|Trade names||Noxafil, Posanol, others|
|Drug class||Antifungal (azole)|
|Main uses||Thrush, aspergillosis, mucormycosis, coccidioidomycosis, fusariosis, chromoblastomycosis|
|Side effects||Nausea, diarrhea, fever, liver problems|
|By mouth (oral suspension, delayed-release tablets), IV|
|Protein binding||98 to 99%|
|Elimination half-life||16 to 31 hours|
|Excretion||Fecal (71–77%) and kidney (13–14%)|
|Chemical and physical data|
|Molar mass||700.778 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Posaconazole, sold under the brand names Noxafil among others, is an antifungal medication use to treat and prevent thrush, aspergillosis, mucormycosis, coccidioidomycosis, fusariosis, and chromoblastomycosis. It is used when other treatments are not appropriate. It is taken by mouth of given by injection into a vein.
Common side effects include nausea, diarrhea, fever, and liver problems. Other side effects may include allergic reactions and QT prolongation. Safety is unclear in pregnancy, with use not recommended in early pregnancy. It is in the azole family of medications and works by blocking lanosterol 14 alpha-demethylase.
Posaconazole was approved for medical use in Europe in 2005 and the United States in 2006. Generic versions have been approved. In the United Kingdom 24 tablets of 100 mg cost the NHS about £600 as of 2021. This amount in the United States costs about 410 USD.
Posaconazole is used to treat invasive Aspergillus and Candida and fungal infections caused by Scedosporium and Fusarium species, which may occur in immunocompromised patients. It is also used for the treatment of oropharyngeal candidiasis (OPC), including OPC refractory to itraconazole and/or fluconazole therapy.
For thrush it is taken at an initial dose of 200 mg by mouth, than is taken as 100 mg per day for 13 days. Other infections are treated with 400 mg twice per day by mouth or 300 mg twice per day by injection followed by 300 mg once per day by injection.
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.
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