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首页> 外文期刊>Applied Microbiology >Chemotherapeutic Evaluation of Clotrimazole [Bay b 5097, 1 (o-Chloro-α-α-Diphenylbenzyl) Imidazole]
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Chemotherapeutic Evaluation of Clotrimazole [Bay b 5097, 1 (o-Chloro-α-α-Diphenylbenzyl) Imidazole]

机译:克霉唑的化学治疗评价[Bay b 5097,1(邻氯-α-α-二苯基苄基)咪唑]

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摘要

Clotrimazole has a broad spectrum of activity against yeast and filamentous fungi in vitro and also in vivo when given orally or parenterally to experimentally infected mice and when administered orally or topically to infected guinea pigs. In vitro a distinct inoculum effect has been observed with a number of strains of Candida and Torulopsis; minimal inhibitory concentrations have tended to increase with increased incubation time. With prolonged incubation times, resistance can be developed to clotrimazole in vitro, but this resistance is readily reversible upon passage in drug-free broth. The degree of in vivo activity of clotrimazole against Candida depends on the severity of infection used. Orally it appears to be more effective when administered by gavage than when given mixed in the diet. Pretreatment with the agent may decrease its efficacy because of drug inactivation. Against dermatophytes, clotrimazole has a degree of activity similar to griseofulvin when given orally, but it is less active than tolnaftate topically in cutaneous infection of Trichophyton mentagrophytes in guinea pigs. In vitro, but not in vivo, some gram-positive and gram-negative bacteria are inhibited by low concentrations of clotrimazole.
机译:当口服或胃肠外给予实验感染的小鼠,口服或局部给予感染的豚鼠时,克霉唑在体外和体内均具有广谱的抗酵母和丝状真菌的活性。在体外,已观察到许多念珠菌和Torulopsis菌株的接种效果。随着孵育时间的增加,最小抑菌浓度趋于增加。随着孵育时间的延长,可以在体外产生对克霉唑的抗药性,但是在无毒肉汤中传代后,这种抗药性很容易逆转。克霉唑对念珠菌的体内活性程度取决于所用感染的严重程度。口服强饲法比混合饮食中更有效。由于药物失活,用该药物进行预处理可能会降低其功效。口服时,克霉唑对皮肤癣菌的活性类似于灰黄霉素,但在豚鼠的癣菌癣菌的皮肤感染中,其活性不如甲苯磺酸盐局部使用。在体外而非体内,低浓度的克霉唑可抑制某些革兰氏阳性和革兰氏阴性细菌。

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