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  • CLASSES

    All Other Topical Musculoskeletal Products
    Topical Neuropathic Pain agents

    DEA CLASS

    OTC

    DESCRIPTION

    External analgesic; used for the temporary relief of minor arthritis, muscle, or joint pain and for neuralgias/neurogenic pain; low-concentration OTC capsaicin is second-line agent for osteoarthritis; Rx-only 8% patch FDA-approved for postherpetic neuralgia.

    COMMON BRAND NAMES

    Arthricare for Women, Capzasin-HP, Capzasin-P, Castiva Warming, Zostrix

    HOW SUPPLIED

    Arthricare for Women/Capsaicin/Capzasin-HP/Capzasin-P/Zostrix Topical Cream: 0.025%, 0.035%, 0.075%, 0.1%, 0.25%
    Capsaicin/Castiva Warming Topical Lotion: 0.035%
    Qutenza Topical Film: 8%

    DOSAGE & INDICATIONS

    For the treatment of mild pain or moderate pain.
    For self-medication of myalgia or arthralgia associated with bruises, simple backache, sprains, or strains.
    Topical dosage (cream, lotion, or solution)
    Adults

    Apply to affected area(s) 3 to 4 times daily; for best results use 3 to 4 times daily continuously.

    Topical dosage (0.025% topical patch)
    Adults, Adolescents, and Children 12 years and Older

    Apply to affected area 3 to 4 times daily for up to 7 days; remove patch within 8 hours.

    For self-medication of pain associated with rheumatoid arthritis or osteoarthritis.
    Topical dosage (cream, lotion, or solution)
    Adults

    Apply to affected joints 3 to 4 times daily; for best results use 3 to 4 times daily continuously.

    For pain associated with postmastectomy pain syndrome†.
    Topical dosage (0.025% or 0.075% cream)
    Adults

    Fourteen patients applied capsaicin 0.025% topically 4 to 5 times per day for 4 weeks. A few patients who did not respond to the 0.025% cream were switched to 0.075% capsaicin applied 4 to 5 times per day. Of those completing the study, 8 patients were either pain free or had only mild pain. At least 50% improvement was observed in 12 of 14 patients. Burning upon initial application of capsaicin was reported to be insignificant.

    For the treatment of neuropathic pain.
    For the treatment of diabetic neuropathy, including diabetic foot pain.
    Topical dosage (Zostrix Neuropathy Cream 0.25%)
    Adults, Adolescents, and Children 10 years and Older

    Apply to the affected area 2 to 4 times daily.

    Topical dosage (0.075% products)
    Adults

    Several controlled studies have shown topical capsaicin 0.075% to be significantly more effective than vehicle cream in reducing neuropathic pain in patients with diabetic neuropathy who were unresponsive or intolerant to conventional therapy. In these studies, capsaicin 0.075% was applied topically to painful areas 4 times per day.

    For the treatment of postherpetic neuralgia (PHN).
    Topical dosage (capsaicin 8% dermal patch)

    NOTE: Do not dispense for self-administration; only health care personnel familiar with use, handling, and disposal of patch should administer.
    NOTE: Pretreat with local anesthetic to treatment area plus 1 to 2 cm of surrounding area; in clinical trials, lidocaine 4% cream was used for 60 minutes prior to patch application.
    NOTE: Ice packs and pain medications, including opioids, may be needed to treat procedure related pain.

    Adults

    Use up to 4 patches per application; patches should be applied for 60 minutes and repeated no more frequently than every 3 months as needed.

    Topical dosage (0.025% cream)
    Adults

    In 33 patients with postherpetic neuralgia, capsaicin 0.025% was applied topically to painful areas 4 to 5 times per day. Several patients (n = 10) withdrew due to intolerable burning upon initial application of capsaicin. Of 23 patients who completed the 4-week study, 56% were either pain free or had only mild neuropathic pain. Additional patients had significant but unsatisfactory improvement.

    MAXIMUM DOSAGE

    Adults

    Capsaicin 8% patch: up to 4 patches/treatment, do not repeat for >= 3 months. Solutions, lotions, and creams: 4 applications/day; the 0.025% and 0.075% concentrations have been used off-label up to 5 times/day for neuropathic pain and postmastectomy pain syndrome.

    Geriatric

    Capsaicin 8% patch: up to 4 patches/treatment, do not repeat for >= 3 months. Solutions, lotions, and creams: 4 applications/day; the 0.025% and 0.075% concentrations have been used off-label up to 5 times/day for neuropathic pain and postmastectomy pain syndrome.

