Okura K, Yamamoto H, Yamaoka K, Kubo K, Mitsuyoshi I, Haruta T, Kobayashi Y
Department of Pediatrics, Kobe Central Municipal Hospital.
Jpn J Antibiot. 1988 Feb;41(2):152-64.
Ceftriaxone (CTRX) was administered to the newborn and its clinical effectiveness as well as its blood and cerebrospinal fluid levels were studied. 1. Average blood levels of CTRX 1 hour after single intravenous administration were 39 micrograms/ml in 2 cases receiving about 10 mg/kg, 70 micrograms/ml in 2 other cases receiving 20 mg/kg and 208 micrograms/ml in one receiving 52.6 mg/kg. As is apparent from these cases data, blood levels of CTRX were dose dependent. Blood levels of the drug were between 3.7 to 12.4 micrograms/ml 24 hours later. Half-lives of the drug in blood in the 5 newborns ranged from 7.13 to 10.6 hours. In a 53-day-old patient receiving 43.4 mg/kg of CTRX via intravenous injection, the one-hour blood level of the drug was 140 micrograms/ml and the half-life was 3.68 hours. The blood level of the drug 36 hours after single intravenous administration with 17.3 to 20.0 micrograms/ml to 5 other cases 0 to 5 days of age ranged from 4.6 to 13.7 micrograms/ml. 2. The cerebrospinal fluid level of CTRX 4 hours after intravenous administration with 49.6 mg/kg to cases of Escherichia coli meningitis was 9.7 micrograms/ml on the first day following the start of the treatment. It increased to 23.6, 25.2 and 31.0 micrograms/ml on the third, fourth and fifth days, respectively, and then gradually decreased. Cerebrospinal level was still 5.8 micrograms/ml on the 22nd day during the recovery period. These levels were far more than 1,000 times as much as the MIC for the pathogen at the highest level, and more than 100 times even at the lowest level. 3. CTRX was administered via intravenous injection once or twice a day (11.0-39.5 mg/kg in total) to 13 newborns and 3 infants. The efficacy of CTRX was good to excellent in 10 cases for treatment of 11 diseases (sepsis 1, pneumonia 4, urinary tract infection 4 and fetal infection 2) and all the pathogens (Streptococcus agalactiae 1, E. coli 3, Klebsiella pneumoniae 2, Citrobacter diversus 1) disappeared. In 6 cases where CTRX was used prophylactically, infection did not occur at all. The efficacy was excellent in another newborn with E. coli meningitis intravenously receiving 49.6 mg/kg of CTRX twice daily for 25 days. 4. No adverse reactions were observed. Mild eosinophilia was observed in 4 cases. Follow-up examinations of 3 of the 4 cases showed that these abnormal levels were returned to normal.(ABSTRACT TRUNCATED AT 400 WORDS)
对新生儿给予头孢曲松(CTRX),并研究其临床疗效以及血液和脑脊液中的药物水平。1. 单次静脉给药1小时后,2例接受约10mg/kg剂量的CTRX平均血药浓度为39μg/ml,另外2例接受20mg/kg剂量的为70μg/ml,1例接受52.6mg/kg剂量的为208μg/ml。从这些病例数据可以明显看出,CTRX的血药浓度与剂量相关。24小时后药物血药浓度在3.7至12.4μg/ml之间。5名新生儿中该药物在血液中的半衰期为7.13至10.6小时。在一名53日龄经静脉注射43.4mg/kg CTXR的患者中,给药1小时后的血药浓度为140μg/ml,半衰期为3.68小时。另外5例0至5日龄的新生儿单次静脉注射17.3至20.0mg/kg后36小时的血药浓度在4.6至13.7μg/ml之间。2. 对大肠杆菌脑膜炎患者静脉注射49.6mg/kg后4小时,脑脊液中CTRX水平在治疗开始后的第一天为9.7μg/ml。在第三天、第四天和第五天分别升至23.6μg/ml、25.2μg/ml和31.0μg/ml,然后逐渐下降。恢复期第22天脑脊液水平仍为5.8μg/ml。这些水平最高时比病原体的最低抑菌浓度(MIC)高出1000倍以上,最低时也高出100倍以上。3. 对13名新生儿和婴儿每天静脉注射CTRX一次或两次(总量为11.0 - 39.5mg/kg)。CTRX对11种疾病(败血症1例、肺炎4例、尿路感染4例、胎儿感染2例)的10例治疗效果良好至极佳,所有病原体(无乳链球菌1例、大肠杆菌3例、肺炎克雷伯菌2例、奇异柠檬酸杆菌1例)均消失。在6例预防性使用CTRX的病例中完全未发生感染。另一名患有大肠杆菌脑膜炎的新生儿每天静脉注射49.6mg/kg的CTRX,共25天,治疗效果极佳。4. 未观察到不良反应。4例出现轻度嗜酸性粒细胞增多。对其中3例的随访检查显示这些异常水平恢复正常。(摘要截选至400字)