Thadani U
Am J Cardiol. 1983 Nov 10;52(9):10D-15D. doi: 10.1016/0002-9149(83)90637-9.
Beta-adrenoceptor antagonists are effective in the management of patients with mild-to-moderate hypertension. Noncardioselective agents, cardioselective agents and beta blockers with intrinsic sympathomimetic activity (ISA) are equally effective, provided they are used in equipotent doses. Beta blockers can be used as first-line therapy in the management of hypertension and can be safely combined with diuretics, vasodilators, or both, for a better control of blood pressure. The exact mechanism by which beta blockers decrease blood pressure remains speculative, but they all reduce cardiac output during long-term therapy; drugs with ISA lower cardiac output and heart rate less than do drugs without ISA. Pharmacokinetic properties of beta blockers differ widely; drugs metabolized by the liver have shorter plasma half-lives than drugs primarily excreted by the kidneys. Although many of the side effects of various beta blockers are similar, differences in water and lipid solubility account for a higher incidence of central nervous system side effects with lipid-soluble drugs (such as propranolol and metoprolol) than with hydrophilic drugs (such as atenolol and timolol). The incidence of cold extremities has been reported to be less with drugs with ISA, and the incidence of bronchospasm less with cardioselective drugs. In the management of uncomplicated mild-to-moderate hypertension, all beta blockers are equally effective and produce less troublesome side effects than alternative antihypertensive agents. For effective therapy beta blockers can be used in 2 divided daily doses or even once daily.(ABSTRACT TRUNCATED AT 250 WORDS)
β-肾上腺素能受体拮抗剂对轻至中度高血压患者的治疗有效。非选择性β受体阻滞剂、选择性β1受体阻滞剂和具有内在拟交感活性(ISA)的β受体阻滞剂,只要使用等效剂量,其疗效相同。β受体阻滞剂可作为高血压治疗的一线用药,且可安全地与利尿剂、血管扩张剂或两者联用,以更好地控制血压。β受体阻滞剂降低血压的确切机制仍属推测,但在长期治疗过程中它们均能降低心输出量;具有ISA的药物降低心输出量和心率的程度小于无ISA的药物。β受体阻滞剂的药代动力学特性差异很大;经肝脏代谢的药物血浆半衰期比主要经肾脏排泄的药物短。尽管各种β受体阻滞剂的许多副作用相似,但脂溶性药物(如普萘洛尔和美托洛尔)比亲水性药物(如阿替洛尔和噻吗洛尔)更容易引起中枢神经系统副作用,这是由于它们在水和脂溶性方面存在差异。据报道,具有ISA的药物引起四肢发冷的发生率较低,而选择性β1受体阻滞剂引起支气管痉挛的发生率较低。在单纯性轻至中度高血压的治疗中,所有β受体阻滞剂疗效相同,且与其他抗高血压药物相比,产生的副作用较少。为了达到有效治疗,β受体阻滞剂可每日分2次给药,甚至每日1次给药。(摘要截选至250词)