The Posaconazole and Its Pharmacologic and clinical Uses: An Antifungal Drugs Potentials of Posaconazole
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Abstract
Posaconazole (PCZ) is a new broad-spectrum azole antifungal drug, that is accepted for the
prevention of persistent aspergillosis and candidiasis in addition to the cure of oropharyngeal
candidiasis. There is proof of efficacy in the treatment and prevention of rarer, difficult to treat
fungal 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 the
bioavailability. The recently approved sustained-release oral tablet and interavenous solutions
provide a smart treatment option. PCZ has fungicidal activities against Aspergillus fumigatus,
Blastomyces dermatitidis, Crytopcoccus neoformans, some Candida species,and Trichosporon
andfungistaticactivities against Candida, Coccidioides, some Fusarium species, Scedosporium,
Histoplasma, and Zygomycetes. PCZ has synergistic effects with caspofungin or amphotericin B
against A. fumigatus, C. glabrata and C. neoformans. The absorption of PCZ is enhanced when
given with food, nutritional supplements, and carbonated beverages. PCZ is highly protein
bound (>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 gastro
intestinal tract who not responds to conventional antifungal therapies. Interavenous injection is
also 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 will
examine the progress history of PCZ and emphasize the most recent progresses.
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