Bristow M R, Roden R L, Lowes B D, Gilbert E M, Eichhorn E J
University of Colorado Health Sciences Center, Division of Cardiology, Denver 80262, USA.
Clin Cardiol. 1998 Dec;21(12 Suppl 1):I3-13. doi: 10.1002/clc.4960211303.
Third-generation beta-blocking agents developed for the hypertension market are proving useful in the treatment of chronic heart failure (HF). These compounds share the ancillary property of vasodilation, which improves acute tolerability by unloading the failing left ventricle at a time when beta-adrenergic withdrawal produces myocardial depression. In the case of carvedilol and bucindolol, this allows for the administration of nonselective beta blockade. Because of blockade of both beta 1 and beta 2 adrenergic receptors as well as other properties, these compounds possess a more comprehensive antiadrenergic profile than second-generation, beta 1-selective compounds. For this and potentially other reasons, third-generation beta-blocking agents have theoretical efficacy advantages that have yet to be demonstrated in large-scale trials. Ongoing trials with either second- or third-generation compounds and one trial directly comparing a compound from each class will provide the answer as to whether third-generation compounds have an advantage in the treatment of chronic HF.
为高血压市场研发的第三代β受体阻滞剂在慢性心力衰竭（HF）治疗中已证明很有用。这些化合物具有血管舒张的辅助特性，在β肾上腺素能撤退导致心肌抑制时，通过减轻衰竭的左心室负荷来改善急性耐受性。就卡维地洛和布新洛尔而言，这使得可以进行非选择性β受体阻滞。由于β1和β2肾上腺素能受体均被阻滞以及其他特性，这些化合物比第二代β1选择性化合物具有更全面的抗肾上腺素能作用谱。鉴于此以及其他潜在原因，第三代β受体阻滞剂在理论上具有疗效优势，但尚未在大规模试验中得到证实。正在进行的关于第二代或第三代化合物的试验以及一项直接比较两类化合物各一种的试验，将为第三代化合物在慢性HF治疗中是否具有优势提供答案。
