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急性心肌梗死中的丙吡胺:药代动力学变化的问题。

Disopyramide in acute myocardial infarction: problems with changing pharmacokinetics.

作者信息

Elliott H L, Thomson A H, Bryson S M

出版信息

Eur J Clin Pharmacol. 1986;30(3):345-7. doi: 10.1007/BF00541541.

DOI:10.1007/BF00541541
PMID:3732373
Abstract

In the acute phase of myocardial infarction it is recognized that serum disopyramide concentrations may be lower than expected. This has generally been attributed to reduced oral bioavailability. This report describes data obtained routinely from 6 patients with acute myocardial infarction and cardiac dysrhythmias treated initially with intravenous disopyramide. Serum disopyramide concentrations were consistently lower than expected, on average by 2.6 micrograms/ml. This was interpreted as being due to relatively high drug clearance, calculated as 6.7 +/- 1.5 l/h, compared to expected values of 3-4 l/h. Dosage schedules determined on the basis of the acute phase pharmacokinetics subsequently produced higher than predicted concentrations at later times on average by 2.8 micrograms/ml. Clearance at this time was calculated to be 3.1 +/- 0.6 l/h. Thus even with intravenous disopyramide therapy there are problems with changing pharmacokinetic parameters after myocardial infarction.

摘要

在心肌梗死急性期,人们认识到血清丙吡胺浓度可能低于预期。这通常归因于口服生物利用度降低。本报告描述了从6例急性心肌梗死并伴有心律失常的患者中常规获得的数据,这些患者最初接受静脉注射丙吡胺治疗。血清丙吡胺浓度始终低于预期,平均低2.6微克/毫升。这被解释为是由于药物清除率相对较高,计算得出为6.7±1.5升/小时,而预期值为3 - 4升/小时。基于急性期药代动力学确定的给药方案随后在后期产生的浓度高于预测值,平均高2.8微克/毫升。此时计算得出的清除率为3.1±0.6升/小时。因此,即使采用静脉注射丙吡胺治疗,心肌梗死后药代动力学参数的变化仍存在问题。

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1
Disopyramide in acute myocardial infarction: problems with changing pharmacokinetics.急性心肌梗死中的丙吡胺:药代动力学变化的问题。
Eur J Clin Pharmacol. 1986;30(3):345-7. doi: 10.1007/BF00541541.
2
Disopyramide pharmacokinetics in patients with acute myocardial infarction.急性心肌梗死患者的丙吡胺药代动力学
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The pharmacokinetics of disopyramide in patients with acute myocardial infarction.急性心肌梗死患者中丙吡胺的药代动力学
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Conversion from intravenous to oral slow-release disopyramide in acute myocardial infarction.急性心肌梗死患者从静脉注射转为口服缓释丙吡胺的转换治疗
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Disopyramide. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiac arrhythmias.丙吡胺。对其药效学和药代动力学特性以及在心律失常治疗中的应用的重新评估。
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Cardiovascular effects of acute normovolemic hemodilution in rats with disopyramide-induced myocardial depression.

本文引用的文献

1
Disposition kinetics of disopyramide in patients with renal insufficiency.肾功能不全患者中丙吡胺的处置动力学
Biopharm Drug Dispos. 1980 Jan-Mar;1(3):133-40. doi: 10.1002/bdd.2510010308.
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Unusual dosage of disopyramide.
Med J Aust. 1981 Oct 31;2(9):455. doi: 10.5694/j.1326-5377.1981.tb112933.x.
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OPT: a package of computer programs for parameter optimisation in clinical pharmacokinetics.OPT:一套用于临床药代动力学参数优化的计算机程序。
Br J Clin Pharmacol. 1982 Aug;14(2):247-56. doi: 10.1111/j.1365-2125.1982.tb01969.x.
丙吡胺诱导心肌抑制的大鼠急性等容血液稀释的心血管效应
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Disopyramide pharmacokinetics during recovery from myocardial infarction.心肌梗死恢复期的丙吡胺药代动力学。
Br J Clin Pharmacol. 1982 Mar;13(3):417-21. doi: 10.1111/j.1365-2125.1982.tb01395.x.
5
Prolonged variability in plasma protein binding of disopyramide after acute myocardial infarction.急性心肌梗死后丙吡胺血浆蛋白结合的长期变异性。
Br J Clin Pharmacol. 1983 Apr;15(4):435-41. doi: 10.1111/j.1365-2125.1983.tb01527.x.
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A placebo-controlled study to determine the efficacy of oral disopyramide phosphate for the prophylaxis of ventricular dysrhythmias after acute myocardial infarction.一项安慰剂对照研究,以确定口服磷酸丙吡胺对急性心肌梗死后室性心律失常的预防效果。
Br J Clin Pharmacol. 1982 Oct;14(4):519-27. doi: 10.1111/j.1365-2125.1982.tb02023.x.
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The acute changes in serum binding of disopyramide and flecainide after myocardial infarction.心肌梗死后丙吡胺和氟卡尼血清结合的急性变化。
Eur J Clin Pharmacol. 1985;28(3):253-5. doi: 10.1007/BF00543319.
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Disopyramide pharmacokinetics in patients with acute myocardial infarction.急性心肌梗死患者的丙吡胺药代动力学
Eur J Clin Pharmacol. 1985;28(1):45-51. doi: 10.1007/BF00635707.
9
The pharmacokinetics of disopyramide following myocardial infarction with special reference to oral and intravenous dose regimens.心肌梗死后丙吡胺的药代动力学,特别涉及口服和静脉给药方案。
J Int Med Res. 1976;4(1 Suppl):49-53.
10
Forecasting individual pharmacokinetics.预测个体药代动力学。
Clin Pharmacol Ther. 1979 Sep;26(3):294-305. doi: 10.1002/cpt1979263294.