Pruss T P, Lamon K D, Hagen N S
Rorer Group Inc., Fort Washington, Pennsylvania.
J Int Med Res. 1988;16 Suppl 1:17A-22A.
The results of an extensive pre-clinical and clinical research programme indicate that celiprolol is a safe and effective treatment for both hypertension and angina pectoris. Celiprolol is well absorbed, is largely unmetabolized, and is excreted equally in the urine and bile. As a result of this pharmacokinetic profile celiprolol can be safely administered to the elderly and to patients with renal or hepatic impairment. Haemodynamic studies indicate that celiprolol lowers arterial blood pressure, and decreases both renal vascular resistance and peripheral vascular resistance. Celiprolol does not depress myocardial function, neither does it induce bronchoconstriction in asthmatic patients. Weak alpha 2-adrenoceptor antagonism, combined with beta 2-adrenoceptor agonism are thought to contribute to these properties. The antihypertensive efficacy of celiprolol, 200 mg/day, is comparable to that of propranolol, atenolol and nadolol. Moreover, the actions of celiprolol last for 24 h, and are accompanied by less resting bradycardia than that seen with other beta-blockers. The anti-anginal efficacy of celiprolol is similar to that of atenolol, propranolol and metoprolol. In addition, celiprolol decreases the ventricular rate in patients with atrial tachyarrhythmias. This effect results from its ability to slow atrioventricular conduction. Celiprolol is generally very well tolerated.
广泛的临床前和临床研究项目结果表明，塞利洛尔是一种治疗高血压和心绞痛的安全有效的药物。塞利洛尔吸收良好，大部分未被代谢，经尿液和胆汁排泄的量相当。由于这种药代动力学特征，塞利洛尔可安全用于老年人以及有肾或肝功能损害的患者。血流动力学研究表明，塞利洛尔可降低动脉血压，并降低肾血管阻力和外周血管阻力。塞利洛尔不会抑制心肌功能，也不会在哮喘患者中诱发支气管收缩。弱α2-肾上腺素能受体拮抗作用与β2-肾上腺素能受体激动作用相结合被认为是产生这些特性的原因。塞利洛尔200毫克/天的降压疗效与普萘洛尔、阿替洛尔和纳多洛尔相当。此外，塞利洛尔的作用持续24小时，与其他β受体阻滞剂相比，静息时心动过缓的情况较少。塞利洛尔的抗心绞痛疗效与阿替洛尔、普萘洛尔和美托洛尔相似。此外，塞利洛尔可降低房性快速心律失常患者的心室率。这种作用源于其减慢房室传导的能力。塞利洛尔一般耐受性良好。
