Products
Itraconazole is commercially available in capsule form and as an oral solution (Sporanox, generic). It has been approved in many countries since 1992. Sporanox infusion concentrate is no longer available.
Structure and properties
Itraconazole (C35H38Cl2N8O4, Mr = 705.6 g/mol) exists as a white powder that is practically insoluble in water. It belongs to the triazole antifungal class. Itraconazole is a mixture of four diastereomers (two pairs of enantiomers). The figure shows one of the four molecules.
Effects
Itraconazole (ATC J02AC02) has antifungal properties against dermatophytes, yeasts, aspergilli, and several other pathogenic fungal species. The effects are due to inhibition of the biosynthesis of ergosterol, an essential component of the fungal cell membrane. The half-life is about 17 hours. With repeated administration, it can increase up to 42 hours.
Indications
For the treatment of fungal infections, such as those caused by yeasts, dermatophytes, and molds.
Dosage
According to the professional information. Capsules are taken once or twice daily immediately after a full meal, depending on the indication.
Contraindications
- Hypersensitivity
- Ventricular dysfunction such as decompensated heart failure
- Concurrent administration of certain CYP3A4 substrates.
- Pregnancy
Full precautions can be found in the drug label.
Interactions
Itraconazole is a substrate and potent inhibitor of CYP3A and consequently has a high potential for drug-drug interactions. High gastric pH reduces absorption (e.g., when taking PPI).
Adverse effects
The most common potential adverse effects include rashes, headache, and digestive disturbances such as nausea, diarrhea, abdominal pain, dyspepsia, and flatulence.