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[不同β受体阻滞剂对体力活动期间代谢和循环参数的影响]

[Effects of various beta-receptor blockers on metabolic and circulatory parameters during physical exertion].

作者信息

Koebe P, Rost R, Reinke A, Nagel N, Merten U

出版信息

Arzneimittelforschung. 1985;35(2):522-9.

PMID:2859861
Abstract

For further elucidation of the effect of various beta-adrenoceptor blockers on metabolism during exercise investigations on the influence of 5 beta-adrenoceptor blockers were carried out in healthy subjects. The 5 beta-adrenoreceptor blockers (acebutolol, metoprolol, penbutolol, pindolol, propranolol) were different regarding cardioselectivity and intrinsic activity (ISA). Each substance was given in 4 different dosages corresponding to 10:20:40:80 mg propranolol. Exercise was performed as bicycle ergometer test over 1 hour. In order to find out different effects during long-term application a medium dosage corresponding to 40 mg propranolol was applied for 4 weeks after the acute trials. The following parameters were measured: heart rate, systolic arterial pressure, parameters of carbohydrate metabolism (glucose, lactate) as well as lipid metabolism (free fatty acids (FFA), cholesterol, triglycerides etc.), serum concentration; for three beta-adrenoceptor blockers hormonal concentrations (catecholamines, insulin, human growth hormone (HGH), adrenocorticotrophic hormone (ACTH] were assessed. The different beta-adrenoceptor blockers demonstrated a varying relation between dosage and effect which was mostly pronounced for propranolol. All beta-adrenoceptor blockers caused a nearly complete blockade of energy release from FFA, and serum glucose concentration decreased. These changes were smaller under the effect of a low dosage of the cardioselective beta-adrenoceptor blocker metoprolol. The hormonal concentrations demonstrated a more pronounced increase of epinephrine during beta-blockade in contrast to only small changes by norepinephrine. Whereas there was no effect to be found on ACTH, HGH increased significantly under beta-blockade but independent of cardioselectivity.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

为了进一步阐明在运动期间各种β-肾上腺素受体阻滞剂对代谢的影响,在健康受试者中开展了关于5种β-肾上腺素受体阻滞剂影响的研究。这5种β-肾上腺素受体阻滞剂(醋丁洛尔、美托洛尔、喷布洛尔、吲哚洛尔、普萘洛尔)在心脏选择性和内在活性(ISA)方面存在差异。每种药物以4种不同剂量给药,分别相当于10:20:40:80mg普萘洛尔。运动通过自行车测力计测试持续1小时进行。为了找出长期应用期间的不同影响,在急性试验后,以相当于40mg普萘洛尔的中等剂量给药4周。测量了以下参数:心率、收缩压、碳水化合物代谢参数(葡萄糖、乳酸)以及脂质代谢参数(游离脂肪酸(FFA)、胆固醇、甘油三酯等)、血清浓度;对3种β-肾上腺素受体阻滞剂评估了激素浓度(儿茶酚胺、胰岛素、人生长激素(HGH)、促肾上腺皮质激素(ACTH))。不同的β-肾上腺素受体阻滞剂在剂量和效应之间呈现出不同的关系,这在普萘洛尔中最为明显。所有β-肾上腺素受体阻滞剂几乎完全阻断了FFA的能量释放,血清葡萄糖浓度降低。在心脏选择性β-肾上腺素受体阻滞剂美托洛尔低剂量作用下,这些变化较小。与去甲肾上腺素仅有微小变化相比,激素浓度显示在β受体阻滞剂作用期间肾上腺素的增加更为明显。虽然未发现对ACTH有影响,但在β受体阻滞剂作用下HGH显著增加,且与心脏选择性无关。(摘要截断于250字)

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