Drugs. 1987;34 Suppl 3:139-48. doi: 10.2165/00003495-198700343-00030.
The role of felodipine, a new calcium antagonist, as monotherapy in mild and moderate hypertension (supine diastolic blood pressure between 95 and 100mm Hg: phase V) was investigated in a placebo-controlled, double-blind study of 109 patients from 13 centres using 3 different doses. After a 2-week placebo run-in phase the patients were randomised in a double-blind fashion to receive felodipine 2.5mg bid (32 patients), 5 mg bid (30 patients), 10mg bid (24 patients) or placebo (25 patients). Clinical and laboratory measurements were performed after 1, 3 and 8 weeks. 94 patients completed the study. Felodipine reduced supine systolic blood pressure by 22mm Hg from baseline after 8 weeks' treatment on 2.5mg bid, 24mm Hg on 5mg bid and 24mm Hg on 10mg bid at 2 hours after dosage. The corresponding reduction in the placebo group was 6mm Hg. There was a reduction in supine diastolic blood pressure from baseline of 13mm Hg on felodipine 2.5mg bid, 14mm Hg on felodipine 5mg bid and 20mm Hg on felodipine 10mg bid, with no reduction in patients receiving placebo. The percentage of patients completing the study who achieved a supine diastolic blood pressure of 90mm Hg or less after 8 weeks' treatment at 2 hours after dosage was 9% on placebo, 67% on felodipine 2.5mg bid, 57% on felodipine 5mg bid and 92% on felodipine 10mg bid; and at 12 hours after dosage those achieving target supine diastolic blood pressure was 17% on placebo, 37% on felodipine 2.5mg bid, 25% on felodipine 5mg bid and 62% on felodipine 10mg bid. Felodipine was generally well tolerated, although 10 patients on felodipine 10mg bid (42%), 1 on felodipine 5mg bid (3%) and 2 on felodipine 2.5mg bid (6%) withdrew from the study because of adverse effects. One serious adverse event, a myocardial infarction, occurred during the study in a patient with a history of postprandial non-exertional chest pain. In conclusion, felodipine monotherapy appreciably reduces blood pressure in mild and moderate hypertension without significant tachycardia in the short term. Doses of felodipine 2.5mg bid and 5mg bid are better tolerated than 10mg bid and can be recommended for initial treatment in this category of patients.
在一项安慰剂对照、双盲研究中，对来自13个中心的109例患者使用3种不同剂量，研究了新型钙拮抗剂非洛地平作为轻度和中度高血压（仰卧位舒张压在95至100mmHg之间：V期）单一疗法的作用。经过2周的安慰剂导入期后，患者以双盲方式随机分组，接受非洛地平2.5mg每日两次（32例患者）、5mg每日两次（30例患者）、10mg每日两次（24例患者）或安慰剂（25例患者）治疗。在第1、3和8周进行临床和实验室测量。94例患者完成了研究。非洛地平在2.5mg每日两次治疗8周后，给药后2小时仰卧位收缩压较基线降低22mmHg，5mg每日两次降低24mmHg，10mg每日两次降低24mmHg。安慰剂组相应的降低值为6mmHg。非洛地平2.5mg每日两次时仰卧位舒张压较基线降低13mmHg，5mg每日两次降低14mmHg，10mg每日两次降低20mmHg，接受安慰剂治疗的患者则无降低。在给药后2小时治疗8周后仰卧位舒张压达到90mmHg或更低的完成研究的患者百分比，安慰剂组为9%，非洛地平2.5mg每日两次组为67%，非洛地平5mg每日两次组为57%，非洛地平10mg每日两次组为92%；给药后12小时达到目标仰卧位舒张压的患者，安慰剂组为17%，非洛地平2.5mg每日两次组为37%，非洛地平5mg每日两次组为25%，非洛地平10mg每日两次组为62%。非洛地平一般耐受性良好，不过10mg每日两次组有10例患者（42%）、5mg每日两次组有1例患者（3%）、2.5mg每日两次组有2例患者（6%）因不良反应退出研究。在一名有餐后非劳力性胸痛病史的患者中，研究期间发生了1例严重不良事件，即心肌梗死。总之，非洛地平单一疗法可在短期内显著降低轻度和中度高血压患者的血压，且无明显心动过速。2.5mg每日两次和5mg每日两次的非洛地平剂量耐受性优于10mg每日两次，可推荐用于此类患者的初始治疗。
