Description

Simple

A medication used to relieve pain in the muscles and joints.

Clinical

A topical analgesic agent used for the symptomatic relief of neuropathic pain associated with post-herpetic neuralgia, as well as other muscle and joint pain.

Overview

Capsaicin is most often used as a topical analgesic and exists in many formulations of cream, liquid, and patch preparations of various strengths; however, it may also be found in some dietary supplements. Capsaicin is a naturally-occurring botanical irritant in chili peppers, synthetically derived for pharmaceutical formulations. The most recent capsaicin FDA approval was Qutenza, an 8% capsaicin patch dermal-delivery system, indicated for neuropathic pain associated with post-herpetic neuralgia.

Pharmacology

Indication

The capsaicin 8% patch is indicated in the treatment of neuropathic pain associated with post-herpetic neuralgia. There are multiple topical capsaicin formulations available, including creams and solutions, indicated for temporary analgesia in muscle and join pain as well as neuropathic pain.

Pharmacodynamic

Capsaicin is a TRPV1 receptor agonist. TRPV1 is a trans-membrane receptor-ion channel complex activated by temperatures higher than 43 degrees Celsius, pH lower than 6, and endogenous lipids. When activated by a combination of these factors, the channel can transiently open and initiate depolarizati... Read more

Mechanism of action

Capsaicin has been shown to reduce the amount of substance P associated with inflammation - however this is not believed to be its main mechanism in the relief of pain [ Read more

Absorption

**Oral**: Following oral administration, capsaicin may be absorbed by a nonactive process from the stomach and whole intestine with an extent of absorption ranging between 50 and 90%, depending on the animal [ Read more

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Following oral ingestion of equipotent dose of 26.6 mg of pure capsaicin, the half life was approximately 24.9 ± 5.0 min [ Read more

Route of elimination

It is proposed that capsaicin mainly undergoes renal excretion, as both the unchanged and glucuronide form. A small fraction of unchanged compound is excreted in the feces and urine. _In vivo_ animal studies demonstrates that less than 10 % of an administered dose was found in faces after 48 h [ Read more

Toxicity

Acute oral LD50 and dermal LD50 in mouse are 47.2 mg/kg and >512 mg/kg, respectively [MSDS]. Capsaicin is shown to be mutagenic for bacteria and yeast [MSDS].

Capsaicin can cause serious irritation, conjunctivitis and lacrimation via contact with eyes. It induces a burning sensation and pain in c... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Supraventricular arrhythmia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Central Line Infection US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Central Line Infection US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Neutropenia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Central Line Infection US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Neutropenia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Neutropenia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Supraventricular arrhythmia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Neutropenia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Supraventricular arrhythmia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Supraventricular arrhythmia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Central Line Infection US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Central Line Infection US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Neutropenia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial
    Supraventricular arrhythmia US
  • Kind: experimental
    • Percent: 6%
  • Clinical Trial

    Contraindications

    Information currently not available.

    Food Interactions

    Information currently not available.