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Other Topical Musculoskeletal AgentsTopical Neuropathic Pain agents
External topical analgesicAvailable over-the-counter for the temporary relief of pain from arthritis, myalgias, arthralgias, and neuralgias; prescription only patch approved for postherpetic neuralgia and diabetic neuropathy of the feetMost common adverse effect is transient skin irritation and/or paresthesias (e.g., burning, stinging, warm sensation) at the site of application; the severity of this effect appears to be dose-related
Arthricare for Women, Capzasin-HP, Capzasin-P, Castiva Warming, Zostrix
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%
Apply to affected area(s) 3 to 4 times daily; for best results use 3 to 4 times daily continuously.
Apply to affected area 3 to 4 times daily for up to 7 days; remove patch within 8 hours.
Apply to affected joints 3 to 4 times daily; for best results use 3 to 4 times daily continuously.
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.
Use up to 4 patches per application; patches should be applied for 30 minutes and repeated no more frequently than every 3 months as needed.
Apply to the affected area 2 to 4 times daily.
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.
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.
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.
Capsaicin 8% patch: up to 4 patches/treatment, wait a minimum of 3 months before repeat application. 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.
Capsaicin 0.025%, 0.075%, and 0.25%: 4 topical applications/day; capsaicin 8% patch: safety and efficacy have not been established.
10 years and older: 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 have not been established.3 to 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 have not been established.1 to 2 years: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
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.
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.
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.Administer the patch in a well ventilated area.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. It is advisable for health care professionals to utilize a face mask and protective glasses.Avoid unnecessary contact with items in the room, including items that the patient may later have contact with, such as horizontal surfaces and bedsheets.Do not hold medicated patch near eyes, nose, or mouth. Avoid application to the face, eyes, nose, or scalp to avoid exposure risk to the eyes or mucous membranes.Treatment location must be identified and marked on the skin by the treating physician. When used for diabetic neuropathy, examine the feet prior to patch application to detect skin lesions related to underlying neuropathy or vascular insufficiency.Trim capsaicin topical patch to fit the size and shape of the 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. Patches can be wrapped around the dorsal, lateral, and plantar foot surfaces of each foot to completely cover the treatment area. Use a 30-minute application time for diabetic neuropathy and a 60-minute application time for postherpetic neuralgia.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 the supplied cleansing gel. Apply gel over the entire area, leave the gel on for 1 minute, then gently remove gel with a dry wipe and wash area with mild soap and water.Thoroughly clean all areas that had contact with the patch and dispose of used and unused cleansing gel, patch(es), and other treatment materials in accordance with local biomedical waste procedures.
Topical Solution Formulations:Massage into the affected area until thoroughly absorbed.Avoid taking a bath or shower within 1 hour before or after application.
Generic:- Protect from direct sunlight- Protect from moistureArthricare for Women:- Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees FCapzasin-HP:- Store at room temperature (between 59 to 86 degrees F)Capzasin-P:- Storage information not listedCastiva Warming:- Storage information not listedQutenza:- Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees FZostrix:- Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
Capsaicin should not be used in patients who are known to be sensitive to the fruits of capsicum plants (e.g., hot peppers).
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 a bath, shower, hot tub, sauna, or strenuous exercise. Do not use capsaicin with a heating pad, hot water bottle, or other sources 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 exercise 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. Screen patients with pre-existing sensory deficits for signs of sensory deterioration or loss prior to each application of capsaicin. Reductions in sensory function have been reported following the administration of the capsaicin 8% patch. If sensory deterioration or loss is detected or pre-existing sensory deficit worsens, continued use of capsaicin treatment should be reconsidered.
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.
Adequate and well-controlled studies of capsaicin in women during pregnancy have not been conducted. Capsaicin is negligibly absorbed systemically following topical administration of the patch, and maternal use is not expected to result in fetal exposure. No malformations were observed when capsaicin was administered daily by the topical route to pregnant rats (patch) and rabbits (liquid) during the period of organogenesis at doses of up to 11 and 37 times, respectively, the maximum recommended human dose (MRHD) of the capsaicin 8% topical patch at 716 mg capsaicin per day (4 patches containing 179 mg/patch). No adverse effects were observed when the capsaicin patch was applied for 3-hours, once daily to rats during gestation and lactation at doses of up to 11 times the MRHD. The effects of capsaicin during labor and obstetric delivery are unknown.
Capsaicin is negligibly absorbed systemically by the mother following topical administration of the capsaicin patch, and breast-feeding is not expected to result in exposure of the infant to capsaicin. There are no data on the effects of capsaicin on milk production. Manufacturer recommendations for breast-feeding mothers are not available for less potent, non-prescription capsaicin formulations. Adequate studies have 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. Since 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. Avoid applying capsaicin directly to the nipple and areola to minimize potential direct exposure to the infant. Consider the developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for capsaicin and any potential adverse effects on the breastfed infant from capsaicin or from the underlying maternal condition.
Unintended exposure to capsaicin can cause severe irritation of eyes, mucous membranes, respiratory tract, and skin. Avoid mucous membrane and ocular exposure to capsaicin. Do not apply the capsaicin patch to the face, eyes, mouth, nose, or scalp. 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. Accidental exposure to the eyes and mucus membrane can occur from touching the patch or items exposed to capsaicin and then touching the eyes and mucus membranes. 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. Administration of the 8% patch should be done in a well-ventilated area. If irritation of eyes or mucous membranes occurs, remove the affected individual from the vicinity of the patch and flush eyes and mucous membranes with cool water. Inhalation of airborne capsaicin can result in coughing or sneezing. If irritation of airways occurs, remove the affected individual from the vicinity of the patch. Provide supportive medical care if shortness of breath develops. If respiratory irritation worsens or does not resolve, do not re-expose the affected health care professional or patient to the patch. If skin not intended to be treated is exposed to the patch, apply the supplied cleansing gel for 1 minute and wipe off with dry gauze. After the cleansing gel has been wiped off, wash the area with soap and water. 
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.
erythema / Early / 2.0-63.0edema / Delayed / 4.0-4.0hypertension / Early / 2.0-2.0burns / Early / 0-0.5hyperesthesia / Delayed / Incidence not knowncontact dermatitis / Delayed / Incidence not knownperipheral edema / Delayed / Incidence not knownperipheral neuropathy / Delayed / Incidence not known
maculopapular rash / Early / 6.0-6.0pruritus / Rapid / 2.0-6.0nausea / Early / 5.0-5.0infection / Delayed / 4.0-4.0vomiting / Early / 3.0-3.0headache / Early / 3.0-3.0xerosis / Delayed / 2.0-2.0cough / Delayed / 2.0-2.0throat irritation / Early / 0-1.0dizziness / Early / 0-1.0dysesthesia / Delayed / 0-1.0ecchymosis / Delayed / Incidence not knowndrug-induced body odor / Delayed / Incidence not knownskin irritation / Early / Incidence not knownparesthesias / Delayed / Incidence not knownurticaria / Rapid / Incidence not knownpharyngitis / Delayed / Incidence not knownsinusitis / Delayed / Incidence not knownnasal irritation / Early / Incidence not knownsneezing / Early / Incidence not knowndysgeusia / Early / Incidence not knownhypoesthesia / Delayed / Incidence not known
There are no drug interactions associated with Capsaicin products.
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.
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, CYP3A4Capsaicin is extensively metabolized by CYP450 isoenzymes; however, clinically significant drug interactions are not expected.
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.