Posaconazole and Its Pharmacologic and clinical Uses: An Antifungal Drugs

Abstract

Posaconazole (PCZ) is a new broad-spectrum azole antifungal drug, that is accepted for theprevention of persistent aspergillosis and candidiasis in addition to the cure of oropharyngealcandidiasis. There is proof of efficacy in the treatment and prevention of rarer, difficult to treatfungal diseases. PCZ oral suspension has revealed limitations with fasting state absorption,raised gastrointestinal pH and high motility. Oral use of PCZ in divided doses increases thebioavailability. The recently approved sustained-release oral tablet and interavenous solutionsprovide a smart treatment option. PCZ has fungicidal activities against Aspergillus fumigatus,Blastomyces dermatitidis, Crytopcoccus neoformans, some Candida species,and Trichosporonandfungistaticactivities against Candida, Coccidioides, some Fusarium species, Scedosporium,Histoplasma, and Zygomycetes. PCZ has synergistic effects with caspofungin or amphotericin Bagainst A. fumigatus, C. glabrata and C. neoformans. The absorption of PCZ is enhanced whengiven with food, nutritional supplements, and carbonated beverages. PCZ is highly proteinbound (>95%) and main elimination route is fecal. PCZ is an inhibitor of the CYP3A4 enzyme.Common adverse effects are headache, fatigue, nausea, vomiting and elevated hepatic enzymes.Oral suspension is suggested in immuno compromised patients with functional gastrointestinal tract who not responds to conventional antifungal therapies. Interavenous injection isalso available for individuals who are unable to take oral drugs. On the basis of clinical studies,PCZ is a valuable drug for the treatment of life-threatening fungal infections. This review willexamine the progress history of PCZ and emphasize the most recent progresses.