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Antimicrobials
Itraconazole

Itraconazole

N/A
Moderate (40 to 70%)
~$40 per #30, 100mg capsules

Spectrum of Activity

General Spectrum of Activity
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Dosing

General Information

  • LFTs

  • QTc

  • Potassium

  • Blood pressure

  • Serum concentrations (toxicity with levels > 3)

  • Negative inotrope

  • Elevated LFTs

  • Nausea, vomiting, abdominal pain

  • Prolonged QTc

  • Hypokalemia

  • Hypertension

Sporanox

  • Absorption:
    • Capsules: Requires gastric acidity (absorption is increased when administered with food)
    • Oral solution: Absorption increased on empty stomach
  • Distribution (Vd): >700 L
  • Protein binding, plasma:
    • 99.8%
    • Metabolite hydroxy-itraconazole: 99.6%
  • Metabolism:
    • Extensively hepatic via CYP3A4 into >30 metabolites including hydroxy-itraconazole (major metabolite)
    • Appears to have in vitro antifungal activity
    • Main metabolic pathway is oxidation
    • May undergo saturation metabolism with multiple dosing
  • Bioavailability:
    • ~55% increases by 30% under fasted conditions (oral solution)
    • Oral solution has a higher degree of bioavailability (149% ± 68%) relative to oral capsules
  • Half-life elimination:
    • 16-28 hours
    • Multiple doses: 34-42 hours
  • Time to peak, plasma:
    • Capsules/tablets: 2-5 hours
    • Oral solution: 2.5 hours
  • Excretion:
    • Urine (<1% active drug, 35% as inactive metabolites)
    • Feces (54%; ~3% to 18% as unchanged drug)