Holt R J, Newman R L
J Clin Pathol. 1972 Dec;25(12):1089-97. doi: 10.1136/jcp.25.12.1089.
Laboratory studies on clotrimazole showed that it had marked activity in vitro against all the Candida spp. and Cryptococcus spp. tested, against almost all strains of dermatophytes, and against Aspergillus spp and other fungal genera responsible for systemic mycoses; it had limited activity towards Gram-positive bacteria. The majority of Candida strains required MICs below 1 mug/ml and MCCs below 2 mug/ml.Serum, urine, and faecal assays of clotrimazole were made by microbiological methods on five children who received 100 mg/kg/day clotrimazole for several weeks. In-vitro sensitivity tests and biological fluid drug assays are also reported on specimens from 18 patients in other hospitals receiving clotrimazole for severe candidosis; several were renal transplant cases. Similar investigations are reported on specimens from 18 patients with pulmonary aspergilloses. The significance of low levels of the drug in body fluids, even after prolonged therapy, is discussed, and it is suggested that clotrimazole may be the first of a long series of imidazole derivatives with varying pharmacological and therapeutic properties.
对克霉唑的实验室研究表明,它在体外对所有测试的念珠菌属和隐球菌属具有显著活性,对几乎所有皮肤癣菌菌株,以及对引起系统性真菌病的曲霉菌属和其他真菌属也有活性;它对革兰氏阳性菌的活性有限。大多数念珠菌菌株的最低抑菌浓度低于1微克/毫升,最低杀菌浓度低于2微克/毫升。通过微生物学方法对5名连续数周接受100毫克/千克/天克霉唑治疗的儿童进行了克霉唑的血清、尿液和粪便检测。还报告了对其他医院18例因严重念珠菌病接受克霉唑治疗的患者标本进行的体外敏感性试验和生物体液药物检测;其中几例是肾移植病例。对18例肺曲霉菌病患者的标本也进行了类似研究。讨论了即使经过长期治疗后体液中药物水平较低的意义,并提出克霉唑可能是一系列具有不同药理和治疗特性的咪唑衍生物中的第一个。