Sato H, Narita A, Nakazawa S, Suzuki H, Matsumoto K, Nakanishi Y, Niino K, Nakazawa S
Department of Pediatrics, Tokyo Metropolitan Ebara General Hospital.
Jpn J Antibiot. 1989 Sep;42(9):1948-62.
A newly developed cephalosporin, cefteram pivoxil (CFTM-PI, T-2588), was evaluated clinically in 40 patients. A pharmacokinetic study was also performed with 8 patients. CFTM-PI was administered as granules. One patient was given CFTM-PI at a dose of 1.5 mg/kg, each of 3 patients was given the drug at a dose of 3 mg/kg and each of 4 patients at a dose of 6 mg/kg. In most cases, serum concentrations of CFTM were determined at 2, 3, 4, and 6 hours after dosing. Urinary concentrations of CFTM were measured for urinary samples collected during periods of 0-2, 2-4, 4-6 and 6-8 hours after dosing. CFTM was assayed using the disk or the cup method using Klebsiella pneumoniae ATCC 10031 as the test organism. The clinical evaluation was conducted in 40 children including 13 patients of acute tonsillitis, 10 of acute lacunar tonsillitis, 10 of scarlet fever, 2 of acute bronchitis, 2 of pneumonia, and 1 each of pneumonia with enteritis, phlegmon and urinary tract infection. The patients were from 4 months to 13 years old. Daily doses were from 8.7 to 12 mg/kg. After CFTM-PI administration in doses 1.5 mg/kg, 3 mg/kg and 6 mg/kg, peak serum concentrations of CFTM were 0.38 microgram/ml, 0.73-2.25 micrograms/ml and 1.2-2.9 micrograms/ml, respectively, and half-lives were 1.55, 0.95-2.30 and 0.80-2.72 hours, respectively. Urinary excretion rates up to 6 or 8 hours after dosing were 10.8-24.7%. Clinical efficacies of CFTM-PI in 40 patients were "excellent" in 27 children, "good" in 12 children and "fair" in 1 with an efficacy rate of 97.5%. Twenty seven strains of causative organisms, including 15 strains of Streptococcus pyogenes, 1 of Escherichia coli, 1 of Salmonella 04, 6 of Haemophilus influenzae, 1 of Haemophilus parainfluenzae and 3 of Branhamella catarrhalis, were isolated. After treatment all strains except 1 strain of B. catarrhalis (unchanged), Salmonella 04 (unknown) and 1 strain of H. parainfluenzae (unknown) were eradicated. Side effects observed clinically were only 1 case of diarrhea. Eosinophilia was observed in 1 case.
一种新研发的头孢菌素——头孢特仑新戊酯（CFTM - PI，T - 2588），对40例患者进行了临床评估。还对8例患者进行了药代动力学研究。CFTM - PI以颗粒剂形式给药。1例患者给予CFTM - PI的剂量为1.5 mg/kg，3例患者各给予3 mg/kg的剂量，4例患者各给予6 mg/kg的剂量。在大多数情况下，给药后2、3、4和6小时测定血清中CFTM的浓度。对给药后0 - 2、2 - 4、4 - 6和6 - 8小时期间收集的尿液样本测量CFTM的尿浓度。使用肺炎克雷伯菌ATCC 10031作为测试菌株，采用纸片法或杯碟法测定CFTM。对40名儿童进行了临床评估，其中包括13例急性扁桃体炎患者、10例急性陷窝性扁桃体炎患者、10例猩红热患者、2例急性支气管炎患者、2例肺炎患者以及各1例合并肠炎、蜂窝织炎和尿路感染的肺炎患者。患者年龄在4个月至13岁之间。每日剂量为8.7至12 mg/kg。给予1.5 mg/kg、3 mg/kg和6 mg/kg剂量的CFTM - PI后，CFTM的血清峰值浓度分别为0.38微克/毫升、0.73 - 2.25微克/毫升和1.2 - 2.9微克/毫升，半衰期分别为1.55、0.95 - 2.30和0.80 - 2.72小时。给药后6或8小时的尿排泄率为10.8 - 24.7%。CFTM - PI对40例患者的临床疗效为“优”的有27例儿童，“良”的有12例儿童，“中”的有1例，有效率为97.5%。分离出27株病原菌，包括15株化脓性链球菌、1株大肠杆菌、1株沙门氏菌04、6株流感嗜血杆菌、1株副流感嗜血杆菌和3株卡他莫拉菌。治疗后，除1株卡他莫拉菌（未改变）、沙门氏菌04（情况不明）和1株副流感嗜血杆菌（情况不明）外，所有菌株均被清除。临床观察到的副作用仅1例腹泻。1例出现嗜酸性粒细胞增多。
