Introduction

Professional athletes and amateurs alike experience pain associated with training and engaging in sporting competition. The cause of pain can be many things; a simple knock, perhaps a sprain or a pulled muscle or simply repetitive stress being placed on frequently used joints and muscles. Regardless of the cause, this pain can be debilitating on multiple fronts. Managing the pain becomes a priority for those who wish to continue training and competing, or simply get on with life after the game is over. For many, pain relief from sporting activities comes in the form of ingestible analgesics (Tylenol, Advil, Motrin) or topical analgesics (Icy Hot, Bengay, Mineral Ice, Tiger Balm).

In this article, we are going to look at managing pain via topical applications. We will take a look at the common ingredients found in many over-the-counter topical analgesics and discuss how they work together. We are also going dive into Cannabidiol (CBD) and why this ingredient is now being incorporated into topical balms, creams and salves designed to help people manage muscle and joint pain.

 

Menthol, Methyl Salicylate & Capsaicin

Commonly used analgesic topicals are typically made utilizing ingredients such as menthol, methyl salicylate and capsaicin.  Menthol is a compound commonly found in peppermint, eucalyptus and pennyroyal herbs. It works by activating a protein in the body known as TRPM8. This protein is a “cold-sensing” receptor that enables the body to recognize changes in temperature and alert us of these changes via the cooling sensation. It is this cooling sensation that makes menthol a popular anesthetic. Methyl salicylate is a natural compound that is found in wintergreen plants such as the Gaultheria procumbens (also known as the eastern teaberry, checkerberry, boxberry or American wintergreen).[i] In low concentration it is favored for its minty aroma. In larger quantities though it performs as an analgesic and skin irritant (used to block pain signals). Capsaicin is a compound commonly found in chili peppers and is incorporated into topical relief balms and creams because of its heating properties.

These ingredients are sometimes referred to as counter irritants because of the way they work together. Specifically, they work by causing the skin to feel a cooling sensation followed by a warming sensation. The alternating sensations are designed to help mask discomfort felt in joints and muscles after training sessions or other strenuous activities.[ii] [iii]

 

Gate Control Theory

But how does the cooling and heating of the skin relieve pain? Well, the underlying premise is that the brain cannot recognize painful inputs and non-painful inputs at the same time. When physical activity causes stress on the body, small nerve fibers send signals of pain to the brain. Counter irritants work by stimulating large nerve fibers which sense general stimulation. If the signals from the large nerve fibers end up being stronger than the signals from the small nerve fibers, then they replace the pain signal to the brain effectively controlling the gate and masking the pain.[iv]

 

CBD as a Pain Management Alternative to Counter Irritants

For a growing number of athletes and otherwise physically active adults, Cannabidiol (CBD) offers an alternative pathway for managing pain symptoms as well as inflammation via topical remedies. Unlike counter irritants referenced above, CBD topicals work by penetrating the dermal and subdermal layers of the skin.[v] They go beyond the surface to activate the body’s endocannabinoid system (ECS). The ECS is comprised of endocannabinoids and cannabinoid receptors (CB1 and CB2) and plays an important role in regulating numerous body functions including the immune system, sleep, mood, pleasure and pain.[vi] [vii]

Endocannabinoids are molecules produced within our bodies on an as needed basis and are crucial in making sure our internal functions are running smoothly. They do this by binding to the receptors in the body when our ECS is out of balance. Amongst other things, studies have shown that endocannabinoids will bind to the CB1 receptor (which is predominantly found within the central nervous system) to help inhibit the signaling of pain to the brain.[viii] They will also bind to the CB2 receptor (which is predominantly found within the peripheral tissues of the immune system) to signal that the body is experiencing inflammation.[ix]

Unlike other molecular signaling systems found within the body, the ECS does not allow for the storage of endocannabinoids. Instead, endocannabinoids are broken down by metabolic enzymes once they have been used.[x] [xi] As such, extending the benefits and effects of endocannabinoids has become an interesting subject matter for researchers and CBD enthusiasts.

 

What is CBD?

CBD is a phytocannabinoid (plant-based cannabinoid) and one of the two major chemical components found within the Cannabis sativa plant. The other major and well-known compound is delta-9-tetrahydrocannabinol (THC), which is the chemical that produces euphoric effects (the “high” effect) Unlike THC, CBD does not produce any euphoric, psychoactive effects but it has gained wide scale attention and popularity because of its potential therapeutic properties.[xii] CBD works by mimicking the effects of our endocannabinoids and interacting with the body’s cannabinoid receptors.

While CBD won’t bind to CB1 or CB2 receptors like endocannabinoids, studies suggest that the similar qualities of the 2 molecules cause the body to react as if more endocannabinoids were in operation. Amongst other things, this enables the endocannabinoids to work for longer periods of time as it takes longer for the metabolic enzymes to break down all the cannabinoids.[xiii] While there is still research to be done on the matter, it follows that CBD may play a role in supplementing the pain and inflammation fighting benefits attributed to endocannabinoids.

 

Could there be value in combining CBD with counter irritants in a topical?

While scientific research around the benefits of combining CBD with counter irritant ingredients is lacking, it is not a stretch to consider the upside of such a product. As discussed above, counter irritants mask pain by shifting the focus of irritation from one body part to another. CBD, on the other hand, has demonstrated pain and inflammation inhibiting qualities via its ability to mimic endocannabinoids that we produce within our own bodies. Neither method is reliant on the other and it would not appear that either method would inhibit the other. As such, test driving a topical that provides athletes and active adults with both pathways to pain management should be an interesting and worthwhile proposition.

 

Masking Pain Does Not Cure Injury

It is important to note that masking pain is not the same thing as curing injury or promoting healing. Neither counter irritants nor CBD are meant to fix or cure the cause of pain. But separately and/or together, they can provide a management tool for pain while the body naturally recovers from stress and pain associated with sporting activities.

 

References

[i] https://en.wikipedia.org/wiki/Gaultheria_procumbens

[ii] https://www.brainspinesurgery.com/is-icy-hot-effective-at-relieving-back-pain/

[iii] https://www.webmd.com/drugs/2/drug-61388/icy-hot-analgesic-balm-topical/details

[iv] https://www.brainspinesurgery.com/is-icy-hot-effective-at-relieving-back-pain/

[v] https://www.healthtechzone.com/topics/healthcare/articles/2020/06/17/445713-technology-behind-cbd-topicals-how-they-work.htm

[vi] https://www.tetrahealth.com.au/the-endocannabinoid-system/

[vii] https://en.wikipedia.org/wiki/Cannabinoid_receptor

[viii] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6277878/#

[ix] https://www.news-medical.net/health/Cannabinoid-Receptors.aspx#

[x] https://www.leafly.com/news/science-tech/what-is-the-endocannabinoid-system

[xi] https://www.healthline.com/health/endocannabinoid-system#how-it-works

[xii] https://myremedyproducts.com/anxiety-and-sports-performance/

[xiii] https://www.healthline.com/health/endocannabinoid-system#cbd