    Adolescents

    Capsaicin 0.025%, 0.075%, and 0.25%: 4 topical applications/day; capsaicin 8% patch: safety and efficacy has not been established.

    Children

    >= 10 years: 4 topical applications/day of 0.25% capsaicin; 4 topical applications/day of 0.025% and 0.075% capsaicin has been suggested; safety and efficacy of capsaicin 8% patch has not been established.
    3—9 years: 4 topical applications/day of 0.025% and 0.075% capsaicin has been suggested; safety and efficacy of capsaicin 0.25% and capsaicin 8% patch has not been established.
    <= 2 years: Safety and efficacy has not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Topical Administration

    Do not apply to open wounds, infections, or irritated skin.
    Do not apply external heat or occlusive dressings to treated areas.
    Avoid contact with eyes and mucous membranes. If eye contact occurs, immediately wash out the eye with water or saline, and consult a physician if irritation persists.

    Cream/Ointment/Lotion Formulations

    Apply sparingly; rub well into the affected area until thoroughly absorbed.
    Wash hands with soap or water after applying to avoid getting into eyes or other sensitive areas of the body. However, if used on arthritic hands, do not wash hands for at least 30 minutes after application.

    Transdermal Patch Formulations

    Capsaicin low-concentration (0.025%, 0.075%, and 0.25%) transdermal patch:
    Clean and dry intended treatment area prior to patch application.
    Apply patch according to package instructions.
    Wash hands with soap or water after applying to avoid getting into eyes or other sensitive areas of the body.
     
    Capsaicin high-concentration (8%) transdermal patch:
    Do not allow patients to self-administer capsaicin 8% topical patch; administration must only be undertaken by a health care professional familiar with proper dosing, handling, and disposal of the product.
    Use nitrile gloves at all times while handling and disposing of capsaicin topical patch and while in contact with treatment area(s); do not use latex gloves as latex gloves do not provide full protection.
    Do not hold medicated patch near eyes, nose, or mouth.
    Treatment location must be identified and marked on the skin by the treating physician.
    Trim capsaicin topical patch to fit size and shape of treatment area as needed.
    Prepare skin for treatment by clipping hair (do not shave) within the area and gently washing with mild soap. Next, apply a topical anesthetic prior to patch application in an effort to reduce capsaicin-induced discomfort. Apply the anesthetic to the entire treatment area, including the 1 to 2 cm surrounding the treatment area. Once the skin is anesthetized, remove the anesthetic with a dry wipe. Wash the treatment area with mild soap and water; dry thoroughly.
    Apply the patch(es) by aligning the patch(es) with the treatment area(s), then slowly removing capsaicin release liner while smoothing patch down on to the skin.
    A dressing, such as rolled gauze, may be used to maintain patch contact with skin.
    Instruct patients to avoid touching the patch or treatment area during treatment.
    Remove patch(es) by gently rolling inward after treatment is complete.
    Clean treatment area with supplied Cleansing Gel by applying gel over entire area, leave gel on for one minute, and then gently remove with a dry wipe and wash area with mild soap and water.
    Dispose of used and unused Cleansing Gel, patch(es), and other treatment materials in accordance with local biomedical waste procedures.

    Other Topical Formulations

    Topical Solution Formulations:
    Massage into the affected area until thoroughly absorbed.
    Avoid taking a bath or shower within 1 hour before or after application.

    STORAGE

    Generic:
    - Storage information not listed
    Arthricare for Women:
    - Store at room temperature (between 59 to 86 degrees F)
    Capzasin-HP:
    - Storage information not listed
    Capzasin-P:
    - Storage information not listed
    Castiva Warming:
    - Storage information not listed
    Qutenza:
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    Zostrix:
    - Store at room temperature (between 59 to 86 degrees F)

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    Capsaicin should not be used in patients who are known to be sensitive to the fruits of capsicum plants (e.g., hot peppers).

    Heating pad, infection, inflammation, skin abrasion, strenuous exercise, sunlight (UV) exposure

    Capsaicin should not be applied to areas with skin abrasion, irritation, infection, or inflammation. Due to the potential for enhanced absorption, do not apply capsaicin within 1 hour before or after bath, shower, hot tub, sauna, or strenuous exercise. Do not use capsaicin with a heating pad, hot water bottle, or other source of heat due to increased burn risk. Do not tightly wrap or bandage the treated area. Treated areas may be sensitive to heat, including hot showers or bath, direct sunlight (UV) exposure, or vigorous excercise for a few days after treatment. If condition worsens or symptoms persist for more than 7 days, or clear up and occur again within a few days, therapy should be discontinued and a physician should be consulted. Patients should discontinue capsaicin and seek immediate medical attention if experience burning, pain, swelling, or blistering of the skin.

