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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-02-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/4/778 |
| _version_ | 1797416006426034176 |
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| author | James N. Campbell Randall Stevens Peter Hanson James Connolly Diana S. Meske Man-Kyo Chung Benedict Duncan X. Lascelles |
| author_facet | James N. Campbell Randall Stevens Peter Hanson James Connolly Diana S. Meske Man-Kyo Chung Benedict Duncan X. Lascelles |
| author_sort | James N. Campbell |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-03-09T05:57:40Z |
| format | Article |
| id | doaj.art-d95a539e6a114b8abd38d751f9ad5443 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T05:57:40Z |
| publishDate | 2021-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-d95a539e6a114b8abd38d751f9ad54432023-12-03T12:12:15ZengMDPI AGMolecules1420-30492021-02-0126477810.3390/molecules26040778Injectable Capsaicin for the Management of Pain Due to OsteoarthritisJames N. Campbell0Randall Stevens1Peter Hanson2James Connolly3Diana S. Meske4Man-Kyo Chung5Benedict Duncan X. Lascelles6Centrexion Therapeutics, Boston, MA 02109, USACentrexion Therapeutics, Boston, MA 02109, USAeGenesis, Cambridge, MA 02139, USACentrexion Therapeutics, Boston, MA 02109, USACentrexion Therapeutics, Boston, MA 02109, USACenter to Advance Chronic Pain Research, Program in Neuroscience, The Department of Neural and Pain Sciences, School of Dentistry, University of Maryland, Baltimore, MD 21201, USATranslational Research in Pain (TRiP) Program, Comparative Pain Research and Education Centre, Department of Clinical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, NC 27606, USACapsaicin 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.https://www.mdpi.com/1420-3049/26/4/778intra-articularcoolingkneedefunctionalizationnociceptive fiberTRPV1 |
| spellingShingle | James N. Campbell Randall Stevens Peter Hanson James Connolly Diana S. Meske Man-Kyo Chung Benedict Duncan X. Lascelles Injectable Capsaicin for the Management of Pain Due to Osteoarthritis Molecules intra-articular cooling knee defunctionalization nociceptive fiber TRPV1 |
| 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 | intra-articular cooling knee defunctionalization nociceptive fiber TRPV1 |
| url | https://www.mdpi.com/1420-3049/26/4/778 |
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