Dahlöf C, Dimenäs E
Department of Clinical Pharmacology, Sahlgrenska Hospital, Gothenburg, Sweden.
Am J Med Sci. 1990 Apr;299(4):236-44. doi: 10.1097/00000441-199004000-00004.
During the last decade beta-adrenoceptor antagonists have become one of the first-line treatments for hypertension. Generally, they have been shown to be safe with a low frequency of serious side effects. However, minor subjective symptoms, usually considered to be CNS-related, have been reported for all beta-blockers used. Thus, all beta-blockers on the market seem to have a high benefit:risk ratio; independent of their physicochemical properties and pharmacodynamic profile, however, they seem to cause CNS-related side effects to about the same extent. These minor side effects, the mechanisms of which are unclear, consist of subtle effects on general well being, decreased initiative, a depressed frame of mind, and disturbed sleep. Generally, however, beta-blockers in therapeutic dosages do not affect the qualitative functions of the brain. The results so far available have been obtained primarily by using objective methods. Further comparison has now been initiated using documented subjective methods to investigate whether the objectively documented differences are of any clinical relevance to the patient's quality of life. Although it cannot be claimed with certainty, nonselective beta-blockers seem to cause CNS-related side effects to a greater extent than beta 1-selective blockers. Differences in the degree of hydrophilicity of the beta-blocker are apparently of no clinical relevance in this respect. Rather, the plasma concentration of the beta-blocking drug (degree of beta-blockade) seems to be the major determinant of whether or not CNS-related symptoms appear in susceptible patients.
在过去十年中，β肾上腺素能受体拮抗剂已成为高血压的一线治疗药物之一。一般来说，它们已被证明是安全的，严重副作用发生率较低。然而，对于所有使用的β受体阻滞剂，均有轻微主观症状的报告，这些症状通常被认为与中枢神经系统有关。因此，市场上所有的β受体阻滞剂似乎都有很高的效益风险比；然而，无论其理化性质和药效学特征如何，它们似乎都会在大致相同程度上引起与中枢神经系统相关的副作用。这些轻微副作用的机制尚不清楚，包括对总体健康的细微影响、主动性降低、情绪低落和睡眠障碍。然而，一般来说，治疗剂量的β受体阻滞剂不会影响大脑的定性功能。目前已获得的结果主要是通过客观方法得到的。现在已经开始使用有记录的主观方法进行进一步比较，以研究客观记录的差异是否与患者的生活质量具有任何临床相关性。虽然不能肯定地说，但非选择性β受体阻滞剂似乎比β1选择性阻滞剂在更大程度上引起与中枢神经系统相关的副作用。在这方面，β受体阻滞剂亲水性程度的差异显然没有临床相关性。相反，β受体阻滞剂的血浆浓度（β受体阻滞程度）似乎是易感患者是否出现与中枢神经系统相关症状的主要决定因素。
