Clinical Pharmacology of Opioids for Pain

  title={Clinical Pharmacology of Opioids for Pain},
  author={Charles E Inturrisi},
  journal={The Clinical Journal of Pain},
  • C. Inturrisi
  • Published 1 July 2002
  • Biology, Medicine
  • The Clinical Journal of Pain
The pharmacological effects of the opioid analgesics are derived from their complex interactions with three opioid receptor types (μ, δ, and κ; morphine is an agonist at the μ opioid receptor). These receptors are found in the periphery, at presynaptic and postsynaptic sites in the spinal cord dorsal horn, and in the brain stem, thalamus, and cortex, in what constitutes the ascending pain transmission system, as well as structures that comprise a descending inhibitory system that modulates pain… 
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Three distinct types of opioid receptors are found in the nervous system: mu, kappa, and delta. Classic clinically used opioid analgesics act primarily as agonists or partial agonists at mu
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Inhibition of Reinforcing, Hyperalgesic, and Motor Effects of Morphine by Buspirone in Rats.
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  • Biology, Psychology
    The journal of pain : official journal of the American Pain Society
  • 2017
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The presence of these metabolites should be recognized in the chronic treatment of cancer pain with morphine, especially in the presence of renal impairment, and should be considered to have an important influence on opioid responsiveness, defined as a balance between the achievement of an optimal analgesia and the occurrence of adverse effects.
Kappa–opioids produce significantly greater analgesia in women than in men
The hypothesis that women report higher pain levels or exhibit less tolerance than men for given stimulus intensities is evaluated and it is concluded that κ–opioid analgesia is greater in females than in males, probably reflecting a difference in κ-opioids–activated endogenous pain modulating circuits.
The metabolite morphine‐6‐glucuronide contributes to the analgesia produced by morphine infusion in patients with pain and normal renal function
The data suggest that morphine‐6‐glucuronide contributes to morphine analgesia in patients with normal renal function, and the role of the metabolite should be considered when morphine is used clinically.
Naloxone reversal of buprenorphine‐induced respiratory depression
  • T. Gal
  • Biology, Medicine
    Clinical pharmacology and therapeutics
  • 1989
It is indicated that high doses of naloxone are required to antagonize buprenorphine and nalOXone's limited efficacy results not from' its short duration of action but rather its relative inability to displace buprelorphine already bound to opioid receptors.
d-Methadone blocks morphine tolerance and N-methyl-D-aspartate-induced hyperalgesia.
The results support the conclusion that d-methadone affects the development of morphine tolerance and NMDA-induced hyperalgesia by virtue of its NMDA receptor antagonist activity.