![]() Ratio of Fluconazole Tissue (Fluid)/Plasma Concentration* † Independent of degree of meningeal inflammation. * Relative to concurrent concentrations in plasma in subjects with normal renal function. In patients with fungal meningitis, fluconazole concentrations in the CSF are approximately 80% of the corresponding plasma concentrations.Ī single oral 150 mg dose of fluconazole administered to 27 patients penetrated into vaginal tissue, resulting in tissue:plasma ratios ranging from 0.94 to 1.14 over the first 48 hours following dosing.Ī single oral 150 mg dose of fluconazole administered to 14 patients penetrated into vaginal fluid, resulting in fluid:plasma ratios ranging from 0.36 to 0.71 over the first 72 hours following dosing. In patients with bronchiectasis, sputum concentrations of fluconazole following a single 150 mg oral dose were equal to plasma concentrations at both 4 and 24 hours post dose. In normal volunteers, saliva concentrations of fluconazole were equal to or slightly greater than plasma concentrations regardless of dose, route, or duration of dosing. Following either single- or multiple oral doses for up to 14 days, fluconazole penetrates into all body fluids studied (see table below). Plasma protein binding is low (11 to 12%). ![]() The apparent volume of distribution of fluconazole approximates that of total body water. Administration of a loading dose (on day 1) of twice the usual daily dose results in plasma concentrations close to steady-state by the second day. Steady-state concentrations are reached within 5 to 10 days following oral doses of 50 to 400 mg given once daily. (SeeĪdministration of a single oral 150 mg tablet of fluconazole to ten lactating women resulted in a mean C Therefore, fluconazole may be taken without regard to meals. ![]() Maxand AUC data from a food-effect study involving administration of fluconazole tablets to healthy volunteers under fasting conditions and with a high-fat meal indicated that exposure to the drug is not affected by food. Maxof 6.72 mcg/mL (range: 4.12 to 8.08 mcg/mL) and after single oral doses of 50 to 400 mg, fluconazole plasma concentrations and AUC (area under the plasma concentration-time curve) are dose proportional. ![]() In fasted normal volunteers, administration of a single oral 400 mg dose of fluconazole leads to a mean 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 to 50 hours) after oral administration. Bioequivalence was established between the 100 mg tablet and both suspension strengths when administered as a single 200 mg dose. In normal volunteers, the bioavailability of orally administered fluconazole is over 90% compared with intravenous administration. The pharmacokinetic properties of fluconazole are similar following administration by the intravenous or oral routes. ![]()
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