capsaicin, Capzasin-HP, Capzasin-P, DiabetAid Pain and Tingling Relief, Qutenza, Salonpas Hot, Zostrix Diabetic Foot Pain, Zostrix, Zostrix-HP

 Indications

Temporary management of pain due to rheumatoid arthritis

and osteoarthritis. Treatment of pain associated

with postherpetic neuralgia (topical and transdermal)

or diabetic neuropathy. Unlabeled Use: Treatment

of postmastectomy pain syndrome. Treatment of complex

regional pain syndrome.

Action

Topical: May deplete and prevent the reaccumulation

of a chemical (substance P) responsible for transmitting

painful impulses from peripheral sites to the CNS.

Transdermal: Initially stimulates the transient receptor

potential vanilloid 1 (TRPV1) receptors on nociceptive

nerve fibers in the skin; this is followed by pain relief

thought to be due to a reduction in TRPV1–

expressing nociceptive nerve endings. Therapeutic

Effects: Relief of discomfort associated with painful

peripheral syndromes.

Pharmacokinetics

Absorption: Unknown.

Distribution: Unknown.

Metabolism and Excretion: Unknown.

Half-life: Unknown. 

TIME/ACTION PROFILE

ROUTE ONSET PEAK DURATION

topical 1–2 wk 2–4 wk† unknown

transdermal unknown unknown unknown

†May take up to 6 wk for head and neck neuralgias.

Contraindications/Precautions

Contraindicated in: Hypersensitivity to capsaicin

or hot peppers; Not for use near eyes or on open or

broken skin.

Use Cautiously in: OB, Lactation: Safety not established;

Pedi: Safety not established in children 18 yr

(transdermal) or 2 yr (topical).

Adverse Reactions/Side Effects

CV: Patch—qBP. Resp: cough. Derm: pain (after

application of patch), transient burning.

Interactions

Drug-Drug: None significant.

Route/Dosage

Topical (Adults and Children 2 yr): Apply to affected

areas 3–4 times daily.

Transdermal (Adults): Apply up to 4 patches for 60

min (single use); may be repeated q 3 mo, as needed

based on pain (should not be used more frequently

than q 3 mo).

Availability (generic available)

Cream: 0.1%OTC, 0.025%OTC, 0.035%OTC, 0.075%OTC.

Gel: 0.025%OTC. Lotion: 0.025%OTC. Topical liquid:

0.15%OTC. Transdermal patch (Qutenza): 0.025%/

patch, 8% (179 mg)/patch. In combination with:

methylsalicylate (ZiksOTC). See Appendix B.