Taylor C R, Baird J R, Blackburn K J, Cambridge D, Constantine J W, Ghaly M S, Hayden M L, McIlhenny H M, Moore P F, Olukotun A Y, Pullman L G, Salsburg D S, Saxton C A, Shevde S
Am Heart J. 1981 Sep;102(3 Pt 2):515-32. doi: 10.1016/0002-8703(81)90740-7.
The animal and human pharmacology of several new drugs (prazosin, trimazosin, pirbuterol, and carbazeran) useful in the treatment of congestive heart failure (CHF) is delineated in relation to the pharmacology of other agents employed for CHF management. Prazosin and trimazosin are selective alpha 1-blockers that cause a balanced increase in cardiac output (CO) and reduction in left ventricular filling pressure (LVFP); the reduction in diastolic blood pressure with these drugs is significantly related to increase in treadmill exercise, fall in LVFP, and increase in CO. Pirbuterol is a relatively selective beta 2-agonist with somewhat greater effects on CO than on LVFP. Early promise in CHF therapy is being shown by a novel series of cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitors with combined direct inotropic and vasodilator effects. Double-blind long-term studies demonstrate persistent efficacy of prazosin and trimazosin in CHF as measured by improvement in New York Heart Association functional class, treadmill exercise performance, and noninvasive measures of cardiac function; these data are supported by studies in which repeat cardiac catheterization has been performed after several months of therapy. Double-blind studies of other CHF drugs are in progress.
阐述了几种用于治疗充血性心力衰竭（CHF）的新药（哌唑嗪、曲马唑嗪、吡布特罗和卡巴西兰）的动物和人体药理学，并与用于CHF治疗的其他药物的药理学进行了关联。哌唑嗪和曲马唑嗪是选择性α1阻滞剂，可使心输出量（CO）平衡增加，左心室充盈压（LVFP）降低；这些药物引起的舒张压降低与跑步机运动增加、LVFP下降和CO增加显著相关。吡布特罗是一种相对选择性的β2激动剂，对CO的作用比对LVFP的作用稍大。一系列具有直接正性肌力和血管舒张联合作用的新型环磷酸腺苷（cAMP）磷酸二酯酶抑制剂在CHF治疗中显示出早期前景。双盲长期研究表明，哌唑嗪和曲马唑嗪在CHF治疗中具有持续疗效，这通过纽约心脏协会功能分级、跑步机运动表现和心脏功能的非侵入性测量的改善来衡量；这些数据得到了在治疗数月后进行重复心导管检查的研究的支持。其他CHF药物的双盲研究正在进行中。
