Antimicrobials
Posaconazole

Posaconazole

N/A
Moderate (40 to 70%)
See Additional Information

Spectrum of Activity

Dosing

General Information

  • LFTs
  • CBC
  • Electrolytes (specifically K+ and Mg++)
  • QTC
  • Serum trough monitoring
  • Elevated LFTs
  • Thrombophlebitis
  • Peripheral edema
  • Headache
  • Infusion reactions
  • Hypokalemia, hypomagnesemia
  • QTc prolongation
  • Nausea, vomiting, diarrhea

See Lexicomp; significant drug-drug interactions

Cost:

  • IV: $313.07/dose
  • Liquid: $12.44/mL
  • Tablet: $34.26/tablet
  • Absorption:
    • Oral suspension: Unpredictable and variable (optimal absorption with a high-fat meal in 4 divided doses; absorption may be sufficient if taken with a nutritional supplement or acidic beverage [eg, ginger ale]).
    • Tablet (delayed-release): Predictable (preferably administered with food, but absorption is sufficient under fasting conditions)
  • Distribution: Vd: Oral: 287 L; Injection: ~261 L
  • Protein binding: >98%; predominantly bound to albumin
  • Metabolism: Not significantly metabolized; 17% undergoes non-CYP-mediated metabolism, primarily via hepatic glucuronidation into metabolites
  • Bioavailability:
    • Oral: Suspension and delayed release tablets are not bioequivalent; higher plasma exposure observed with delayed release tablets
    • Suspension: Dependent upon gastric pH environment (decreased with higher pH or increased motility) and fed-conditions (increased in high-fat environment)
    • Delayed release tablets: Dependent upon fed condition: Fasted conditions: 54%; higher under high-fat fed conditions (51% increase in AUC).
  • Half-life elimination:
    • Suspension: 35 hours (range: 20 to 66 hours)
    • Tablets: 26 to 31 hours
    • Injection: ~27 hours
  • Time to Peak, Plasma:
    • Suspension: ~3 to 5 hours
    • Tablets: ~4 to 5 hours
  • Excretion: Feces 71% (~66% of the total dose as unchanged drug); urine 13% (<0.2% of the total dose as unchanged drug)