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儿童地高辛动力学与肾脏排泄

Digitoxin kinetics and renal excretion in children.

作者信息

Larsen A, Storstein L

出版信息

Clin Pharmacol Ther. 1983 Jun;33(6):717-26. doi: 10.1038/clpt.1983.98.

Abstract

Digitoxin kinetics were investigated in 11 children, three girls and eight boys, with a mean age of 7.1 yr (5.9 to 9.2). Five children received digitoxin, 17.5 to 20 micrograms/kg IV, and six other children received 20 micrograms/kg as an oral solution. Digitoxin was given as a single dose 24 to 48 hr after cardiac surgery, and patients were monitored in an intensive care unit for 24 hr. Serum and urine digitoxin concentrations were determined by radioimmunoassay. Children had larger apparent volumes of distribution (1 l/kg) than adults (0.57 l/kg). Mean serum elimination t 1/2 was 6.4 days in children (3 to 11.2) and 8.2 days in adults (5.9 to 11.3). Total body clearance was much greater in children (0.085 ml X min-1 X kg-1) than in adults (0.036 ml X min-1 X kg-1). This was because of an increase in metabolic clearance, although there was no difference in renal clearance in children and adults. Absolute oral bioavailability, measured by comparing serum AUCs after intravenous and oral doses, was complete. Peak serum concentrations of 23 to 50 ng/ml developed 90 to 120 min after the oral dose. A single digitalization dose of 20 micrograms/kg was well tolerated and did not induce arrhythmias.

摘要

对11名儿童(3名女孩和8名男孩)进行了洋地黄毒苷动力学研究,平均年龄为7.1岁(5.9至9.2岁)。5名儿童静脉注射洋地黄毒苷,剂量为17.5至20微克/千克,另外6名儿童口服20微克/千克溶液。在心脏手术后24至48小时给予单次剂量的洋地黄毒苷,并在重症监护病房对患者进行24小时监测。通过放射免疫测定法测定血清和尿液中的洋地黄毒苷浓度。儿童的表观分布容积(1升/千克)比成人(0.57升/千克)大。儿童的平均血清消除半衰期为6.4天(3至11.2天),成人为8.2天(5.9至11.3天)。儿童的总体清除率(0.085毫升·分钟-1·千克-1)比成人(0.036毫升·分钟-1·千克-1)高得多。这是由于代谢清除率增加,尽管儿童和成人的肾脏清除率没有差异。通过比较静脉注射和口服剂量后的血清AUC测量的绝对口服生物利用度是完全的。口服剂量后90至120分钟血清峰值浓度达到23至50纳克/毫升。20微克/千克的单次洋地黄化剂量耐受性良好,未诱发心律失常。

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