Posaconazole

Structural formula
General
Non-proprietary name	Posaconazole
other names	Latin : Posaconazolum
Molecular formula	C 37 H 42 F 2 N 8 O 4
Brief description	White dust
External identifiers / databases
CAS number 171228-49-2 EC number 682-747-8 ECHA InfoCard 100.208.201 PubChem 468595 ChemSpider 411709 DrugBank DB01263 Wikidata Q906453
Drug information
ATC code	J02 AC04
Drug class	Antifungal agent
Mechanism of action	Inhibition of the biosynthesis of ergosterol in mushrooms
properties
Molar mass	700.78 g · mol -1
Physical state	firmly
Melting point	170-172 ° C
solubility	almost insoluble in water
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances danger H and P phrases H: 361-372-410 P: ?
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

1. ↑ ^{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.
2. ^ The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals . 14th edition, 2006, p. 1313, ISBN 978-0-911910-00-1 .
3. ↑ There is not yet a 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.
4. ^ 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.

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !