Gruber W C, Rench M A, Garcia-Prats J A, Edwards M S, Baker C J
Antimicrob Agents Chemother. 1985 Apr;27(4):511-4. doi: 10.1128/AAC.27.4.511.
The single-dose pharmacokinetics of imipenem (N-formimidoyl thienamycin), a beta-lactam antibiotic, used in combination with cilastatin, a renal dehydropeptidase I inhibitor, were evaluated in 10 neonates 1 to 8 days of age. The imipenem-cilastatin combination was given intravenously over a 15-min period at a dose of 15 or 25 mg/kg. Drug concentrations in serum, urine, and cerebrospinal fluid (when available) were determined by high-pressure liquid chromatography, and plasma disposition of the drugs was described by a two-compartment open model. The mean peak plasma levels of imipenem 30 min postinfusion were 55.4 and 27.2 micrograms/ml, and the mean t1/2 beta values were 2.1 and 1.8 h at doses of 25 and 15 mg/kg, respectively. The calculated volume of distribution was 0.41 liters/kg. In two patients from whom cerebrospinal fluid was obtained 1.5 h postinfusion, imipenem levels were 5.6 and 1.1 micrograms/ml at doses of 25 and 15 mg/kg, respectively, representing 10 and 4% of the 1-h serum levels. No side effects attributable to a single dose of imipenem-cilastatin were noted.
对10名1至8日龄的新生儿评估了亚胺培南（N-甲酰亚胺基硫霉素）（一种β-内酰胺类抗生素）与西司他丁（一种肾脱氢肽酶I抑制剂）联合使用时的单剂量药代动力学。亚胺培南-西司他丁组合在15分钟内静脉给药，剂量为15或25mg/kg。通过高压液相色谱法测定血清、尿液和脑脊液（如有）中的药物浓度，并采用二室开放模型描述药物的血浆处置情况。输注后30分钟时，亚胺培南的平均血浆峰浓度在25mg/kg和15mg/kg剂量下分别为55.4和27.2μg/ml，平均t1/2β值分别为2.1和1.8小时。计算得出的分布容积为0.41升/千克。在输注后1.5小时获取脑脊液的两名患者中，亚胺培南浓度在25mg/kg和15mg/kg剂量下分别为5.6和1.1μg/ml，分别占1小时血清浓度的10%和4%。未观察到单剂量亚胺培南-西司他丁所致的副作用。
