Abstract
Posaconazole (PCZ) is a relatively new addition to the azole antifungals. It has fungicidal activities against Aspergillus fumigatus, Blastomyces dermatitidis, selected Candida species, Crytopcoccus neoformans, and Trichosporon. PCZ also has fungistatic activities against Candida, Coccidioides, selected Fusarium spp., Histoplasma, Scedosporium and Zygomycetes. In addition, combining the drug with caspofungin or amphotericin B results in a synergistic interaction against A. fumigatus, C. glabrata and C. neoformans. The absorption of PCZ suspension is enhanced when given with food, nutritional supplements, and carbonated beverages. Oral administration of PCZ in divided doses also increases its bioavailability. PCZ has a large volume of distribution and is highly protein bound (>95%). The main elimination route of PCZ is fecal. PCZ is an inhibitor of the CYP3A4 enzyme; therefore, monitoring for drug-drug interactions is warranted with other CYP3A4 substrates/inhibitors/inducers. The most common adverse effects include headache, fatigue, nausea, vomiting and elevated hepatic enzymes. PCZ, with its unique antifungal activities, expands the azole class of antifungal agents. Because of its limit in formulation, PCZ oral suspension is recommended in immunocompromised patients with functional gastrointestinaltracts who fail conventional antifungal therapies or who are suspected to have a breakthrough fungal infection. However, a delayed-release tablet formulation and intravenous (IV) injection became available in 2014, expanding the use of PCZ in other patient populations, including individuals who are unable to take oral formulations.
Highlights
Posaconazole (PCZ) oral suspension (NoxafilTM, Schering-Plough Corporation) has received approval from the U.S Food and Drug Administration (FDA) for prophylaxis against invasive aspergillosis and candidiasis in immunocompromised patients, 13 years of age and older [1,2]
The most common organisms causing the fungal infections were Candida species which was responsible for eight cases, Aspergillus species which affected two patients, and a combination of Aspergillus species with Coccidioides immitis in one patient
PCZ plasma concentrations were not initially monitored since a target concentration of PCZ has not been established and a dose of 200 mg three times a day has been proven to be efficacious in previous studies; after the development of IFIs in several patients, peak and trough plasma levels of PCZ were measured on days 2, 8, and 15 after transplantation in 15, 14, and 10 patients with neutropenia, respectively
Summary
Posaconazole (PCZ) oral suspension (NoxafilTM, Schering-Plough Corporation) has received approval from the U.S Food and Drug Administration (FDA) for prophylaxis against invasive aspergillosis and candidiasis in immunocompromised patients, 13 years of age and older [1,2]. PCZ is considered an extended-spectrum antifungal agent due to its unique spectrum of activity against various fungi, including the majority of yeasts, filamentous fungi and azole resistant Candida species (spp.) [3]. The patterns of Candida infections have shifted from the previous most common fluconazole (FCZ) sensitive C. albicans to other FCZ dose-dependent sensitive and FCZ resistant Candida species since the year 2000 [4]. These Candida species include, but are not limited to, C. glabata, C. parapsilosis and C. tropicalis.
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
