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Updated: Feb 23, 2026

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
07:23

Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities

Published on: July 29, 2014

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Pharmacokinetics of Morphine in Rats with Adjuvant-induced Arthritis

Yoshiaki Kimura1,2, Mika Shibata1, Mika Tamada1

  • 1Faculty of Pharmacy, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kanazawa, Japan.

In Vivo (Athens, Greece)
|September 9, 2017
PubMed

Insights

In chronic inflammation models, morphine

Area of Science:

  • Pharmacology
  • Pharmacokinetics
  • Pain Management

Background:

  • Morphine, an opioid analgesic, is metabolized via glucuronidation by UDP-glucuronosyltransferase (UGT).
  • Chronic inflammation, such as adjuvant-induced arthritis (AA) in rats, can alter drug metabolism and efficacy.
  • ATP-binding cassette, sub-family B (MDR/TAP), member 1 (ABCB1) is involved in morphine excretion.

Purpose of the Study:

  • To investigate the in vivo pharmacokinetics and pharmacodynamics of morphine in an adjuvant-induced arthritis (AA) rat model.
  • To determine the impact of chronic inflammation on morphine metabolism and analgesic effects.

Main Methods:

  • Adjuvant-induced arthritis (AA) rat model was used to simulate chronic inflammation.
  • UGT activity, serum fractions, ABCB1 expression, and blood concentrations of morphine and its metabolite were analyzed.
  • The analgesic effect of morphine was assessed in AA rats compared to controls.

Main Results:

  • UGT activity and ABCB1 expression were reduced in AA rats.
  • Despite no significant changes in blood morphine concentrations, the analgesic effect of morphine increased 4-fold in AA rats.
  • Morphine-free serum fractions were decreased in AA rats.

Conclusions:

  • Chronic inflammation in AA rats alters morphine pharmacokinetics, specifically reducing UGT activity and ABCB1 expression.
  • The pharmacokinetics of morphine remain unchanged, but its pharmacodynamics (analgesic effect) are significantly enhanced in chronic inflammation.
  • These findings suggest a potential for increased morphine efficacy in inflammatory conditions, warranting further investigation into the underlying mechanisms.
Keywords:
ABCB1MorphineUDP-glucuronosyltransferaseadjuvant-induced arthritisinflammation

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