POSACONAZOLE

4-(p-(4-(p-(((3R,5R)-5-(2,4-Difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furyl)methoxy) phenyl)-1- piperazinyl)phenyl)-1-((1S,2S)-1-ethyl-2-hydroxypropyl)-delta(2)-1,2,4-triazolin-5-one; Noxafil; 4-(4-(4-(4-(((3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl)methoxy)phenyl) piperazin-1-yl)phenyl)-2-((2S,3S)-2-hydroxypentan-3-yl)-1,2,4-triazol-3-one; Spriafil;

POSACONAZOLE

 

PRODUCT IDENTIFICATION

CAS RN

171228-49-2

EINECS RN

C37H42F2N8O4

FORMULA

700.78

MOLE WEIGHT

 

CLASSIFICATION

Antifungal

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE

white to off-white crystalline powder

MELTING POINT

168 - 172 C

BOILING POINT

 

DENSITY

 

SOLUBILITY IN WATER

 

pH

 

VAPOR DENSITY

 

REFRACTIVE INDEX

 

FLASH POINT

 

 

STABILITY AND REACTIVITY
STABILITY Stable under normal conditions

INCOMPATIBLE MATERIALS

Strong oxidizing agents.

DECOMPOSITION PRODUCTS

Carbon oxides. nitrogen oxides.

POLYMERIZATION Has not been reported

NFPA RATINGS

Health: 2 Flammability: 0 Reactivity: 0

 

SAFETY

HAZARD NOTES

Delayed target organ effects. Toxic by ingestion. Target Organs: Liver, Male reproductive system.

EYE

May cause eye irritation.

SKIN

May be harmful if absorbed through skin. May cause skin irritation.

INGESTION

Toxic if swallowed.

INHALATION

May be harmful if inhaled. May cause respiratory tract irritation.

MAIN RISKS AND TARGET ORGANS  

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

2811
HAZARD CLASS

6.1

PACKING GROUP

III

HAZARD SYMBOL

T

RISK PHRASES

25

SAFETY PHRASES

36-45

 

EXTERNAL LINKS & GENERAL INFORMATION
Posaconazole successful in treating fluconazole- and itraconazole-resistant candidiasis An open-label study of oral posaconazole has found that it safely and effectively treats oropharyngeal and oesophageal candidiasis in people resistant to fluconazole and/or itraconazole. The study was published in the February 15th issue of Clinical Infectious Diseases. Mucosal candidiasis (‘thrush’) is an infection of the mouth and throat (oropharyngeal candidiasis) and/or oesophagus (oesophageal candidiasis) by the fungi Candida albicans and, more rarely, C. glabrata. Oral fluconazole is still the mainstay of antifungal treatment for mucosal candidiasis (MC). After repeated fluconazole treatment, 4 - 5% of people with advanced HIV (especially with CD4 cells counts below 100 cells/mm3) will develop fluconazole-resistant MC. Alternative treatments include itraconazole and voriconazole (which may be hampered by cross-resistance and drug interactions), and the more highly toxic intravenous drugs amphotericin B and caspofungin. (http://www.aidsmap.com/)

Posaconazole belongs to the class of medications called antifungals. It is used to prevent certain serious fungal infections for people 13 years of age and older whose immune systems may be weakened by other medications or diseases. Posaconazole is also used for people 13 years of age and older to treat Candida infections of the mouth or throat (thrush). It is also used to treat Aspergillus infections that have not improved with other antifungal medications or when these medications have caused side effects. Posaconazole works by killing or stopping the growth of some types of fungi that can cause infections in people.(http://www.healthyontario.com/)

Posaconazole is a member of the azole class of antifungals recently approved for the prophylaxis and treatment of invasive fungal infections. Posaconazole has a large volume of distribution and distributes well into tissues. Posaconazole-induced fungal killing is optimal when peak drug concentrations achieved are 2–10 times the organism’s minimum inhibitory concentration. Posaconazole demonstrates fungistatic activity against most species of Candida, Cryptococcus, and Trichosporon. In a direct comparison, posaconazole appeared 2–4 times more active than itraconazole against most pathogenic yeast species. Posaconazole also showed activity against Candida and Aspergillus isolates resistant to the other azoles and amphotericin B. Posaconazole has superior activity to the other azoles against Zygomycetes isolates. It has demonstrated activity equal or superior to other antifungal agents against almost all varieties of yeast and mold. The most common treatment-related adverse events associated with posaconazole are nausea, vomiting, diarrhea, rash, hypokalemia, thrombocytopenia, and abnormal liver function test values. Significant drug interactions include cimetidine, rifabutin, and phenytoin, for which concomitant use should be avoided, as well as cyclosporine, tacrolimus, and midazolam, for which dosage reductions are recommended. (http://www.ajhp.org/)

Pharmacological Actions

  • Anti-Infective
  • Antibiotics
  • Antifungal
  • Antiparasitic
  • Antiprotozoal
  • Trypanocidal

 

SALES SPECIFICATION

APPEARANCE

white to off-white crystalline powder

PURITY

98.0% min

MELTING POINT

168 - 172 C

 

PRICE INFORMATION

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