Morehead C D, Shelton S, Kusmiesz H, Nelson J D
Antimicrob Agents Chemother. 1972 Oct;2(4):267-71. doi: 10.1128/AAC.2.4.267.
A single intramuscular dose of 100 mg carbenicillin/kg produced measured peak concentrations of approximately 150 to 175 mug/ml in newborn infants. The carbenicillin serum half-life of 1.0 hr in normal adults was prolonged to 2.7 hr in infants of normal birth weight and to 4.0 hr in babies of low birth weight in the first week of life. One-third of a dose administered to babies of low birth weight and two-thirds of that given to babies weighing over 2,500 g was excreted by the kidney in 12 hr. Postadministration 6-hr urinary carbenicillin concentrations averaged 1,399 mug/ml after an intramuscular dose of 50 mg/kg and 2,689 mug/ml after a 100 mg/kg injection. Although carbenicillin is excreted by both glomerular and tubular mechanisms in adults, serum half-life and urinary carbenicillin excretion correlated well with creatinine clearance. Recommendations for dosage of carbenicillin and intervals of administration in the neonatal period are made based upon mathematical predictions from pharmacokinetic data.
对新生儿单次肌内注射100毫克羧苄青霉素/千克后,测得的峰值浓度约为150至175微克/毫升。正常成人羧苄青霉素的血清半衰期为1.0小时,在出生体重正常的婴儿中延长至2.7小时,在出生后第一周体重低的婴儿中延长至4.0小时。给低体重婴儿注射的剂量的三分之一以及给体重超过2500克的婴儿注射剂量的三分之二在12小时内由肾脏排出。肌内注射50毫克/千克后,给药后6小时尿中羧苄青霉素浓度平均为1399微克/毫升,注射100毫克/千克后为2689微克/毫升。虽然在成人中羧苄青霉素通过肾小球和肾小管机制排泄,但血清半衰期和尿中羧苄青霉素排泄与肌酐清除率密切相关。根据药代动力学数据的数学预测,给出了新生儿期羧苄青霉素的剂量和给药间隔建议。