Drug

D1429 | itraconazole

Molecular Formula C35H38Cl2N8O4
Molecular Weight 705.6
Structure
State solid
Clearance * 381 +/- 95 mL/minute [IV administration]
Volume of distribution * 796 ± 185 L
Route of elimination Itraconazole is metabolized predominately by the cytochrome P450 3A4 isoenzyme system (CYP3A4) in the liver, resulting in the formation of several metabolites, including hydroxyitraconazole, the major metabolite. Fecal excretion of the parent drug varies between 3-18% of the dose. Renal excretion of the parent drug is less than 0.03% of the dose. About 40% of the dose is excreted as inactive metabolites in the urine. No single excreted metabolite represents more than 5% of a dose.
Protein binding 0.998
Half life 21 hours
Absorption The absolute oral bioavailability of itraconazole is 55%, and is maximal when taken with a full meal.
Description antifungal

J

J02AC02 Itraconazole


[J02AC] Triazole derivatives


[J02A] ANTIMYCOTICS FOR SYSTEMIC USE


[J02] ANTIMYCOTICS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use


Toxicity Dose Time Species Model Method Action Positive criterion Reference
LIPID PEROXIDATION 4mg/ml Aspergillus fumigatus lipid peroxidation using the thiobarbituric acid assay induce 304
LIPID PEROXIDATION 4mg/ml Aspergillus fumigatus mitochondrion-specific lipid peroxidation probe MitoPerOx induce 304
ROS PRODUCTION 4mg/ml Aspergillus fumigatus oxidant-sensing fluorescent probe 2′,7′-dichlorofluorescin diacetate t induce 304


  • DrugBank DB01167
    CAS Number 84625-61-6
    PubChem Compound 55283