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Capsaicin

Pronunciation

Pronunciation

(kap SAY sin)

Index Terms

  • Capsaicin/Menthol
  • 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 [DSC]) [contains benzyl alcohol]

Zostrix Arthritis Pain Relief: 0.025% (56.6 g) [contains benzyl alcohol]

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

Zostrix Diabetic Pain Relief: 0.025% (56.6 g) [contains benzyl alcohol, menthol 2%]

Zostrix Foot Pain Relief: 0.075% (56.6 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%]

Allevess: 0.05% (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 [DSC]) [contains menthol 5%]

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

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

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

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

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

Solaice: 0.05% (15s [DSC]) [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]
  • Allevess [OTC]
  • Captracin [DSC]
  • Capzasin-HP [OTC]
  • Capzasin-P [OTC]
  • DiabetAid Pain and Tingling Relief [OTC]
  • Flexin
  • Levatio
  • MaC Patch [DSC]
  • MenCaps [OTC]
  • Neuvaxin [DSC]
  • Qroxin [DSC]
  • Qutenza
  • Releevia
  • Releevia MC
  • RelyyT [DSC]
  • Renovo
  • Salonpas Gel-Patch Hot [OTC]
  • Salonpas Hot [OTC] [DSC]
  • Sinelee [DSC]
  • Solaice [DSC]
  • Trixaicin HP [OTC]
  • Trixaicin [OTC]
  • Zostrix Arthritis Pain Relief [OTC]
  • Zostrix Diabetic Foot Pain [OTC]
  • Zostrix Diabetic Pain Relief [OTC]
  • Zostrix Foot Pain Relief [OTC]
  • Zostrix [OTC] [DSC]
  • 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 concentrations, most fell below the limit of quantitation at 3-6 hours postapplication.

Onset of Action

OTC products (capsaicin 0.025% to 0.1%): 2 to 4 weeks of continuous therapy; Qutenza patch: 1 week after application

Half-Life Elimination

Topical patch (capsaicin 8%): 1.64 hours (Babbar 2009)

Use: Labeled Indications

Muscle/Joint pain: Temporary relief of minor aches and pain of muscles and joints associated with backache, strains, sprains, arthritis, bruises, cramps, or muscle stiffness or soreness.

Neuropathic pain: Management of neuropathic pain associated with diabetic neuropathy or postherpetic neuralgia.

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

Hypersensitivity to capsaicin, menthol, or any component of the formulation.

OTC labeling: When used for self-medication, do not use on wounds, damaged, broken, or irritated skin; do not cover with bandage; do not use in combination with external heat source (eg, heating pad).

Dosing: Adult

Muscle/joint pain: Topical:

Cream, gel, liquid, lotion: Apply thin film to affected areas 3 to 4 times daily.

Patch:

0.025%, 0.03%, 0.0375%, 0.05% (Sinelee only): Apply 1 patch to affected area for up to 8 hours (maximum: 4 patches/day); do not use for >5 consecutive days (product specific)

0.05% (Solaice only): Apply 1 patch to affected area for up to 8 hours (maximum: 4 patches/day)

Neuropathic pain: Topical: Patch (Qutenza): 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): Topical: Cream (0.075%): Apply 4 times/day (Bril 2011)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Muscle/joint pain: Topical: Patch:

0.025%, 0.03%, 0.0375%, 0.05% (Sinelee only): Children ≥12 years and Adolescents: Refer to adult dosing.

0.05% (Solaice only): Adolescents ≥16 years: Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Administration

Topical products (cream, gel, liquid, lotion): Gently rub into painful area until thoroughly absorbed. Wash hands with soap and water immediately after applying (unless hands are part of the treatment area). If applying cream to hands, wait 30 minutes before washing hands.

Topical patch: Apply patch externally to clean and dry affected area. Remove protective film prior to application. May cut patch to desired size prior to removing the film (product specific). Do not use within 1 hour prior to a bath or immediately after bathing. Do not use with a heating pad.

Topical patch (Qutenza): Patch should only be applied by a health care provider. The treatment area must be identified and marked by a physician. May cut patch to match size/shape of treatment area. If necessary, excessive hair present on and surrounding the treatment area, may be clipped (not shaved). Prior to application, the treatment area should be cleansed with mild soap and water and dried thoroughly. The treatment area and surrounding 1 to 2 cm should be anesthetized with a topical anesthetic prior to patch application; keep the local anesthetic in place until the skin is anesthetized and then remove with a dry wipe; cleanse area again with soap/water, and dry thoroughly. 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. Remove cleansing gel with a dry wipe and gently wash the area with mild soap and water and dry thoroughly. All treatment materials should be disposed of according to biomedical waste procedures.

Storage

Store at room temperature; protect from light.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

The following adverse events occurred with topical patch administration.

>10%: Local: Localized erythema (63%), local pain (42%)

1% to 10%:

Cardiovascular: Hypertension (2%; transient)

Dermatologic: Papule (6%), local dryness (2%), pruritus (2%)

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

Local: Local pruritus (6%), localized edema (4%), local swelling (2%)

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

<1% (Limited to important or life-threatening): Abnormal skin odor, application site reactions (includes bruise, dermatitis, desquamation, excoriation, hyperesthesia, inflammation, paresthesia, urticaria), burning sensation of skin, cough, dizziness, dysgeusia, headache, hypoesthesia, peripheral edema, peripheral sensory neuropathy, 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).

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

Disease-related concerns:

• Cardiovascular disease: 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 RX patch.

• Cerebrovascular disease: 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 RX 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.

• Patch: Avoid inhaling airborne material from dried residue. Remove patches gently and slowly to decrease risk of aerosolization; inhalation of airborne capsaicin may result in coughing or sneezing.

• Qutenza: If skin not intended to be treated comes in contact with capsaicin, apply provided cleansing gel for one minute and wipe off with dry gauze; then wash the area with soap and water. Post-application pain should be treated with local cooling methods (ice pack) and/or analgesics.

Other warnings/precautions:

• Appropriate use: For external use only; avoid contact with eyes, mouth, genitals, or any or other mucous membranes. Do not use immediately before or after activities such as bathing, swimming, showering, sun bathing, strenuous exercise, steam bath, sauna, or other heat or sunlight exposure to the treated area. Stop use and consult a healthcare provider if excessive redness, blistering burning or irritation develops, symptoms get worse, symptoms persist for >7 days, symptoms resolve and then recur, or if difficulty breathing or swallowing occurs. Do not handle contact lenses for 1 hour after handling, applying, or removing capsaicin (product specific).

• OTC labeling: Transient burning may occur and generally disappears after several days.

• RX labeling: Do not cover with bandage or compression. Use only on intact skin; do not use on wounds, damaged, broken, infected, sensitive or inflamed skin. Do not apply to face or scalp. Do not use concurrently with other external pain-relieving products.

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 to 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 itching, scaling, or stinging sensation. Have patient report immediately to prescriber shortness of breath, dysphagia, severe skin irritation, or severe burning or burning that does not go away (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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