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昔莫特罗的药理学:心脏自主控制调节的基础。

The pharmacology of xamoterol: a basis for modulation of the autonomic control of the heart.

作者信息

Snow H M

机构信息

ICI Pharmaceuticals, Macclesfield, Cheshire.

出版信息

Br J Clin Pharmacol. 1989;28 Suppl 1(Suppl 1):3S-13S. doi: 10.1111/j.1365-2125.1989.tb03569.x.

Abstract
  1. Xamoterol (Corwin, Carwin, Corwil, Xamtol, ICI 118,587) is a beta-adrenoceptor partial agonist which is of benefit in the chronic treatment of heart failure (e.g. The German and Austrian Xamoterol Study Group, 1988). These results contrast with those obtained with other beta-adrenoceptor drugs, prenalterol and pirbuterol which were unsuccessful on chronic dosing (Currie et al., 1984; Glover et al., 1985). 2. Unlike prenalterol and pirbuterol, xamoterol has no significant agonist activity at the beta 2-adrenoceptor and has shown no tachyphylaxis in animals or man. 3. The overall action of xamoterol is to modulate sympathetic control of the heart such that at rest and at low levels of exercise the heart receives inotropic support whilst during more severe exercise, heart rate is reduced. In patients with left ventricular dysfunction these effects lead to an improvement in the relation between filling pressure and cardiac output at all levels of activity such that a given cardiac output is achieved with a lower filling pressure. It is suggested that this alteration in the pattern of cardiac activity over a long period of time results in a beneficial adaptation of the myocardium and is a possible explanation of the observed clinical improvement.
摘要
  1. 克仑特罗(Corwin、Carwin、Corwil、Xamtol、ICI 118,587)是一种β肾上腺素能受体部分激动剂,对心力衰竭的长期治疗有益(例如,德国和奥地利克仑特罗研究组,1988年)。这些结果与其他β肾上腺素能药物普瑞特罗和吡布特罗的结果形成对比,后者长期给药未成功(柯里等人,1984年;格洛弗等人,1985年)。2. 与普瑞特罗和吡布特罗不同,克仑特罗在β2肾上腺素能受体上没有显著的激动剂活性,并且在动物或人类中未显示出快速耐受性。3. 克仑特罗的总体作用是调节心脏的交感神经控制,使得在静息和低强度运动时心脏获得正性肌力支持,而在更剧烈运动时心率降低。在左心室功能不全的患者中,这些作用导致在所有活动水平下充盈压与心输出量之间的关系得到改善,从而以较低的充盈压实现给定的心输出量。有人认为,这种长期心脏活动模式的改变导致心肌有益的适应性变化,这可能是观察到临床改善的一种解释。

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Modulation of the autonomic control of the failing heart.
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Long-term studies with xamoterol in heart failure.关于xamoterol治疗心力衰竭的长期研究。
Br J Clin Pharmacol. 1989;28 Suppl 1(Suppl 1):53S-58S. doi: 10.1111/j.1365-2125.1989.tb03573.x.
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Focus on diastolic dysfunction: a new approach to heart failure therapy.关注舒张功能障碍:心力衰竭治疗的新方法。
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本文引用的文献

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Effects of xamoterol (ICI 118,587) in asthmatic patients.羟甲特罗(ICI 118,587)对哮喘患者的影响。
Br J Clin Pharmacol. 1984 Oct;18(4):597-601. doi: 10.1111/j.1365-2125.1984.tb02510.x.
7
Operational models of pharmacological agonism.药理学激动作用的操作模型。
Proc R Soc Lond B Biol Sci. 1983 Dec 22;220(1219):141-62. doi: 10.1098/rspb.1983.0093.

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