Topical antimycotics

Because of their limited, activity, small spectmm, and side effects, the older topical antimycotics have generally been surpassed by newer antimycotic chemotherapeutic agents. These newer antimycotics for topical use iaclude the imida2ole derivatives clotrimazole, miconazole, econazole, isoconazole, sulconazole, fenticonazole, oxiconazole, bifonazole, butoconazole, ziaoconazole, tioconazole, and the triazole derivative, terconazole (Table 2) (5—7). The iatroduction of the azole derivatives represents a milestone ia the treatment of mycoses. 

Fig. 3. Developmental topical antimycotics. Butocona2ole (11), oxicona2ole (12), omocona2ole (13), and sulcona2ole (14).

Management Besides measures as boiling or disinfecting clothes, topical antimycotic therapy is the treatment of choice. Ointments should be applied several centimeters beyond the border of the lesion and treatment should be continued over at least 1 week after clearance of the lesions. However, these recommendations are seldom followed, resulting in chronic or recurrent disease (apart from the problem of resistance). In these cases, and when multilocular lesions or an infection of extensive spread have to be treated, systemic antifun-gals usually for 1-2 weeks are necessary, terbinafine usually giving the best results in dermatophytosis. 

Management Topical antimycotic therapy is sufficient for skin infection, whereas systemic infection demands systemic therapy with amphotericin B and/or fluconazole. 

A patient with a contact allergic reaction to a topical antimycotic drug formulation that contained benzoyl alcohol had positive patch tests on day 4 and a positive repeated open application test to benzoyl alcohol 5% in petroleum jelly (3). 

Podda M, Zollner T, Grundmann-Kollmann M, Kaufmann R, Boehncke WH. Allergic contact dermatitis from benzyl alcohol during topical antimycotic treatment. Contact Dermatitis 1999 41(5) 302-3. 

There were positive patch tests to diethyl sebacate (10 and 30% in ether and 1 and 10% in petrolatum) in a 48-year-old woman who had been using a topical antimycotic ointment (1). 

Ibrahim SA, Hafez E, El-Shanawany SM, et al. Eormulation and evaluation of some topical antimycotics. Part 3. Effect of promoters on the in vitro and in vivo efficacy of clotrimazole ointment. Bull Pharm Sci Assiut XJniv 1991 14(1-2) 82-94. Swafford SK, Bergmann WR, Migliorese KG, et al. Characterization of swollen micelles containing linoleic acid in a microemulsion system. / Soc Cosmet Chem 1991 42 235-247. 

In addition to topical antimycotic therapy, systemic NSAIDs and topical atropine sulfate are used to the control pain and ameliorate the effects of anterior segment injury associated with the iridocyclitis that inevitably accompanies ker-atomycosis. Topical proteinase inhibitor therapy is of significant clinical benefit in controlling stromal breakdown and, since potentially pathogenic bacteria contaminate most mycotic lesions, concurrent broad-spectrum, topical antibacterial agents should be used. 

Developmental Topical Antimycotics. Most of the topical antimycotics still being developed are azole derivatives (mostly imidazole), including butoconazole, oxiconazole, omoconazole, zinoconazole, and sulconazole (Fig. 3). Generally speaking, these newer azoles offer no additional therapeutic advantages compared to existing substances. These drugs are already available in certain countries, but are not yet commercialized on a worldwide scale. 

Van Hecke E (1969) Contact allergy to the topical antimycotic fluoro-4-dichloro-3,5 -thio-carbanilid. Dermatologica 138 480-482... 

Uses Expectorant counterirritant scabicide rubefacient topical antimycotic used to treat fungus infections such as athlete s foot antiseptic for cuts natural flavoring agent in foods and pharmaceuticals Regulatory FDA 21CFR 172.510 FEMA GRAS Japan approved... 

Formaldehyde aqua contains 37-40% formaldehyde gas by weight, usually with 10-15% methanol added to prevent polymerization. It is a well-known sensitizer, but also a local irritant in low concentrations (Glass 1961). Employed chiefly as a disinfectant, it has also been used as a topical antimycotic, as a treatment... 

Tom LW (2000) Ototoxicity of common topical antimycotic preparations. Laryngoscope 110 (4) 509-516. doi 10.1097/00005537-200004000-00003 van Ruijven MW, de Groot J, Klis S, Smoorenburg G (2005) The cochlear targets of cisplatin an electrophysiological and morphological time-sequence study. Hear Res 205(l-2) 241-248. doi 10.1016/j.heares.2005.03.023... 

Fig. 1. Structural Evolution from Clotrimazole (I, topical antimycotic) to Agricultural Fungicides (F) and Oral Antimycotics (M) (Reproduced with permission from ref. 26. The preparation was assisted by Masanori Yoshida).

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