Antimicrobials
Itraconazole

Itraconazole

N/A
Moderate (40 to 70%)

Spectrum of Activity

Dosing

General Information

  • LFTs
  • QTc
  • Potassium
  • Blood pressure
  • Serum concentrations (toxicity with levels > 3)
  • For invasive aspergillosis (treatment or prolonged prophylaxis), guidelines recommend monitoring serum trough concentrations (IDSA 2016]). Consider monitoring serum trough concentrations
  • Negative inotrope
  • Elevated LFTs - Severe hepatitis
  • Nausea, vomiting, abdominal pain
  • Prolonged QTc
  • Hypokalemia
  • Hypertension

Avoid use of acid suppressant as they can decrease the absorption due to reduced gastric acidity.

Significant drug interactions with multiple drugs, please refer to Micromedex for drug interaction checking.

Sporanox

Solution and capsules are not bioequivalent and are not interchangeable

  • 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%
  • 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)
  • Pregnancy: Category C - Generally not recommended in pregnancy
  • Breastfeeding: The safety was not evaluated, the use should be avoided

Adapted from the AdventHealth Orlando Antimicrobial Stewardship Program