Fluconazole Tablets

Rx Only<p>DESCRIPTION<p>Fluconazole, the first of a new subclass of synthetic triazole antifungal agents, is available as tablets for oral administration.<p>Fluconazole is designated chemically as 2,4-difluoro-α,α 1 -bis(1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol with an empirical formula of C 13 H 12 F 2 N 6 O and molecular weight 306.3. The structural formula is:<p>Fluconazole is a white crystalline solid which is slightly soluble in water and saline.<p>Fluconazole tablets contain 50, 100, 150, or 200 mg of fluconazole and the following inactive ingredients: croscarmellose sodium, dibasic calcium phosphate anhydrous, FD&C Red No. 40 aluminum lake dye, magnesium stearate, microcrystalline cellulose and povidone.<p>Structural Formula of Fluconazole<p>CLINICAL PHARMACOLOGY<p>Pharmacokinetics and Metabolism<p>The pharmacokinetic properties of fluconazole are similar following administration by the intravenous or oral routes. In normal volunteers, the bioavailability of orally administered fluconazole is over 90% compared with intravenous administration.<p>Peak plasma concentrations (C max ) in fasted normal volunteers occur between 1 and 2 hours with a terminal plasma elimination half-life of approximately 30 hours (range: 20 - 50 hours) after oral administration.<p>In fasted normal volunteers, administration of a single oral 400 mg dose of fluconazole leads to a mean C max of 6.72 μg/mL (range: 4.12 to 8.08 μg/mL) and after single oral doses of 50 - 400 mg, fluconazole plasma concentrations and AUC (area under the plasma concentration-time curve) are dose proportional.<p>Administration of a single oral 150 mg tablet of fluconazole to ten lactating women resulted in a mean C max of 2.61 μg/mL (range: 1.57 to 3.65 μg/mL).<p>Steady-state concentrations are reached within 5...