Lammintausta R, Syvälahti E, Iisalo E, Kanto J, Mäntylä R
Acta Pharmacol Toxicol (Copenh). 1977 Nov;41(5):489-96. doi: 10.1111/j.1600-0773.1977.tb02160.x.
The effects of two beta-adrenergic receptor blocking drugs, the non-selective propranolol and the beta1selective metoprolol, were studied on hemodynamics and plasma renin activity (PRA) of healthy volunteers in an ergometric exercise test. Oral doses of 160 mg of propranolol and 200 mg of metoprolol were tested against placebo. The drug plasma concentrations were determined. Heart rate and systolic blood pressure were equal and significantly lower during treatment with both active drugs when compared to placebo. The effect of drugs on exercise heart rate was correlated with the logarithm of drug plasma concentration with both propranolol and metoprolol. Propranolol, but not metoprolol, decreased the basal level of PRA. The ergometric exercise induced a significant rise in PRA after placebo but this increase was partially inhibited by the both active drugs. On the basis of these findings it is suggested that in man the basal level of PRA could be decreased mainly by blocking the beta2-adrenoceptors. Instead the exercise induced increase of PRA could be inhibited by blocking the beta1-adrenergic receptors.
在一项测力计运动试验中,研究了两种β-肾上腺素能受体阻断药物,即非选择性的普萘洛尔和β1选择性的美托洛尔,对健康志愿者血流动力学和血浆肾素活性(PRA)的影响。口服160毫克普萘洛尔和200毫克美托洛尔的剂量,并与安慰剂进行对照测试。测定了药物血浆浓度。与安慰剂相比,两种活性药物治疗期间心率和收缩压均相等且显著降低。普萘洛尔和美托洛尔对运动心率的影响均与药物血浆浓度的对数相关。普萘洛尔降低了PRA的基础水平,但美托洛尔没有。安慰剂后测力计运动导致PRA显著升高,但两种活性药物均部分抑制了这种升高。基于这些发现,提示在人体中,PRA的基础水平可能主要通过阻断β2-肾上腺素能受体而降低。相反,运动诱导的PRA升高可通过阻断β1-肾上腺素能受体而被抑制。