Fagher B, Liedholm H, Monti M
Department of Internal Medicine, University Hospital of Lund, Lund University, Sweden.
Eur J Clin Pharmacol. 1993;45(6):571-6. doi: 10.1007/BF00315317.
A double blind placebo-controlled study was conducted of the effects of oral propranolol (beta 1 beta 2-adrenoceptor antagonist) and terbutaline (beta 2-adrenoceptor agonist) on erythrocyte heat production, measured by direct microcalorimetry under static conditions at 37 degrees C and pH 7.4. Propranolol 80 mg and terbutaline slow-release 7.5 mg were randomly administered twice daily for one week to 15 healthy males, using a cross-over design. No thermogenic difference was detected. Serum potassium was significantly decreased by terbutaline but was only slightly increased by propranolol, but no relationship was found between changes in the extra- and intracellular levels. In the placebo group, 10% of total cell energy was consumed by the Na-K pump, as assessed by ouabain inhibition, and this value was not significantly affected by the treatments. Thus, it seems unlikely that there is a clinically relevant influence on the Na-K pump in erythrocytes during continuous terbutaline or propranolol medication. It is concluded that short term medication with propranolol and terbutaline in therapeutic doses has almost no thermal or metabolic effect on human erythrocytes. The results indirectly imply that no clinically relevant beta-adrenoceptor effects are mediated in erythrocytes and this may also be true with regard to the 'membrane effect' of propranolol.
进行了一项双盲安慰剂对照研究,以探讨口服普萘洛尔(β1β2肾上腺素能受体拮抗剂)和特布他林(β2肾上腺素能受体激动剂)对红细胞产热的影响,产热通过在37℃和pH 7.4的静态条件下直接微量量热法进行测量。采用交叉设计,将80毫克普萘洛尔和7.5毫克缓释特布他林随机每日两次给予15名健康男性,持续一周。未检测到产热差异。特布他林使血清钾显著降低,而普萘洛尔仅使其略有升高,但细胞外和细胞内水平的变化之间未发现相关性。在安慰剂组中,通过哇巴因抑制评估,钠钾泵消耗了总细胞能量的10%,该值不受治疗的显著影响。因此,在持续使用特布他林或普萘洛尔药物期间,对红细胞中的钠钾泵似乎不太可能存在临床相关影响。得出的结论是,治疗剂量的普萘洛尔和特布他林短期用药对人体红细胞几乎没有热效应或代谢效应。结果间接表明,红细胞中未介导临床相关的β肾上腺素能受体效应,这对于普萘洛尔的“膜效应”可能也是如此。