Drug Characteristics
  • Formulation

    Capsules: 100 mg

    Oral liquid: 10 mg/ml

    Intravenous infusion: 10 mg/ml

    (The oral solution should always be used in preference to capsules due to the poor bioavailability of the capsules)

  • Dose

    Therapeutic drug level monitoring should be performed to ensure adequate drug levels are achieved

    Oropharyngeal candidiasis: 200–400 mg orally daily for 7–14 days

    Fluconazole resistant oral or oesophageal candidiasis:

    100–200mg orally twice a day for up to 14 days

    Other systemic fungal infections (aspergillosis, histoplasmosis, cryptococcosis, coccidioidomycosis): Up to 400 mg orally daily

    Oropharyngeal candidiasis: fluconazole resistance 200–400 mg orally daily for 5–14 days

    Other systemic fungal infections – second line options (aspergillosis, histoplasmosis, cryptococcosis, coccidioidomycosis): Up to 400 mg orally daily

    Histoplasmosis - disseminated: Itraconazole 200 mg three times a day for 3 days then 200 mg twice a day for at least 12 months

    Pulmonary infection

    Acute infection: Itraconazole 200 mg orally once or twice a day for 6–12 weeks, may be more prolonged if CD4 count <300.

  • Side Effects

    Gastrointestinal disturbances (dyspepsia, nausea, abdominal pain, constipation); headache; increases in LFTs; rash; dizziness.

    CSM advice (heart failure)

    Caution in older patients, those receiving high doses or long courses or those taking negative inotropic drugs e.g. calcium channel blockers

  • Interactions

    Antacids, H2 antagonists, proton pump inhibitors and didanosine tablets reduce absorption (acid environment required).

    Plasma concentration reduced by rifampicin and phenytoin; warfarin effect enhanced; terfenadine and astemizole contraindicated – risk of arrhythmias; delayed metabolism of vincristine; increased risk of myopathy with simvastatin – avoid concomitant use; increased plasma levels of sildenafil

    Itraconazole levels are reduced by both efavirenz and nevirapine and the dose of itraconazole may need to be increased if given with an NNRTI

  • Renal

    Dose as in normal renal function

    The IV formulation contains hydroxypropyl-b-cyclodextrin, which is contraindicated in patients with a creatinine clearance of less than 30

  • Hepatic

    Itraconazole is predominantly metabolized in the liver. The terminal half-life of itraconazole in cirrhotic patients may be prolonged and dosage adjustment should be considered.

  • Pregnancy

    Human Data Suggest Low Risk

  • Other Information