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Capsaicin

Medically reviewed by Drugs.com. Last updated on May 30, 2020.

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:

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

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

Capzix: 0.1% (56.6 g) [contains benzyl alcohol, cetyl alcohol]

Sure Result SR Relief: 0.025% (118 mL)

Zostrix HP: 0.1% (56.6 g) [contains benzyl alcohol]

Zostrix Natural Pain Relief: 0.033% (56.6 g) [contains benzyl alcohol]

Generic: 0.025% (25 g, 50 g, 60 g, 120 g); 0.1% (42.5 g)

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:

Allevess: 0.05% (15s) [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%] [DSC]

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

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

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

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

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

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

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

Salonpas Hot: 0.025% (3s) [contains natural rubber/natural latex in packaging]

Generic: 0.0225% (15s); 0.025% (10s)

Brand Names: U.S.

  • Allevess [OTC]
  • Capzasin-HP [OTC]
  • Capzasin-P [OTC]
  • Capzix [OTC]
  • DiabetAid Pain and Tingling Relief [OTC]
  • Flexin
  • Levatio
  • MaC Patch [DSC]
  • MenCaps [OTC]
  • Qutenza
  • Releevia MC [DSC]
  • Releevia [DSC]
  • Renovo
  • Salonpas Gel-Patch Hot [OTC]
  • Salonpas Hot [OTC]
  • Sinelee [DSC]
  • Sure Result SR Relief [OTC]
  • Zostrix HP [OTC]
  • Zostrix Natural Pain Relief [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 to 6 hours post application.

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 pains of muscles and joints associated with simple backache, muscle strains, sprains, arthritis, bruises, or cramps.

Neuropathic pain (8% patch): Management of neuropathic pain associated with postherpetic neuralgia and diabetic peripheral neuropathy of the feet in adults.

Off Label Uses

Burning mouth syndrome (topical)

Data from a prospective, double-blinded, placebo-controlled, randomized cross-over study in patients with burning mouth syndrome suggests that capsaicin 0.02% oral rinse (unavailable in the US) may be beneficial for the treatment of this condition (Silvestre 2012). In addition, data from a limited number of patients studied (single case report) suggest that topical capsaicin (Tabasco sauce diluted in water), may be beneficial for the treatment of burning mouth syndrome (Spice 2004). Data from a prospective, triple-blind, randomized, placebo-controlled study demonstrated that the use of systemic capsaicin 0.25% capsules (unavailable in the US) is effective for the short-term treatment of burning mouth syndrome but significant gastrointestinal side effects were seen (Petruzzi, 2004). Because of the side effects seen with systemic capsaicin, some authors do not recommend the use of capsaicin for this condition. Instead, other treatments are recommended (eg, topical clonazepam) (Minquez Serra 2007). Additional data may be necessary to further define the role of capsaicin in treatment of burning mouth syndrome. Optimal dosing has yet to be established.

Diabetic neuropathy

Based on the American Academy of Neurology, the American Association of Neuromuscular and Electrodiagnostic Medicine, and the American Academy of Physical Medicine and Rehabilitation guidelines for the treatment of painful diabetic neuropathy, capsaicin 0.075% given for diabetic neuropathy is probably effective and recommended in the management of this condition.

Pain associated with psoriasis and intractable pruritus

Data from two double-blind randomized clinical trials in patients with pruritic psoriasis suggest that capsaicin cream may be beneficial for the treatment of pain associated with psoriasis and intractable pruritus (Bernstein, 1986; Ellis, 1993). Additional trials may be necessary to further define the role of capsaicin in this condition.

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, irritated skin, or into skin folds; do not cover with bandage; do not apply within 1 hour before or after bath, shower, hot tub, or sauna; do not use in combination with external heat source (eg, heating pad); do not use concurrently with other topical analgesics.

Dosing: Adult

Diabetic neuropathy: Topical:

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

Patch (Qutenza): Apply patch to most painful areas of the feet for 30 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.

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%: Apply 1 patch to affected area for up to 8 hours (maximum: 4 patches/day); do not use for >5 consecutive days (product specific).

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.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Muscle ache and joint pain, minor: Topical:

Lotion 0.025% (DiabetAid Tingling and Pain Relief) Children ≥2 years and Adolescents: Topical: Apply to affected area not more than 3 to 4 times/day

Patch: Note: With OTC products, approved ages and uses may vary; consult product specific labeling.

Product strength <0.05%: Adolescents ≥12 years: Topical:

Flexin (0.0375%): Apply 1 patch to affected area; may change 2 to 3 times/day; maximum daily dose: 3 patches/day

Levatio (0.03%): Apply 1 patch to affected area for up to 8 hours; change patch 1 to 2 times daily; maximum daily dose: 4 patches/day; do not use for >5 consecutive days

MaC (0.0375%): Apply 1 patch to affected area for up to 8 hours; change patch 2 to 3 times/day; maximum daily dose: 4 patches/24 hours

MenCaps (0.0225%): Apply 1 patch to affected area for up to 8 hours; may change patch up to 3 times daily

Releevia MC (0.0375%), Renovo (0.0375%): Apply 1 patch to affected area; may change patch 1 to 2 times daily; maximum daily dose: 3 patches/day

Salonpas Pain Relieving Hot Patch (0.025%): Apply 1 patch to affected area for up to 8 hours; may change patch up to 3 to 4 times daily

Product strength 0.05%: Adolescents ≥16 years: Topical: Allevess patch: Apply 1 patch to affected area; may change patch 1 to 2 times daily

Administration

Topical products (cream, gel, liquid, lotion): Avoid contact with eyes and mucous membranes. 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:

≤0.05% products: 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.

