Pharmacokinetics and Metabolism of Diflucan
The pharmacokinetic homes of fluconazole are equivalent subsequent administration by the or oral routes. In usual volunteers, the bioavailability of orally administered fluconazole is around ninety% in comparison with intravenous administration. Bioequivalence was established amongst the a hundred mg tablet and the two suspension strengths when administered as a single two hundred mg dose.
Peak plasma concentrations (Cmax) in fasted normal volunteers take place amongst 1 and two hrs with a terminal plasma elimination 50 %-daily life of about thirty several hours (selection: 20-fifty hours) following oral administration.
Before usageContinuous-state concentrations are achieved inside of five-ten days subsequent oral doses of fifty-400 mg presented after day-to-day. Administration of a loading dose (on day 1) of 2 times the usual every day dose benefits in plasma concentrations close to continual-state by the second day. The obvious quantity of distribution of fluconazole approximates that of somme human body h2o. Plasma protein binding is minimal (eleven-12%). Subsequent either single- or numerous oral doses for up to 14 days, fluconazole penetrates into all entire body fluids studied (see table under). In standard volunteers, saliva concentrations of fluconazole were equal to or slightly better than plasma concentrations irregardless of dose, route, or length of dosing. In patients with bronchiectasis, sputum concentrations of fluconazole following a simple 150 mg oral dose had been equal to plasma concentrations at each 4 and 24 several hours submit dose. In clients with fungal meningitis, fluconazole concentrations in the CSF are somewhere around 80% of the corresponding plasma concentrations.
A simple oral one hundred fifty mg dose of fluconazole administered to 27 clients penetrated into vaginal tissue, resulting in tissue:plasma ratios ranging from .94 to one.14 above the initially forty eight hours subsequent dosing.
A single oral one hundred fifty mg dose of fluconazole administered to 14 sufferers penetrated into vaginal fluid, resulting in fluid:plasma ratios ranging from .36 to .71 about the initially 72 several hours subsequent dosing.
Tissue or Fluid Ratio of Fluconazole Tissue (Fluid)/Plasma Concentration* Cerebrospinal fluid .5-.nine Saliva 1 Sputum one Blister fluid one Urine 10 Typical skin ten Nails one Blister pores and skin two Vaginal tissue one Vaginal fluid .4-.seven * Relative to concurrent concentrations in plasma in topics with usual renal perform. Independent of diploma of meningeal inflammation.
In typical volunteers, fluconazole is cleared mainly by renal excretion, with roughly eighty% of the administered dose showing in the urine as unchanged pill. About eleven% of the dose is excreted in the urine as metabolites.
In regular volunteers, Diflucan administration (doses ranging from 200 mg to four hundred mg the moment every day for up to 14 days) was linked with small and inconsistent results on testosterone concentrations, endogenous corticosteroid concentrations, and the ACTH-stimulated cortisol reaction.