
Zostrix® cream 0.025% & 0.075%
Capsaicin, the active component derived from the fruit of capsicum, is used to relieve pain, improve circulation, to treat cluster headaches and psoriasis, and for weight loss. Capsicum or cayenne pepper, a shrub prevalent in many tropical and subtropical climates, is an important ingredient of many cuisines around the world. It has been used in traditional medical systems as a remedy for digestive and circulatory problems, poor appetite, and to relieve muscle and arthritic pain. Capsaicin is marketed in capsule form and as an ingredient in topical creams. A prescription-strength dermal capsaicin product, approved by the FDA, is available for the management of postherpetic neuralgia.
Capsaicin is thought to reduce pain sensation by temporarily depleting a neurotransmitter, substance P, which relays pain signals to the brain.
Studies support benefits of topical capsaicin for psoriasis (5), prurigo nodularis (6), pruritis ani (15), of intranasal application for rhinitis (16) and for cluster headaches (8). A dermal capsaicin patch was shown safe and effective for the treatment of postherpetic neuralgia (24).
Intravesical capsaicin injections were shown to induce diuresis (7). A small study found improved hair growth with a combination of capsaicin and isoflavone in healthy volunteers with alopecia (18).
Capsaicin cream did not relieve HIV-associated distal symmetrical peripheral neuropathy (2) and a review of studies of capsaicin for neuropathic pain associated with HIV, diabetes, and mastectomy concluded that available data are limited to enable full assessment of its benefits (19). Its utility for arthritic pain also remains inconclusive (3) (4).
Capsaicin, originally thought by some to be a carcinogen, was shown to be safe in animal studies (10). Interestingly, it demonstrated chemopreventive (17) and antiproliferative (26) effects against prostate cancer cells. A case report of a patient with prostate cancer suggests that capsaicin may slow doubling time of prostate specific antigen (PSA) (25). Data also suggest that capsaicin cream can effectively control post-surgical pain in cancer patients (1).
Cayenne peppers
Capsaicin is believed to cause depolarization of C-fiber polymodal nociceptors (11) (12) thereby releasing substance P, which is a neurotransmitter that relays pain signals to the brain. The sensation of pain actually increases upon application of capsaicin due to release of substance P, but subsides when its levels are depleted at the afferent neurons (13). Effective use of capsaicin requires topical application 4 or 5 times daily for a period of at least 4 weeks (2).
Capsaicin was also found to induce coronary vasodilation by releasing calcitonin gene-related peptide (CGRP), a potent vasodilator. Depletion in CGRP leads to subsequent increase in blood pressure (22).
Studies on various cancer cell lines have shown that capsaicin demonstrates chemopreventive properties by causing cell cycle arrest, inducing apoptosis (20) or by generating reactive oxygen species and depolarizing mitochondrial membranes (21). Orally administered capsaicin significantly slowed the growth of PC-3 prostate cancer cells in mice not only by down-regulating expression of androgen receptor, but also by a direct inhibitory effect on prostate specific antigen (PSA) transcription (26).
Capsaicin is absorbed through the skin and mucous membranes.
Because capsaicin can irritate mucous membranes and eyes, it should not be applied to broken skin and the eyes. The use of gloves is recommended for topical application.
Common (topical): Burning, urticaria, and contact dermatitis (9).
Case Reports:
Increased arterial blood pressure and acute myocardial infarction were reported in a 59-year-old man with high levels of thyroid stimulating hormone following ingestion of large amounts of chilli peppers (22).
Coronary vasospasm and acute myocardial infarction were observed in a 29-year-old man following use of a topical capsaicin patch for 6 days. Improvement was seen after treating the symptoms and removal of the patch (23).
Capsaicin preparations may interact with the following:
ACE inhibitors: Capsaicin can increase the incidence of cough that is associated with ACE inhibitors.
Sedatives: Capsaicin may increase sedation.
Theophylline: Concurrent administration with capsaicin may increase absorption.
(14)
Antihypertensives: Capsaicin may affect their actions (22).
Bottom Line: Capsaicin is effective in the treatment of psoriasis, rhinitis, and cluster headaches. The evidence is limited on its ability to relieve neuropathic pain.
Capsaicin is the pungent ingredient in hot chilli or cayenne peppers. Of the various uses for capsaicin, its topical use to treat pain has been studied most extensively. When applied to the skin, capsaicin is absorbed and is thought to block pain fibers by preventing the transmission of pain signals to the brain. This effect does not occur immediately, and requires repeated applications four or five times daily for a period of at least four weeks to be effective.
Capsaicin was originally thought to induce tumors, however studies in mice have shown that this is not the case. It was found to have chemopreventive properties, but this has to be verified in humans.
Capsaicin, when used topically to treat pain, usually takes about four weeks involving four to five applications a day to start working.