摘要

OBJECTIVES:We aimed to compare the effects of the angiotensin II receptor blocker (ARB) olmesartan versus the calcium channel blocker (CCB) amlodipine on coronary endothelial dysfunction in patients with hypertension.
BACKGROUND:Angiotensin II receptor blockers are thought to have greater beneficial effects than CCBs on coronary vasomotion by directly blocking action of angiotensin II.
METHODS:Twenty-six patients with untreated essential hypertension were prospectively assigned to treatment with either olmesartan (27.7 +/- 12.4 mg/day, n = 13) or amlodipine (5.6 +/- 1.5 mg/day, n = 13) for 12 weeks. Changes of corrected myocardial blood flow (DeltaMBF) and coronary vascular resistance (DeltaCVR) from rest to cold pressor were measured by using 15O-water and positron emission tomography before and after treatment. Blood biomarkers including lipids, glucose, insulin, high-sensitivity C-reactive protein, interleukin-6, tumor necrosis factor-alpha, and superoxide dismutase (SOD) were also measured.
RESULTS:Olmesartan and amlodipine reduced blood pressure (BP) to the same extent (-28.7 +/- 16.2 mm Hg vs. -26.7 +/- 10.8 mm Hg). In the olmesartan group, DeltaMBF tended to be greater (-0.15 +/- 0.19 ml/g/min vs. 0.03 +/- 0.17 ml/g/min, p = 0.09 by 2-way analysis of variance), and DeltaCVR was significantly decreased (7.9 +/- 23.5 mm Hg/[ml/g/min] vs. -16.6 +/- 18.0 mm Hg/[ml/g/min], p < 0.05) after treatment, whereas these parameters did not change in the amlodipine group (DeltaMBF: -0.15 +/- 0.12 ml/g/min vs. -0.12 +/- 0.20 ml/g/min; DeltaCVR: 6.5 +/- 18.2 mm Hg/[ml/g/min] vs. 4.8 +/- 23.4 mm Hg/[ml/g/min]). Serum SOD activity tended to increase (4.74 +/- 4.77 U/ml vs. 5.57 +/- 4.74 U/ml, p = 0.07 by 2-way analysis of variance) only in the olmesartan group.
CONCLUSIONS:Olmesartan, but not amlodipine, improved endothelium-dependent coronary dilation in hypertensive patients independent of BP reduction. These beneficial effects on coronary vasomotion might be via an antioxidant property of ARBs.

译文

目的: 我们旨在比较血管紧张素 II 受体阻滞剂 (ARB) 奥美沙坦与钙通道阻滞剂 (CCB) 氨氯地平对高血压患者冠状动脉内皮功能障碍的影响。
背景: 血管紧张素 ⅱ 受体阻滞剂被认为通过直接阻断血管紧张素 ⅱ 的作用,对冠状动脉血管舒缩有比 CCBs 更大的有益作用。
方法: 26 名未经治疗的高血压患者被前瞻性地分配到奥美沙坦 (27.7/-12.4 毫克/天,n = 13) 或氨氯地平 (5.6/-1.5 毫克/天, n = 13) 持续 12 周。使用 15o-水和正电子发射断层扫描测量治疗前后从休息到冷加压的校正心肌血流量 (DeltaMBF) 和冠状动脉血管阻力 (DeltaCVR) 的变化。血液生物标志物包括血脂、葡萄糖、胰岛素、高敏 C 反应蛋白、 interleukin-6 、肿瘤坏死因子-α 和超氧化物歧化酶 (SOD) 也被测量。
结果: 奥美沙坦和氨氯地平在相同程度上降低了血压 (BP) (-28.7/-16.2毫米 Hg vs.-26.7/-10.8毫米 Hg)。在奥美沙坦组中,DeltaMBF 趋于更大 (-0.15/-0.19 ml/g/min vs.0.03/-0.17 ml/g/min,2-方差分析 p = 0.09), deltaCVR 显著降低 (7.9/-23.5毫米 Hg/[ml/g/min] vs.-16.6/-18.0毫米 Hg/[ml/g/min],p <0.05) 治疗后,而这些参数在氨氯地平组中没有变化 (DeltaMBF:-0.15/-0.12 ml/g/min vs.-0.12/-0.20 ml/g/min; DeltaCVR: 6.5/-18.2毫米汞柱/[ml/g/min] vs.4.8/-23.4毫米汞柱/[ml/g/min])。仅在奥美沙坦组中,血清 SOD 活性有增加的趋势 (4.74/-4.77 U/ml vs.5.57/-4.74 U/ml,双向方差分析 p = 0.07)。
结论: 奥美沙坦,而不是氨氯地平,改善高血压患者的内皮依赖性冠状动脉扩张,独立于血压降低。这些对冠状动脉血管舒缩的有益作用可能是通过 ARBs 的抗氧化特性。

Amlodipine

心血管 高血压、钙离子拮抗药 药物
概述  :  

功效应用氨氯地平为钙离子拮抗药,可用于治疗各种类型高血压。药理作用氨氯地平是一个外周动脉血管扩张剂,它直接作用于血管平滑肌,从而降低外周血管阻力和血压。氨氯地平能够缓解心绞痛。药代动力学给予口服本品治疗剂量后,6~12小时血药浓度达至高峰,绝对生物利用度为64%~80%,本品的生物利用度不受摄入食物的影响。氨氯地平通过肝脏被广泛(约90%)代谢为无活性的代谢产物,其他10%以原药形式排出,60%的代谢物经尿液排出,连续每日给药7~8天后,氨氯地平的血药浓度达至稳态。氨氯地平的药代动力学不受肾功能

Amlodipine

释义   n. 氨氯地平(抗高血压药)

例句   Amlodipine at therapeutic dose might be effective and safe for the treatment of chronic heart failure. 

治疗剂量的氨氯地平是治疗慢性心功能不全较为理想的药物。


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