Drug Groups

approved

Description

Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS. [PubChem]

Indication

For the treatment of fungal infections.

Pharmacology

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.

Toxicity

Symptoms of overdose include hallucinations and paranoid behavior.

Affected Organisms

Biotransformation

Hepatic

Absorption

90%

Half Life

30 hours (range 20-50 hours)

Protein Binding

11 to 12%

Elimination

In normal volunteers, fluconazole is cleared primarily by renal excretion, with approximately 80% of the administered dose appearing in the urine as unchanged drug.

Clearance

* 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]

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