Nayler W G
Department of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australia.
J Cardiovasc Pharmacol. 1994;24 Suppl A:S12-7.
Hypertension is a complex disease, the treatment of which should not only lower systolic and diastolic blood pressure but also attenuate the secondary consequences of the disease. These include vascular injury (including atherosclerosis), stroke, left ventricular hypertrophy, and renal damage. To establish whether the long-acting, vascular-selective calcium antagonist amlodipine attenuates some of these secondary consequences of hypertension, 5-week-old stroke-prone hypertensive and 8-week-old spontaneously hypertensive rats were treated (orally) with 5 mg/kg/day and 10 mg/kg/day amlodipine, respectively, for 30 weeks. The treatment resulted in a significant lowering of systolic blood pressure, accompanied by reduced cardiac hypertrophy and prolonged survival. Evidence for a protective effect of amlodipine on the vasculature was obtained by treating cholesterol-fed rabbits with 1-5 mg/kg/body weight/day. This resulted in a reduction in vascular Ca2+ overloading and a reduced incidence of sudanophilic lesion formation. Protection against ischemia-induced changes in the myocardium included a reduction in the ischemia-induced externalization of endothelin-1 binding sites.
高血压是一种复杂的疾病，其治疗不仅应降低收缩压和舒张压，还应减轻该疾病的继发性后果。这些后果包括血管损伤（包括动脉粥样硬化）、中风、左心室肥厚和肾损伤。为了确定长效、血管选择性钙拮抗剂氨氯地平是否能减轻高血压的一些继发性后果，分别对5周龄的易中风高血压大鼠和8周龄的自发性高血压大鼠进行了为期30周的治疗（口服），剂量分别为5毫克/千克/天和10毫克/千克/天。治疗导致收缩压显著降低，同时心脏肥厚减轻，生存期延长。通过给喂食胆固醇的兔子每天按1 - 5毫克/千克体重的剂量给药，获得了氨氯地平对血管有保护作用的证据。这导致血管钙超载减少，嗜苏丹性病变形成的发生率降低。对心肌缺血诱导变化的保护作用包括减少缺血诱导的内皮素 - 1结合位点的外化。
