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Capsaicin

Pronunciation

Pronunciation

(kap SAY sin)

Index Terms

  • NGX-4010

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Cream, topical: 0.025% (60 g)

Capzasin-HP: 0.1% (42.5 g) [contains benzyl alcohol]

Capzasin-P: 0.035% (42.5 g) [contains benzyl alcohol]

Trixaicin: 0.025% (60 g) [contains benzyl alcohol]

Trixaicin HP: 0.075% (60 g) [contains benzyl alcohol]

Zostrix: 0.025% (60 g) [contains benzyl alcohol]

Zostrix Diabetic Foot Pain: 0.075% (60 g) [contains benzyl alcohol]

Zostrix-HP: 0.075% (60 g) [contains benzyl alcohol]

Gel, topical:

Capzasin-P: 0.025% (42.5 g) [contains menthol]

Liquid, topical:

Capzasin-P: 0.15% (29.5 mL)

Lotion, topical:

DiabetAid Pain and Tingling Relief: 0.025% (120 mL)

Patch, topical:

Aflexeril MC: 0.0375% (15s) [contains menthol 5%]

Aleveer: 0.0375% (15s) [contains menthol 5%, and aloe] [DSC]

Captracin: 0.0375% (15s [DSC]) [contains menthol 5%]

Flexin: 0.0375% (15s) [contains menthol 5%]

Levatio: 0.03% (15s) [contains menthol 5%]

MaC Patch: 0.0375% (15s) [contains menthol 5%]

MenCaps: 0.0225% (15s) [contains menthol 4.5%]

Neuvaxin: 0.0375% (15s) [contains menthol 5%]

Qroxin: 0.0375% (15s) [contains menthol 5%]

Qutenza: 8% (1s, 2s) [contains metal; supplied with cleansing gel]

Releevia: 0.0375% (15s) [contains menthol 5%]

Releevia MC: 0.0375% (15s) [contains menthol 5%]

RelyyT: 0.025% (15s) [contains menthol 5%]

Renovo: 0.0375% (15s) [contains menthol 5%]

Sinelee: 0.0375%, 0.05% (15s) [contains menthol 5%]

Solaice: 0.05% (15s) [contains menthol 5%]

Salonpas Gel-Patch Hot: 0.025% (3s, 6s) [contains menthol]

Salonpas Hot: 0.025% (1s [DSC]) [contains natural rubber/natural latex in packaging]

Brand Names: U.S.

  • Aflexeryl-MC [OTC]
  • Aleveer [OTC] [DSC]
  • Captracin [DSC]
  • Capzasin-HP [OTC]
  • Capzasin-P [OTC]
  • DiabetAid Pain and Tingling Relief [OTC]
  • Flexin
  • Levatio
  • MaC Patch
  • MenCaps [OTC]
  • Neuvaxin
  • Qroxin
  • Qutenza
  • Releevia
  • Releevia MC
  • RelyyT
  • Renovo
  • Salonpas Gel-Patch Hot [OTC]
  • Salonpas Hot [OTC] [DSC]
  • Sinelee
  • Solaice
  • Trixaicin HP [OTC]
  • Trixaicin [OTC]
  • Zostrix Diabetic Foot Pain [OTC]
  • Zostrix [OTC]
  • Zostrix-HP [OTC]

Pharmacologic Category

  • Analgesic, Topical
  • Topical Skin Product
  • Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist

Pharmacology

Capsaicin, a transient receptor potential vanilloid 1 receptor (TRPV1) agonist, activates TRPV1 ligand-gated cation channels on nociceptive nerve fibers, resulting in depolarization, initiation of action potential, and pain signal transmission to the spinal cord; capsaicin exposure results in subsequent desensitization of the sensory axons and inhibition of pain transmission initiation. In arthritis, capsaicin induces release of substance P, the principal chemomediator of pain impulses from the periphery to the CNS , from peripheral sensory neurons; after repeated application, capsaicin depletes the neuron of substance P and prevents reaccumulation. The functional link between substance P and the capsaicin receptor, TRPV1, is not well understood.

Absorption

Topical patch (capsaicin 8%): Systemic absorption is transient and low (<5 ng/mL) in approximately one-third of patients when measured following 60-minute application. In patients with quantifiable levels, most fell below the limit of quantitation at 3-6 hours post application.

Half-Life Elimination

Half-life elimination: Topical patch (capsaicin 8%): 1.64 hours (Babbar, 2009)

Use: Labeled Indications

Topical patch (Qutenza): Management of postherpetic neuralgia (PHN)

OTC labeling: Temporary treatment of minor pain associated with muscles and joints due to backache, strains, sprains, bruises, cramps, or arthritis; temporary relief of pain associated with diabetic neuropathy

Use: Unlabeled

Diabetic neuropathy; treatment of pain associated with psoriasis and intractable pruritus. Potential use as topical agent in burning mouth syndrome and oral mucositis.

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Dosage

Topical:

Children ≥12 years and Adults: Pain relief: OTC labeling: Patch (Salonpas®-Hot): Apply patch to affected area up to 3-4 times/day for 7 days. Patch may remain in place for up to 8 hours.

