Frishman W H, Lazar E J, Gorodokin G
Department of Medicine Division, Albert Einstein College of Medicine, Bronx, New York.
Clin Pharmacokinet. 1991 Apr;20(4):311-8. doi: 10.2165/00003088-199120040-00005.
beta-Adrenergic blockade has provided one of the major pharmacotherapeutic advances of this century. The drugs in this class have the common property of blocking the binding of catecholamines to beta-adrenergic receptor sites; however, there are pharmacodynamic and pharmacokinetic differences between the individual agents which are of clinical importance. Among these differences are the completeness of gastrointestinal absorption, degree of hepatic first-pass metabolism, lipid solubility, protein binding, brain penetration, concentration within cardiac tissue, rate of hepatic biotransformation, and renal clearance of drug and/or metabolites. Long-acting formulations of existing beta-blockers are currently in use, and ultrashort-acting agents are also available. The pharmacokinetics of beta-blocking drugs can also be influenced by race, age, cigarette smoking and concomitant drug therapy. The wide interpatient variability in plasma drug concentration observed with beta-blockers makes this parameter unreliable in routine patient management. Despite the pharmacokinetic differences among the beta-blockers, these drugs should always be titrated in the individual patient to achieve the desired clinical response.
β-肾上腺素能阻滞剂是本世纪主要的药物治疗进展之一。这类药物具有阻断儿茶酚胺与β-肾上腺素能受体部位结合的共同特性；然而，各药物之间在药效学和药代动力学方面存在具有临床重要性的差异。这些差异包括胃肠道吸收的完全程度、肝脏首过代谢程度、脂溶性、蛋白结合、脑内渗透、心脏组织内浓度、肝脏生物转化速率以及药物和/或代谢产物的肾清除率。现有β受体阻滞剂的长效制剂目前正在使用，超短效制剂也已问世。β受体阻滞剂的药代动力学也会受到种族、年龄、吸烟以及合并药物治疗的影响。使用β受体阻滞剂时，患者间血浆药物浓度存在很大差异，这使得该参数在常规患者管理中不可靠。尽管β受体阻滞剂之间存在药代动力学差异，但这些药物在个体患者中始终应进行滴定以获得所需的临床反应。
