ABSTRACT
Miconazole (Mycatin, Monistat) is a phenethyl imidazole derivative that was synthesized in 1969 (Godefroi et al., 1969). It is practically insoluble in water and needs to be solubilized in polyethoxylated castor oil (1% Cremophor EL) and ethanol (10%) for intravenous (i.v.) administration. In vitro, miconazole is effective against dermatophytes, yeasts, and some molds as well as Gram-positive cocci and bacilli. Miconazole is considered the only azole with fungicidal activity (Thevissen et al. 2007; Vazquez and Sobel, 2012). Although it has a wide antifungal spectrum of activity in vitro, the toxicity associated with its use, limited therapeutic efficacy, and the lack of comparative trials limit its use as a systemic antifungal agent. In 1978, miconazole was marketed as an i.v. preparation for certain systemic fungal illnesses; its therapeutic role, however, was limited, and this formulation was ultimately withdrawn from the market (Terrell, 1999). Hence miconazole is primarily used topically to treat superficial fungal infections, including candidal vulvovaginitis and superficial dermatophyte infections. A new oral formulation (dissolvable miconazole buccal tablets) was recently approved by the US Food and Drug Administration (FDA) for the treatment of oropharyngeal candidiasis (Package Insert, 2010).
