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阿莫西林和氨苄西林在婴幼儿及儿童中的比较药代动力学

Comparative pharmacokinetics of amoxicillin and ampicillin in infants and children.

作者信息

Ginsburg C M, McCracken G H, Thomas M L, Clahsen J

出版信息

Pediatrics. 1979 Nov;64(5):627-31.

PMID:492836
Abstract

The pharmacokinetics of amoxicillin and ampicillin were studied in 24 infants and children. Mean peak serum concentrations of 5.4 micrograms/ml in fasting and 3.2 micrograms/ml in nonfasting patients were observed after 15 mg/kg amoxicillin doses. Area under the curve values and serum half-life values were similar in fasting and nonfasting patients. The pharmacokinetics of amoxicillin (15 mg/kg) were compared to those of ampicillin (25 mg/kg). Peak serum concentrations, area under the curve values and half-life times were comparable for the two drugs. Amoxicillin (25 mg/kg) and ampicillin (25 mg/kg) were compared in cross-over fashion in 11 children. Serum concentrations of amoxicillin were consistently larger than those of ampicillin; the differences were of borderline significance at one and two hours and statistically significant at four and six hours after the dosage. The bioavailability of amoxicillin was twice that of ampicillin. Amoxicillin was detected in approximately half of the saliva samples studied. Although the salivary concentrations in many children exceeded the inhibitory level for most pneumococci and group A streptococci and for many non-beta lactamase-producing Haemophilus influenzae type b strains, the clinical relevance of these observations is unknown.

摘要

对24名婴幼儿和儿童进行了阿莫西林和氨苄西林的药代动力学研究。给予15mg/kg阿莫西林剂量后,空腹患者的平均血清峰值浓度为5.4微克/毫升,非空腹患者为3.2微克/毫升。空腹和非空腹患者的曲线下面积值和血清半衰期值相似。将阿莫西林(15mg/kg)的药代动力学与氨苄西林(25mg/kg)进行了比较。两种药物的血清峰值浓度、曲线下面积值和半衰期相当。对11名儿童采用交叉方式比较了阿莫西林(25mg/kg)和氨苄西林(25mg/kg)。阿莫西林的血清浓度始终高于氨苄西林;给药后1小时和2小时差异接近显著,4小时和6小时差异具有统计学意义。阿莫西林的生物利用度是氨苄西林的两倍。在所研究的大约一半唾液样本中检测到了阿莫西林。尽管许多儿童的唾液浓度超过了大多数肺炎球菌、A组链球菌以及许多非β-内酰胺酶产生的b型流感嗜血杆菌菌株的抑制水平,但这些观察结果的临床意义尚不清楚。

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