    Pregnancy

    Capsaicin is classified as FDA pregnancy risk category B. Adequate and well-controlled studies of capsaicin in pregnant women have not been conducted. No evidence of fetal teratogenicity was demonstrated in rats using Qutenza capsaicin patches at doses of up to 11 times the recommended human maximum dose or in rabbits using capsaicin liquid at doses of up to 37 times the recommended human maximum dose. During use of capsaicin patches in pregnant rats, there were no adverse effects observed on survival, growth, learning and memory tests, sexual maturation, mating, pregnancy, or fetal development. Because animal studies are not always predictive of human response, capsaicin topical products should be used during pregnancy only when clearly indicated. The effects of capsaicin during labor and obstetric delivery are unknown.

    Children, infants, neonates

    Generally, use of capsaicin topical cream is not recommended in children, except under the direction of a physician. The manufacturers of some over-the-counter capsaicin 0.25% products include directions for use in children as young as 10 years of age; refer to specific package directions. The safety and efficacy of capsaicin 8% topical patch has not been established in patients less than 18 years of age. Capsacian may cause skin irritation in infants and neonates, so they generally should not come in contact with the products.

    Breast-feeding

    According to the manufacturer of Qutenza (single-application 8% capsaicin patch), breast-feeding mothers can reduce infant capsaicin exposure by not breast-feeding after treatment on their treatment day as any absorbed capsaicin is rapidly eliminated from the bloodstream. During one rat study using Qutenza patches at doses up to 32 mg for 3 hours per day, measurable levels of capsaicin were observed in the milk of lactating females. Manufacturer recommendations for breast-feeding mothers are not available for less potent, non-prescription capsaicin formulations (capsaicin 0.025—0.1%). Adequate study has not been conducted in infants exposed to capsaicin, a component of cayenne peppers, via breast milk or direct administration. Adverse effects, including erythematous rash with desquamation, have been reported in nursing infants whose mothers ingested foods flavored with red pepper. Because mild to severe skin irritation may occur following topical application of capsaicin, the infant's skin should not come into direct contact with areas of the mother's skin that have been treated. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    Accidental exposure, ocular exposure

    Avoid mucous membrane and ocular exposure to capsaicin. Do not use capsaicin on the face. If capsaicin comes in contact with the eyes, rinse well with water; advise patients to seek medical help if irritation persists. Handle capsaicin products with care, using appropriate precautions to avoid accidental exposure to non-treatment areas of skin. Aerosolization of capsaicin from the 8% patch is possible if the patches are rapidly removed; take care to remove patches gently by slowly rolling the adhesive side inward. Do not dispense capsaicin 8% topical patch for self-administration; administration must be undertaken only by physicians or other health care professionals, under the supervision of the treating physician, who are familiar with the administration, handling, and disposal of the capsaicin 8% topical patch.

    Hypertension, myocardial infarction, stroke

    When treated with topical products that contain 8% capsaicin patients may experience substantial procedural pain, even after use of a local anesthetic; acute pain should be treated with local cooling and appropriate analgesic medications. During the procedure, some patients experienced an elevation in blood pressure, likely induced by pain. Patients with poorly controlled hypertension, a recent cardiovascular event (e.g., myocardial infarction), or a recent cerebrovascular event (e.g., stroke) may be at an increased risk for an adverse cardiovascular event during treatment with capsaicin 8% topical patch because of the associated transient increase in blood pressure. In clinical trials, blood pressure elevations averaged less than 10 mmHg and appeared to be related to treatment-related increases in pain and not to pretreatment blood pressure. Further, blood pressure returned to baseline within two hours of patch removal with no lasting effect measured at the 4, 8, or 12 week follow-up visits. Monitor blood pressure and manage pain during treatment.

