Posaconazole
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Posaconazole
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| Systematic (IUPAC) name | |
| 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro- 5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy] phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S)-1-ethyl- 2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one |
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| Identifiers | |
| CAS number | |
| ATC code | J02 |
| PubChem | |
| Chemical data | |
| Formula | C37H42F2N8O4 |
| Mol. mass | 700.778 g/mol |
| Pharmacokinetic data | |
| Bioavailability | High |
| Protein binding | 98 to 99% |
| Metabolism | Hepatic glucuronidation |
| Half life | 16 to 31 hours |
| Excretion | Fecal (77%) and renal (14%) |
| Therapeutic considerations | |
| Licence data |
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| Pregnancy cat. | |
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| Routes | Oral |
Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients. There is also limited clinical evidence for its utility in treatment of invasive disease caused by Fusarium species (fusariosis).[1] Two studies published in the January 25, 2007 issue of the New England Journal of Medicine 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.[2][3]
Posaconazole is marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil.
[edit] References
- ^ Raad I, Hachem R, Herbrecht R, et al. (2006). "Posaconazole as salvage treatment for invasive fusariosis in patients with underlying hematologic malignancy and other conditions" ([dead link]). Clin Infect Dis 42 (10): 1398–1403.
- ^ Cornely O, Maertens J, Winston D, Perfect J, Ullmann A, Walsh T, Helfgott D, Holowiecki J, Stockelberg D, Goh Y, Petrini M, Hardalo C, Suresh R, Angulo-Gonzalez D (2007). "Posaconazole vs. fluconazole or itraconazole prophylaxis in patients with neutropenia". N Engl J Med 356 (4): 348–59. doi:. PMID 17251531.
- ^ Ullmann A, Lipton J, Vesole D, Chandrasekar P, Langston A, Tarantolo S, Greinix H, Morais de Azevedo W, Reddy V, Boparai N, Pedicone L, Patino H, Durrant S (2007). "Posaconazole or fluconazole for prophylaxis in severe graft-versus-host disease". N Engl J Med 356 (4): 335–47. doi:. PMID 17251530.
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Can cause very severe kidney problems in otherwise healthy young individuals within days of starting course.
