Antimicrobials
Itraconazole (Sporanox)

Itraconazole (Sporanox)

N/A
Moderate (40 to 70%)
~$15.00/day

Spectrum of Activity

Dosing

General Information

Liver function in patients with preexisting hepatic dysfunction, and in all patients as clinically indicated; renal function; signs/symptoms of HF.

For invasive aspergillosis (treatment or prolonged prophylaxis):

  • Guidelines recommend monitoring serum trough concentration
  • Consider monitoring serum trough concentrations for other infections; itraconazole has a variable pharmacokinetic profile and high concentrations may increase the risk of adverse events
  • Timing of concentrations: 
    • Obtain trough after steady state has been reached (4-7 days after therapy initiation); the need for continued or repeat monitoring is a patient specific decision influenced by many factors (e.g. infection severity, cost, assay availability)
  • Recommended range: 
    • Most experts recommend dosing to achieve trough concentrations >0.5 to 1mcg/mL
    • Limited data suggest trough concentrations >3mcg/mL may be associated with increased toxicity
  • Nausea / vomiting / diarrhea 
  • Hypertriglyceridemia
  • Hypokalemia and elevated hepatic aminotransferases
  • Grapefruit decreases itraconazole absorption whereas acidic beverages such as colas or cranberry juice enhance absorption
  • Potent inhibitor of CYP3A4 enzyme with many important drug interactions (e.g. may increase plasma levels of phenytoin, carbamazepine, cyclophosphamide, cyclosporine, phenobarbital, tacrolimus, methadone, vincristine if used concomitantly)
  • Oral midazolam and methadone plasma concentrations increase markedly when given with itraconazole; avoid concurrent use

Oral solution and capsule dosage should NOT be used interchangeably.

Administer capsules immediately after a full meal for maximal absorption. Administering with acidic beverage (i.e. cola, orange or cranberry juice) can increase absorption. If patient is on a PPI, administer with acidic beverage.

Oral solution should be taken on an empty stomach (1 hour before or 2 hours after meals) for maximal absorption.

Antimicrobial class: Triazole antifungal

Pregnancy category: C

Average serum half life: 35-40 hours

Biliary penetration: Therapeutic

CSF penetration: Low

Lung penetration: Therapeutic

Urine penetration: Low