Iwai N, Sasaki A, Taneda Y, Mizoguchi F, Nakamura H, Tauchi N, Kawamura M, Ozaki T
Jpn J Antibiot. 1983 Sep;36(9):2336-48.
Basic and clinical studies were carried out on latamoxef (LMOX) in relation to the use of this antibiotic in the treatment of infections in newborn infants. The results were as follows. The MICs of LMOX were determined for various clinical isolates of Gram-negative bacteria: 22 strains of E. coli, 18 strains of K. pneumoniae, 4 strains of K. oxytoca, 19 strains of P. mirabilis, 4 strains of P. vulgaris, 5 strains of P. morganii and 3 strains of C. freundii and 60 strains of H. influenzae. The MIC distributions against all of these strains for each species were 0.1, 0.2, 0.1, 0.2, 0.1, 0.1, 6.25 and 0.78 microgram/ml or less, respectively. The antibacterial activity of LMOX against all of these Gram-negative isolates was thus found to be excellent. For 38 strains of P. aeruginosa, the MIC distribution was from 6.25 to 200 micrograms/ml; accordingly, although this antibiotic does show antibacterial activity against this microbe, it is not very potent. As Gram-positive bacteria, 28 clinical isolates of S. pyogenes and 34 strains of S. aureus were tested; their respective MIC distributions were 0.39--1.56 micrograms/ml and 3.13--25 micrograms/ml. Therefore, it is clear that the antibacterial activity of LMOX against these Gram-positive bacteria is not as good as against the above-mentioned Gram-negative species. LMOX was injected intravenously as a one-shot dose of 20 mg/kg to 5 newborn infants (ranging in age from 0 to 13 days) and to 2 suckling infants (49 and 60 days of age), and then the concentration of the drug in the serum was monitored with time. The mean serum concentrations in the newborn group at various times were as follows: 38.5 micrograms/ml at 0.5 hour, 31.6 micrograms/ml at 1 hour, 26.9 micrograms/m l at 2 hours, 17.8 micrograms at 4 hours and 15.5 micrograms/ml at 6 hours. For the 2 suckling infants, the mean values at those same time points were 30.5, 23.9, 16.3, 7.4 and 4.0 micrograms/ml. In addition the value for the mean serum half-life was 4.46 hours in the newborn infant group and 1.96 hours in the suckling infant group. The urinary recovery rate was 32.3% in the newborn infant group and 49.7% in the suckling infant group during 6 hours or 8 hours.(ABSTRACT TRUNCATED AT 400 WORDS)
针对拉氧头孢(LMOX)用于治疗新生儿感染进行了基础和临床研究。结果如下。测定了LMOX对各种革兰氏阴性菌临床分离株的最低抑菌浓度(MIC):22株大肠杆菌、18株肺炎克雷伯菌、4株产酸克雷伯菌、19株奇异变形杆菌、4株普通变形杆菌、5株摩根氏菌、3株弗氏柠檬酸杆菌和60株流感嗜血杆菌。针对每个菌种的所有这些菌株的MIC分布分别为0.1、0.2、0.1、0.2、0.1、0.1、6.25和0.78微克/毫升或更低。因此发现LMOX对所有这些革兰氏阴性分离株的抗菌活性极佳。对于38株铜绿假单胞菌,MIC分布为6.25至200微克/毫升;因此,尽管这种抗生素对该微生物确实有抗菌活性,但效力不是很强。作为革兰氏阳性菌,测试了28株化脓性链球菌和34株金黄色葡萄球菌的临床分离株;它们各自的MIC分布分别为0.39 - 1.56微克/毫升和3.13 - 25微克/毫升。因此,很明显LMOX对这些革兰氏阳性菌的抗菌活性不如对上述革兰氏阴性菌种。给5名新生儿(年龄从0至13天)和2名乳儿(49和60天龄)静脉注射20毫克/千克的单次剂量LMOX,然后随时间监测血清中药物浓度。新生儿组在不同时间的平均血清浓度如下:0.5小时时为38.5微克/毫升,1小时时为31.6微克/毫升,2小时时为26.9微克/毫升,4小时时为17.8微克,6小时时为15.5微克/毫升。对于2名乳儿,相同时间点的平均值分别为30.5、23.9、16.3、7.4和4.0微克/毫升。此外,新生儿组的平均血清半衰期值为4.46小时,乳儿组为1.96小时。新生儿组在6小时或8小时内的尿回收率为32.3%,乳儿组为49.7%。(摘要截短于400字)