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Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival?
Clin J Pain. 2008 Feb; 24(2):142-54.CJ

Abstract

OBJECTIVE

In this review, we explain our current understanding of the molecular basis for pain relief by capsaicin and other transient receptor potential vanilloid subfamily, member 1 (TRPV1) agonists. We summarize disease-related changes in TRPV1 expression and its implications for therapy and potential adverse effects. Last, we provide an overview of the current clinical uses of topical and injectable TRPV1 agonist preparations in both oncologic and nononcologic populations.

METHOD

Search of MEDLINE and other databases.

RESULTS

The capsaicin receptor TRPV1 is a polymodal nociceptor exhibiting a dynamic threshold of activation that could be lowered under inflammatory conditions. Consistent with this model, TRPV1 knock-out mice are devoid of post-inflammatory thermal hyperalgesia. TRPV1 desensitization of primary sensory neurons is a powerful approach to relieve symptoms of nociceptive behavior in animal models of chronic pain. However, over-the-counter capsaicin creams have shown moderate to poor analgesic efficacy. This is in part related to low dose, poor skin absorption, and compliance factors. Recently developed site-specific capsaicin therapy with high-dose patches and injectable preparations seem to be safe and reportedly provide long-lasting analgesia with rapid onset.

CONCLUSIONS

We argue that TRPV1 agonists and antagonists are not mutually exclusive but rather complimentary pharmacologic approaches for pain relief and we predict a "revival" for capsaicin and other TRPV1 agonists in the clinical management of pain associated with inflammation, metabolic imbalances (eg, diabetes), infections (HIV), and cancer, despite the current focus of the pharmaceutical industry on TRPV1 antagonists.

Authors+Show Affiliations

Department of Pain Medicine and Palliative Care, Research Division, Beth Israel Medical Center Medicine, New York, NY, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

18209521

Citation

Knotkova, Helena, et al. "Capsaicin (TRPV1 Agonist) Therapy for Pain Relief: Farewell or Revival?" The Clinical Journal of Pain, vol. 24, no. 2, 2008, pp. 142-54.
Knotkova H, Pappagallo M, Szallasi A. Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival? Clin J Pain. 2008;24(2):142-54.
Knotkova, H., Pappagallo, M., & Szallasi, A. (2008). Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival? The Clinical Journal of Pain, 24(2), 142-54. https://doi.org/10.1097/AJP.0b013e318158ed9e
Knotkova H, Pappagallo M, Szallasi A. Capsaicin (TRPV1 Agonist) Therapy for Pain Relief: Farewell or Revival. Clin J Pain. 2008;24(2):142-54. PubMed PMID: 18209521.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Capsaicin (TRPV1 Agonist) therapy for pain relief: farewell or revival? AU - Knotkova,Helena, AU - Pappagallo,Marco, AU - Szallasi,Arpad, PY - 2008/1/23/pubmed PY - 2008/3/25/medline PY - 2008/1/23/entrez SP - 142 EP - 54 JF - The Clinical journal of pain JO - Clin J Pain VL - 24 IS - 2 N2 - OBJECTIVE: In this review, we explain our current understanding of the molecular basis for pain relief by capsaicin and other transient receptor potential vanilloid subfamily, member 1 (TRPV1) agonists. We summarize disease-related changes in TRPV1 expression and its implications for therapy and potential adverse effects. Last, we provide an overview of the current clinical uses of topical and injectable TRPV1 agonist preparations in both oncologic and nononcologic populations. METHOD: Search of MEDLINE and other databases. RESULTS: The capsaicin receptor TRPV1 is a polymodal nociceptor exhibiting a dynamic threshold of activation that could be lowered under inflammatory conditions. Consistent with this model, TRPV1 knock-out mice are devoid of post-inflammatory thermal hyperalgesia. TRPV1 desensitization of primary sensory neurons is a powerful approach to relieve symptoms of nociceptive behavior in animal models of chronic pain. However, over-the-counter capsaicin creams have shown moderate to poor analgesic efficacy. This is in part related to low dose, poor skin absorption, and compliance factors. Recently developed site-specific capsaicin therapy with high-dose patches and injectable preparations seem to be safe and reportedly provide long-lasting analgesia with rapid onset. CONCLUSIONS: We argue that TRPV1 agonists and antagonists are not mutually exclusive but rather complimentary pharmacologic approaches for pain relief and we predict a "revival" for capsaicin and other TRPV1 agonists in the clinical management of pain associated with inflammation, metabolic imbalances (eg, diabetes), infections (HIV), and cancer, despite the current focus of the pharmaceutical industry on TRPV1 antagonists. SN - 0749-8047 UR - https://www.unboundmedicine.com/medline/citation/18209521/Capsaicin__TRPV1_Agonist__therapy_for_pain_relief:_farewell_or_revival L2 - https://doi.org/10.1097/AJP.0b013e318158ed9e DB - PRIME DP - Unbound Medicine ER -