Sever P S
Department of Clinical Pharmacology, Imperial College School of Medicine, St Mary's Hospital, London, UK.
Blood Press Suppl. 2000;1:19-22.
Potency and efficacy, duration of action, organ-specific effects and tolerability are the main considerations when choosing among antihypertensive therapies. Candesartan has been shown in in vitro animal models to bind insurmountably to the angiotensin II type 1 (AT1) receptor, thus providing effective blockade of all the major negative cardiovascular effects of angiotensin II. Its binding characteristics differentiate candesartan from other AT1-receptor blockers. Candesartan cilexetil has been found to produce a predictable and pronounced dose-dependent decrease in blood pressure, with placebo-like tolerability even at the highest doses studied. In comparison with the standard 50-mg dose of losartan, candesartan cilexetil, 16 mg, was significantly more effective in suppressing the renin-angiotensin system and in reducing trough diastolic blood pressure. Pooled results from placebo-controlled trials also indicate that candesartan cilexetil has equivalent efficacy to irbesartan. In addition, the extent of blood pressure lowering by candesartan cilexetil has been shown to be similar to that of agents in the other major classes of antihypertensive drugs, and to be effective in combination therapy with diuretics and calcium channel blockers. Candesartan cilexetil combines 24-h blood pressure lowering with placebo-like tolerability and is therefore an important advance in antihypertensive therapy.
在选择抗高血压治疗方法时，效力和疗效、作用持续时间、器官特异性效应和耐受性是主要考虑因素。在体外动物模型中已表明，坎地沙坦与1型血管紧张素II（AT1）受体具有不可逾越的结合，从而有效阻断血管紧张素II的所有主要负面心血管效应。其结合特性使坎地沙坦与其他AT1受体阻滞剂有所不同。已发现坎地沙坦酯可使血压产生可预测的、明显的剂量依赖性降低，即使在研究的最高剂量下也具有类似安慰剂的耐受性。与标准50毫克剂量的氯沙坦相比，16毫克的坎地沙坦酯在抑制肾素-血管紧张素系统和降低舒张压谷值方面明显更有效。安慰剂对照试验的汇总结果还表明，坎地沙坦酯与厄贝沙坦具有同等疗效。此外，坎地沙坦酯降低血压的程度已显示与其他主要类别的抗高血压药物相似，并且与利尿剂和钙通道阻滞剂联合治疗有效。坎地沙坦酯将24小时血压降低与类似安慰剂的耐受性相结合，因此是抗高血压治疗的一项重要进展。
