- Molecular NameItraconazole
- SynonymITC; ITCZ; ITR; Itraconazol [Spanish]; itraconazole; Itraconazolum [Latin]; ITZ
- Weight705.647
- Drugbank_IDDB01167
- ACS_NO84625-61-6
- Show 3D model
- LogP (experiment)5.66
- LogP (predicted, AB/LogP v2.0)5.72
- pka3.7
- LogD (pH=7, predicted)5.71
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-6.34
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors0
- No.of HBond Acceptors12
- No.of Rotatable Bonds11
- TPSA100.79
- StatusFDA approved
- AdministrationOral and i.v. (US), Oral only (UK)
- PharmacologyA triazole antifungal agent that is prescribed to patients with fungal infections.
- Absorption_value80.0
- Absorption (description)Itraconazole is slowly but well absorbed after oral administration with peak concentrations reached in approx. 4 h. Absorption is enhanced in the presence of food and in an acidic intragastric environment.
- Caco_2N/A
- Bioavailability55.0
- Protein binding99.8
- Volume of distribution (VD)14 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolized predominantly by CYP3A4 to an active metabolite, hydroxyitraconazole, and other sequential metabolites.
- Half life20 h (following a 100 mg single dose); increases to 30 h on multiple dosing.
- Excretion3 to 18 % is excreted in the faeces as unchanged drug.
- Urinary Excretion<1
- Clerance23 ml/min/kg
- ToxicityThe serum toxic concentration is 6 mg/L (sum of itraconazole and its hydroxy metabolite).
- LD50 (rat)N/A
- LD50 (mouse)LD50=46.4 (iv)