How Do Topical TRPV1 Agonists Work?

Reviewed on 6/17/2021

HOW DO TOPICAL TRPV1 AGONISTS WORK?

Topical TRPV1 agonists (transient receptor potential cation channel subfamily V member 1) are a class of drugs used to treat minor aches and pains of the muscles and joints caused by sprains, strains, arthritis, bruises, cramps, and neuralgias. Neuralgia is a shooting or burning pain that comes from the nerves near the surface of your skin.

TRPV1 is a cation (a positively charged ion) that is activated by various exogenous and endogenous physical and chemical stimuli (high temperature, acidic conditions, and capsaicin). The activation of TRPV1 leads to a painful, burning sensation. TRPV1 agonists (capsaicin) are an active ingredient in chili peppers which make them hot.

Topical TRPV1 agonists work in the following ways:

  • TRPV1 receptor is useful to measure how an organism can sense temperature change.
  • TRPV1 agonists upon prolonged application cause TRPV1 activity to decrease (a process called desensitization), leading to alleviation of pain initially and then subsequent decrease in the pain.
  • They also help in decreasing certain natural substances (substance P) in our body responsible for passing the pain signals to the brain.
  • They help block pain messages to the nerves by decreasing the nerve cell activity, thus reducing the perception of pain.

Topical TRPV1 agonists are available in the form of creams, lotions, and gels.

HOW ARE TOPICAL TRPV1 AGONISTS USED?

TRPV1 agonists are used in conditions such as:

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WHAT ARE SIDE EFFECTS OF TOPICAL TRPV1 AGONISTS?

TRPV1 agonists can make your skin sensitive to the sun, so make sure you use sunscreen before going outdoors. Do not use them on open wounds or on sunburned, dry, chapped, or irritated skin.

Common side effects include:

  • Erythema (redness) at the application site
  • Pain at the application site
  • Nausea
  • Vomiting
  • Skin irritation
  • Dryness
  • Pruritis (itching)
  • Burning and/or stinging

Other rare side effects include:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

WHAT ARE NAMES OF TOPICAL TRPV1 AGONISTS?

Drug names include:                              

  • Axsain
  • Capsaicin topical
  • Capzasin P
  • Capzasin-HP
  • Menthac
  • No Pain-HP
  • Pain Doctor
  • Pain-X
  • Rid-A-Pain
  • Salonpas Hot
  • Trixaicin
  • Zostrix
References
https://reference.medscape.com/drugs/trpv1-agonists-topical

https://www.webmd.com/drugs/2/drug-4181/capsaicin-topical/details

https://www.webmd.com/pain-management/what-is-capsaicin

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3169333/

https://medlineplus.gov/druginfo/meds/a620055.html

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