Chou K, Takimoto M, Yoshioka H, Tachibana K, Tanagawa N, Anakura M, Nanbu H, Nagamatsu K
Jpn J Antibiot. 1979 Nov;32(11):1107-16.
I. Pharmacokinetics (1) CXM 24.4 and 31.9 mg/kg were administered by intravenous drip infusion for 4 hours. The plateau levels were obtained at 1 approximately 2 hours, the blood levels at which time were 25.6 and 33.8 micrograms/ml respectively with dose response observed. (2) The respective half-lives were as short as 49.4 and 36.2 minutes. (3) The total clearances were 74.6 and 127.2 ml/min respectively; when calculated on plateau level and infusion rate, these were 81.6 and 111.0 ml/min. These differently determined values were near each other. (4) The respective renal clearances were 157.8 and 101.9 ml/min. II. Clinical results CXM for intravenous use was administered to 21 pediatric patients, and the clinical results were good and excellent in 19 (90.5%). Excluding 2 cases with elevation of cold hemagglutination values, the efficacy rate of 94.7% (18/19 cases) was achieved. The doses administered ranged 44 approximately 100 mg/kg body weight, and this dosage level was considered enough to achieve clinical effect. With the current clinical trial we considered that although the effectiveness of this drug was proved in 3 approximately 7 day intravenous drip infusion and intravenous injection, the continued treatment with other oral antibiotic following CXM treatment would be necessary from the patients' general conditions and laboratory examination findings. No noteworthy side effects were observed in any of the patients. No abnormality was seen in biochemistry and electrolyte findings, either.
一、药代动力学
(1)以24.4毫克/千克和31.9毫克/千克的剂量通过静脉滴注给药4小时。大约在2小时时达到稳态血药浓度,此时血药浓度分别为25.6微克/毫升和33.8微克/毫升,并观察到剂量反应。
(2)各自的半衰期分别短至49.4分钟和36.2分钟。
(3)总清除率分别为74.6毫升/分钟和127.2毫升/分钟;根据稳态血药浓度和输注速率计算,分别为81.6毫升/分钟和111.0毫升/分钟。这些不同测定值相近。
(4)各自的肾清除率分别为157.8毫升/分钟和101.9毫升/分钟。
二、临床结果
对21例儿科患者静脉使用了静脉用头孢克肟,19例(90.5%)的临床结果为良好和优秀。排除2例冷凝集值升高的病例后,有效率为94.7%(18/19例)。给药剂量范围为44至约100毫克/千克体重,该剂量水平被认为足以达到临床效果。通过当前的临床试验,我们认为尽管该药物在3至7天的静脉滴注和静脉注射中被证明有效,但根据患者的一般状况和实验室检查结果,在头孢克肟治疗后继续使用其他口服抗生素进行治疗是必要的。在任何患者中均未观察到值得注意的副作用。生化和电解质检查结果也未见异常。