McNeil J J, Drummer O H, Anderson A I, Louis W J
J Cardiovasc Pharmacol. 1986 Nov-Dec;8(6):1201-7. doi: 10.1097/00005344-198611000-00016.
The pharmacokinetic handling of the beta 1 selective adrenoceptor blocking drug, bevantolol, was studied in 12 healthy volunteers. After intravenous (i.v.) administration of 50 mg of the drug, there was a biexponential decline in plasma levels with a terminal elimination half life (t1/2) of 1.9 h (range 1.4-2.3 h) and a total apparent volume of distribution at equilibrium of 62 L. After oral administration of the same dose, the bioavailability averaged 57% (range 26-98%) and peak plasma levels varied over a threefold range. On average, less than 1% of the dose was eliminated unchanged in the urine, indicating that the clearance of the drug was accounted for almost entirely by metabolism. Plasma levels after oral dosing with food showed an average 75-min delay in achievement of peak plasma levels and an average 14% increase in the extent of bioavailability of the drug. A positive correlation (r = 0.79) existed between the logarithm of the plasma bevantolol level and the percentage of reduction in postexercise heart rate. A plasma drug level of approximately 200 ng/ml produced a 10% reduction in postexercise heart rate. Pharmacological studies using guinea pig atrial and tracheal tissue demonstrated that the beta-blocking potency and beta-selectivity of bevantolol were intermediate between those of metoprolol and atenolol.
在12名健康志愿者中研究了β1选择性肾上腺素能受体阻断药物倍凡洛尔的药代动力学特征。静脉注射50毫克该药物后，血浆浓度呈双指数下降，终末消除半衰期（t1/2）为1.9小时（范围1.4 - 2.3小时），平衡时的总表观分布容积为62升。口服相同剂量后，生物利用度平均为57%（范围26 - 98%），血浆峰值浓度变化范围达三倍。平均而言，不到1%的剂量以原形经尿液排出，这表明药物清除几乎完全由代谢所致。与食物同服后口服给药的血浆浓度显示，达到血浆峰值浓度的时间平均延迟75分钟，药物生物利用度的程度平均增加14%。血浆倍凡洛尔浓度的对数与运动后心率降低百分比之间存在正相关（r = 0.79）。血浆药物浓度约为200纳克/毫升时，运动后心率降低10%。使用豚鼠心房和气管组织进行的药理学研究表明，倍凡洛尔的β受体阻断效能和β选择性介于美托洛尔和阿替洛尔之间。