    ADVERSE REACTIONS

    Moderate

    erythema / Early / 63.0-63.0
    edema / Delayed / 4.0-4.0
    hypertension / Early / 2.0-2.0
    burns / Early / 0-0.5
    hyperesthesia / Delayed / Incidence not known
    contact dermatitis / Delayed / Incidence not known
    peripheral edema / Delayed / Incidence not known
    peripheral neuropathy / Delayed / Incidence not known

    Mild

    pruritus / Rapid / 2.0-6.0
    maculopapular rash / Early / 6.0-6.0
    nausea / Early / 5.0-5.0
    vomiting / Early / 3.0-3.0
    xerosis / Delayed / 2.0-2.0
    cough / Delayed / 0-1.0
    throat irritation / Early / 0-1.0
    urticaria / Rapid / Incidence not known
    drug-induced body odor / Delayed / Incidence not known
    skin irritation / Early / Incidence not known
    paresthesias / Delayed / Incidence not known
    ecchymosis / Delayed / Incidence not known
    sneezing / Early / Incidence not known
    pharyngitis / Delayed / Incidence not known
    nasal irritation / Early / Incidence not known
    sinusitis / Delayed / Incidence not known
    headache / Early / Incidence not known
    dizziness / Early / Incidence not known
    dysgeusia / Early / Incidence not known
    hypoesthesia / Delayed / Incidence not known

    DRUG INTERACTIONS

    There are no drug interactions associated with Capsaicin products.

    PREGNANCY AND LACTATION

    Pregnancy

    Capsaicin is classified as FDA pregnancy risk category B. Adequate and well-controlled studies of capsaicin in pregnant women have not been conducted. No evidence of fetal teratogenicity was demonstrated in rats using Qutenza capsaicin patches at doses of up to 11 times the recommended human maximum dose or in rabbits using capsaicin liquid at doses of up to 37 times the recommended human maximum dose. During use of capsaicin patches in pregnant rats, there were no adverse effects observed on survival, growth, learning and memory tests, sexual maturation, mating, pregnancy, or fetal development. Because animal studies are not always predictive of human response, capsaicin topical products should be used during pregnancy only when clearly indicated. The effects of capsaicin during labor and obstetric delivery are unknown.

    According to the manufacturer of Qutenza (single-application 8% capsaicin patch), breast-feeding mothers can reduce infant capsaicin exposure by not breast-feeding after treatment on their treatment day as any absorbed capsaicin is rapidly eliminated from the bloodstream. During one rat study using Qutenza patches at doses up to 32 mg for 3 hours per day, measurable levels of capsaicin were observed in the milk of lactating females. Manufacturer recommendations for breast-feeding mothers are not available for less potent, non-prescription capsaicin formulations (capsaicin 0.025—0.1%). Adequate study has not been conducted in infants exposed to capsaicin, a component of cayenne peppers, via breast milk or direct administration. Adverse effects, including erythematous rash with desquamation, have been reported in nursing infants whose mothers ingested foods flavored with red pepper. Because mild to severe skin irritation may occur following topical application of capsaicin, the infant's skin should not come into direct contact with areas of the mother's skin that have been treated. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Capsaicin depletes and prevents reaccumulation of substance P in peripheral sensory neurons. Substance P is found in slow-conducting, unmyelinated type C neurons that innervate the dermis and epidermis. Substance P is thought to be the primary chemical mediator of pain impulses from the periphery to the central nervous system. It can also be released into joint tissues, where it activates inflammatory substances involved in the development of rheumatoid arthritis. By depleting substance P, capsaicin renders skin and joints insensitive to pain since local pain impulses cannot be transmitted to the brain. When capsaicin therapy is discontinued, substance P reaccumulates and neuronal sensitivity returns to normal.

    PHARMACOKINETICS

    Capsaicin is administered topically. Capsaicin binds to the TRPV1 proteins located on pain and heat neurons. Capsaicin is metabolized by CYP450 enzymes and carboxyesterase class enzymes; metabolites possess less potential at VR1 receptors.
     
    Affected cytochrome P450 isoenzymes (Capsaicin): CYP1A1, CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4
    Capsaicin is extensively metabolized by CYP450 isoenzymes; however, clinically significant drug interactions are not expected.

    Topical Route

    Following the topical application of capsaicin, systemic exposure is minimal. Application of a single capsaicin 8% topical patch resulted in low systemic exposure to capsaicin in one-third of an unstated number of studied patients; Cmax was less than 5 ng/mL in all patients and occurred at 60 minutes after patch application. The capsaicin plasma concentration of most patients was undetectable within 3 to 6 hours following patch removal. Use of a single 60 minute patch results in >= 30% relief of postherpetic neuralgia in as soon as 1 week and persisting for up to 12 weeks following application.