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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral |
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| ECHA InfoCard | 100.005.273 |
| Chemical and physical data | |
| Formula | C19H25NO |
| Molar mass | 283.415 g·mol−1 |
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Levallorphan (INN,BAN;USANlevallorphan tartrate; brand namesLorfan,Naloxifan, andNaloxiphan) is anopioid modulator of themorphinan family used as anopioidanalgesic andopioid antagonist/antidote.[1][2][3] It acts as anantagonist of theμ-opioid receptor (MOR) and as anagonist of theκ-opioid receptor (KOR),[4] and as a result, blocks the effects of stronger agents with greaterintrinsic activity such asmorphine whilst simultaneously producinganalgesia.[5]
Levallorphan was formerly widely used ingeneral anesthesia, mainly to reverse therespiratory depression produced by opioid analgesics andbarbiturates used for induction ofsurgical anaesthesia whilst maintaining a degree of analgesia (via KOR agonism). It is now less commonly employed for this purpose as the newer drugnaloxone tends to be used instead. Levallorphan was also used in combination with opioid analgesics to reduce theirside effects, mainly inobstetrics, and a very small dose of levallorphan used alongside afull agonist of the MOR can produce greater analgesia than when the latter is used by itself.[6] The combination of levallorphan withpethidine (meperidine) was indeed used so frequently, a standardized formulation was made available, known asPethilorfan.[7]
As an agonist of the KOR, levallorphan can produce severe mental reactions at sufficient doses includinghallucinations,dissociation, and otherpsychotomimetic effects,dysphoria,anxiety,confusion,dizziness,disorientation,derealization, feelings ofdrunkenness,delusions, paranoia, and bizarre, unusual, or disturbingdreams.[8][9][10]