Giles Thomas D, Cockcroft John R, Pitt Bertram, Jakate Abhijeet, Wright Harold M
aDepartment of Medicine, Tulane University, New Orleans, Louisiana, USA bDepartment of Cardiology, University of Cardiff, University Hospital, Wales Heart Research Institute, University Hospital of Wales, Cardiff, Wales, UK cSchool of Medicine, University of Michigan, Ann Arbor, Michigan dForest Research Institute, Inc, An Allergan affiliate, Jersey City, New Jersey, USA.
J Hypertens. 2017 Sep;35(9):1758-1767. doi: 10.1097/HJH.0000000000001412.
: To treat hypertension, combining two or more antihypertensive drugs from different classes is often necessary. β-Blockers and renin-angiotensin-aldosterone system inhibitors, when combined, have been deemed 'less effective' based on partially overlapping mechanisms of action and limited evidence. Recently, the single-pill combination (SPC) of nebivolol (Neb) 5 mg - a vasodilatory β1-selective antagonist/β3 agonist - and valsartan 80 mg, an angiotensin II receptor blocker, was US Food and Drug Administration-approved for hypertension. Pharmacological profiles of Neb and valsartan, alone and combined, are well characterized. In addition, a large 8-week randomized trial in stages I-II hypertensive patients (N = 4161) demonstrated greater blood pressure-reducing efficacy for Neb/valsartan SPCs than component monotherapies with comparable tolerability. In a biomarkers substudy (N = 805), Neb/valsartan SPCs prevented valsartan-induced increases in plasma renin, and a greater reduction in plasma aldosterone was observed with the highest SPC dose vs. valsartan 320 mg/day. This review summarizes preclinical and clinical evidence supporting Neb/valsartan as an efficacious and well tolerated combination treatment for hypertension.
为治疗高血压，通常需要联合使用两种或更多种不同类型的抗高血压药物。β受体阻滞剂和肾素-血管紧张素-醛固酮系统抑制剂联合使用时，由于作用机制部分重叠且证据有限，被认为“效果较差”。最近，5毫克奈必洛尔（一种血管舒张性β1选择性拮抗剂/β3激动剂）与80毫克缬沙坦（一种血管紧张素II受体阻滞剂）的单片复方制剂已获美国食品药品监督管理局批准用于治疗高血压。奈必洛尔和缬沙坦单独及联合使用时的药理学特性已得到充分表征。此外，一项针对I-II期高血压患者的大型为期8周的随机试验（N = 4161）表明，奈必洛尔/缬沙坦单片复方制剂在降低血压方面比具有相当耐受性的单一成分单药治疗更有效。在一项生物标志物亚研究（N = 805）中，奈必洛尔/缬沙坦单片复方制剂可防止缬沙坦引起的血浆肾素升高，并且与缬沙坦每日320毫克相比，最高剂量的单片复方制剂可使血浆醛固酮有更大程度的降低。本综述总结了支持奈必洛尔/缬沙坦作为一种有效且耐受性良好的高血压联合治疗方案的临床前和临床证据。
