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[磷酸二酯酶III抑制剂的抗缺血作用]

[The anti-ischemic effect of phosphodiesterase III inhibitors].

作者信息

Schlepper M

机构信息

Max-Planck-Institut für Physiologische und Klinische Forschung Kerckhoff-Klinik GmbH, Bad Nauheim.

出版信息

Z Kardiol. 1994;83 Suppl 2:27-36.

PMID:8091822
Abstract

When enoximone is acutely administered to patients with stable angina and angiographically proven relevant coronary stenosis i.v. application of 0.75 mg/kg exhibits pronounced antiischemic effects. This could be observed in patients during exercise and in those in whom the ischemia was provoked by rapid cardiac stimulation. The antiischemic effects were documented by relief of symptoms, reduction of ST-depression, improvement of impaired myocardial wall motion, decrease to normalization of pathologically elevated filling pressure, amelioration of coronary blood flow as evidenced by myocard scintigraphy and washout time of an intracoronarily injected echo-contrast medium. There was also a definite improvement of ischemia-caused mitral regurgitation. Similar observations were found when the drug was injected in the diseased coronary arteries in a small dose (0.075 mg/kg) so that peripheral effects were not present. In comparison to the Ca(++)-blocker Gallopamil the antiischemic effects of Enoximone were more pronounced, a synergistic action was, however, observed. Negative dromotropic effects of Gallopamil could be abolished by Enoximone. With oral administration of the drug over a period of one week antiischemic effects could also be documented with Holter monitoring as well as during exercise. There was a reduction of ST-depression both at spontaneously occurring ischemic episodes and during exercise, in the number and duration of episodes of silent ischemia, particularly, however, a decrease in symptomatic episodes. In none of the patients under study proarrhythmic effects were observed.

摘要

当对稳定型心绞痛且经血管造影证实存在相关冠状动脉狭窄的患者静脉注射依诺昔酮时,0.75毫克/千克的剂量表现出明显的抗缺血作用。这在运动患者以及通过快速心脏刺激诱发缺血的患者中均可观察到。抗缺血作用通过症状缓解、ST段压低减轻、受损心肌壁运动改善、病理性升高的充盈压降低至正常、心肌闪烁显像显示冠状动脉血流改善以及冠状动脉内注射超声造影剂的清除时间得以证实。缺血所致的二尖瓣反流也有明显改善。当以小剂量(0.075毫克/千克)将该药物注入病变冠状动脉时,也发现了类似的观察结果,此时不存在外周效应。与钙通道阻滞剂加洛帕米相比,依诺昔酮的抗缺血作用更为明显,不过观察到了协同作用。加洛帕米的负性变传导作用可被依诺昔酮消除。在为期一周的口服给药期间,动态心电图监测以及运动期间也证实了抗缺血作用。自发性缺血发作以及运动期间的ST段压低均有所降低,无症状性缺血发作的次数和持续时间减少,尤其是有症状发作减少。在所研究的患者中均未观察到促心律失常作用。

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