Dajani A S, Thirumoorthi M C, Bawdon R E, Buckley J A, Pfeffer M, Van Harken D R, Smyth R D
Antimicrob Agents Chemother. 1982 Feb;21(2):282-7. doi: 10.1128/AAC.21.2.282.
We studied the pharmacokinetics of intramuscular ceforanide in 46 infants, children, and adolescents, ranging in age from 1 month to 17 years. After the subjects were given 20-mg doses of ceforanide per kg, the mean peak plasma concentration was 56.3 microgram/ml (range, 27.0 to 95.0), the mean 8-h level was 5.9 microgram/ml (range, 1.5 to 13.5), and the mean 12-h level was 1.5 microgram/ml (range, 0.2 to 4.2). Ceforanide half-life varied with the ages of the patients: in 1- to 2-year-old children, in half-life was significantly shorter (1.5 h) than in younger or older children. Plasma concentrations at 8 and 12 h after a dose were lowest in 1- to 2-year-old children. There was no relationship between the area under the curve, the volume of distribution, or the body clearance of ceforanide to the ages of the patients. Within 6 h of administration of the drug, a mean of 77.5% of a dose was excreted in urine, and at the end of 12 h, virtually all (93.9%) of the administered dose was recovered in urine samples. The administration of ceforanide every 12 h did not result in drug accumulation. A dose of 20 mg of ceforanide per kg every 12 h is recommended for most pediatric patients. Dosage recommendations for 1- to 2 year-old children are presented.
我们研究了46名年龄在1个月至17岁之间的婴儿、儿童和青少年肌内注射头孢雷特的药代动力学。在受试者按每千克体重给予20毫克头孢雷特剂量后,血浆平均峰浓度为56.3微克/毫升(范围为27.0至95.0),8小时平均血药浓度为5.9微克/毫升(范围为1.5至13.5),12小时平均血药浓度为1.5微克/毫升(范围为0.2至4.2)。头孢雷特的半衰期随患者年龄而异:在1至2岁儿童中,半衰期明显短于年龄更小或更大的儿童(1.5小时)。给药后8小时和12小时的血浆浓度在1至2岁儿童中最低。头孢雷特的曲线下面积、分布容积或机体清除率与患者年龄之间无相关性。给药后6小时内,平均77.5%的剂量经尿液排出,12小时结束时,几乎所有(93.9%)给药剂量均可在尿液样本中回收。每12小时给予头孢雷特不会导致药物蓄积。建议大多数儿科患者每12小时给予每千克体重20毫克头孢雷特的剂量。文中给出了1至2岁儿童的剂量建议。