Posaconazole
{{Drugbox| |IUPAC_name = 4-{4-[4-(4-{[(5R)-5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-1-[(2S,3S)-2-hydroxypentan-3-yl]-4,5-dihydro-1H-1,2,4-triazol-5-one | image=Posaconazole.svg | width=280 | image2=Posaconazole3d.png | CAS_number=171228-49-2 | ATC_prefix=J02 | ATC_suffix=AC04 | ATC_supplemental= | PubChem=147912 | DrugBank= | C = 37 | H = 42 | F = 2 | N = 8 | O = 4 | molecular_weight = 700.778 g/mol | bioavailability= High | metabolism = Hepatic glucuronidation | elimination_half-life= 16 to 31 hours | protein_bound = 98 to 99% | excretion = Fecal (77%) and renal (14%) | pregnancy_AU = B3 | pregnancy_US = C | licence_EU = Noxafil | licence_US = Posaconazole | legal_US = Rx-only | routes_of_administration= Oral }} Posaconazole is a triazole antifungal drug.[1][2]
Posaconazole is marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil.
Uses
It is used to treat invasive infections by Candida species[3] and Aspergillus species[4] in severely immunocompromised patients.
There is also limited clinical evidence for its utility in treatment of invasive disease caused by Fusarium species (fusariosis).[5]
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.[6][7]
References
- ^ Schiller DS, Fung HB (2007). "Posaconazole: an extended-spectrum triazole antifungal agent". Clin Ther. 29 (9): 1862–86. doi:10.1016/j.clinthera.2007.09.015. PMID 18035188.
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ignored (help) - ^ Rachwalski EJ, Wieczorkiewicz JT, Scheetz MH (2008). "Posaconazole: an oral triazole with an extended spectrum of activity". Ann Pharmacother. 42 (10): 1429–38. doi:10.1345/aph.1L005. PMID 18713852.
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ignored (help)CS1 maint: multiple names: authors list (link) - ^ Li X, Brown N, Chau AS; et al. (2004). "Changes in susceptibility to posaconazole in clinical isolates of Candida albicans". J. Antimicrob. Chemother. 53 (1): 74–80. doi:10.1093/jac/dkh027. PMID 14657086.
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ignored (help)CS1 maint: multiple names: authors list (link) - ^ Walsh TJ, Raad I, Patterson TF; et al. (2007). "Treatment of invasive aspergillosis with posaconazole in patients who are refractory to or intolerant of conventional therapy: an externally controlled trial". Clin. Infect. Dis. 44 (1): 2–12. doi:10.1086/508774. PMID 17143808.
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ignored (help)CS1 maint: multiple names: authors list (link) - ^ 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.
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- ^ 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:10.1056/NEJMoa061094. PMID 17251531.
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: CS1 maint: multiple names: authors list (link) - ^ 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:10.1056/NEJMoa061098. PMID 17251530.
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