Posaconazole: A new oral antifungal agent with an expanded spectrum of activity

Research output: Contribution to journalReview article

27 Scopus citations

Abstract

Summary. Posaconazole isa member of the azole class of antifungals recently approved for the prophylaxis and treatment of invasive fungal infections. Posaconazole has a large volume of distribution and distributes well into tissues. Posaconazole-induced fungal killing is optimal when peak drug concentrations achieved are 2-10 times the organism's minimum inhibitory concentration. Posaconazole demonstrates fungistatic activity against most species of Candida, Cryptococcus, and Trichosporon. In a direct comparison, posaconazole appeared 2-4 times more active than itraconazole against most pathogenic yeast species. Posaconazole also showed activity against Candida and Aspergillus isolates resistant to the other azoles and amphotericin B. Posaconazole has superior activity to the other azoles against Zygomycetes isolates. It has demonstrated activity equal or superior to other antifungal agents against almost all varieties of yeast and mold. The most common treatment-related adverse events associated with posaconazole are nausea, vomiting, diarrhea, rash, hypokalemia, thrombocytopenia, and abnormal liver function test values. Significant drug interactions include cimetidine, rifabutin, and phenytoin, for which concomitant use should be avoided, as well as cyclosporine, tacrolimus, and midazolam, for which dosage reductions are recommended. Conclusion. Posaconazole is an oral antifungal agent with a broader spectrum of activity and better clinical efficacy than other available antifungals. It is less nephrotoxic than the polyenes and probably less likely to be involved in drug-drug interactions than the mold-active azoles.

Original languageEnglish (US)
Pages (from-to)225-236
Number of pages12
JournalAmerican Journal of Health-System Pharmacy
Volume66
Issue number3
DOIs
StatePublished - Feb 1 2009

Keywords

  • Antifungals
  • Blood levels
  • Dosage
  • Drug administration
  • Drug interactions
  • Drugs, body distribution
  • Minimum inhibitory concentration
  • Mycoses
  • Pharmacokinetics
  • Posaconazole
  • Resistance
  • Spectrum microbial
  • Toxicity

ASJC Scopus subject areas

  • Pharmacology
  • Health Policy

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