Adults:

Pain relief: OTC labeling: Topical products (cream, gel, liquid, lotion): Apply to affected area 3-4 times/day; efficacy may be decreased if used less than 3 times/day; best results seen after 2-4 weeks of continuous use

Postherpetic neuralgia: Patch (Qutenza™ [capsaicin 8%]): Apply patch to most painful area for 60 minutes. Up to 4 patches may be applied in a single application. Treatment may be repeated ≥3 months as needed for return of pain (do not apply more frequently than every 3 months). Area should be pretreated with a topical anesthetic prior to patch application.

Diabetic neuropathy (off-label use): Cream (0.075%): Apply 4 times/day (Bril, 2011)

Administration

Topical products (cream, gel, liquid, lotion): Wear gloves to apply; wash hands with soap and water after applying to avoid spreading to eyes or other sensitive areas of the body.

Topical patch (Salonpas®-Hot): Apply patch externally to clean and dry affected area. Backing film should be removed prior to application. Do not use within 1 hour prior to a bath or immediately after bathing. Do not use with a heating pad.

Topical patch (Qutenza™[capsaicin 8%]): Patch should only be applied by a physician or by a healthcare professional under the close supervision of a physician. The treatment area must be identified and marked by a physician. The patch can be cut to match size/shape of treatment area. If necessary, excessive hair present on and surrounding the treatment area, may be clipped (not shaved) to promote adherence. Prior to application, the treatment area should be cleansed with mild soap and water and dried thoroughly. The treatment area should be anesthetized with a topical anesthetic prior to patch application. Anesthetic should be removed with a dry wipe, and area should be cleansed again with soap/water, and dried. Patch may then be applied to dry, intact skin within 2 hours of opening the patch; apply patch using nitrile gloves (latex gloves should not be used). During application, slowly peel back the release liner under the patch. Patch should remain in place for 60 minutes. Remove patches gently and slowly. Following patch removal, apply cleansing gel to the treatment area and leave in place for at least 1 minute. All treatment materials should be disposed of according to biomedical waste procedures.

Storage

DiabetAid Pain and Tingling Relief, Zostrix®, Zostrix®-HP: Store at 15°C to 30°C (59°F to 86°F).

Qutenza™: Store at room temperature between 20°C to 25°C (68°F to 77°F).

Drug Interactions

There are no known significant interactions.

Adverse Reactions

Topical patch (Qutenza™, capsaicin 8%):

>10%: Local: Erythema (63%), pain (42%)

1% to 10%:

Cardiovascular: Hypertension (2%; transient)

Dermatologic: Pruritus (2%)

Gastrointestinal: Nausea (5%), vomiting (3%)

Local: Pruritus (6%), papules (6%), edema (4%), dryness (2%), swelling (2%)

Respiratory: Nasopharyngitis (4%), sinusitis (3%), bronchitis (2%)

<1% (Limited to important or life-threatening): Application site reactions (bruising, dermatitis, excoriation, exfoliation, hyperesthesia, inflammation, paresthesia, urticaria), burning sensation, cough, dizziness, dysgeusia, headache, hypoesthesia, peripheral edema, peripheral sensory neuropathy, skin odor (abnormal), throat irritation

Warnings/Precautions

Concerns related to adverse effects:

• Burns: May cause serious burns (eg, first- to third-degree chemical burns) at the application site. In some cases, hospitalization has been required. Discontinue use and seek medical attention if signs of skin injury (eg, pain, swelling, or blistering) occur following application (FDA Drug Safety Communication, 2012).

Disease-related concerns:

• Cardiovascular disease: Qutenza: Use with caution in patients with uncontrolled hypertension or a history of cardiovascular events; transient increases in blood pressure due to treatment-related pain have occurred during and after application of patch.

• Cerebrovascular disease: Qutenza: Use with caution in patients with a history of cerebrovascular events; transient increases in blood pressure due to treatment-related pain have occurred during and after application of patch.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

• Topical patch: Qutenza: Do not apply to face, scalp, or allow contact with eyes or mucous membranes. If an unintended area of skin is inadvertently exposed, the cleansing gel should be used. Post-application pain should be treated with local cooling methods and/or analgesics (opioids may be necessary). Avoid rapid removal of patches to decrease risk of aerosolization of capsaicin; inhalation of airborne capsaicin may result in coughing or sneezing; if shortness of breath occurs, medical care is required; remove patches gently and slowly to decrease risk of aerosolization.

Other warnings/precautions:

• OTC labeling: For external use only; avoid contact with eyes or mucous membranes. Should not be applied to broken or irritated skin. Treated area should not be exposed to heat or direct sunlight. Affected area should not be bandaged. Transient burning may occur and generally disappears after several days; discontinue use if severe burning develops. Stop use and consult a healthcare provider if redness or irritation develops, symptoms get worse, or symptoms resolve and then recur.

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies with capsaicin patch or liquid. Systemic absorption is limited following topical administration of the patch; plasma concentrations are below the limit of detection 3-6 hours after the patch is removed.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience burning or stinging sensation. Have patient report immediately to prescriber dyspnea, dysphagia, severe skin irritation, significant dizziness, or syncope (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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