Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance

Objective – An analysis of the basic science and clinical publications found in PubMed, Medline, and Web of Science. The search covered modern laboratory and clinical mechanisms of peripheral mu opioid analgesia, the role of peripheral mu receptors in systemic analgesia and the development of tolera...

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Main Author: Yu. A. Kolesnikov
Format: Article
Language:Russian
Published: New Terra Publishing House 2020-03-01
Series:Вестник анестезиологии и реаниматологии
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Online Access:https://www.vair-journal.com/jour/article/view/398
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author Yu. A. Kolesnikov
author_facet Yu. A. Kolesnikov
author_sort Yu. A. Kolesnikov
collection DOAJ
description Objective – An analysis of the basic science and clinical publications found in PubMed, Medline, and Web of Science. The search covered modern laboratory and clinical mechanisms of peripheral mu opioid analgesia, the role of peripheral mu receptors in systemic analgesia and the development of tolerance to the analgesic effect of opioids. The review discusses the regulatory mechanisms of synthesis and transport of mu-opioid receptors in the primary afferent neurons and the molecular mechanisms responsible for modulating the conduction of nociceptive information from the periphery to the spinal cord. According to some authors, the peripheral component can account for 50-90% of the total analgesic effect after the systemic administration of morphine and methadone. The review reports on the important role of glycoprotein-P and the blood-brain barrier transport system in modulating the peripheral component of the analgesic effect of morphine as well as the synergistic interaction between central and peripheral mu receptors. The results of the reviewed studies convincingly show the key role of peripheral mu receptors in the development of tolerance to the analgesic effect of morphine after its systemic administration. The mechanisms of opioid tolerance also involve peripheral anti-opioid, pronociceptive systems such as NMDA receptors. It is well known that the same mechanisms are involved in maintaining peripheral hyperalgesia and allodynia. The development of analgesic drugs that act on peripheral antinociceptive systems offers a promising perspective on the possible treatment of acute and chronic pain.
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spelling doaj-art-3dd44f9c368a487f8661b99930aa05fc2025-08-20T03:18:55ZrusNew Terra Publishing HouseВестник анестезиологии и реаниматологии2078-56582541-86532020-03-0117192010.21292/2078-5658-2020-16-1-9-20360Сentral and peripheral mechanisms of mu-opioid analgesia and toleranceYu. A. Kolesnikov0Medical Center Medicum, Pain DepartmentObjective – An analysis of the basic science and clinical publications found in PubMed, Medline, and Web of Science. The search covered modern laboratory and clinical mechanisms of peripheral mu opioid analgesia, the role of peripheral mu receptors in systemic analgesia and the development of tolerance to the analgesic effect of opioids. The review discusses the regulatory mechanisms of synthesis and transport of mu-opioid receptors in the primary afferent neurons and the molecular mechanisms responsible for modulating the conduction of nociceptive information from the periphery to the spinal cord. According to some authors, the peripheral component can account for 50-90% of the total analgesic effect after the systemic administration of morphine and methadone. The review reports on the important role of glycoprotein-P and the blood-brain barrier transport system in modulating the peripheral component of the analgesic effect of morphine as well as the synergistic interaction between central and peripheral mu receptors. The results of the reviewed studies convincingly show the key role of peripheral mu receptors in the development of tolerance to the analgesic effect of morphine after its systemic administration. The mechanisms of opioid tolerance also involve peripheral anti-opioid, pronociceptive systems such as NMDA receptors. It is well known that the same mechanisms are involved in maintaining peripheral hyperalgesia and allodynia. The development of analgesic drugs that act on peripheral antinociceptive systems offers a promising perspective on the possible treatment of acute and chronic pain.https://www.vair-journal.com/jour/article/view/398peripheral mu receptorsperipheral analgesiamorphinemethadoneopioid tolerancetopical
spellingShingle Yu. A. Kolesnikov
Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance
Вестник анестезиологии и реаниматологии
peripheral mu receptors
peripheral analgesia
morphine
methadone
opioid tolerance
topical
title Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance
title_full Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance
title_fullStr Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance
title_full_unstemmed Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance
title_short Сentral and peripheral mechanisms of mu-opioid analgesia and tolerance
title_sort сentral and peripheral mechanisms of mu opioid analgesia and tolerance
topic peripheral mu receptors
peripheral analgesia
morphine
methadone
opioid tolerance
topical
url https://www.vair-journal.com/jour/article/view/398
work_keys_str_mv AT yuakolesnikov sentralandperipheralmechanismsofmuopioidanalgesiaandtolerance