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硝酸酯贴片:作用持续时间与疗效丧失。关于硝酸酯类作用方式的思考。

Nitrate patches: duration of action and loss of efficacy. Reflections on the nitrates' mode of action.

作者信息

Bussmann W D

机构信息

Department of Cardiology, University of Frankfurt, Federal Republic of Germany.

出版信息

Eur J Clin Pharmacol. 1990;38 Suppl 1:S27-9. doi: 10.1007/BF01417562.

Abstract

Nitroglycerin patches deliver 0.003 mg nitroglycerin per minute through the skin. This small dose led to an antianginal effect in the short term and when applied with a nitrate pause at night also during sustained use. Minimal doses of i.v. nitroglycerin (0.025 mg) do have antianginal activity. This dose has no effect on pre- and afterload, but increases the diameter at the point of the stenosis. These findings are in accordance with newly won insights into the mode of action of nitrate in coronary heart disease. In the area of the stenosis EDRF cannot be produced by the intima because of damage resulting from arteriosclerotic plaques. EDRF is identical with NO. Thus, the administration of low doses of nitrates that act by means of the NO radical can increase the diameter in the stenosis, since the physiological dilator (EDRF) is no longer present. The increased flow caused by dilatation is the main factor in the antianginal activity of nitrates.

摘要

硝酸甘油贴片每分钟可透过皮肤释放0.003毫克硝酸甘油。这一小剂量在短期内可产生抗心绞痛作用,且在持续使用时,夜间配合硝酸盐停药期使用也能产生该作用。静脉注射最小剂量的硝酸甘油(0.025毫克)确实具有抗心绞痛活性。该剂量对前负荷和后负荷无影响,但可增加狭窄部位的血管直径。这些发现与最近对硝酸盐在冠心病中作用方式的新认识相符。在狭窄部位,由于动脉粥样硬化斑块造成的损伤,内膜无法产生内皮舒张因子(EDRF)。EDRF与一氧化氮(NO)相同。因此,通过NO自由基起作用的低剂量硝酸盐给药可增加狭窄部位的血管直径,因为生理舒张剂(EDRF)已不存在。扩张引起的血流增加是硝酸盐抗心绞痛活性的主要因素。

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