Topical Capsaicin Formulations in the Management of Neuropathic Pain

Author(s):  
Mark Schumacher ◽  
George Pasvankas
Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 778
Author(s):  
James N. Campbell ◽  
Randall Stevens ◽  
Peter Hanson ◽  
James Connolly ◽  
Diana S. Meske ◽  
...  

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.


2017 ◽  
Vol 2 (20;2) ◽  
pp. 27-35
Author(s):  
PyungBok Lee

Background: Topical capsaicin therapy may be of benefit in providing pain relief in patients with peripheral neuropathy. Objectives: To investigate the efficacy and safety of 0.625% (50 µg/cm2 ) and 1.25% (100 µg/cm2 ) capsaicin patches (CPs) compared to conventional 0.075% capsaicin cream or placebo patches in patients suffering from peripheral neuropathy. Study Design: Early Phase II, multi-center, randomized, semi-double-blind, and placebocontrolled clinical trial. Setting: Two medical college teaching hospitals. Methods: Sixty patients were randomized to the 0.625% CP, 1.25% CP, placebo-controlled patch, or 0.075% capsaicin cream. The primary efficacy endpoint was the mean difference in the change of daily numerical rating scale (NRS) pain score. Secondary endpoints included values for the Daily Sleep Interference Scale, the percentage of patients achieving a ≥ 30% or ≥ 50% reduction in pain, and data for Global Impression Change (GIC) and EQ-5D. Results: Patients treated with the 0.625% CP and 0.075% capsaicin cream showed statistically significant improvements in pain after 6-weeks of test drug application. Daily sleep disorder scores were improved only for those patients applying the 0.075% capsaicin cream. For patient-derived GIC scores, the majority (11 of 12) of patients in the 0.625% CP group reported that their pain was improved. For the safety evaluation, 2 severe adverse events were reported for the 0.075% capsaicin cream group only. Repetitive patch application was related to minor skin problems such as a burning sensation, erythema, pruritus, and vesicles in 28 patients (46.67%). Limitations: The small sample size and relatively high dropout rates. Conclusion: Our data indicate that the 0.625% CP may prove to be an effective and safe alternative with which to treat patients with peripheral neuropathy and could replace the high concentration (8%) CP. Further studies are now needed to definitively establish efficacy. Key words: Capsaicin, patch, CP, topical capsaicin, neuropathic pain, peripheral neuropathic pain, PNP, high concentration CP


Author(s):  
Sheena Derry ◽  
Andrew S C Rice ◽  
Peter Cole ◽  
Toni Tan ◽  
R Andrew Moore

Author(s):  
Sheena Derry ◽  
Rosalind Lloyd ◽  
R Andrew Moore ◽  
Henry J McQuay

1997 ◽  
Vol 15 (8) ◽  
pp. 2974-2980 ◽  
Author(s):  
N Ellison ◽  
C L Loprinzi ◽  
J Kugler ◽  
A K Hatfield ◽  
A Miser ◽  
...  

PURPOSE A minority of cancer survivors develops long-term postsurgical neuropathic pain. Based on evidence that capsaicin, the pungent ingredient in hot chili peppers, might be useful for treating neuropathic pain, we developed the present clinical trial. PATIENTS AND METHODS Ninety-nine assessable patients with postsurgical neuropathic pain were entered onto this study. After stratification, patients were to receive 8 weeks of a 0.075% capsaicin cream followed by 8 weeks of an identical-appearing placebo cream, or vice versa. A capsaicin/placebo cream was to be applied to the painful site four times daily. Treatment evaluation was performed by patient-completed weekly questionnaires. RESULTS During the first 8-week study period, the capsaicin-cream arm was associated with substantially more skin burning, skin redness, and coughing (P < .0001 for each). Nonetheless, treatment was stopped for patient refusal or toxicity just as often while patients were receiving the placebo as compared with the capsaicin. The capsaicin cream arm had substantially more pain relief (P = .01) after the first 8 weeks, with an average pain reduction of 53% versus 17%. On completion of the 16-week study period, patients were asked which treatment period was most beneficial. Of the responding patients, 60% chose the capsaicin arm, 18% chose the placebo arm, and 22% chose neither (P = .001). CONCLUSION A topical capsaicin cream decreases postsurgical neuropathic pain and, despite some toxicities, is preferred by patients over a placebo by a three-to-one margin among those expressing a preference.


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