Easthope Stephanie E, Jarvis Blair
Adis International Limited, Auckland, New Zealand.
Drugs. 2002;62(8):1253-87. doi: 10.2165/00003495-200262080-00016.
Candesartan cilexetil is converted to the angiotensin II receptor antagonist candesartan during absorption from the gastrointestinal tract. The selective and competitive binding of candesartan to the angiotensin II type 1 (AT(1)) receptor prevents binding of angiotensin II, a key mediator in the renin-angiotensin system. Significant reductions in systolic BP and diastolic BP are achieved with a once-daily dosage of candesartan cilexetil 2 to 32 mg/day in patients with mild to moderate hypertension. In randomised studies, candesartan cilexetil 8 to 16 mg/day was at least as effective as therapeutic dosages of losartan or other angiotensin II receptor antagonists. At a dosage of up to 32 mg/day candesartan cilexetil demonstrated greater antihypertensive efficacy than losartan 50 or 100 mg/day. In comparative trials, candesartan cilexetil demonstrated similar or greater antihypertensive efficacy compared with enalapril or hydrochlorothiazide and equivalent efficacy compared with amlodipine. The efficacy of candesartan cilexetil is not affected by age, and the drug provided significant BP reductions in Black patients and in those with severe hypertension. Long-term clinical studies to assess the effects of treatment with candesartan cilexetil on cardiovascular morbidity and mortality are ongoing. Regression of left ventricular hypertrophy has been seen with candesartan cilexetil treatment in patients with hypertension. Furthermore, the drug has favourable effects on renal function in patients with hypertension with or without coexisting diabetes mellitus. Renal vascular resistance and albumin excretion were reduced following treatment with candesartan cilexetil. Glucose homeostasis and lipid metabolism were not affected by treatment in patients with type 2 diabetes mellitus. Candesartan cilexetil is well tolerated and is not associated with cough, a common adverse effect of angiotensin converting enzyme inhibitor treatment. A pooled analysis of clinical trials found that the tolerability profile of candesartan cilexetil is not significantly different from that of placebo. Adverse events are not dose-related and are generally of mild to moderate severity.
Candesartan cilexetil is an effective antihypertensive agent with a tolerability profile similar to that of placebo. Comparative data indicate that candesartan cilexetil has antihypertensive efficacy equivalent to that of other major classes of antihypertensive agents and has a long duration of action. Therefore, candesartan cilexetil is a useful therapeutic option in the management of patients with hypertension.
坎地沙坦酯在从胃肠道吸收过程中转化为血管紧张素II受体拮抗剂坎地沙坦。坎地沙坦对血管紧张素II 1型（AT(1)）受体的选择性和竞争性结合可防止血管紧张素II（肾素-血管紧张素系统中的关键介质）的结合。对于轻度至中度高血压患者，每日一次服用2至32毫克/天的坎地沙坦酯可显著降低收缩压和舒张压。在随机研究中，8至16毫克/天的坎地沙坦酯至少与治疗剂量的氯沙坦或其他血管紧张素II受体拮抗剂一样有效。在高达32毫克/天的剂量下，坎地沙坦酯显示出比50或100毫克/天的氯沙坦更强的降压效果。在比较试验中，坎地沙坦酯与依那普利或氢氯噻嗪相比显示出相似或更强的降压效果，与氨氯地平相比效果相当。坎地沙坦酯的疗效不受年龄影响，该药物在黑人患者和重度高血压患者中也能显著降低血压。评估坎地沙坦酯治疗对心血管发病率和死亡率影响的长期临床研究正在进行中。高血压患者使用坎地沙坦酯治疗可出现左心室肥厚消退。此外，该药物对伴有或不伴有糖尿病的高血压患者的肾功能有有利影响。坎地沙坦酯治疗后肾血管阻力和白蛋白排泄减少。2型糖尿病患者的治疗对葡萄糖稳态和脂质代谢无影响。坎地沙坦酯耐受性良好，且不引起咳嗽（血管紧张素转换酶抑制剂治疗的常见不良反应）。一项临床试验汇总分析发现，坎地沙坦酯的耐受性与安慰剂无显著差异。不良事件与剂量无关，一般为轻度至中度严重程度。
坎地沙坦酯是一种有效的抗高血压药物，其耐受性与安慰剂相似。比较数据表明，坎地沙坦酯的降压效果与其他主要抗高血压药物相当，且作用持续时间长。因此，坎地沙坦酯是治疗高血压患者的一种有用的治疗选择。
