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非洛地平,一种新型血管扩张药物:对高血压患者血压、心脏、肾脏及体液的影响

Felodipine, a new vasodilating drug: blood pressure, cardiac, renal, and humoral effects in hypertensive patients.

作者信息

Leonetti G, Gradnik R, Terzoli L, Fruscio M, Rupoli L, Zanchetti A

出版信息

J Cardiovasc Pharmacol. 1984 May-Jun;6(3):392-8.

PMID:6202963
Abstract

We studied the antihypertensive action of felodipine, a new dihydropyridine vasodilator interfering with intracellular calcium mechanisms, in 11 patients with essential hypertension whose supine blood pressure averaged 181/109 mm Hg after 5 days of placebo administration. Felodipine, 12.5 mg t.i.d., for 3 days, caused a marked reduction (-39/-19 mm Hg) of supine systolic and diastolic pressures. Doses of 25 and 50 mg t.i.d., for three consecutive days, caused only a slight further reduction of blood pressure. At the highest dose tested all patients had their supine blood pressure brought down to values below 150 mm Hg systolic and 90 mm Hg diastolic at all six daily measurements. The antihypertensive effect was of the same magnitude when the patients lay supine or stood upright. Lowering of blood pressure was accompanied by tachycardia, which was quite moderate after the 12.5 mg t.i.d. dose, but more conspicuous with the two higher doses. There was some increase in plasma renin activity and in plasma aldosterone. A significant decrease in renal sodium and water excretion occurred only during administration of the highest dose of 50 mg t.i.d., when reduction in blood pressure was pronounced and there were reflex increases in plasma renin activity and plasma aldosterone.

摘要

我们对非洛地平(一种干扰细胞内钙机制的新型二氢吡啶类血管扩张剂)的降压作用进行了研究,研究对象为11例原发性高血压患者,这些患者在服用5天安慰剂后仰卧位血压平均为181/109 mmHg。非洛地平,每日3次,每次12.5 mg,服用3天,可使仰卧位收缩压和舒张压显著降低(-39/-19 mmHg)。连续3天每日3次服用25 mg和50 mg剂量,血压仅进一步轻微降低。在所有每日6次测量中,在测试的最高剂量下,所有患者的仰卧位血压均降至收缩压低于150 mmHg和舒张压低于90 mmHg。无论患者仰卧还是直立,降压效果相同。血压降低伴有心动过速,每日3次服用12.5 mg剂量后心动过速相当轻微,但在两个较高剂量时更为明显。血浆肾素活性和血浆醛固酮有所增加。仅在每日3次服用最高剂量50 mg时,肾钠和水排泄显著减少,此时血压明显降低,血浆肾素活性和血浆醛固酮出现反射性增加。

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