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广谱抗真菌药益康唑的生物学和毒理学特性

Bilogical and toxicological properties of econazole, a broad-spectrum antimycotic.

作者信息

Thienpont D, Van Cutsem J, Van Nueten J M, Niemegeers C J, Marsboom R

出版信息

Arzneimittelforschung. 1975 Feb;25(2):224-30.

PMID:1173036
Abstract

The spectrum of activity of 1-(2,4-dichloro-beta-[(p-chlorobenzoyl)oxy]phenethyl)imidazole-nitrate (econazole, R 14827) was tested in vitro on various pathogenic fungi and bacteria, and also in vivo in guinea-pigs and rats experimentally infected with dermatophytes and C. albicans. The in vitro activity spectrum is very broad: the dermatophytes, the yeasts, the dimorphic fungi, the aspergilli, the mycetoma causing agents and the Gram-positive bacteria being most sensitive. Guinea-pigs infected with T. mentagrophytes, M. canis or C. albicans and treated topically or orally with econazole, were cured. In each of these tests the activity of econazole was compared with that of different reference drugs. Vaginal candidiasis in rats was cured after oral administration of econazole. Toxicity and teratogenicity studies in different laboratory animals indicate that econazole is well tolerated.

摘要

对1-(2,4-二氯-β-[(对氯苯甲酰基)氧基]苯乙基)咪唑硝酸盐(益康唑,R 14827)的活性谱进行了体外测试,测试对象为各种致病真菌和细菌,还在体内对感染皮肤癣菌和白色念珠菌的豚鼠和大鼠进行了实验。体外活性谱非常广泛:皮肤癣菌、酵母菌、双相真菌、曲霉菌、引起足菌肿的病原体以及革兰氏阳性菌最为敏感。感染须癣毛癣菌、犬小孢子菌或白色念珠菌的豚鼠,经局部或口服益康唑治疗后痊愈。在每项此类试验中,都将益康唑的活性与不同参比药物的活性进行了比较。大鼠口服益康唑后,阴道念珠菌病得以治愈。在不同实验动物身上进行的毒性和致畸性研究表明,益康唑耐受性良好。

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