It was approved for medical use in the European Union in October 2005,[6] and in the United States in September 2006.[5][9] It is available as a generic medication.[10][11]
Posaconazole works by disrupting the functions of certain fungal and protozoal membrane-bound enzyme systems. It does this by blocking the synthesis and turnover of the eukaryoticcell membrane component ergosterol via inhibition of an enzyme known as CYP51. Posaconazole is significantly more potent at binding to CYP51 than itraconazole.[5][16][17]
Pharmacokinetics
Posaconazole is absorbed within three to five hours. It is predominantly eliminated through the liver, and has a half-life of about 35 hours. Oral administration of posaconazole taken with a high-fat meal exceeds 90% bioavailability and increases the concentration by four times compared to fasting state.[5][18]
↑"First Generic Drug Approvals". U.S. Food and Drug Administration. 17 October 2022. Archived from the original on 26 January 2021. Retrieved 28 November 2022.
↑ Fatemizadeh R, Rodman E, Demmler-Harrison GJ, Dinu D (April 2020). "Rhizopus Infection in a Preterm Infant: A Novel Use of Posaconazole". Pediatr Infect Dis J. 39 (4): 310–312. doi:10.1097/INF.0000000000002554. PMID32084112.
↑Brunton L, Lazo J, Parker K. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 11th ed. San Francisco: McGraw-Hill; 2006. ISBN978-0-07-142280-2
↑Ashley ED, Perfect JR (October 2017). "Pharmacology of azoles". In Kauffman CA (ed.). UpToDate. Waltham, MA: UpToDate. Retrieved 18 February 2010.{{cite book}}: CS1 maint: deprecated archival service (link)
External links
Media related to Posaconazole at Wikimedia Commons