Cargando…

Injectable Capsaicin for the Management of Pain Due to Osteoarthritis

Capsaicin is a potent agonist of the TRPV1 channel, a transduction channel that is highly expressed in nociceptive fibers (pain fibers) throughout the peripheral nervous system. Given the importance of TRPV1 as one of several transduction channels in nociceptive fibers, much research has been focuse...

Descripción completa

Detalles Bibliográficos
Autores principales: Campbell, James N., Stevens, Randall, Hanson, Peter, Connolly, James, Meske, Diana S., Chung, Man-Kyo, Lascelles, Benedict Duncan X.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7913147/
https://www.ncbi.nlm.nih.gov/pubmed/33546181
http://dx.doi.org/10.3390/molecules26040778
_version_ 1783656738433531904
author Campbell, James N.
Stevens, Randall
Hanson, Peter
Connolly, James
Meske, Diana S.
Chung, Man-Kyo
Lascelles, Benedict Duncan X.
author_facet Campbell, James N.
Stevens, Randall
Hanson, Peter
Connolly, James
Meske, Diana S.
Chung, Man-Kyo
Lascelles, Benedict Duncan X.
author_sort Campbell, James N.
collection PubMed
description Capsaicin is a potent agonist of the TRPV1 channel, a transduction channel that is highly expressed in nociceptive fibers (pain fibers) throughout the peripheral nervous system. Given the importance of TRPV1 as one of several transduction channels in nociceptive fibers, much research has been focused on the potential therapeutic benefits of using TRPV1 antagonists for the management of pain. However, an antagonist has two limitations. First, an antagonist in principle generally only affects one receptor. Secondly, most antagonists must have an ongoing presence on the receptor to have an effect. Capsaicin overcomes both liabilities by disrupting peripheral terminals of nociceptive fibers that express TRPV1, and thereby affects all of the potential means of activating that pain fiber (not just TRPV1 function). This disruptive effect is dependent on the dose and can occur within minutes. Thus, unlike a typical receptor antagonist, continued bioavailability at the level of the receptor is not necessary. By disrupting the entire terminal of the TRPV1-expressing nociceptive fiber, capsaicin blocks all the activation mechanisms within that fiber, and not just TRPV1 function. Topical capsaicin, an FDA approved treatment for neuropathic pain, addresses pain from abnormal nociceptor activity in the superficial layers of the skin. Effects after a single administration are evident over a period of weeks to months, but in time are fully reversible. This review focuses on the rationale for using capsaicin by injection for painful conditions such as osteoarthritis (OA) and provides an update on studies completed to date.
format Online
Article
Text
id pubmed-7913147
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-79131472021-02-28 Injectable Capsaicin for the Management of Pain Due to Osteoarthritis Campbell, James N. Stevens, Randall Hanson, Peter Connolly, James Meske, Diana S. Chung, Man-Kyo Lascelles, Benedict Duncan X. Molecules Review Capsaicin is a potent agonist of the TRPV1 channel, a transduction channel that is highly expressed in nociceptive fibers (pain fibers) throughout the peripheral nervous system. Given the importance of TRPV1 as one of several transduction channels in nociceptive fibers, much research has been focused on the potential therapeutic benefits of using TRPV1 antagonists for the management of pain. However, an antagonist has two limitations. First, an antagonist in principle generally only affects one receptor. Secondly, most antagonists must have an ongoing presence on the receptor to have an effect. Capsaicin overcomes both liabilities by disrupting peripheral terminals of nociceptive fibers that express TRPV1, and thereby affects all of the potential means of activating that pain fiber (not just TRPV1 function). This disruptive effect is dependent on the dose and can occur within minutes. Thus, unlike a typical receptor antagonist, continued bioavailability at the level of the receptor is not necessary. By disrupting the entire terminal of the TRPV1-expressing nociceptive fiber, capsaicin blocks all the activation mechanisms within that fiber, and not just TRPV1 function. Topical capsaicin, an FDA approved treatment for neuropathic pain, addresses pain from abnormal nociceptor activity in the superficial layers of the skin. Effects after a single administration are evident over a period of weeks to months, but in time are fully reversible. This review focuses on the rationale for using capsaicin by injection for painful conditions such as osteoarthritis (OA) and provides an update on studies completed to date. MDPI 2021-02-03 /pmc/articles/PMC7913147/ /pubmed/33546181 http://dx.doi.org/10.3390/molecules26040778 Text en © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Campbell, James N.
Stevens, Randall
Hanson, Peter
Connolly, James
Meske, Diana S.
Chung, Man-Kyo
Lascelles, Benedict Duncan X.
Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
title Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
title_full Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
title_fullStr Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
title_full_unstemmed Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
title_short Injectable Capsaicin for the Management of Pain Due to Osteoarthritis
title_sort injectable capsaicin for the management of pain due to osteoarthritis
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7913147/
https://www.ncbi.nlm.nih.gov/pubmed/33546181
http://dx.doi.org/10.3390/molecules26040778
work_keys_str_mv AT campbelljamesn injectablecapsaicinforthemanagementofpainduetoosteoarthritis
AT stevensrandall injectablecapsaicinforthemanagementofpainduetoosteoarthritis
AT hansonpeter injectablecapsaicinforthemanagementofpainduetoosteoarthritis
AT connollyjames injectablecapsaicinforthemanagementofpainduetoosteoarthritis
AT meskedianas injectablecapsaicinforthemanagementofpainduetoosteoarthritis
AT chungmankyo injectablecapsaicinforthemanagementofpainduetoosteoarthritis
AT lascellesbenedictduncanx injectablecapsaicinforthemanagementofpainduetoosteoarthritis