Folgering H, van Bussel M
Eur J Clin Pharmacol. 1980 Oct;18(3):225-9. doi: 10.1007/BF00563003.
The treatment of hypertension with a single daily-dose of a beta-blocker gives rise to high peak-plasma concentrations 1.5 h after ingestion. After slow release-preparations of beta-blockers, the peak concentrations are half those produced by the conventional preparation at the same oral dose. A frequently occurring side-effect of beta-blocker therapy is fatigue. In this study the effect of a single dose of metoprolol 300 mg, 200 mg, 200 mg slow-release and a placebo on maximal exercise power was tested in 6 healthy subjects, 1.5 h and 24 h after ingestion. Maximal exercise power was significantly reduced 1.5 h after ingestion of metoprolol 300 mg and 200 mg. No change was found 1.5 h after 200 mg of a slow-release preparation. The possible reasons for reduced maximal exercise power are discussed. It is concluded that use of a beta-blocker for the treatment of hypertension in a single daily-dose regimen may be a reason to prefer a slow-release preparation.
每日单次服用β受体阻滞剂治疗高血压会在服药后1.5小时产生较高的血浆峰浓度。服用β受体阻滞剂缓释制剂后,在相同口服剂量下,峰浓度仅为传统制剂的一半。β受体阻滞剂治疗常见的副作用是疲劳。在本研究中,对6名健康受试者在服用300毫克、200毫克美托洛尔、200毫克缓释美托洛尔和安慰剂后1.5小时及24小时的最大运动能力进行了测试。服用300毫克和200毫克美托洛尔后1.5小时,最大运动能力显著降低。服用200毫克缓释制剂后1.5小时未发现变化。文中讨论了最大运动能力降低的可能原因。得出的结论是,每日单次服用β受体阻滞剂治疗高血压时,可能有理由优先选择缓释制剂。