Fluconazole

Fluconazole is one of the most commonly-used triazoles in clinic. Like other azoles, it is a compound composed of aromatic rings. Fluconazole is effective against Candida albicans, C. dubliniensis, C. guilliermondii, C. kefyr, C. parapsilosis, C. lusitaniae, and C. tropicalis. C. krusei is naturally resistant to fluconazole and many strains of C. glabrata are either resistant or less sensitive. Fluconazole exerts its antifungal effects by inhibiting the synthesis of ergosterol, which is an integral part of the fungal cell membrane. Development of resistance is rare, but when occurs, it is in the form of cross-resistance to all azoles. In order to predict the therapeutic effectiveness of fluconazole in an individual case; the ratios of the maximum drug concentration (Cmax) on fluconazole concentration – time curve, the area under the curve, and the time needed to reach the serum drug concentration above minimum inhibitory concentration (Ttau) to the minimum inhibitory concentration should be taken into account. Fluconazole may be administered via oral or intravenous route. Oral and intravenous pharmacokinetics of fluconazole are similar since the drug is absorbed almost completely (≥%90) from the gastrointestinal system. Fluconazole penetrates into all body fluids, including cerebrospinal fluid and human milk. Main indications include blastomycosis, candidemia, systemic candida infections, candidiasis prophylaxis in high-risk patients, coccidioidomycosis, and cryptococcosis. In clinical usage, it is thought that fluconazole will interact favorably with anidulafungin, caspofungin, amphotericin B, or flucytosine in either simultaneous or sequential usage. Concomitant administration with other drugs which act as hepatic CYP2C9 or CYP3A4 isoenzyme substrates or prolong the QT interval requires close monitoring. Although fluconazole may cause a congenital anomaly syndrome in infants born to women who have received the drug in high-doses in the first trimestre, its side effects are rare