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Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
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Pharmacokinetics of antifungal drugs: practical implications for optimized treatment of patients

Romuald Bellmann1, Piotr Smuszkiewicz2

  • 1Clinical Pharmacokinetics Unit, Division of Intensive Care and Emergency Medicine, Department of Internal Medicine I, Medical University of Innsbruck, Anichstrasse 35, 6020, Innsbruck, Austria. romuald.bellmann@i-med.ac.at.

Infection
|July 14, 2017
PubMed
Abstract

Insights

Understanding antifungal pharmacokinetics is vital for treating invasive fungal infections (IFIs). This review details drug metabolism, interactions, and tissue penetration for key antifungals.

Area of Science:

  • Pharmacology
  • Infectious Diseases
  • Clinical Pharmacy

Background:

  • Invasive fungal infections (IFIs) are associated with high mortality rates.
  • Optimizing antifungal exposure is critical for effective treatment and patient safety.

Purpose of the Study:

  • To review pharmacokinetic data of systemically administered antifungals.
  • To focus on the impact of co-morbidities, target-site penetration, and combination therapy.

Main Methods:

  • Systematic review of published pharmacokinetic data.
  • Analysis of drug metabolism, protein binding, and elimination pathways.
  • Evaluation of drug-drug interactions and tissue distribution.

Main Results:

  • Amphotericin B is eliminated unchanged; Flucytosine and fluconazole are renally eliminated.
  • Azoles (itraconazole, voriconazole, posaconazole, isavuconazole) are hepatically metabolized via CYP enzymes, leading to drug-drug interactions.
  • Echinocandins (anidulafungin, caspofungin, micafungin) undergo non-CYP hepatic metabolism with lower interaction potential.
  • Antifungals exhibit varied tissue penetration; azoles and flucytosine distribute widely, while amphotericin B and echinocandins show specific tissue accumulation patterns.
  • Combination antifungal therapy is standard for cryptococcosis but debated for other IFIs like aspergillosis and mucormycosis.

Conclusions:

  • Antifungal pharmacokinetics vary significantly, influencing efficacy and safety.
  • Drug metabolism, interactions, and tissue distribution are key considerations for optimizing IFI treatment.
  • Further research is needed to clarify the role of combination antifungal therapy in various IFIs.
Keywords:
Amphotericin B lipid formulationsCaspofunginCritically illEchinocandinsExtracorporeal membrane oxygenationItraconazoleLiposomal amphotericin BPolyenesRenal replacement therapyVoriconazole

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