• Magazine
    • Past Issues
    • Subscribe
    • Change Mailing Address
    • Surveys
    • Guidelines for Authors
    • Editorial Calendar
    • Editorial Deadlines
  • Practice
    • Business Tips
    • Chiropractic Schools
    • Clinical & Technique
    • eBooks
    • eCourses
    • Infographics
    • Quizzes
    • Wellness & Nutrition
    • Personal Growth
    • Podcast
  • Resource Centers
  • Products & Services
    • Buyer’s Guide
    • Products Directory
    • Submit a Product
    • Vendor Login
  • Datebook
    • Become an Events Poster
    • Post an Event
    • View Events
  • Jobs
    • Jobs
    • Post a Job
  • Advertise
    • Advertising Information
    • Media Kit
    • Contact Us
    • Upload Advertising

Your Online Chiropractic Community

Chiropractic Economics Your Online Chiropractic Community
Subscribe
  • Home
  • Current Issue
  • News
  • Webinars
  • Chiropractic Research
  • Students
  • Coronavirus (COVID-19)

How topical analgesics provide immediate relief via mechanisms of action

Tina Beychok June 9, 2020

Topical analgesics with menthol and capsaicin have been used since ancient times to relieve pain, and are effective for a wide range of sports injuries...

Topical analgesics with menthol and capsaicin have been used since ancient times to relieve pain, and are effective for a wide range of sports injuries, osteoarthritis, and neuropathic pain

Given the increasing concern about the opioid crisis, the leading edge research in analgesics is focused on topicals. Topical analgesics are not only less invasive than oral analgesics for certain pain conditions, so have a greatly reduced risk of addiction, but are more effective at targeting localized pain.

With this shift toward the use of topical analgesics at the site of pain, understanding both their mechanisms of action and the importance of penetration depth becomes more important.

Types of topicals

Topical analgesics come in a variety of formulations, including creams, foams, gels, lotions, patches, sprays, or ointments. Although different types of analgesics have different properties, the general concept is to relieve pain directly at the affected site.

Menthol and capsaicin, which are two of the most common active ingredients in topical analgesics, have been used since ancient times to relieve pain. While they work along different routes, both have been shown very effective for treating both acute and chronic pain. Two separate reviews, which examined the results from other studies, found that topical analgesics containing either menthol or capsaicin were effective for a wide range of uses, including sports injuries, osteoarthritis, or neuropathic pain.1,2

Mechanisms of action

Menthol: Menthol is the active volatile oil extract from the mint (genus Mentha) plant. It acts on the transient receptor potential melastatin‐8 (TRPM8) ion-channel receptor by producing a cooling sensation on the skin at the affected site.2 Furthermore, menthol works as a local vasodilator to increase its analgesic effectiveness.

TRPM8 is the primary thermoreceptor for cellular and behavioral response to a variety of temperatures, ranging from pleasant to painful. TRPM8 is rather unique in that it is sensitive enough to provide mild to moderate cooling, but not extreme cold, which may produce a burning sensation.2 Because of this, TRPM8 is often referred to as the menthol regulator.

Capsaicin: Capsaicin is the active ingredient in chili peppers that produces the sensation of heat.3,4 As part of a topical analgesic, capsaicin reduces pain and hypersensitivity by desensitizing the affected area by repeated application.

This unique mechanism of action works by stimulating the transient receptor potential vanilloid-1 (TRPV1), which initially produces a burning pain sensation, followed by a warming sensation to help relieve pain. Depending upon the individual patient, it may take several applications for the affected area to become desensitized to the capsaicin.

Topical analgesic penetration

Topical analgesics are localized, meaning that they are formulated to reduce pain at the skin’s surface. In comparison, transdermal analgesics, such as opioid patches are meant to deliver the analgesic through the skin to the peripheral nervous system.

However, both menthol and capsaicin topical analgesics do penetrate just below the surface of the skin to maximize their effectiveness. Recent research has shown that a 3% menthol solution can increase the penetration effectiveness for topical analgesics containing ibuprofen.5 There is also ongoing research into the use of topical patches containing an analgesic with 8% capsaicin.4 The patches may provide greater pain relief for a longer period of time than creams with a lower percentage of capsaicin.

The main benefit of topical analgesics that use either menthol or capsaicin is that they will provide immediate, effective pain relief directly at the affected site. Additionally, there is less risk of side effects that often come from systemic analgesics. All of this is good news, both for you and your patients.

References

  1. Derry S, Wiffen PJ, Kalso EA, et al. Topical analgesics for acute and chronic pain in adults – an overview of Cochrane Reviews. Cochrane Database of Systematic Reviews. 2017;5(5):CD008609.
  2. Pergolizzi JV Jr, Taylor R Jr, LeQuang JA, et al. The role and mechanism of action of menthol in topical analgesic products. Journal of Clinical Pharmacy and Therapeutics. 2018;43(3):313-319.
  3. Wang XR, Gao SQ, Niu XQ, et al. Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation. International Journal of Nanomedicine. 2017;12:3881-3898.
  4. Peppin JF, Pappagallo M. Capsaicinoids in the treatment of neuropathic pain: A review. Therapeutic Advances in Neurologic Disorders. 2014;7(1):22-32.
  5. Brain KR, Green DM, Dykes PJ, Marks R, Bola TS. The role of menthol in skin penetration from topical formulations of ibuprofen 5% in vivo. Skin Pharmacology & Physiology. 2006;19(1):17-21.

Related Posts

  • Can a topical analgesic replace opioids for pain?Can a topical analgesic replace opioids for pain?
  • Menthol for chronic pain reliefMenthol for chronic pain relief
  • All natural topical botanical helps provide universal pain reliefAll natural topical botanical helps provide universal pain relief
  • Topical vs. oral NSAIDs for joint and arthritis painTopical vs. oral NSAIDs for joint and arthritis pain
  • CBD creams and topicals for back painCBD creams and topicals for back pain
  • You should be recommending topicals for knee painYou should be recommending topicals for knee pain

Filed Under: Resource Center, Soft Tissue Pain Therapy

Current Issue

Follow Us

  • Facebook
  • Twitter
  • Instagram
  • LinkedIn
  • YouTube logoYouTube logoYouTube

820 A1A N Highway W18,

Ponte Vedra Beach, FL 32082

Phone 904.285.6020

Fax 904.395.9118

CONTACT US »

Privacy Policy & Terms of Service

Copyright © 2021, All Rights Reserved

SUBSCRIBE TO THE MAGAZINE

Get Chiropractic Economics magazine
delivered to your home or office. Just
fill out our form to request your FREE
subscription for 20 issues a year,
including two annual Buyers Guides.

SUBSCRIBE NOW »

Latest Chiropractic News

  • Troy Healthcare debuts clinically-validated topical migraine and headache formula
  • Colorado allows chiropractors to give COVID-19 vaccine shots
  • American Chiropractic Association lauds U.S. Congress passing fair competition health legislation
    The American Chiropractic Association (ACA) lauded the U.S. Congress for passing legislation that will promote fair competition in health...