Unidirectional analgesic cross-tolerance between morphine and levorphanol in the rat

Dwight E. Moulin, Geoffrey Ling, Gavril W. Pasternak

Research output: Contribution to journalArticle

Abstract

Clinically, patients often demonstrate incomplete cross-tolerance between opiate analgesics. Although dispositional and pharmacokinetic factors may be a factor, our results suggest that differences in selectivity of various opioids for those opioid receptor subtypes involved in analgesia, mu1, kappa and delta, also play an important role. In binding studies, levorphanol potently labelled all 3 classes whereas morphine was relatively selective for mu sites. Levorphanol infusions yielded tolerance to both morphine and levorphanol while morphine infusions selectively produced tolerance to morphine. This unidirectional tolerance might be due to the selectivity of morphine for mu receptors compared to levorphanol's ability to interact more potently with other relevant receptor subtypes. These observations raise the possibility that the order in which different opioid analgesics are administered may be of clinical significance.

Original languageEnglish (US)
Pages (from-to)233-239
Number of pages7
JournalPain
Volume33
Issue number2
DOIs
StatePublished - Jan 1 1988
Externally publishedYes

Fingerprint

Levorphanol
Morphine
Analgesics
mu Opioid Receptor
Opioid Analgesics
Opiate Alkaloids
Opioid Receptors
Analgesia
Pharmacokinetics

Keywords

  • Analgesia
  • Morphine
  • Opiate receptor

ASJC Scopus subject areas

  • Clinical Neurology
  • Psychiatry and Mental health
  • Neuroscience(all)
  • Neurology
  • Pharmacology
  • Clinical Psychology

Cite this

Unidirectional analgesic cross-tolerance between morphine and levorphanol in the rat. / Moulin, Dwight E.; Ling, Geoffrey; Pasternak, Gavril W.

In: Pain, Vol. 33, No. 2, 01.01.1988, p. 233-239.

Research output: Contribution to journalArticle

Moulin, Dwight E. ; Ling, Geoffrey ; Pasternak, Gavril W. / Unidirectional analgesic cross-tolerance between morphine and levorphanol in the rat. In: Pain. 1988 ; Vol. 33, No. 2. pp. 233-239.
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