| Indication |
For the treatment of fungal infections. |
| Pharmacodynamics |
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. |
| 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. |
| Absorption |
90% |
| Volume of distribution |
Not Available |
| Protein binding |
11 to 12% |
| Metabolism |
Hepatic |
| Route of 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. |
| Half life |
30 hours (range 20-50 hours) |
| 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]
|
| Toxicity |
Symptoms of overdose include hallucinations and paranoid behavior. |
