Autret E, Laugier J, Marimbu J, Vaillant M C, Furet Y, Breteau M
Service de Pharmacologie Clinique, CHR Bretonneau, Tours.
Arch Fr Pediatr. 1988 Nov;45(9):679-82.
Twenty-one full-term neonates who had a diagnosis of bacterial colonization were randomly assigned to receive amoxicillin 40 mg.kg-1 every 12 hours by either IV or oral route. Plasma levels of amoxicillin were assayed by HPLC at 0.5 (H0.5), 2 (H2), 6 (H6), 9 (H9) hours after the amoxicillin dose for both administration routes and also at the end of the infusion for the IV route. Average levels of plasma amoxicillin with IV and oral routes were not different except at H0.5 where they were higher with the IV route. With oral route Cmax was measured at H2 (6 times) or H6 (4 times). At the end of the infusion, plasma levels were between 55 and 154 mg.l-1 (81 +/- 32 mg.l-1). They decreased quickly so half life of amoxicillin by IV route was between 1.79 and 8.9 hs (4.28 +/- 2.4 hs). They were always above MIC for germs encountered in neonates except at H9 twice with IV and once with oral route. Pharmacokinetic data of this study allow to use oral route for amoxicillin for bacterial colonization in neonates: this administration route could also be proposed in infections following IV route as soon as hemodynamic and gastrointestinal conditions permit. The efficacy of such an attitude could be evaluated by a clinical trial.
21名被诊断为细菌定植的足月儿被随机分配,通过静脉注射或口服途径每12小时接受40mg/kg的阿莫西林。在阿莫西林给药后0.5小时(H0.5)、2小时(H2)、6小时(H6)、9小时(H9),采用高效液相色谱法测定两种给药途径的阿莫西林血浆水平,静脉注射途径还在输注结束时进行测定。除H0.5时静脉注射途径的血浆阿莫西林水平较高外,静脉注射和口服途径的血浆平均水平无差异。口服途径的Cmax在H2时测定6次,在H6时测定4次。输注结束时,血浆水平在55至154mg/L之间(81±32mg/L)。其迅速下降,因此静脉注射途径阿莫西林的半衰期在1.79至8.9小时之间(4.28±2.4小时)。除静脉注射途径在H9时出现两次、口服途径在H9时出现一次外,其水平始终高于新生儿中所遇细菌的最低抑菌浓度(MIC)。本研究的药代动力学数据支持在新生儿细菌定植时使用口服途径给予阿莫西林:一旦血流动力学和胃肠道状况允许,在静脉注射途径后的感染中也可采用这种给药途径。这种做法的疗效可通过临床试验进行评估。