Lancaster S G, Sorkin E M
ADIS Drug Information Services, Manchester, England.
Drugs. 1988 Sep;36(3):256-85. doi: 10.2165/00003495-198836030-00002.
Bisoprolol is a beta 1-adrenoceptor antagonist with no partial agonist (intrinsic sympathomimetic) activity or membrane stabilising (local anaesthetic) activity. The oral bioavailability of bisoprolol is high (90%) and the drug has a long elimination half-life which allows once-daily administration; in addition, it is hepatically and renally cleared in equal proportions. In non-comparative studies, and comparative trials, bisoprolol proved effective, and as efficacious as atenolol, low doses of metoprolol, diuretics and nifedipine SR in hypertension, and atenolol and verapamil in stable angina pectoris. Bisoprolol has been well tolerated in most patients. Thus, bisoprolol is an effective alternative to other beta-adrenoceptor antagonists in patients with mild to moderate essential hypertension or stable angina pectoris. Furthermore, its unique pharmacokinetic properties may offer advantages in selected patients. However, the results of further comparative studies with established agents in the treatment of hypertension and angina pectoris are still awaited so that a final assessment of the relative place in therapy of bisoprolol in these disease states may be made.
比索洛尔是一种β1肾上腺素能受体拮抗剂，无部分激动剂（内在拟交感神经）活性或膜稳定（局部麻醉）活性。比索洛尔的口服生物利用度高（90%），且药物消除半衰期长，允许每日一次给药；此外，其经肝脏和肾脏清除的比例相等。在非对照研究和对照试验中，比索洛尔被证明是有效的，在高血压治疗中与阿替洛尔、低剂量美托洛尔、利尿剂和硝苯地平缓释片疗效相当，在稳定型心绞痛治疗中与阿替洛尔和维拉帕米疗效相当。大多数患者对比索洛尔耐受性良好。因此，对于轻度至中度原发性高血压或稳定型心绞痛患者，比索洛尔是其他β肾上腺素能受体拮抗剂的有效替代药物。此外，其独特的药代动力学特性可能在特定患者中具有优势。然而，仍有待进一步开展与现有药物治疗高血压和心绞痛的对比研究，以便对比索洛尔在这些疾病状态下治疗中的相对地位作出最终评估。
