Itraconazole

Asia Bio-Pharmaceutical Research Institute

Itraconazole

Product name:Itraconazole
CAS:84625-61-6
Molecular Formula:C35H38Cl2N8O4
Formula Weight:705.63
Specification:1g
Description:
Itraconazole is a triazole antifungal agent that is prescribed to patients with fungal infections. The drug may be given orally or intravenously.
The mechanism of action of itraconazole is the same as the other azole antifungals: it inhibits the fungal cytochrome P450 oxidase-mediated synthesis of ergosterol. Because of its ability to inhibit cytochrome P450 3A4 CC-3, caution should be used when considering interactions with other medications.
Itraconazole for three synthetic nitrogen thiazole derivatives, is a synthetic broad-spectrum antifungal drugs, the antibacterial spectrum and antibacterial mechanism and clotrimazole are similar, but has strong antibacterial activity to the aspergillus, by changing the fungal cell membrane permeability of antimicrobial activity, the shallow and deep fungal infection of pathogenic bacteria have antibacterial activity, its antibacterial spectrum is ketone health zun more stronger, inhibits fungal cell membrane, the synthesis of ergosterol and antifungal effect into full play. Itraconazole ringworm fungi to the skin (tinea bacteria genera, microspore bacteria genera, MAO flocculent skin ringworm fungi), yeast [new cryptococcus, sugar abortive spore bacteria genera, candida (including candida albicans, candida smooth soft candida and g)], aspergillus species, cytoplasm bacteria genera, Brazilian vice ball spore bacteria, shenk spore silk, coloring fungi genera, branch spore mildew, and other kinds of blastomyces dermatitidis in yeast and fungi have inhibition. But itraconazole did not inhibit the growth of rhizopus and mucor.

A nitrogen atom of the itraconazole molecules with fungal cell P450 in the molecular combination of ferrous ions on heme, thereby inhibiting P450 hydroxylase catalytic lanosterol 14 alpha methylation reaction and make the lanosterol to the transformation of the ergosterol, lanosterol precursor accumulation, such as membrane chemical composition change, membrane coupling enzyme function disorder, permeability increases, the fluid within the cell, thus suppressing and bactericidal action. Itconazole binds strongly to the fungal P450 system and weakly to the mammalian P450 system, making the drug significantly less toxic to humans. Itraconazole is mainly used for systemic infections caused by deep fungi, such as blastomycosis, histoplasmosis, coccidiomycosis, chromomycosis, sporotrichosis and coccidiomycosis. It can also be used for candidiasis and aspergillosis.

 

 

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