One-week treatment with once-daily fluorouracil cream 0.5% in participants with actinic keratoses
Baylor University Medical Center, Division of Dermatology, Dallas, TX 75246, USA.Cutis; cutaneous medicine for the practitioner (Impact Factor: 0.72). 07/2008; 81(6):509-16.
Actinic keratoses (AKs) are common in fair-skinned individuals with a history of chronic and excessive sun exposure and may progress to squamous cell carcinoma (SCC). Topical fluorouracil is an effective therapeutic option for patients with AKs, but it is associated with substantial skin irritation. The efficacy and tolerability of 1-week treatment using microsponge-based fluorouracil cream 0.5% were analyzed in 356 participants with AK lesions. One-week treatment with once-daily fluorouracil cream 0.5% was significantly more effective than vehicle control in reducing AK lesions and in achieving complete clearance (P<.001). No serious treatment-related adverse events occurred. The most frequent treatment-related adverse events were facial and eye irritations, which were predominantly mild to moderate in severity. No participants in the fluorouracil cream 0.5% treatment group discontinued the study because of treatment-related adverse events. One-week treatment with once-daily fluorouracil cream 0.5% is an effective well-tolerated therapy for AKs. Using this short treatment duration period in combination with cryosurgery may prove beneficial in clinical practice. Extending treatment for up to 4 weeks will further improve AK lesion clearance rates.
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ABSTRACT: Topical drug application is less prone to severe systemic side-effects than systemic application. Starting with the liposomes, various types of nanosized and microsized drug carriers have been developed to increase the notoriously low penetration of active agents into the skin, which limits not only the topical therapy of skin disease but also transdermal therapy. Today, liposome- and microsponge-based preparations are approved for dermatomycosis, acne and actinic keratosis. Under investigation are drug carriers such as lipid nanoparticles, polymeric particles, dendrimers, and dendritic-core multi-shell nanotransporters. According to the rapidly increasing research in this field, both in academia and industry, a breakthrough appears likely, once stability problems (nanoparticles) and safety concerns (dendrimers) are overcome. Technical approaches and results of in vitro, ex vivo and in vivo testing are described, taking into account pharmacokinetic, efficacy and safety aspects.Handbook of experimental pharmacology 01/2010; 197(197):435-68. DOI:10.1007/978-3-642-00477-3_15
Article: 5-fluorouracil for actinic keratoses[Show abstract] [Hide abstract]
ABSTRACT: Fluorouracil (FU), or 5-FU, is an antimetabolite, pyrimide analog with thymidylate synthase as its target, which alters DNA replication. It is available in 250-mg doses for systemic use, and is administered intravenously or orally as adjuvant chemotherapy in cancer treatment. Currently, 5% 5-FU cream is applied twice daily for 2--4 weeks for superficial actinic keratoses treatment. It is approved for superficial basal cell carcinoma when conventional methods are impractical, such as in cases of multiple lesions or difficult treatment sites. Despite high efficacy, irritation limits adherence. Alternatives for better tolerability are low-concentration creams (0.5, 1 and 2%) or superficial peels, with 5% 5-FU in propylenoglycol, weekly or biweekly, until the desired end point is reached. Off-label topical uses include the following: Bowen''s disease, warts, extramammary Paget''s disease, Darier''s disease, linear verrucous epidermal nevus, porokeratosis and chromoblastomycosis. Intralesional 5-FU is also used for treatment of keloids and hypertrophic scars. Studies comparing 5% 5-FU cream to new options for the treatment of actinic keratoses, such as 0.5% 5-FU cream, photodynamic therapy, 5% imiquimod cream and 3% diclofenac gel, demonstrated similar efficacy. All the listed 5-FU options have skin irritation as a side effect and low cost as a considerable advantage.Expert Review of Dermatology 03/2010; 5(2):131-139. DOI:10.1586/edm.10.13
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ABSTRACT: Actinic keratoses (AKs) are cutaneous neoplasms composed of proliferations of cytologically aberrant, epidermal keratinocytes caused by prolonged exposure to ultraviolet radiation. Combining the evidence that AKs are the second most common reason for visits to the dermatologist and it is generally believed that they should be treated, it is no surprise that the direct cost of the management of actinic keratoses in the United States (U.S.) is exceedingly high. There are currently numerous treatment modalities with more on the way as there is a demand for formulating newer, cheaper, less painful and less invasive means. The future of AK treatment involves both the continued investigation of current novel therapies, as well as the development of new treatment modalities.Journal of drugs in dermatology: JDD 05/2010; 9(5 Suppl ODAC Conf Pt 1):s45-9. · 1.45 Impact Factor
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