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氟司喹南:一种具有正性肌力活性的血管扩张剂。

Flosequinan: a vasodilator with positive inotropic activity.

作者信息

Corin W J, Monrad E S, Strom J A, Giustino S, Sonnenblick E S, LeJemtel T

机构信息

Division of Cardiology, Albert Einstein College of Medicine, Bronx, NY 10461.

出版信息

Am Heart J. 1991 Feb;121(2 Pt 1):537-40. doi: 10.1016/0002-8703(91)90723-u.

DOI:10.1016/0002-8703(91)90723-u
PMID:1990760
Abstract

Flosequinan is an oral arterial and venous vasodilator that is currently under investigation for the treatment of congestive heart failure. The effects of flosequinan on ventricular performance and myocardial contractility were studied in 10 patients with severe congestive heart failure during right and left cardiac catheterization. Sixty minutes after a 100 mg oral dose of flosequinan, the peak rate of rise in left ventricular pressure (dP/dt) increased from 940 +/- 180 to 1050 +/- 240 mm Hg/sec (p less than 0.05), while left ventricular end-diastolic pressure decreased from 32 +/- 5 to 26 +/- 8 mm Hg (p less than 0.05), and cardiac index increased (2.1 +/- 0.4 to 2.3 +/- 0.5 L/min/m2, (p less than 0.05). The mean pulmonary artery pressure and vascular resistance decreased from 40 +/- 8 to 33 +/- 12 mm Hg (p less than 0.05) and from 330 +/- 240 to 290 +/- 170 dyne-sec/cm5 (p less than 0.05), respectively. Heart rate, mean aortic pressure, right atrial pressure, systemic vascular resistance, and serum norepinephrine levels did not change significantly. The increase in left ventricular peak dP/dt that was concomitant with a decrease in left ventricular end-diastolic pressure, and no change in systemic arterial pressure or sympathetic tone, argue for a direct positive inotropic effect of flosequinan.

摘要

氟司喹南是一种口服的动静脉血管扩张剂,目前正处于治疗充血性心力衰竭的研究阶段。在10例严重充血性心力衰竭患者进行左右心导管插入术期间,研究了氟司喹南对心室功能和心肌收缩力的影响。口服100mg氟司喹南60分钟后,左心室压力上升的峰值速率(dP/dt)从940±180增加到1050±240mmHg/秒(p<0.05),而左心室舒张末期压力从32±5下降到26±8mmHg(p<0.05),心脏指数增加(从2.1±0.4增加到2.3±0.5L/min/m2,p<0.05)。平均肺动脉压和血管阻力分别从40±8下降到33±12mmHg(p<0.05)和从330±240下降到290±170达因-秒/厘米5(p<0.05)。心率、平均主动脉压、右心房压力、全身血管阻力和血清去甲肾上腺素水平没有显著变化。左心室峰值dP/dt的增加伴随着左心室舒张末期压力的降低,且体动脉压或交感神经张力没有变化,这表明氟司喹南具有直接的正性肌力作用。

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1
Flosequinan: a vasodilator with positive inotropic activity.氟司喹南:一种具有正性肌力活性的血管扩张剂。
Am Heart J. 1991 Feb;121(2 Pt 1):537-40. doi: 10.1016/0002-8703(91)90723-u.
2
Effects of low-dose flosequinan on left ventricular systolic and diastolic chamber performance.低剂量氟司喹南对左心室收缩和舒张功能的影响。
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Sustained hemodynamic response to flosequinan in patients with heart failure receiving angiotensin-converting enzyme inhibitors.接受血管紧张素转换酶抑制剂治疗的心力衰竭患者对氟司喹南的持续血流动力学反应。
J Am Coll Cardiol. 1993 Oct;22(4):963-7. doi: 10.1016/0735-1097(93)90404-o.
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Flosequinan, a new vasodilator: systemic and coronary hemodynamics and neuroendocrine effects in congestive heart failure.氟司喹南,一种新型血管扩张剂:充血性心力衰竭中的全身及冠状动脉血流动力学和神经内分泌效应
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Positive inotropic and lusitropic effects of intravenous flosequinan in patients with heart failure.静脉注射氟司喹南对心力衰竭患者的正性肌力和变时性作用。
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Central and regional hemodynamic effects of flosequinan for congestive heart failure.氟司喹南对充血性心力衰竭的中心和区域血流动力学效应
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Positive inotropic and hemodynamic properties of flosequinan, a new vasodilator, and a sulfone metabolite.新型血管扩张剂氟司喹南及其砜代谢产物的正性肌力和血流动力学特性。
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Effects of balanced vasodilator, flosequinan, on aortic impedance in failing heart.平衡血管扩张剂氟司喹南对衰竭心脏主动脉阻抗的影响。
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Positive inotropy contributes to the hemodynamic mechanism of action of flosequinan (BTS 49465) in the intact dog.正性肌力作用有助于氟司喹南(BTS 49465)在完整犬体内的血流动力学作用机制。
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Positive inotropic and vasodilator actions of milrinone in patients with severe congestive heart failure. Dose-response relationships and comparison to nitroprusside.米力农对重症充血性心力衰竭患者的正性肌力和血管舒张作用。剂量反应关系及与硝普钠的比较。
J Clin Invest. 1985 Feb;75(2):643-9. doi: 10.1172/JCI111742.

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Poster communications.壁报交流
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Effect of flosequinan on exercise capacity and cardiac function in patients with chronic mild heart failure: a double-blind placebo-controlled study.氟司喹南对慢性轻度心力衰竭患者运动能力和心功能的影响:一项双盲安慰剂对照研究。
Heart Vessels. 1992;7(3):133-40. doi: 10.1007/BF01744866.
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Flosequinan does not affect systemic and regional vascular responses to simulated orthostatic stress in healthy volunteers.氟司喹南不影响健康志愿者对模拟直立性应激的全身和局部血管反应。
Br J Clin Pharmacol. 1992 Sep;34(3):207-14. doi: 10.1111/j.1365-2125.1992.tb04126.x.
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Differential inotropic effects of flosequinan in ventricular muscle from normal ferrets versus patients with end-stage heart failure.氟司喹南对正常雪貂与终末期心力衰竭患者心室肌的变力作用差异。
Br J Pharmacol. 1992 Jul;106(3):511-6. doi: 10.1111/j.1476-5381.1992.tb14367.x.