API

Itraconazole (200mg)

Drug classification

Antifungal agent; triazole subclass.

Dosage form

Hard gelatin capsule containing 200 mg of itraconazole for oral administration.

API strength per dosage

Dose

Itraconazole 200mg capsules are typically dosed at 200mg once or twice daily for adults, depending on indication and severity. Capsules should be taken with food. Use in children is not well established. Caution is advised in hepatic or renal impairment; dose adjustment or monitoring may be necessary. Always refer to local guidelines and product information.

Mechanism of action

Itraconazole inhibits fungal cytochrome P450 enzyme 14α-demethylase, blocking the conversion of lanosterol to ergosterol, an essential component of fungal cell membranes. This disruption increases membrane permeability, impairs cellular processes, and inhibits fungal growth. It is selective for fungal over mammalian cytochrome P450 enzymes.

Indications

Treatment of Fungal infections

Side effects

Nausea Abdominal pain Constipation Dizziness Headache Indigestion Vomiting

Pregnancy category

Itraconazole may cause fetal harm; avoid use in pregnancy unless potential benefit justifies risk. Effective contraception recommended during treatment and for time after discontinuation.

Precautions

Assess liver function before and during treatment, monitor for signs of hepatotoxicity, avoid in patients with ventricular dysfunction or heart failure, check for drug interactions (CYP3A4 substrates), monitor for neuropathy, use caution in renal impairment, avoid in pregnancy, monitor therapeutic response, assess for gastrointestinal adverse effects.

Contraindications

Hypersensitivity to itraconazole or excipients, co-administration with CYP3A4 substrates (e.g., quinidine, cisapride, pimozide, dofetilide, ergot alkaloids), history of ventricular dysfunction or heart failure.