Clinical pharmacodynamics and pharmacokinetics of the antifungal extended-spectrum triazole posaconazole: an overview

Br J Clin Pharmacol. 2010 Oct;70(4):471-80. doi: 10.1111/j.1365-2125.2010.03680.x.


In recent years, the antifungal triazole posaconazole has become increasingly important for the prophylaxis and treatment of systemic mycoses. Although oral bioavailability of posaconazole can be enhanced by concomitant food intake and administration in divided daily doses, increased gastric pH or gut motility, as well as enzyme-inducing drugs, can result in lower plasma concentrations than expected. Whether therapeutic drug monitoring can reduce the risk of treatment failures by avoiding sub-therapeutic plasma concentrations needs further examination. Based on the ability of posaconazole to inhibit cytochrome P450 3A4, several drug interactions can be expected, especially with agents that undergo extensive first-pass effect through the gut and the liver. However, more information is needed regarding dose modifications during concomitant administration of posaconazole with drugs in certain categories, such as vinca alkaloids and retinoids, along with selected individual drugs such as everolimus.

MeSH terms

  • Antifungal Agents / pharmacokinetics*
  • Antifungal Agents / pharmacology*
  • Area Under Curve
  • Biological Availability
  • Drug Interactions
  • Drug Resistance, Fungal
  • Fungi / drug effects
  • Humans
  • Triazoles / pharmacokinetics*
  • Triazoles / pharmacology*


  • Antifungal Agents
  • Triazoles
  • posaconazole