Pharmacology of peripheral opioid receptors

Curr Opin Anaesthesiol. 2011 Aug;24(4):408-13. doi: 10.1097/ACO.0b013e32834873e5.


Purpose of review: Since the detection of morphine by the pharmacologist Friedrich Sertürner in 1806, opioids have been used as potent centrally acting analgesics. In addition to the central site of action, peripheral endogenous opioid analgesic systems have been extensively studied, especially in the past two decades. This review is not only mentioned to give a brief summary in this well investigated field of peripheral opioid receptors, but also to highlight the role of peripheral opioid receptors in other physiological and pathophysiological conditions.

Recent findings: A number of studies, which initially focused on nociception, also revealed an important role of the peripheral opioid receptor system in opioid-induced bowel dysfunction and pruritus, as well as in wound healing, cardioprotection, and the analgesic effects of celecoxib.

Summary: Efforts continue to develop opioid analgesics unable to cross the blood-brain barrier, which act only peripherally in low doses, thus providing adequate analgesia without central and systemic side-effects.The awareness of the influence of peripheral opioid receptors beyond nociception may also have therapeutic ramifications on the other fields mentioned above. For example, the treatment of opioid-induced bowel dysfunction by methylnaltrexone is one of the major findings in the previous years.

Publication types

  • Review

MeSH terms

  • Analgesics / pharmacology
  • Analgesics, Opioid / adverse effects
  • Animals
  • Celecoxib
  • Constipation / chemically induced
  • Humans
  • Pain Perception
  • Pruritus / chemically induced
  • Pyrazoles / pharmacology
  • Receptors, Opioid / physiology*
  • Sulfonamides / pharmacology
  • Wound Healing


  • Analgesics
  • Analgesics, Opioid
  • Pyrazoles
  • Receptors, Opioid
  • Sulfonamides
  • Celecoxib