Chapter 13. Antifungal Agents

Abstract

This chapter presents an overview of some reviews that focus on antifungal agents. A review of pharmacokinetics of antifungal therapy included data on several systemic antifungals. Griseofulvin and clotrimazole were reviewed relative to their mechanism of action. Two reviews cover chemotherapy of mycoses, including most clinically useful antifungal agents, and hamycin, 5-fluorocytosine and clotrimazoles. Experimental dermatophyte infections in man are reviewed but therapeutic discussions are limited to griseofulvin and sodium omadine. A review related to problems in therapy and diagnosis of systemic candidiasis covers therapeutic evaluation of amphotericin B, 5-fluorocytosine, and clotrimazole. Side effects of intravenous amphotericin B therapy were evaluated; fever, chills, weakness, nausea, and nephrotoxicity were the prime consistent toxic manifestations. A series of 5,7-difluoro, dichloro, dibromo and diiodo quinolines, and 8 amino auinolhnes were prepared and tested for antifungal activity. The 5,7-difluoro derivative of quinoline was most active, while other halo derivatives were less active. Eight nitro quinolines showed greater activity than quinoline but halo substituted 8 nitro quinolines other than fluoro were less active. Amongst 8-aminoquinolines, all halo analogs were less active than the parent compounds.