Ogihara T, Higashimori K, Masuo K, Mikami H
Department of Geriatric Medicine, Osaka University Medical School, Japan.
Clin Ther. 1993 Jul-Aug;15(4):684-91.
After a 1-week placebo control period, six hypertensive patients (mean age, 67 years) each received single doses of 1, 2.5, and 5 mg of TCV-116 at 2- to 3- day intervals. Systolic and diastolic blood pressures were significantly lower after the final dose (5 mg) of TCV-116 than on the last day of the placebo period. Blood pressures were decreased after each dose of TCV-116 in a dose-dependent fashion from 2 hours after administration and reached a nadir at 4 to 6 hours. After 2.5 and 5 mg of TCV-116, the hypotensive effect was sustained for 24 hours. Pulse rate did not change significantly. Plasma renin activity and angiotensin I levels increased in a dose-dependent fashion after TCV-116, but the changes were not significant. No changes were noted in plasma aldosterone or angiotensin II levels. One patient reported mild light-headedness after 5 mg of TCV-116. No other side effects or abnormal laboratory tests results were noted. It appears that TCV-116 is a safe and effective antihypertensive agent.
在为期1周的安慰剂对照期后，6名高血压患者（平均年龄67岁）每隔2至3天分别接受1、2.5和5毫克的TCV - 116单剂量给药。在服用TCV - 116的最后一剂（5毫克）后，收缩压和舒张压显著低于安慰剂期的最后一天。服用TCV - 116的每一剂后，血压自给药后2小时起呈剂量依赖性下降，并在4至6小时达到最低点。服用2.5毫克和5毫克的TCV - 116后，降压作用持续24小时。脉搏率无显著变化。服用TCV - 116后，血浆肾素活性和血管紧张素I水平呈剂量依赖性升高，但变化不显著。血浆醛固酮或血管紧张素II水平无变化。1名患者在服用5毫克的TCV - 116后报告有轻度头晕。未观察到其他副作用或异常实验室检查结果。看来TCV - 116是一种安全有效的抗高血压药物。
