Burges R A
Pfizer Central Research, Kent, UK.
J Hum Hypertens. 1991 Aug;5 Suppl 1:49-54.
Amlodipine is a 1,4-dihydropyridine calcium antagonist which, although structurally related to nifedipine, has a number of important distinguishing properties. A high oral bioavailability of amlodipine has been demonstrated in a number of animal species and man, together with a long elimination half-life. In vitro studies have demonstrated a slow onset of action which is consistent with the findings from receptor binding studies which show that amlodipine binds to receptor sites with slow rates of association and dissociation. These studies have also shown that amlodipine may interact with both dihydropyridine and diltiazem binding sites. In vivo animal experiments have confirmed the gradual onset of action observed in vitro and have shown amlodipine to have sustained antihypertensive effects with no change in heart rate. Amlodipine has also been shown to attenuate the cardiac hypertrophy associated with the development of hypertension in spontaneously hypertensive rats. Animal studies have clearly demonstrated the mild natriuretic and diuretic properties of amlodipine. The pharmacodynamic and pharmacokinetic properties of amlodipine make this drug an optimal choice of treatment for the control of hypertension with once daily administration.
氨氯地平是一种1,4 - 二氢吡啶类钙拮抗剂，尽管在结构上与硝苯地平相关，但具有许多重要的区别特性。在多种动物物种和人类中已证实氨氯地平具有高口服生物利用度，以及长消除半衰期。体外研究表明其起效缓慢，这与受体结合研究结果一致，该研究表明氨氯地平以缓慢的结合和解离速率与受体位点结合。这些研究还表明氨氯地平可能与二氢吡啶和地尔硫䓬结合位点相互作用。体内动物实验证实了体外观察到的起效缓慢，并表明氨氯地平具有持续的降压作用，心率无变化。氨氯地平还被证明可减轻自发性高血压大鼠与高血压发展相关的心脏肥大。动物研究清楚地证明了氨氯地平具有轻度的利钠和利尿特性。氨氯地平的药效学和药代动力学特性使其成为每日一次给药控制高血压的最佳治疗选择。
