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布新洛尔治疗原发性高血压

Bucindolol in essential hypertension.

作者信息

Reid J L, Curzio J, Vincent J

出版信息

Int J Clin Pharmacol Res. 1985;5(5):293-301.

PMID:2866166
Abstract

The effects of bucindolol a new nonselective beta blocker were studied after short-term dosing and for up to six months in eight patients with essential hypertension. Bucindolol 100 mg acutely lowered supine and erect systolic and diastolic pressure without orthostatic features and without increases or decreases in heart rate. Plasma noradrenaline increased, but plasma renin activity fell. Long-term dosing of 100-400 mg/day led to modest decreases in blood pressure. The duration of the hypotensive effect after multiple dosing ranged from six to ten hours. After long-term dosing there was evidence of marked nonselective beta blockade but not of alpha 1 blockade from the responses to intravenous isoprenaline and phenylephrine respectively. In six out of eight patients the plasma creatinine phosphokinase rose transiently above the normal range. The increase appeared to be of muscle origin and was associated with myalgia in one patient. Bucindolol is a nonselective beta blocker, possibly with other vasodilator properties. These do not appear to be mediated by alpha blockade.

摘要

对8例原发性高血压患者短期服用及长达6个月服用新型非选择性β受体阻滞剂布新洛尔的效果进行了研究。布新洛尔100mg可使仰卧位和直立位收缩压及舒张压急性降低,无体位性特征,心率无增减。血浆去甲肾上腺素升高,但血浆肾素活性降低。每日100 - 400mg长期给药导致血压适度下降。多次给药后降压作用持续时间为6至10小时。长期给药后,分别根据对静脉注射异丙肾上腺素和去氧肾上腺素的反应,有明显非选择性β受体阻滞的证据,但无α1受体阻滞的证据。8例患者中有6例血浆肌酸磷酸激酶短暂升至正常范围以上。这种升高似乎源于肌肉,且1例患者伴有肌痛。布新洛尔是一种非选择性β受体阻滞剂,可能具有其他血管舒张特性。这些特性似乎不是由α受体阻滞介导的。

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Bucindolol, a beta-adrenoceptor blocker with vasodilatory action: its effect in systemic hypertension.
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