Customization: | Available |
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Varieties: | Infectious Disease Prevention Medicine |
Component: | Chemical Synthetic Drugs |
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Product Name: Itraconazole
Packing: 10kg/drum
Specification: EP USP
CAS: 84625-61-6
MF: C35H38Cl2N8O4
MW: 705.63
Itraconazole is an artificially synthetic clotrimazole, being a broad-spectrum synthetic antifungal agent. Its antimicrobial spectrum and antimicrobial mechanism is similar to clotrimazole, but has strong antibacterial activity against Aspergillus. It exerts its anti-fungal effect through changing the fungal cell membrane permeability with antibacterial activity against superficial and deep fungal pathogens. Its antibacterial spectrum is broader and stronger than ketoconazole, being able to inhibit the ergosterol synthesis of fungal cell membrane, thus playing the antifungal effect. This product is suitable for the treatment of Dermatophytes (Trichophyton, Microsporum, Flocculent Epidermophyton), Yeast [Cryptococcus neoformans, Pityrosporum, Candida (including Candida albicans, Candida glabrata and candida krusei)], Aspergillus, Histoplasma, Paracoccidioides brasiliensis, Sporothrix schenckii, Hormodendrum, Cladosporium, Blastomyces dermatitidis and various kinds of other types of yeasts and fungi. Itraconazole is not able to inhibit the growth of Rhizopus and Mucor.
One nitrogen atom contained in the itraconazole molecule can bind to the ferrous ion on the heme of the P450 molecule in the fungal cell, thereby inhibiting the P450 hydroxylase-catalyzed de-methylation of lanosterol, Sterol to ergosterol conversion blocked, lanosterol and other precursors accumulation, membrane chemical composition changes, membrane associated enzyme dysfunction, increased permeability, intracellular fluid spill, so as to achieve the inhibition and sterilization. The combination of this product with the fungus P450 system is quite strong while its combination with the mammalian P450 system is weak, so that the toxicity of drugs on human is greatly reduced. Clinical Itraconazole is mainly used for the treatment of systemic deep fungal infections caused by systems such as blastomycosis, histoplasmosis, coccidioidomycosis, chromoblastomycosis, sporotrichosis and coccidioidomycosis. It can also be used for the treatment of candidiasis and aspergillosis.
Uses: The imidazole antifungal agents for the triazole ring, through inhibiting the activation of cytochrome P-450, including oxidase and peroxidase, disable the 14, α-methyl sterols to be dehydrogenated and be converted to ergosterol, so that the growth and proliferation of fungi are inhibited. They have strong lipophilicity and penetrate through the biofilm to inhibit the binding of the membrane to the fungus. The antibacterial spectrum is similar to ketoconazole. It is effective in the treatment of superficial fungal diseases such as vaginal and oral candidiasis as well as skin mycosis. Furthermore, it is expected to become the highly-efficient and safe drugs for the treatment of deep fungal infections such as cryptococcal encephalitis (AIDS). It is used for the treatment of vulvovaginal candidiasis, pityriasis and skin fungal disease pityriasis caused by sensitive fungi.
It can be used for the synthesis of broad-spectrum azole antifungal agents for the treatment of systemic infection caused by deep fungus. It can also be used for the treatment of candidiasis and aspergillosis.
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