Fluconazole properties

Jezequel, S. G., Fluconazole interspecies scaling and allometric relationships of pharmacokinetic properties, J. Pharm. Pharmacol. 1994, 46, 196-199. 

Absorption/Distribution - The pharmacokinetic properties of fluconazole are similar following administration by the IV or oral routes. In healthy volunteers, the bioavailability of oral fluconazole is more than 90% compared with IV administration. 

Many antimicrobial agents have similar pharmacokinetic properties when given orally or parenterally (ie, tetracyclines, trimethoprim-sulfamethoxazole, quinolones, chloramphenicol, metronidazole, clindamycin, rifampin, linezolid and fluconazole). In most cases, oral therapy with these drugs is equally effective, is less costly, and results in fewer complications than parenteral therapy. 

A rabbit model study suggested that topical 0.2% fluconazole has pharmacokinetic properties, low toxicity, and selective MICs that merit further studies as an ophthalmic agent (Yee et al.). 

Grant SM, Clissold SP. Fluconazole. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in superficial and systemic mycoses. Drugs 1990 39(6) 877-916. Erratum in Drugs 1990 40(6) 862. 

Goa KL, BarradeU LB. Fluconazole. An update of its pharmacodynamic and pharmacokinetic properties and therapeutic use in major superficial and systemic mycoses in immunocompromised patients. Drugs 1995 50(4) 658-90. Erratum in Drugs 1996 51(3) 505. 

Voriconazole is a triazole that is structurally related to fluconazole. It has two interesting properties, activity against Aspergillus species and sufficient solubility in... 

B. Azole antifungals include systemic agents such as keto-conazole, fluconazole, itraconazole, and voriconazole. Topical agents used for the treatment of vaginal candidiasis and thrush include miconazole and clotrimazole. The pharmacologic properties of the systemic azoles differ considerably. Ketoconazole, the first oral azole developed, has poor bioavailability and requires an acidic environment for enhanced absorption. Thus, initial studies required ketoconazole to be administered with a cola to increase bioavailability. Fluconazole, unlike itraconazole and ketoconazole, is hydrophillic and has increased penetration across the blood-brain barrier. Fluconazole is also the only azole that is renally eliminated. 

Fluconazole, USP. a-(2.4-Difluorophenyl)-benzyl alcohol (Diflucan) is a water-soluble bis-triazole with broad-spectrum antifungai properties that is suitable for both oral and intravenous administration a.s the free ba.se. Intravenous solutions of fluconazole contain 2 mg of the free base in I mL of isotonic sodium chloride or 5% dextrose vehicle. 

Perry CM, Whittington R, McTavish D. Fluconazole An update of its antimicrobial activity, pharmacokinetic properties, and ther eutic use in vaginal candidiasis. Drugs 1995 49 984-1006. 

Some imidazoles (miconazole, fluconazole) are known to interact with oral hypogly-caemic drugs (Chapter 6) by enhancing their activity and they may increase the risk of myopathy with lipid-lowering drugs statins (Chapter 4). Some imidazoles enhance the anticoagulant properties of warfarin. 

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