Mace P J, Stallard T J, Littler W A
Eur J Clin Pharmacol. 1985;29(4):383-9. doi: 10.1007/BF00613449.
Felodipine, a selective arteriolar dilator, was given to 13 hypertensive patients to assess its hypotensive effects and duration of action. Nine patients were treated with 5 mg three times a day and 4 with 10 mg three times a day. Mean blood pressures fell with both treatment regimens: 5 mg placebo 170/103 mmHg; 5 mg felodipine 148/91 mmHg; 10 mg placebo 154/93 mmHg; 10 mg felodipine 137/82 mmHg. Heart rates increased as blood pressures fell with both treatments. However, in the patients given 5 mg three times a day this effect was less noticeable after successive doses. Plasma concentrations of noradrenaline, both resting and tilted, increased after felodipine. There was a negative correlation between the fall in blood pressure and the increase in noradrenaline, suggesting that those patients with good baroreceptor reflexes were better able to counteract the effects of vasodilatation. Four of the nine patients treated with 5 mg felodipine three times a day experienced mild and transient adverse effects. Of the four patients treated with 10 mg three times a day, three experienced moderate to severe headache, and for this reason recruitment into this group was stopped. Felodipine at a divided daily dose of 15 mg effectively lowered blood pressure.
非洛地平是一种选择性小动脉扩张剂，对13名高血压患者进行给药以评估其降压效果和作用持续时间。9名患者每日3次服用5毫克，4名患者每日3次服用10毫克。两种治疗方案均使平均血压下降：5毫克安慰剂组为170/103毫米汞柱；5毫克非洛地平组为148/91毫米汞柱；10毫克安慰剂组为154/93毫米汞柱；10毫克非洛地平组为137/82毫米汞柱。随着两种治疗使血压下降，心率增加。然而，在每日3次服用5毫克的患者中，连续给药后这种效应不太明显。服用非洛地平后，静息和倾斜状态下的去甲肾上腺素血浆浓度均升高。血压下降与去甲肾上腺素升高之间存在负相关，这表明压力感受器反射良好的患者更能抵消血管扩张的影响。每日3次服用5毫克非洛地平的9名患者中有4名出现轻度短暂不良反应。在每日3次服用10毫克的4名患者中，3名出现中度至重度头痛，因此停止招募该组患者。每日分剂量15毫克的非洛地平可有效降低血压。
