Antimycotic drugs

Griseofulvin is the first antimycotic drug detected that is only active against dermatophytes. Its activity manifests as nuclear and mitotic abnormalities followed by distortions in the hyphal motphology. 

Aleksic et al. [47] estimated the hydrophobicity of miconazole and other antimycotic drugs by a planar chromatographic method. The retention behavior of the drugs have been determined by TLC by using the binary mobile phases acetone-n-hexane, methanol toluene, and methyl ethyl ketone toluene containing different amounts of organic modifier. Hydrophobicity was established from the linear relationships between the solute RM values and the concentration of organic modifier. Calculated values of RMO and CO were considered for application in quantitative structure activity relationship studies of the antimycotics. 

FIGURE 13.10 Generic setup for (a) on-line SPE-HPLC implemented with a simple valve-switching system (G. Maio, R. Morello, F. Arnold, and K.-S. Boos, Analysis of Antimycotic Drugs in Biofluids by On-Line SPE-LC Application note LPN 1859-01 06/06 Diones Corporation, Sunnyvale, CA 94088-3603 Figure 2, p. 1, 2006. With permission.) and for (b) on-line SPE-GC implemented with a large volume injector with a solvent venting option. 

Resistance Resistance can develop during therapy and is the reason that flucytosine is not used as a single antimycotic drug except for chromoblastomycosis. The rate of emergence of resistant fungal cells is lower with the combination of amphotericin B and flucytosine than it is with flucytosine alone. Decreased levels of any of the enzymes in the conversion of 5-FC to 5-FU and beyond, or increased synthesis of cytosine, can confer resistance. 

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). 

Di Pietra, A.M. Cavrini, V. Andrisano, V Gatti, R. HPLC analysis of imidazole antimycotic drugs in pharmaceutical formulations. J.Pharm.Biomed.Anal., 1992, 10, 873-879... 

Viudes A, Peman J, Canton E, et al The activity of combinations of systemic antimycotic drugs. Rev Esp... 

Ajoene was also studied for short-term therapy of Tinea pedis. The use of ajoene as a 0.4% (w/w) cream resulted in complete clinical and mycological cure in 27 of 34 patients (79%) after 7 days of treatment. The remaining seven patients (21%) achieved complete cure after seven additional days of treatment. All patients were evaluated for recurrence of mycotic infections 90 days after the end of treatment, yielding negative cultures for fungus. These results show that ajoene is an alternative, efficient and low-cost antimycotic drug for short-term therapy of Tinea pedis [97]. 

Back DJ, Tjia JF. Comparative effects of the antimycotic drugs ketoconazole, fluconazole, itraconazole and terbinafine on the metabolism of cyclosporin by human Uver microsomes. BrJ Clin Pharmacol (1991) 32, 624-6. 

Undecylenic acid is known as an antimycotic agent. Cross-reactions were reported to occur with zinc undecylenate (another antimycotic drug) (Gelfarb and Leiden i960). Patch-test concentrations are 2-5% pet. Allergic reactions are considered rare. 

Flucytosine, or 5-fluorocytosine, is a synthetic antimycotic drug discovered in 1957. 

Thoma, K. Kiibler, N. Untersuchung der Photostabilitat von Antimykotika. 1. Mitt. Photostabilitat von Azolantimykotika [Photodegradation of antimycotic drugs. Part 1 Photodegradation of azole antimycotics], Pharrnazie, 1996, 51, 885-892. 

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