|Systematic (IUPAC) name|
|Trade names||Noxafil, Posanol|
|Protein binding||98 to 99%|
|Half-life||16 to 31 hours|
|Excretion||Fecal (77%) and renal (14%)|
|(what is this?)|
Posaconazole is a triazole antifungal drug marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil. In Canada, posaconazole is marketed by Schering-Plough under the trade name Posanol.
Mode of action
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.
Posaconazole is absorbed within three to five hours. It is predominately 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.
Two studies suggest posaconazole may be superior to other triazoles, such as fluconazole or itraconazole, in the prevention of invasive fungal infections, although it may cause more serious side effects.
There is also some indication that posaconazole may be the most effective treatment for both chronic and acute Chagas disease, showing much better efficacy than benznidazole. Schering-Plough is currently recruiting participants for a phase 2 clinical trial in Argentina to test its efficacy against asymptomatic, chronic Chagas.
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