酮康唑
中文同义词: 顺-1-乙酰基-4-[4-[[2-(2,4-二氯苯基)-2-(1H-咪唑-1-基甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]哌嗪;酮康唑;酮康唑 CP2005;酮亢唑;酶康灵
化学性质 白色结晶性粉末。熔点146℃,不溶于水。
用途:酮康唑是一种咪唑类广谱抗真菌药,市面上销售的商品名称为金达克宁、霉康灵和可宁,通过高度选择性干扰真菌的细胞色素P-450的活性,从而抑制真菌细胞膜上麦角固醇的生物合成。酮康唑洗剂作为皮肤外用药,临床主要用于治疗和预防由马拉色菌引起的各种感染。
用途: 由皮肤真菌和酵母菌所致的皮肤真菌病、花斑癣及发癣,当局部治疗或口服灰黄霉素无效,或难以接受灰黄霉素治疗的严重顽固性皮肤真菌感染,可用本品治疗。
药理作用 1.药理学酮康唑属吡咯类抗真菌药,对深部感染真菌如念珠菌属、着色真菌属、球孢子菌属、组织浆胞菌属、孢子丝菌属等均具抗菌作用,对毛发癣菌等亦具抗菌活性。本品对曲霉、申克氏孢子丝菌、某些暗色孢科、毛霉属等作用较弱。本品通过干扰细胞色素P-450的活性,从而抑制真菌细胞膜主要固醇类-麦角固醇的生物合成,损伤真菌细胞膜并改变其通透性,以致重要的细胞内物质外漏。酮康唑可抑制真菌的三酰甘油和磷脂的生物合成,抑制氧化酶和过氧化酶的活性,引起细胞内过氧化氢积聚导致细胞亚微结构变性和细胞坏死。对白念珠菌则可抑制其自芽孢转变为侵袭性菌丝的过程。
2.毒理学动物长期毒性实验表明,酮康唑可使碱性磷酸酶明显上升,肝细胞变性。
Ketoconazole
Synonym: 3-dioxolan-4-yl)methoxy)phenyl)-,cis-;fungarest;fungoral;ketoconazol;ketoderm;ketoisdin;kw-1414;nizoral
CAS: 65277-42-1
MF: C26H28Cl2N4O4
MW: 531.43
EINECS: 265-667-4
Assay: 99%
Appearance: white powder
Specification: CP
Chemical Property: Melting point 146 Centigrade, insoluble in water
Usage:
1. Ketoconazole is a broad-spectrum imidazole antifungal drugs, the market sales of commodity names, mycophenolate Kang Ling gold miconazole and Ning, through cytochrome P-450 highly selective interference with fungal activity, thereby inhibiting the biosynthesis of ergosterol on fungal cell membrane. Ketoxonazole Lotion as skin external use, mainly used for a variety of treatment and prevention of Malassezia caused by infection.
2. The skin fungus and yeast fungal skin disease, caused by Trichophyton tinea versicolor and, when local treatment or oral griseofulvin is invalid, severe refractory fungal infection or unacceptable griseofulvin therapy, available for the treatment of.
Pharmacological effects:
1. Pharmacology of ketoconazole belongs to azole antifungals, deep infection of fungi such as Candida, Fonsecaea, Coccidioides, tissue slurry Pseudomonas, Sporothrix are antibacterial effect, the hair tinea also with antibacterial activity.
2. Long term toxicity test showed that the animal toxicology, ketoconazole can make alkaline phosphatase increased significantly, the liver cell degeneration.
Package: 25kg/drum
Price: USD 111/kg
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