Levallorphan

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Levallorphan
File:Levallorphan.png
Systematic (IUPAC) name
(-)-17-allylmorphinan-3-ol
Clinical data
Routes of
administration
Oral
Legal status
Legal status
  • ℞ (Prescription only)
Identifiers
CAS Number 152-02-3
ATC code none
PubChem CID 5359371
DrugBank DB00504
ChemSpider 4514267
Chemical data
Formula C19H25NO
Molar mass 283.4079 g/mol[[Script error: No such module "String".]]
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Levallorphan (Lorfan, Naloxiphan) is a drug of the morphinan family which is used as an opioid antidote or antagonist.[1] It acts as a μ-opioid receptor weak partial agonist, and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine or endogenous β-endorphin.[2]

Levallorphan was formerly widely used in general anaesthesia, mainly to reverse the respiratory depression produced by the opioid analgesics and barbiturates which are 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 when a very small dose of levallorphan is used alongside an opioid full agonist this can in fact produce greater analgesia than when the agonist is used by itself.[3] The combination of levallorphan with pethidine (meperidine) was indeed used so frequently that a standardized formulation was made available, known as Pethilorfan.[4]

See also

References

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  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. 
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  3. Bullough J. Use of premixed pethidine and antagonists in obstetrical analgesia; with special reference to cases in which levallorphan was used. British Medical Journal. 1959 Oct 31;2(5156):859-62. PMID 13805887
  4. Williams G, Cope I. An evaluation of a combination of pethidine and levallorphan ("pethilorfan") in labour. Medical Journal of Australia. 1962 Sep 29;49(2):499-503. PMID 14000851