Posaconazole, sold under the brand name Noxafil among others, is a triazole antifungal medication.
It was approved for medical use in the European Union in October 2005,
Medical uses
Posaconazole is used to treat invasive
Aspergillus and
Candida infections.
It is also used for the treatment of
Oral candidiasis (OPC), including OPC refractory to other drugs such as
itraconazole and
fluconazole.
Clinical evidence of efficacy in treatment of invasive disease caused by Fusarium species (fusariosis) is limited.
It appears to be helpful in a mouse model of naegleriasis
It has been used to treat mucormycosis (black fungus disease) caused by Rhizopus mold. [ ]
Pharmacology
Pharmacodynamics
Posaconazole works by disrupting the close packing of acyl chains of
phospholipids, impairing the functions of certain membrane-bound enzyme systems such as ATPase and enzymes of the electron transport system, thus inhibiting growth of the fungi. It does this by blocking the synthesis of
ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors. Posaconazole is significantly more potent at inhibiting 14-alpha demethylase than
itraconazole.
[Brunton L, Lazo J, Parker K. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 11th ed. San Francisco: McGraw-Hill; 2006. ]
Microbiology
Posaconazole is active against the following microorganisms:
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.
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