TRPV1 agonist
Transient receptor potential vanilloid 1 agonist
- Initial burning and nociceptor firing (topical)
- Prolonged activation desensitizes the nerve → sustained pain relief
- same receptor target as capsaicin
- May contribute to antiepileptic effect
Drugs with this mechanism (3)
- Acetaminophen — OTC analgesic/antipyretic; hepatotoxic in overdose, minimal anti-inflammatory effect.
- Cannabidiol — Purified, nonintoxicating cannabinoid for severe developmental epilepsies.
- Capsaicin — TRPV1 agonist; topical for neuropathic pain via defunctionalization.
Self-check
- How does prolonged TRPV1 activation produce sustained pain relief?
Nerve desensitization. - Which possible nonanalgesic effect is noted for TRPV1 activation?
An antiepileptic contribution.
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