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头孢泊肟酯在儿科领域的细菌学、药代动力学及临床研究

[Bacteriological, pharmacokinetic and clinical studies on cefpodoxime proxetil in the pediatric field].

作者信息

Kimura H, Takeuchi H, Ishikawa H, Hayakawa F, Yamamoto N, Nakao Y, Kuno K

机构信息

Department of Pediatrics, Anjo Kosei Hospital.

出版信息

Jpn J Antibiot. 1989 Jul;42(7):1593-606.

PMID:2562789
Abstract

Bacteriological, pharmacokinetic and clinical studies on cefpodoxime proxetil (CPDX-PR, CS-807), a new oral cephem antibiotic, were carried out in the field of pediatrics. The results obtained are summarized as follows. 1. Antibacterial activities of R-3746 (Na-salt of cefpodoxime (CPDX] against clinically isolated strains of Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, Enterococcus faecalis, Branhamella catarrhalis, Escherichia coli, Proteus mirabilis and Haemophilus influenzae were compared with those of cefaclor, cephalexin and cefadroxil. R-3746 is superior to other antibiotics against S. pneumoniae, S. pyogenes, B. catarrhalis and Gram-negative rods. 2. Serum concentrations of CPDX after administration of CPDX-PR at doses of 3 mg/kg (fasting), 6 mg/kg (non-fasting) and 6 mg/kg (fasting) were determined. Mean AUC (area under curve)'s of CPDX obtained were 9.60, 31.35 and 17.89 micrograms.hr/ml, respectively for the 3 dosages. The mean half-lives of CPDX were 3.35, 1.88 and 1.76 hours, respectively. The mean urinary recovery rate within 8 hours after administration of CPDX-PR at a dose of 3 mg/kg (fasting) was 39.2%. 3. CPDX-PR was administered to 37 pediatric patients with various bacterial infections (pyelonephritis 9, cystitis 4, pneumonia 7, acute bronchitis 3, otitis media 2, tonsillitis 10, subcutaneous abscess 1 and purulent lymphadenitis 1). The overall clinical efficacy rate was 91.9% and the overall bacteriological eradication rate was also 91.9%. 4. No adverse reactions were observed. Abnormal laboratory findings were moderate, eosinophilia in 2 and slight elevation of GOT and GPT in 1. The taste and the odor of the CPDX-PR preparation was sufficiently tolerable. From the above results we have concluded that CPDX-PR is a useful oral antibiotic in the treatment of bacterial infections in children.

摘要

在儿科领域开展了对新型口服头孢菌素抗生素头孢泊肟酯(CPDX-PR,CS-807)的细菌学、药代动力学及临床研究。获得的结果总结如下。1. 将头孢泊肟(CPDX)的钠盐R-3746对肺炎链球菌、化脓性链球菌、金黄色葡萄球菌、粪肠球菌、卡他布兰汉菌、大肠杆菌、奇异变形杆菌和流感嗜血杆菌等临床分离菌株的抗菌活性与头孢克洛、头孢氨苄和头孢羟氨苄进行了比较。R-3746在抗肺炎链球菌、化脓性链球菌、卡他布兰汉菌及革兰氏阴性杆菌方面优于其他抗生素。2. 测定了分别以3 mg/kg(空腹)、6 mg/kg(非空腹)和6 mg/kg(空腹)剂量给予CPDX-PR后CPDX的血清浓度。这3种剂量下CPDX的平均AUC(曲线下面积)分别为9.60、31.35和17.89微克·小时/毫升。CPDX的平均半衰期分别为3.35、1.88和1.76小时。以3 mg/kg(空腹)剂量给予CPDX-PR后8小时内CPDX的平均尿回收率为39.2%。3. 对37例患有各种细菌感染(肾盂肾炎9例、膀胱炎4例、肺炎7例、急性支气管炎3例、中耳炎2例、扁桃体炎10例、皮下脓肿1例和化脓性淋巴结炎1例)的儿科患者给予了CPDX-PR。总体临床有效率为91.9%,总体细菌清除率也为91.9%。4. 未观察到不良反应。实验室检查异常情况较轻,2例出现嗜酸性粒细胞增多,1例谷草转氨酶和谷丙转氨酶轻度升高。CPDX-PR制剂的味道和气味完全可以耐受。根据上述结果,我们得出结论,CPDX-PR是治疗儿童细菌感染的一种有用的口服抗生素。

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