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。
相似文献
1
Digoxin pharmacokinetics: multicompartmental analysis and its clinical implications.地高辛药代动力学：多房室分析及其临床意义。
Br J Clin Pharmacol. 1976 Apr;3(2):221-9. doi: 10.1111/j.1365-2125.1976.tb00596.x.
2
Dose-independent pharmacokinetics of digoxin in humans.
Am Heart J. 1978 Oct;96(4):507-11. doi: 10.1016/0002-8703(78)90162-x.
3
Evidence of nonlinearity in digoxin pharmacokinetics.
J Pharmacokinet Biopharm. 1981 Apr;9(2):147-66. doi: 10.1007/BF01068079.
4
Changes in steady state digoxin pharmacokinetics during quinidine therapy in cardiac patients: influence of plasma quinidine concentration.心脏病患者接受奎尼丁治疗期间地高辛稳态药代动力学的变化：血浆奎尼丁浓度的影响
Acta Pharmacol Toxicol (Copenh). 1983 May;52(5):357-63. doi: 10.1111/j.1600-0773.1983.tb01115.x.
5
Effect of dose on bioavailability of oral digoxin.
Eur J Clin Pharmacol. 1981 Jan;19(1):53-5. doi: 10.1007/BF00558384.
6
[Effect of propafenone on the pharmacokinetics of digoxin administered orally: a study in healthy volunteers].普罗帕酮对口服地高辛药代动力学的影响：一项在健康志愿者中的研究
G Ital Cardiol. 1986 Mar;16(3):237-40.
7
Effects of amiodarone on oral and intravenous digoxin kinetics in healthy subjects.
J Cardiovasc Pharmacol. 1987 Apr;9(4):385-90. doi: 10.1097/00005344-198704000-00001.
8
Pharmacokinetics of beta-methyldigoxin in healthy humans I: intravenous studies.健康人体中β-甲基地高辛的药代动力学I：静脉注射研究
J Pharm Sci. 1977 Feb;66(2):242-53. doi: 10.1002/jps.2600660228.
9
Pharmacokinetic studies of nifedipine and digoxin co-administration.
Int J Clin Pharmacol Ther Toxicol. 1986 Jan;24(1):39-42.
10
Absolute bioavailability of digoxin tablets.地高辛片的绝对生物利用度。
Arzneimittelforschung. 1978;28(4):701-3.
引用本文的文献
1
Supine Parasympathetic Withdrawal and Upright Sympathetic Activation Underly Abnormalities of the Baroreflex in Postural Tachycardia Syndrome: Effects of Pyridostigmine and Digoxin.平卧位副交感神经抑制和直立位交感神经兴奋是直立性心动过速综合征压力反射异常的基础：吡啶斯的明和地高辛的作用。
Hypertension. 2021 Apr;77(4):1234-1244. doi: 10.1161/HYPERTENSIONAHA.120.16113. Epub 2021 Jan 11.
2
Development of Human Membrane Transporters: Drug Disposition and Pharmacogenetics.人类膜转运蛋白的发展：药物处置与药物遗传学
Clin Pharmacokinet. 2016 May;55(5):507-24. doi: 10.1007/s40262-015-0328-5.
3
Some comments and suggestions concerning population pharmacokinetic modeling, especially of digoxin, and its relation to clinical therapy.关于群体药代动力学建模的一些意见和建议，特别是地高辛及其与临床治疗的关系。
Ther Drug Monit. 2012 Aug;34(4):368-77. doi: 10.1097/FTD.0b013e31825c88bb.
4
Cardiovascular drug therapy in the elderly: theoretical and practical considerations.老年人的心血管药物治疗：理论与实践考量
Drugs Aging. 2003;20(6):445-63. doi: 10.2165/00002512-200320060-00004.
5
Differential pharmacokinetics of digoxin in elderly patients.地高辛在老年患者中的差异药代动力学。
Drugs Aging. 2000 Nov;17(5):353-62. doi: 10.2165/00002512-200017050-00003.
6
Modeling of drug response in individual subjects.个体受试者药物反应的建模。
J Pharmacokinet Biopharm. 1980 Apr;8(2):115-30. doi: 10.1007/BF01065188.
7
Comparative pharmacokinetics and pharmacodynamics of cardiac glycosides.强心苷的比较药代动力学和药效学
Br J Clin Pharmacol. 1980 Aug;10(2):135-43. doi: 10.1111/j.1365-2125.1980.tb01730.x.
8
The changing pattern of toxicity of digoxin.地高辛毒性模式的变化
Postgrad Med J. 1981 Jun;57(668):358-62. doi: 10.1136/pgmj.57.668.358.
9
Re-examination of digoxin dosage regimen: comparison of the proposed nomograms or formulae in elderly patients.地高辛给药方案的重新审视：老年患者中拟议的列线图或公式比较。
Br J Clin Pharmacol. 1982 Apr;13(4):493-500. doi: 10.1111/j.1365-2125.1982.tb01410.x.
10
Drug metabolites in renal failure: pharmacokinetic and clinical implications.肾衰竭中的药物代谢产物：药代动力学及临床意义
Clin Pharmacokinet. 1981 Sep-Oct;6(5):329-45. doi: 10.2165/00003088-198106050-00001.
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.氚标记地高辛排泄与肾功能的关系。
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.氚标记地高辛经肾脏排泄的定位
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.液体闪烁计数法。使用外标道比法测定猝灭样品的本底计数。
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.禁食和餐后状态下口服地高辛后的血浆浓度。
不过你提供的原文“postprandial ste”似乎有误，推测应该是“postprandial state”（餐后状态） 。
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.血浆地高辛浓度——心房颤动患者中其与地高辛剂量及临床疗效的关系
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.居家医疗中老年人肾功能对血浆地高辛水平的影响。
Br Med J. 1972 Feb 5;1(5796):338-41. doi: 10.1136/bmj.1.5796.338.
Zotero 插件