Metelitsa V I, Martsevich S Iu, Kokurina E V, Bochkareva E V, Kozyreva M P, Kutishenko N P, Rumiantsev D O, Blagodatskikh S V, Vodop'ianova R S, Kukushkin S K
Eksp Klin Farmakol. 1995 Mar-Apr;58(2):3-7.
This paper provides the basic advances made in studying the clinical pharmacology of antianginal agents (AAs), demonstrates the contribution of current tools for evaluating their antianginal effects, namely pharmacodynamic studies using pair bicycle ergometry and repeated treadmill exercises, 24-hour ECG monitoring, pharmacokinetic studies. It shows that AAs can be chosen on an individual basis. The authors present pharmacodynamic characteristics of a number of new AAs from nitrates (trinitrolong, dinitrosorbilong, etc.), calcium antagonists, beta-adrenoblockers (proxodolol, etc.). They have developed a method for assessing the biological equivalence of AAs. The paper discusses the tolerance that can be developed to nitrates and how it can be prevented. It first demonstrates that nifedipine tolerance can develop and that the withdrawal syndrome can occur if nitrates and calcium antagonists are discontinued. There are screening data on various combinations of AAs. A two-stage scheme for choosing an AA therapy is given.
本文介绍了抗心绞痛药物(AAs)临床药理学研究取得的基本进展,展示了当前评估其抗心绞痛作用的工具的贡献,即使用双人自行车测力计和重复跑步机运动的药效学研究、24小时心电图监测、药代动力学研究。结果表明,可以根据个体情况选择AAs。作者介绍了多种新型AAs的药效学特征,这些AAs来自硝酸盐类(长效三硝酸甘油酯、长效二硝酸异山梨酯等)、钙拮抗剂、β-肾上腺素能阻滞剂(心得舒等)。他们开发了一种评估AAs生物等效性的方法。本文讨论了对硝酸盐类可能产生的耐受性以及如何预防。首先证明硝苯地平可能产生耐受性,并且如果停用硝酸盐类和钙拮抗剂可能会出现撤药综合征。文中还有关于AAs各种组合的筛选数据。给出了选择AA治疗的两阶段方案。