Goldberg A I, Dunlay M C, Sweet C S
Merck Research Laboratories, West Point, PA 19486, USA.
J Hypertens Suppl. 1995 Jul;13(1):S77-80. doi: 10.1097/00004872-199507001-00012.
To examine the safety profile and tolerability of losartan potassium (losartan), a selective antagonist of the angiotensin II type 1 (AT1) receptor.
Approximately 2000 hypertensive patients were treated in double-blind clinical trials with losartan, placebo or other antihypertensive drug classes.
Headache (14.1%), upper respiratory infection (6.5%), dizziness (4.1%), asthenia/fatigue (3.8%) and coughing (3.1%) were the most commonly reported clinical adverse experiences in patients treated with losartan. These adverse experiences were also commonly reported in patients treated with a placebo: 17.2, 5.6, 2.4, 3.9 and 2.6%, respectively. A dry cough was reported by 8.8% of patients treated with angiotensin converting enzyme (ACE) inhibitors, statistically greater than that reported in patients treated with losartan and placebo, 3.1 and 2.6%, respectively (P < 0.001, losartan versus ACE inhibitors). Only dizziness was more often considered drug-related in losartan-treated patients (2.4%) than in patients who received placebo (1.3%). In controlled clinical trials, losartan was better tolerated than other antihypertensive agents as determined by the incidence of patients reporting any drug-related adverse experiences. The rate of withdrawal due to clinical adverse experiences in patients treated with losartan was 2.3% compared to 3.7% in patients treated with a placebo. No adverse laboratory results were unexpected or of clinical importance. First-dose hypotension occurred rarely with losartan, and withdrawal effects such as rebound hypertension were not observed in clinical trials. There were no clinically important differences in the clinical or laboratory safety profiles for the demographic subgroups of age, sex or race.
In controlled clinical trials losartan has demonstrated an excellent tolerability profile.
研究血管紧张素II 1型（AT1）受体选择性拮抗剂氯沙坦钾（氯沙坦）的安全性和耐受性。
约2000名高血压患者在双盲临床试验中接受氯沙坦、安慰剂或其他抗高血压药物治疗。
头痛（14.1%）、上呼吸道感染（6.5%）、头晕（4.1%）、乏力/疲劳（3.8%）和咳嗽（3.1%）是接受氯沙坦治疗患者中最常报告的临床不良事件。这些不良事件在接受安慰剂治疗的患者中也很常见，分别为17.2%、5.6%、2.4%、3.9%和2.6%。8.8%接受血管紧张素转换酶（ACE）抑制剂治疗的患者报告干咳，在统计学上高于接受氯沙坦和安慰剂治疗的患者，分别为3.1%和2.6%（P<0.001，氯沙坦与ACE抑制剂相比）。在接受氯沙坦治疗的患者中，只有头晕被认为与药物相关的频率（2.4%）高于接受安慰剂的患者（1.3%）。在对照临床试验中，根据报告任何与药物相关不良事件的患者发生率，氯沙坦的耐受性优于其他抗高血压药物。接受氯沙坦治疗的患者因临床不良事件而停药的比例为2.3%，而接受安慰剂治疗的患者为3.7%。没有出现意外的不良实验室结果或具有临床重要性的结果。氯沙坦很少发生首剂低血压，并且在临床试验中未观察到诸如反跳性高血压等撤药效应。在年龄、性别或种族的人口统计学亚组的临床或实验室安全性方面没有临床重要差异。
在对照临床试验中，氯沙坦已证明具有出色的耐受性。
