Antimicrobials
Itraconazole

Itraconazole

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

Spectrum of Activity

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 to 28 hours, Multiple doses: 34 to 42 hours

  • Time to peak, plasma: Capsules/tablets: 2 to 5 hours; Oral solution: 2.5 hours

  • Excretion: Urine (<1% active drug, 35% as inactive metabolites); feces (54%; ~3% to 18% as unchanged drug)