title: Posaconazole: a review of the gastro-resistant tablet and intravenous solution in invasive fungal infections.
abstract: Posaconazole (Noxafil(®)) is a triazole antifungal agent with an extended spectrum of antifungal activity. It is approved for the prophylaxis of invasive fungal infections in patients with neutropenia or in haematopoietic stem cell transplant recipients undergoing high-dose immunosuppressive therapy for graft-versus-host disease, and for the treatment of fungal infections. The efficacy and good tolerability of posaconazole oral suspension administered three or four times daily is well established. However, in order to overcome pharmacokinetic limitations associated with the suspension, a new gastro-resistant tablet and intravenous (IV) solution were developed. This article reviews the pharmacokinetic properties of the new posaconazole formulations and briefly summarizes efficacy data relating to the suspension. The pharmacokinetic advantages of the posaconazole gastro-resistant tablet compared with the suspension formulation include less interpatient variability, better systemic availability enabling once-daily administration, and absorption that is unaffected by changes in gastric pH or motility; in addition the tablets may be taken with or without food. The posaconazole tablet achieves higher and more consistent mean plasma concentrations than the suspension and, therefore, it is the preferred option to optimize efficacy in the prophylaxis or treatment of invasive fungal disease. The posaconazole IV solution provides an option for these same indications in patients who are unable to receive oral formulations.
authors.affiliation: Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand, demail@springer.com.
authors.forename: Kate
authors.initials: K
authors.lastname: McKeage
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D002986:Clinical Trials as Topic / Q000379:methods; D041981:Gastrointestinal Tract / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D007262:Infusions, Intravenous; D009181:Mycoses / Q000188:drug therapy* / Q000378:metabolism; D013608:Tablets, Enteric-Coated; D014230:Triazoles / Q000008:administration & dosage* / Q000378:metabolism
chemical_list: D000935:Antifungal Agents; D013608:Tablets, Enteric-Coated; D014230:Triazoles; C101425:posaconazole