地高辛药代动力学：多房室分析及其临床意义。
Digoxin pharmacokinetics: multicompartmental analysis and its clinical implications.
作者信息
Sumner D J, Russell A J
出版信息
Br J Clin Pharmacol. 1976 Apr;3(2):221-9. doi: 10.1111/j.1365-2125.1976.tb00596.x.
Abstract
The kinetics of digoxin have been investigated in healthy volunteers using an isotopic tracer technique. A three compartment open kinetic model has been proposed as the simplest model consistent with the plasma, urinary and faecal data obtained. The renal clearance of digoxin (mean +/- s.d.) was found to be 119+/-10 ml/min, which did not differ significantly from the glomerular filtration rate (110+/-14 ml/min). Digoxin extra-renal clearance (mean+/-s.d.) was found to be 47+/-7 ml/min. The model predicts that the tissue concentration attained after four 0.25 mg oral doses spread over 24 h can be achieved within a period of 4 h following a single oral loading dose of 1 mg. Maintenance doses can be derived from a simple formula based on the glomerular filtration rate, extra-renal clearance and bioavailability of the digoxin preparation used.
摘要
采用同位素示踪技术在健康志愿者中研究了地高辛的动力学。已提出三室开放动力学模型作为与所获得的血浆、尿液和粪便数据一致的最简单模型。发现地高辛的肾清除率（均值±标准差）为119±10 ml/min，与肾小球滤过率（110±14 ml/min）无显著差异。发现地高辛肾外清除率（均值±标准差）为47±7 ml/min。该模型预测，在24小时内分四次口服0.25 mg剂量后所达到的组织浓度，可在单次口服1 mg负荷剂量后的4小时内实现。维持剂量可根据所用的地高辛制剂的肾小球滤过率、肾外清除率和生物利用度，从一个简单公式得出。
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本文引用的文献
1
The distribution and excretion of tritiated substances in experimental animals following the administration of digoxin-3H.
J Lab Clin Med. 1966 May;67(5):764-77.
2
Relationship of the excretion of tritiated digoxin to renal function.
Am J Med Sci. 1966 Feb;251(2):133-44. doi: 10.1097/00000441-196602000-00002.
3
Localization of the renal excretion of the tritiated digoxin.
Am J Med Sci. 1969 Sep;258(3):181-9. doi: 10.1097/00000441-196909000-00005.
4
Liquid scintillation counting. Determination of background counts of quenched samples using an external standard channels ratio.
Anal Biochem. 1969 Apr 11;29(1):154-63. doi: 10.1016/0003-2697(69)90019-0.
5
Tritiated digoxin. XIV. Enterohepatic circulation, absorption, and excretion studies in human volunteers.
Circulation. 1970 Nov;42(5):867-73. doi: 10.1161/01.cir.42.5.867.
6
Plasma concentrations of digoxin after oral administration in the fasting and postprandial ste.
Br Med J. 1971 Feb 13;1(5745):380-1. doi: 10.1136/bmj.1.5745.380.
7
A computerized cummulative integral method for the precise measurement of the glomerular filtration rate. 1.
Proc Soc Exp Biol Med. 1972 Sep;140(4):1148-55. doi: 10.3181/00379727-140-36630.
8
The binding of digoxin by the serum proteins.
Eur J Pharmacol. 1972 May;18(2):236-44. doi: 10.1016/0014-2999(72)90247-6.
9
Plasma digoxin concentration--its relation to digoxin dosage and clinical effects in patients with atrial fibrillation.
Br Heart J. 1972 Apr;34(4):383-91. doi: 10.1136/hrt.34.4.383.
10
Effects of renal function on plasma digoxin levels in elderly ambulant patients in domiciliary practice.
Br Med J. 1972 Feb 5;1(5796):338-41. doi: 10.1136/bmj.1.5796.338.
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