Butorphanol agonist effects and acute physical dependence in opioid abusers: Comparison with morphine

Mark K. Greenwald, Maxine L. Stitzer

Research output: Contribution to journalArticlepeer-review

Abstract

This study compared the direct effects and acute physical dependence of butorphanol and morphine, opioids with differing actions at μ versus κ receptors. Six non-dependent heroin-using volunteers were exposed to six conditions in a within-subject, Latin square design using double-blind procedures. In each session, agonist effects of single i.m. injections of butorphanol (3 and 6 mg/70 kg), morphine (15 and 30 mg/70 kg), lorazepam (4 mg/70 kg) or saline were evaluated. Butorphanol and morphine produced effects of comparable magnitude on miosis and reports of 'any drug effect'. Volunteers reported dysphoria, confusion and sedation after butorphanol, subjective effects that overlapped with those of lorazepam, whereas morphine produced euphoria and stimulation. Acute physical dependence (i.e. precipitated withdrawal responses to naloxone 10 mg/70 kg i.m. administered 6 h after each treatment) significantly increased after 30 mg/70 kg morphine but not after butorphanol treatments. These differences in naloxone sensitivity are likely due to differences in opioid receptor (μ versus κ) activity, affinity and efficacy of these compounds. Pharmacological ramifications of these results are discussed. Copyright (C) 1998 Elsevier Science Ireland Ltd.

Original languageEnglish (US)
Pages (from-to)17-30
Number of pages14
JournalDrug and alcohol dependence
Volume53
Issue number1
DOIs
StatePublished - Dec 1 1998

Keywords

  • Butorphanol
  • Human drug abusers
  • Morphine
  • Naloxone
  • Narcotic dependence
  • Opioid withdrawal

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology
  • Psychiatry and Mental health
  • Pharmacology (medical)

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