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新生儿期头孢美唑的研究(作者译)

[A study on cefmetazole in the neonatal period (author's transl)].

作者信息

Iwai N, Sasaki A, Taneda Y, Inokuma K

出版信息

Jpn J Antibiot. 1981 Jun;34(6):881-92.

PMID:6945448
Abstract

The authors studied the antibacterial activity, absorption and excretion, and clinical use of cefmetazole in neonatal period, and obtained the following results. 1. The minimal inhibitory concentrations (MICs) of cefmetazole (CMZ) were measured, to compare with those of cefazolin (CEZ), for clinical isolates of S. aureus (31 strains), E. coli (29 strains) and K. pneumoniae (30 strains). On a cumulative percentage basis, 77% of S. aureus, 76% of E. coli and 90% of K. pneumoniae were inhibited by less than or equal to 3.13 microgram/ml of CMZ with a higher inoculum size. When compared with CEZ, MICs of CMZ were found to be superior or equal against E. coli, K. pneumoniae and some of S. aureus, but to be inferior against most of S. aureus. Most of strains which were resistant to CEZ were most sensitive to CMZ. These results suggest that CMZ is highly active against Gram-negative bacteria and is stable to beta-lactamase. 2. The serum concentration was measured in 7 neonates (5 approximately equal to 25 day-old) and 5 infants (1 approximately 3 month-old) after a single intravenous administration of 20 approximately 25 mg/kg of CMZ. The mean concentration in neonates was 68.3 microgram/ml at 1/2 hour postinjection, 57.0 microgram/ml at 1 hour, 35.4 microgram/ml at 2 hours, 18.1 microgram/ml at 2 hours, 18.1 microgram/ml at 4 hours and 9.5 microgram/ml at 6 hours. The mean half-life was 2.04 hours. The peak concentration of each neonate seemed to be related more to individual variation than to the days after birth. The mean concentration in infants was 60.7 microgram/ml at 1/2 hour, 42.8 microgram/ml at 1 hour, 22.2 microgram ml at 2 hours, 9.2 microgram/ml at 4 hours and 3.2 microgram/ml at 6 hours. The mean half-life was 1.31 hours. There was little difference in the mean peak concentration between neonates and infants, but the mean concentration after that were higher in neonates than infants. It was apparent that the half-life tends to be shortened in proportion to advanced age in days and months. 3. CMZ was administered clinically in 3 cases of acute bronchopneumonia. Its clinical effect was excellent or good in all of the cases. No adverse reaction or abnormal laboratory values were found.

摘要

作者研究了头孢美唑在新生儿期的抗菌活性、吸收与排泄以及临床应用,并得出以下结果。1. 测定了头孢美唑(CMZ)对金黄色葡萄球菌(31株)、大肠杆菌(29株)和肺炎克雷伯菌(30株)临床分离株的最低抑菌浓度(MIC),并与头孢唑林(CEZ)的MIC进行比较。以累积百分比计算,接种量较高时,小于或等于3.13微克/毫升的CMZ可抑制77%的金黄色葡萄球菌、76%的大肠杆菌和90%的肺炎克雷伯菌。与CEZ相比,CMZ对大肠杆菌、肺炎克雷伯菌和部分金黄色葡萄球菌的MIC相同或更低,但对大多数金黄色葡萄球菌的MIC更高。大多数对CEZ耐药的菌株对CMZ最为敏感。这些结果表明,CMZ对革兰氏阴性菌具有高度活性,且对β-内酰胺酶稳定。2. 对7例新生儿(5例约25日龄)和5例婴儿(1例约3月龄)单次静脉注射20~25毫克/千克的CMZ后测定血清浓度。新生儿注射后半小时的平均浓度为68.3微克/毫升,1小时为57.0微克/毫升,2小时为35.4微克/毫升,4小时为18.1微克/毫升,6小时为9.5微克/毫升。平均半衰期为2.04小时。每个新生儿的峰值浓度似乎更多地与个体差异有关,而非出生后天数。婴儿注射后半小时的平均浓度为60.7微克/毫升,1小时为42.8微克/毫升,2小时为22.2微克/毫升,4小时为9.2微克/毫升,6小时为3.2微克/毫升。平均半衰期为1.31小时。新生儿和婴儿的平均峰值浓度差异不大,但之后新生儿的平均浓度高于婴儿。显然,半衰期往往会随着年龄(以天数和月数计)的增长而缩短。3. 对3例急性支气管肺炎患者进行了CMZ的临床给药。所有病例的临床效果均为优或良。未发现不良反应或实验室值异常。

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