氟康唑（UK 49,858）和酮康唑对酮康唑敏感及耐药白色念珠菌的活性。
Activities of fluconazole (UK 49,858) and ketoconazole against ketoconazole-susceptible and -resistant Candida albicans.
作者信息
Hughes C E, Bennett R L, Tuna I C, Beggs W H
机构信息
Infectious Diseases Section, Veterans Administration Medical Center, Minneapolis, Minnesota 55417.
出版信息
Antimicrob Agents Chemother. 1988 Feb;32(2):209-12. doi: 10.1128/AAC.32.2.209.
Abstract
We have compared the activities of fluconazole and ketoconazole against ketoconazole-susceptible and -resistant strains of Candida albicans in a neutropenic-site rabbit model. Oral treatment with fluconazole resulted in much higher serum and extravascular concentrations of this antifungal agent than did comparable doses of ketoconazole. Fluconazole had no additional in vivo activity against the ketoconazole-susceptible strains; no fungicidal activity was observed with peak drug levels as high as approximately 75 micrograms/ml in the infection sites. Significant fungistatic activity against the ketoconazole-resistant strains was observed with fluconazole treatment (80 mg/kg), but not with less fluconazole (20 mg/kg) or with ketoconazole (approximately 67 mg/kg). In vitro susceptibility tests separated the ketoconazole-susceptible strains from the ketoconazole-resistant strains, but the results were variable when the resistant strains were tested with fluconazole.
摘要
我们在中性粒细胞减少部位的兔模型中，比较了氟康唑和酮康唑对酮康唑敏感及耐药白色念珠菌菌株的活性。与同等剂量的酮康唑相比，口服氟康唑导致该抗真菌剂在血清和血管外的浓度要高得多。氟康唑对酮康唑敏感菌株没有额外的体内活性；在感染部位，即使药物峰值水平高达约75微克/毫升，也未观察到杀菌活性。用氟康唑治疗（80毫克/千克）时，观察到对酮康唑耐药菌株有显著的抑菌活性，但使用较少剂量的氟康唑（20毫克/千克）或酮康唑（约67毫克/千克）时则未观察到。体外药敏试验将酮康唑敏感菌株与酮康唑耐药菌株区分开来，但在用氟康唑检测耐药菌株时，结果存在差异。
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本文引用的文献
1
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Antimicrob Agents Chemother. 1984 Mar;25(3):316-8. doi: 10.1128/AAC.25.3.316.
2
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Sabouraudia. 1984;22(1):53-63.
3
Ketoconazole and the liver.
Lancet. 1982 Apr 10;1(8276):860. doi: 10.1016/s0140-6736(82)91915-8.
4
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J Clin Microbiol. 1985 Aug;22(2):157-60. doi: 10.1128/jcm.22.2.157-160.1985.
5
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J Antimicrob Chemother. 1986 Jul;18(1):65-72. doi: 10.1093/jac/18.1.65.
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7
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8
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