Nalbuphine coadministered with morphine prevents tolerance and dependence

Anesth Analg. 1997 Apr;84(4):810-5. doi: 10.1097/00000539-199704000-00021.

Abstract

Nalbuphine, an opioid mixed agonist-antagonist, prevents many morphine-related side effects. In this study, we compared the effects of nalbuphine versus naloxone on the prevention of morphine tolerance and dependence in Sprague-Dawley rats. Group 1 received a morphine 5 mg/kg intraperitoneal (I.P.) injection. Groups 2 and 3 received single doses of nalbuphine (0.01 to 5 mg/kg I.P.) or naloxone (1 to 500 microg/kg I.P.) coadministered with morphine (5 mg/kg I.P.), respectively. Group 4 received a saline I.P. injection. Treatments were continued for 4 days. The occurrence of tolerance was estimated by comparing the antinociceptive effect of morphine on Day 1 (Group 1) and Day 5 (each group). The severity of dependence was determined by precipitated withdrawal signs (incidence of diarrhea and teeth chattering) induced by naloxone (10 mg/kg I.P.). We found that coadministration of nalbuphine or naloxone with morphine dose-dependently blocked the development of morphine tolerance and dependence. However, unlike naloxone, nalbuphine did not attenuate the antinociceptive effect of morphine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • Analgesics, Opioid / administration & dosage*
  • Animals
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Drug Tolerance
  • Male
  • Morphine / administration & dosage*
  • Nalbuphine / administration & dosage*
  • Naloxone / administration & dosage
  • Naltrexone / analogs & derivatives
  • Naltrexone / pharmacology
  • Narcotic Antagonists / administration & dosage*
  • Opioid-Related Disorders / prevention & control*
  • Pyrrolidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Analgesics, Opioid
  • Narcotic Antagonists
  • Pyrrolidines
  • Naloxone
  • Naltrexone
  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • beta-funaltrexamine
  • Morphine
  • Nalbuphine