{"title":"Topical fenticonazole in dermatology and gynaecology: current role in therapy.","authors":"S. Veraldi, R. Milani","doi":"10.18370/2309-4117.2018.47.78-82","DOIUrl":null,"url":null,"abstract":"Fenticonazole is an imidazole derivative with a broad spectrum of antimycotic activity against dermatophytes and yeasts in in vitro and clinical studies. Fenticonazole exerts its unique antimycotic mechanism of action in the following three ways: (i) inhibition of the secretion of protease acid by Candida albicans; (ii) damage to the cytoplasmic membrane; and (iii) by blocking cytochrome oxidases and peroxidises. Fenticonazole has also been shown to exhibit antibacterial action, with a spectrum of activity that includes bacteria commonly associated with superinfected fungal skin and vaginal infections, and antiparasitic action against the protozoan Trichomonas vaginalis. Therefore, fenticonazole may be an ideal topical alternative to multi-agent treatment of mixed infections involving mycotic, bacterial, dermatophyte and/or Trichomonas spp.Open-label clinical studies show that fenticonazole, in different pharmaceutical preparations administered once or twice daily, is effective in the treatment of superficial mycoses of the skin. In particular, fenticonazole is very effective (often with 100% of patients achieving a negative mycological assay) in pityriasis versicolor and candidiasis. For example, a large (n = 760) study showed fenticonazole 2% cream, spray or powder to be associated with a mycological response in 100% of patients with pityriasis versicolor, 96.3% of those with tinea infections and 95.2% of patients with Candida infections. Comparative clinical studies show fenticonazole once or twice daily to be at least as effective as six different topical antimycotics (miconazole, clotrimazole, econazole, bifonazole, naftifine and cyclopyroxolamine) in the treatment of superficial mycoses of the skin. Intravaginal administration of fenticonazole is associated with a high rate of microbiological efficacy in patients with vaginal candidiasis, trichomoniasis, mixed infection and bacterial vaginosis. Intravaginal fenticonazole is at least as effective as clotrimazole and shows similar efficacy to miconazole in patients with vaginal candidiasis. Fenticonazole has a rapid onset of action and clinical efficacy is generally observed within days of commencing treatment.Topical fenticonazole is very well tolerated; adverse events are generally mild to moderate in severity and transient. The most frequent adverse events are burning sensation/cutaneous irritation and itch when applied to the skin. In a large, open-label study in superficial mycoses of the skin, the incidence of adverse events was <5% and these were rarely responsible for treatment discontinuation. Burning sensation is the most common adverse event seen with fenticonazole when administered intravaginally. However, this symptom of vaginal fungal infection was often present in patients prior to drug administration.Given the rising incidence of superficial fungal, and possibly mixed, infections, topical fenticonazole represents an important part of the topical antimycotic armamentarium.","PeriodicalId":11482,"journal":{"name":"Drugs","volume":null,"pages":null},"PeriodicalIF":13.0000,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"13","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drugs","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.18370/2309-4117.2018.47.78-82","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 13
Abstract
Fenticonazole is an imidazole derivative with a broad spectrum of antimycotic activity against dermatophytes and yeasts in in vitro and clinical studies. Fenticonazole exerts its unique antimycotic mechanism of action in the following three ways: (i) inhibition of the secretion of protease acid by Candida albicans; (ii) damage to the cytoplasmic membrane; and (iii) by blocking cytochrome oxidases and peroxidises. Fenticonazole has also been shown to exhibit antibacterial action, with a spectrum of activity that includes bacteria commonly associated with superinfected fungal skin and vaginal infections, and antiparasitic action against the protozoan Trichomonas vaginalis. Therefore, fenticonazole may be an ideal topical alternative to multi-agent treatment of mixed infections involving mycotic, bacterial, dermatophyte and/or Trichomonas spp.Open-label clinical studies show that fenticonazole, in different pharmaceutical preparations administered once or twice daily, is effective in the treatment of superficial mycoses of the skin. In particular, fenticonazole is very effective (often with 100% of patients achieving a negative mycological assay) in pityriasis versicolor and candidiasis. For example, a large (n = 760) study showed fenticonazole 2% cream, spray or powder to be associated with a mycological response in 100% of patients with pityriasis versicolor, 96.3% of those with tinea infections and 95.2% of patients with Candida infections. Comparative clinical studies show fenticonazole once or twice daily to be at least as effective as six different topical antimycotics (miconazole, clotrimazole, econazole, bifonazole, naftifine and cyclopyroxolamine) in the treatment of superficial mycoses of the skin. Intravaginal administration of fenticonazole is associated with a high rate of microbiological efficacy in patients with vaginal candidiasis, trichomoniasis, mixed infection and bacterial vaginosis. Intravaginal fenticonazole is at least as effective as clotrimazole and shows similar efficacy to miconazole in patients with vaginal candidiasis. Fenticonazole has a rapid onset of action and clinical efficacy is generally observed within days of commencing treatment.Topical fenticonazole is very well tolerated; adverse events are generally mild to moderate in severity and transient. The most frequent adverse events are burning sensation/cutaneous irritation and itch when applied to the skin. In a large, open-label study in superficial mycoses of the skin, the incidence of adverse events was <5% and these were rarely responsible for treatment discontinuation. Burning sensation is the most common adverse event seen with fenticonazole when administered intravaginally. However, this symptom of vaginal fungal infection was often present in patients prior to drug administration.Given the rising incidence of superficial fungal, and possibly mixed, infections, topical fenticonazole represents an important part of the topical antimycotic armamentarium.
期刊介绍:
Drugs is a journal that aims to enhance pharmacotherapy by publishing review and original research articles on key aspects of clinical pharmacology and therapeutics. The journal includes:
Leading/current opinion articles providing an overview of contentious or emerging issues.
Definitive reviews of drugs and drug classes, and their place in disease management.
Therapy in Practice articles including recommendations for specific clinical situations.
High-quality, well designed, original clinical research.
Adis Drug Evaluations reviewing the properties and place in therapy of both newer and established drugs.
AdisInsight Reports summarising development at first global approval.
Moreover, the journal offers additional digital features such as animated abstracts, video abstracts, instructional videos, and podcasts to increase visibility and educational value. Plain language summaries accompany articles to assist readers with some knowledge of the field in understanding important medical advances.