Posaconazole
Structural formula | ||||||||||||||||||||||
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General | ||||||||||||||||||||||
Non-proprietary name | Posaconazole | |||||||||||||||||||||
other names |
Latin : Posaconazolum |
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Molecular formula | C 37 H 42 F 2 N 8 O 4 | |||||||||||||||||||||
Brief description |
White dust |
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Drug information | ||||||||||||||||||||||
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Mechanism of action |
Inhibition of the biosynthesis of ergosterol in mushrooms |
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properties | ||||||||||||||||||||||
Molar mass | 700.78 g · mol -1 | |||||||||||||||||||||
Physical state |
firmly |
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Melting point |
170-172 ° C |
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solubility |
almost insoluble in water |
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safety instructions | ||||||||||||||||||||||
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As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Posaconazole is an antifungal from the triazole group . It inhibits ergosterol biosynthesis and has been on the market since October 2005 under the trade name Noxafil (Essex Pharma). Posaconazole is currently considered an antifungal agent to be used in severe or itraconazole or amphotericin B- resistant fungal infections, especially in immunocompromised patients. It is also currently only approved for the treatment of adults. In other patients or uncomplicated fungal infections, the azoles itraconazole and fluconazole continue to be the first choice.
Scedosporium apiospermum and Sporothrix species show gaps in their effectiveness .
pharmacology
Posaconazole inhibits 14 α- demethylase, a fungus-specific cytochrome P450 isoenzyme ( CYP51A1 ) which is responsible for the conversion of lanosterol into ergosterol . Ergosterol precursors are built into the membrane and the permeability for cell components increases.
literature
- Analytics: Antimicrob Agents Chemother , 45 (3), 857-69 (2001 Mar), Petraitiene; Petraitis; Resentment
- Pharmacology: Expert Opinion on Investigational Drugs 9 (8), 1797-1813 (2000 Aug); Hossain; Ghannoum
Individual evidence
- ↑ a b c d Noxafil: SCIENTIFIC DISCUSSION for Posaconazole, as of October 28, 2005 on the website of the European Medicines Agency EMEA (PDF, 309.88 kB), accessed on August 4, 2009.
- ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals . 14th edition, 2006, p. 1313, ISBN 978-0-911910-00-1 .
- ↑ harmonized classification for this substance . A labeling of 2,5-anhydro-1,3,4-trideoxy-2-C- (2,4-difluorophenyl) -4 - [[4- [4- [4- [[4- [4- [4- [] is shown, which is derived from a self-classification by the distributor 1 - [(1S, 2S) -1-ethyl-2-hydroxypropyl] -1,5-dihydro-5-oxo-4H-1,2,4-triazol-4-yl] phenyl] -1-piperazinyl] phenoxy ] methyl] -1- (1H-1,2,4-triazol-1-yl) -D-threo-pentitol in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on July 11, 2020. There is not yet a
- ^ Marianne Abele-Horn: Antimicrobial Therapy. Decision support for the treatment and prophylaxis of infectious diseases. With the collaboration of Werner Heinz, Hartwig Klinker, Johann Schurz and August Stich, 2nd, revised and expanded edition. Peter Wiehl, Marburg 2009, ISBN 978-3-927219-14-4 , p. 272.