Naloxone Reversal of Opioid-Induced Respiratory Depression With Special Emphasis on the Partial agonist/antagonist Buprenorphine

Adv Exp Med Biol. 2008;605:486-91. doi: 10.1007/978-0-387-73693-8_85.

Abstract

Buprenorphine is relatively resistant to reversal by naloxone. We tested the effect of various doses and infusion schemes of naloxone on buprenorphine-induced respiratory depression and compared the data with naloxone-reversal of morphine and alfentanil-induced respiratory depression. Both morphine and alfentanil were easily reversed by low doses of naloxone (0.4 mg). Increasing doses of naloxone caused a bell-shaped reversal curve of buprenorphine with maximal reversal at naloxone doses between 2 and 4 mg. However, reversal was short-lived. The bell-shaped reversal curve may be related to the existence of two mu-opioid receptor subtypes, one mediating the agonist effects of opioids at low dose, the other mediating antagonistic effects at high dose.

MeSH terms

  • Alfentanil / pharmacology
  • Analgesics, Opioid / pharmacology
  • Animals
  • Buprenorphine / pharmacology*
  • Dose-Response Relationship, Drug
  • Fentanyl / pharmacology*
  • Humans
  • Morphine / pharmacology
  • Naloxone / pharmacology*
  • Rats
  • Respiratory Mechanics / drug effects
  • Respiratory Mechanics / physiology*

Substances

  • Analgesics, Opioid
  • Alfentanil
  • Naloxone
  • Buprenorphine
  • Morphine
  • Fentanyl