capsaicin topical

Action and Spectrum

Actions and Spectrum: 

Capsaicin activates C-fibers which transmit pain signals to the brain by reducing pain perception. It also inhibits cytokine production thus reduces swelling and inflammation. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Pain (42%) 

Application site erythema (63%) 

1-10% 

Nausea (5%) 

Dryness (2%) 

Swelling (2%) 

Vomiting (3%) 

Hypertension (2%) 

Pruritus (6%) 

Sinusitis (3%) 

Bronchitis (2%) 

Papules (6%) 

Edema (4%) 

<1% 

Dizziness 

Exfoliation 

Skin Odor 

Cough 

Dysgeusia 

Headache 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications include hypersensitivity and irritated skin. 

Pregnancy / Lactation

Pregnancy consideration:  

Category B. 

Breastfeeding warnings:  

No data is available regarding the excretion of drugs in breast milk. Do not apply the topical product on the areola or nipple. 

Pregnancy category: 

• Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Pharmacodynamics: 

Capsaicin modulates neurotransmitter release by affecting pain perception and CGRP release and inhibits inflammatory cytokines and mediators. 

Pharmacokinetics: 

Absorption 

capsaicin absorbed through skin after topical application. The absorption rate may vary depending on factors like concentration of capsaicin in the formulation, area of application, and the integrity of the skin barrier. Distribution 

 It has a high affinity for nerve endings where it exerts its analgesic effects by interacting with sensory neurons.  

Metabolism 

Metabolized by the enzyme cytochrome P450 2C9. 

Elimination and Excretion  

Metabolites are eliminated through renal excretion.  

Adminstartion

Administration: 

Clean affected area, wear gloves, apply thin layer, avoid eye contact, follow instructions, follow dose recommendations, wash hands, and be patient as this process takes time. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: capsaicin topical 

Pronounced: kap-SAY-sin-TOP-i-kal 

Why do we use capsaicin topical? 

Capsaicin activates VR1 receptors on sensory nerve endings providing pain relief for musculoskeletal conditions by reducing joint pain and improves mobility with enhancing comfort.