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新型血管扩张性钙拮抗剂非洛地平对高血压患者的降压及水钠平衡作用

Antihypertensive and water and sodium balance effects of felodipine, a new vasodilating calcium antagonist, in hypertensive patients.

作者信息

Leonetti G, Fruscio M, Terzoli L, Rupoli L, Gradnik R, Sampieri L, Cuspidi C, Boselli L, Bolla G, Zanchetti A

出版信息

Drugs. 1985;29 Suppl 2:185-91. doi: 10.2165/00003495-198500292-00033.

Abstract

Felodipine, a new dihydropyridine derivative with a selective action on vascular smooth muscle, was investigated in 2 short term studies in hypertensive patients. In the first study, oral administration of felodipine 12.5 mg three times daily in a preliminary tablet formulation for 3 days significantly reduced supine and upright blood pressure with only a slight increase in heart rate and no clinically relevant signs of sodium and water retention. By increasing each dose to 25 and 50 mg three times daily, there was a further, but quite moderate, decrease in blood pressure; however, this was accompanied by an increase in heart rate and a tendency towards a reduction of creatinine clearance and urinary sodium output. In the second study, a new oral formulation containing 10 mg felodipine, administered twice daily for 7 days, was effective in lowering blood pressure without a clinically relevant tachycardia. Following the first dose of felodipine, urinary sodium excretion was slightly increased while potassium excretion showed only minor changes. The new calcium antagonist, felodipine, lowers blood pressure without the clinically relevant adverse reactions commonly related to other direct vasodilator antihypertensive drugs.

摘要

非洛地平是一种对血管平滑肌有选择性作用的新型二氢吡啶衍生物,在两项针对高血压患者的短期研究中对其进行了调查。在第一项研究中,以初步片剂剂型每日三次口服12.5毫克非洛地平,连续服用3天,可显著降低仰卧位和直立位血压,心率仅略有增加,且无钠水潴留的临床相关体征。将每次剂量增加至每日三次25毫克和50毫克后,血压进一步但相当适度地下降;然而,这伴随着心率增加以及肌酐清除率和尿钠排出量有降低的趋势。在第二项研究中,一种含10毫克非洛地平的新型口服制剂,每日服用两次,连续服用7天,可有效降低血压,且无临床相关的心动过速。服用第一剂非洛地平后,尿钠排泄略有增加,而钾排泄仅有轻微变化。新型钙拮抗剂非洛地平可降低血压,且无通常与其他直接血管扩张剂类抗高血压药物相关的临床相关不良反应。

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