8% product (Qutenza): Patch should only be applied by a health care provider in a well-ventilated area. The treatment area must be identified and marked by the health care provider. May cut patch (prior to removing the protective release liner) 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. Keep patch in sealed pouch until immediately before use; patch may then be applied to dry, intact skin using nitrile gloves (latex gloves should not be used). Use of a face mask and protective glasses are also recommended during application. During administration, avoid unnecessary contact with items in room (eg, items patient may later have contact with, including bedsheets, horizontal surfaces). If applying to feet, examine feet to detect skin lesions prior to patch application. During application, slowly peel back the release liner under the patch and use other hand to smooth patch onto skin. If applying to feet, patch may be wrapped around the dorsal, lateral, and plantar surfaces of each foot to completely cover treatment area. Patch should remain in place for 30 minutes if applying to feet or 60 minutes for all other areas; to ensure patch remains on treatment area, a dressing (eg, rolled gauze) may be used. Remove patches gently and slowly by rolling adhesive side inward. 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. Clean all areas that came in contact with patch; all treatment materials (including used and unused cut patches, associated packaging, cleansing gel, gloves, other 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 drug reactions and incidences are derived from product labeling unless otherwise specified. The following adverse events occurred with topical patch administration.

>10%:

Local: Application site burning (14%), application site erythema (2% to 63%), application site pain (10% to 42%)

Neuromuscular & skeletal: Limb pain (11%)

1% to 10%:

Cardiovascular: Hypertension (2%)

Dermatologic: Excoriation of skin (2%), local dryness of skin (application site: 2%), papule of skin (application site: 6%), pruritus (2%)

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

Local: Application site edema (2% to 4%), application site pruritus (6%)

Nervous system: Headache (3%)

Respiratory: Bronchitis (2%), cough (2%), nasopharyngitis (4%), sinusitis (3%), upper respiratory tract infection (4%)

<1%:

Cardiovascular: Palpitations, tachycardia

Dermatologic: Skin blister

Local: Application site reaction (includes dermatitis, hyperesthesia, paresthesia, urticaria)

Nervous system: Dizziness, dysesthesia

Ophthalmic: Eye pruritus

Postmarketing:

Dermatologic: Cicatrix of skin

Nervous system: Abnormal sensory symptoms

Ophthalmic: Eye irritation, eye pain

Respiratory: Throat irritation

Miscellaneous: Accidental injury, burn (second degree)

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, driving).

• Irritation (8% patch): Severe irritation to the eyes, mucous membranes, respiratory tract, or skin may occur due to unintended capsaicin exposure. If irritation of the eyes or mucous membranes occurs, remove the individual from the area of the capsaicin patch and flush eyes and mucous membranes with cool water. If respiratory tract irritation (eg, coughing, sneezing) occurs, remove the individual from the area of the capsaicin patch and provide supportive care if shortness of breath develops. If skin not intended to be treated is exposed to the patch, apply cleansing gel for 1 minute and remove with dry gauze; after cleansing gel has been removed, wash the area with soap and water; postapplication pain should be treated with local cooling methods (ice pack) and/or analgesics. Clean all areas that had contact with capsaicin.

• Sensory function reduction (8% patch): Decreased sensory function, including to thermal and other harmful stimuli, has been reported; effects are usually minor and temporary. Patients with preexisting sensory deficits should be assessed for sensory deterioration or loss prior to each patch application. Continued use should be reevaluated for new onset or worsening of existing sensory deficits.

Disease-related concerns:

• Cardiovascular disease: Use the 8% patch with caution in patients with uncontrolled hypertension or a history of cardiovascular events; transient increases in BP due to treatment-related pain have occurred during and after application. Monitor BP periodically during and following treatment.

• Cerebrovascular disease: Use the 8% patch with caution in patients with a history of cerebrovascular events; transient increases in BP due to treatment-related pain have occurred during and after application of RX patch. Monitor BP periodically during and following treatment.

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 suggest 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 (8%): 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.

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, sunbathing, strenuous exercise, steam bath, sauna, or other heat or sunlight exposure to the treated area. Stop use and consult a health care 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.

Monitoring Parameters

8% patch: BP periodically during and following treatment; sensory deficits.

Pregnancy Considerations

Systemic absorption is limited following topical administration of the patch, and fetal exposure is not expected following maternal use; plasma concentrations are below the limit of detection 3 to 6 hours after the patch is removed.

Patient Education

What is this drug used for?

• It is used to ease muscle and joint aches and pain.

• It is used to help diabetic nerve pain.

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Skin irritation

• Burning or stinging feeling

• Application site pain

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Severe headache

• Severe dizziness

• Passing out

• Vision changes

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.