Fluconazole
Unchecked
Fluconazole
Diflucan
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Summary
Classes
Common uses
Oropharyngeal and esophageal candidiasis0, Vulvovaginal candidiasis0, Invasive candidiasis (non-glabrata, non-krusei)0, Cryptococcal meningitis (consolidation/maintenance)0, Candida prophylaxis (immunocompromised)0
Pharmacy
Starting dose
Vulvovaginal: 150 mg PO single dose; oropharyngeal: 200 mg PO day 1, then 100 mg daily ×14 days; invasive candidiasis: 800 mg load, then 400 mg PO/IV daily; cryptococcal meningitis: 400-800 mg/d
Preparations
50, 100, 150, 200 mg tablets; 10, 40 mg/mL oral suspension; 2 mg/mL IV
US FDA Max
800 mg/d (severe invasive disease)
Pharmacology
Routes
Oral, IV
Onset
Clinical improvement within 24-72 hours
Duration
24 hours
Half-life
~30 hours (long, supports once-daily dosing and substantial drug-interaction window after discontinuation)[1]
Bioavailability
>90% (oral; not affected by food or gastric pH — a major practical advantage over itraconazole)[1]
Pregnancy
Single low dose (150 mg for vulvovaginitis) widely used; cumulative or high-dose use in first trimester carries teratogenic signal (skeletal, craniofacial); avoid prolonged courses where alternatives exist.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Fluconazole inhibits fungal cytochrome P450 14α-demethylase (CYP51), blocking conversion of lanosterol to ergosterol and disrupting fungal cell membrane integrity; the triazole structure improves selectivity over imidazoles (ketoconazole) for fungal vs human CYPs.0 Active against most Candida species (notably not C. krusei, often not C. glabrata) and Cryptococcus. CYP2C9 and CYP3A4 inhibitor — clinically meaningful interactions with warfarin, sulfonylureas, statins, calcineurin inhibitors, and many others[1].
References
[edit | edit source]- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Diflucan (fluconazole), Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019949s060,020090s044lbl.pdf