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双吡啶类药物氨力农和米力农的药代动力学。

Pharmacokinetics of the bipyridines amrinone and milrinone.

作者信息

Edelson J, Stroshane R, Benziger D P, Cody R, Benotti J, Hood W B, Chatterjee K, Luczkowec C, Krebs C, Schwartz R

出版信息

Circulation. 1986 Mar;73(3 Pt 2):III145-52.

PMID:3510771
Abstract

The pharmacokinetics of milrinone were studied in sequential ascending doses in New York Heart Association Class III and IV patients receiving oral and intravenous medication. The parameters determined after parenteral administration were estimated by fitting the plasma concentration data to an open two-compartment body model. After oral medication, regression-independent parameters were determined. After either oral or parenteral administration of milrinone, plasma levels were dose dependent and the drug had an apparent first-order terminal elimination half-life of approximately 2 hr. The apparent volume of distribution was approximately 400 to 500 ml/kg, and total body clearance was approximately 130 ml/kg/hr. These values obtained in patients receiving milrinone were compared with those obtained for milrinone in volunteers, as well as those noted with the other inotropic bipyridine, amrinone. Milrinone's elimination from the blood stream patients was slower that that in normal healthy subjects and faster than amrinone's elimination in patients with congestive heart failure. Milrinone's pharmacokinetic parameters in these patients were unchanged after approximately 30 days of continuous oral medication.

摘要

在接受口服和静脉用药的纽约心脏协会III级和IV级患者中,以递增剂量序贯研究了米力农的药代动力学。通过将血浆浓度数据拟合到开放二室模型来估计胃肠外给药后测定的参数。口服给药后,确定与回归无关的参数。口服或胃肠外给予米力农后,血浆水平呈剂量依赖性,且该药物的表观一级末端消除半衰期约为2小时。表观分布容积约为400至500 ml/kg,全身清除率约为130 ml/kg/hr。将接受米力农治疗的患者获得的这些值与志愿者中米力农的相应值以及其他强心双吡啶氨力农的相应值进行比较。米力农在患者血流中的消除比正常健康受试者慢,且比充血性心力衰竭患者中氨力农的消除快。在连续口服给药约30天后,这些患者中米力农的药代动力学参数未发生变化。

相似文献

1
Pharmacokinetics of the bipyridines amrinone and milrinone.双吡啶类药物氨力农和米力农的药代动力学。
Circulation. 1986 Mar;73(3 Pt 2):III145-52.
2
Milrinone, a new agent for the treatment of congestive heart failure.米力农,一种用于治疗充血性心力衰竭的新药。
Clin Pharm. 1986 Mar;5(3):201-5.
3
New positive inotropic agents in the treatment of congestive heart failure. Mechanisms of action and recent clinical developments. 2.用于治疗充血性心力衰竭的新型正性肌力药物。作用机制及近期临床进展。2.
N Engl J Med. 1986 Feb 6;314(6):349-58. doi: 10.1056/NEJM198602063140605.
4
Pharmacokinetics and hemodynamics of amrinone in patients with chronic cardiac failure of diverse etiology.不同病因慢性心力衰竭患者氨力农的药代动力学和血流动力学
Res Commun Chem Pathol Pharmacol. 1987 Apr;56(1):3-19.
5
New positive inotropic agents for congestive heart failure.用于充血性心力衰竭的新型正性肌力药物。
N Engl J Med. 1986 Aug 7;315(6):396-7. doi: 10.1056/NEJM198608073150614.
6
Assessment of long-term therapy with milrinone and the effects of milrinone withdrawal.米力农长期治疗的评估及米力农撤药的影响。
Circulation. 1986 Mar;73(3 Pt 2):III205-12.
7
Pharmacokinetics and pharmacodynamics of milrinone in chronic congestive heart failure.米力农在慢性充血性心力衰竭中的药代动力学和药效学
Am J Cardiol. 1985 Oct 1;56(10):685-9. doi: 10.1016/0002-9149(85)91036-7.
8
Intravenous amrinone for congestive heart failure.静脉注射氨力农治疗充血性心力衰竭。
Med Lett Drugs Ther. 1984 Nov 23;26(675):104-5.
9
Amrinone in severe congestive heart failure: another look at an intriguing new cardioactive drug.氨力农治疗严重充血性心力衰竭:再探一种引人关注的新型强心药物。
J Pharmacol Exp Ther. 1984 Feb;228(2):319-26.
10
[Effects of amrinone administered orally and by injection in heart failure].
Ann Med Interne (Paris). 1985;136(3):251-5.

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