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Posaconazole



Posaconazole
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
Identifiers
CAS number 171228-49-2
ATC code J02AC04
PubChem 147912
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

EU US

Pregnancy cat.

B3(AU) C(US)

Legal status

-only(US)

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]

Additional recommended knowledge

Posaconazole is marketed in the U.S. by Schering-Plough under the trade name Noxafil.

References

  1. ^ 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". Clin Infect Dis 42 (10): 1398–1403.
  2. ^ 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. PMID 17251531.
  3. ^ 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. PMID 17251530.

Can cause very severe kidney problems in otherwise healthy young individuals within days of starting course.

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Posaconazole". A list of authors is available in Wikipedia.
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