Ogihara T, Arakawa K
Department of Geriatric Medicine, Osaka University, Suita, Japan.
J Hum Hypertens. 1999 Jan;13 Suppl 1:S27-31; discussion S33-4. doi: 10.1038/sj.jhh.1000746.
Clinical trials of candesartan cilexetil conducted in Japan are reviewed. Candesartan cilexetil inhibited the pressor response to intravenous angiotensin II in healthy volunteers, with peak effects observed at 4 or 8 h after oral dosing; suppressing effects persisted up to 24 h. In 14 multicentre studies with 928 hypertensive patients treated for 8 to 12 weeks, candesartan cilexetil had an efficacy rate (reduction of systolic/diastolic blood pressure > or = 20/10 mm Hg and/or mean blood pressure > or = 13 mm Hg) of 72% and 63%, and an adverse effect rate of 9.9% and 7.3%, in patients with mild-to-moderate essential hypertension and those with impaired renal function, respectively. When data for elderly patients were analysed, there was no difference in efficacy and tolerability compared to non-elderly patients. In a double-blind comparative study, candesartan cilexetil was superior to enalapril in hypertensive patients: efficacy rate, 74% vs 66% (NS); adverse symptom rate, 10.4% vs 27.3% (P < 0.01); incidence of cough, 1.5% vs 14.8% (P < 0.01). Treatment with 2-8 mg of candesartan cilexetil once daily for 8 to 12 weeks reduced the left ventricular mass index without deterioration of cardiac function. In conclusion, 4-12 mg of candesartan cilexetil once daily is effective and well tolerated in patients with essential hypertension, including elderly patients, those with severe hypertension, and hypertensive patients with renal insufficiency. Its improved tolerability profile over angiotensin-converting enzyme inhibitors, as well as its end-organ protective effects, suggest that candesartan cilexetil is useful as a first-line antihypertensive drug.
对在日本开展的坎地沙坦酯临床试验进行了综述。坎地沙坦酯可抑制健康志愿者对静脉注射血管紧张素II的升压反应，口服给药后4或8小时观察到峰值效应；抑制作用可持续长达24小时。在14项多中心研究中，928例高血压患者接受了8至12周的治疗，坎地沙坦酯在轻度至中度原发性高血压患者和肾功能受损患者中的有效率（收缩压/舒张压降低≥20/10 mmHg和/或平均血压降低≥13 mmHg）分别为72%和63%，不良反应率分别为9.9%和7.3%。对老年患者的数据进行分析时，与非老年患者相比，疗效和耐受性没有差异。在一项双盲对照研究中，坎地沙坦酯在高血压患者中优于依那普利：有效率分别为74%和66%（无显著性差异）；不良症状率分别为10.4%和27.3%（P<0.01）；咳嗽发生率分别为1.5%和14.8%（P<0.01）。每日一次服用2 - 8 mg坎地沙坦酯，持续8至12周，可降低左心室质量指数，且心功能无恶化。总之，每日一次服用4 - 12 mg坎地沙坦酯对原发性高血压患者有效且耐受性良好，这些患者包括老年患者、重度高血压患者以及肾功能不全的高血压患者。其相对于血管紧张素转换酶抑制剂而言更好的耐受性，以及对靶器官的保护作用，表明坎地沙坦酯可作为一线抗高血压药物。
