Cruickshank J M, Neil-Dwyer G
Eur J Clin Pharmacol. 1985;28 Suppl:21-3. doi: 10.1007/BF00543705.
Patients with subarachnoid haemorrhage (SAH) have been shown to benefit from beta-blockade. SAH patients who came to surgery were investigated if they had been receiving chronic (approximately one week) oral treatment with either hydrophilic atenolol (100 mg/day) or one of the following lipophilic beta-blockers: propranolol (80 mg b.i.d.), oxprenolol (80 mg b.i.d.), or metoprolol (100 mg b.i.d.). Cerebrospinal fluid concentrations of beta-blockers did not reflect their concentrations in the brain. Brain concentrations of the three lipophilic beta-blockers were 10-20 times higher than those of atenolol. The approximate brain/plasma concentration ratios were 26 for propranolol, 50 for oxprenolol, 12 for metoprolol, and 0.2 for atenolol. The brain is thus buffered from peak blood concentrations of atenolol, and this may account for the low incidence of CNS-related side-effects with this hydrophilic beta-blocker.
蛛网膜下腔出血（SAH）患者已被证明可从β受体阻滞剂治疗中获益。对接受手术治疗的SAH患者进行了调查，了解他们是否一直在接受为期约一周的慢性口服治疗，所用药物为亲水性阿替洛尔（100毫克/天）或以下亲脂性β受体阻滞剂之一：普萘洛尔（80毫克，每日两次）、氧烯洛尔（80毫克，每日两次）或美托洛尔（100毫克，每日两次）。脑脊液中β受体阻滞剂的浓度并不能反映其在大脑中的浓度。三种亲脂性β受体阻滞剂在大脑中的浓度比阿替洛尔高10至20倍。普萘洛尔、氧烯洛尔、美托洛尔和阿替洛尔的大脑/血浆浓度近似比值分别为26、50、12和0.2。因此，大脑可免受阿替洛尔血药峰值浓度的影响，这可能是这种亲水性β受体阻滞剂中枢神经系统相关副作用发生率较低的原因。
