan.
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- 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.
- 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. doi:10.1136/bmj.2.5156.859. PMC 1990381. PMID 13805887.
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- 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.