Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.
Active Ingredient / Synonyms
2-(2,4-DIFLUOROPHENYL)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-ol | 2,4-Difluoro-alpha,alpha-bis(1H-1,2,4-triazol-1-ylmethyl)benzyl alcohol | Biozole | Elazor | Fluconazol | Fluconazolum | Triflucan | Fluconazole |
Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS. [PubChem]
For the treatment of fungal infections.
Mechanism of Action
Fluconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Fluconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
Fluconazole, a synthetic antifungal agent of the imidazole class, is used to treat vaginal candidiasis. It inhibits the fungal lanosterol 14 alpha-demethylase which thereby prevents the formation of ergosterol which is an essential component in the fungal cell membrane.
In normal volunteers, fluconazole is cleared primarily by renal excretion, with approximately 80% of the administered dose appearing in the urine as unchanged drug.
30 hours (range 20-50 hours)
* 0.23 mL/min/Kg [adults] * 0.18 mL/min/Kg [In premature newborns within 36 hours of birth] * 0.22 mL/min/Kg [In premature newborns 6 days old] * 0.33 mL/min/Kg [In premature newborns 12 days old] * 0.4 mL/min/kg [9 Months-13 yearsreceiving single-oral 2 mg/kg] * 0.51 mL/min/Kg [9 Months-13 yearsreceiving single-oral 8 mg/kg] * 0.49 mL/min/Kg [5-15 yearsreceiving multiple IV 2 mg/kg] * 0.59 mL/min/Kg [5-15 yearsreceiving multiple IV 4 mg/kg] * 0.66 mL/min/Kg [5-15 yearsreceiving multiple IV 8 mg/kg]
Symptoms of overdose include hallucinations and paranoid behavior.
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