曲马多抑制离体人肌层的收缩性

N. H. Shah, E. Thomas, R. Jose, J. Peedicayil
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引用次数: 15

摘要

本研究旨在确定非典型阿片类镇痛药曲马多是否能抑制离体非妊娠人肌层的收缩性。采用55 mm氯化钾(KCl)刺激10条未怀孕的人子宫肌层,用3种浓度(30、100和300 μm)的曲马多处理,观察曲马多的抑制作用。同时研究了β肾上腺素受体拮抗剂普萘洛尔(1 μm)、冠酰环化酶和一氧化氮合酶抑制剂亚甲基蓝(20 μm)和阿片受体拮抗剂纳洛酮(100 μm)与曲马多同时给药的效果。曲马多引起的kcl诱导的子宫肌力的浓度依赖性抑制,这在使用的所有三种浓度的曲马多具有统计学意义。普萘洛尔能显著逆转100 μm曲马多对kcl诱导的子宫肌力的抑制作用,而300 μm曲马多则不能。亚甲蓝和纳洛酮均不能逆转曲马多对氯化钾诱导的子宫肌收缩性的抑制作用。这些结果表明曲马多抑制kcl诱导的离体人肌层收缩性。他们还认为曲马多通过刺激ß1肾上腺素受体而使肌层松弛。然而,松弛肌层所需的曲马多浓度很高,而且可能在曲马多的中毒剂量而不是治疗剂量下达到。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Tramadol inhibits the contractility of isolated human myometrium

  1. This study was conducted to determine whether the atypical opioid analgesic tramadol inhibits the contractility of isolated non-pregnant human myometrium. Ten strips of non-pregnant human myometrium stimulated with 55 mm potassium chloride (KCl) were treated with three concentrations (30, 100 and 300 μm) of tramadol to test for any inhibitory effect of tramadol. The effects of concurrent administration of the ß adrenoceptor antagonist propranolol (1 μm), the guanylyl cyclase and nitric oxide synthase inhibitor methylene blue (20 μm) and the opioid receptor antagonist naloxone (100 μm) with tramadol were also studied.
  2. Tramadol caused a concentration-dependent inhibition of KCl-induced myometrial contractility, which was statistically significant at all three concentrations of tramadol used. Propranolol significantly reversed the inhibitory effect of 100 μm tramadol on KCl-induced myometrial contractility but not that of 300 μm tramadol. Neither methylene blue nor naloxone reversed the inhibitory effect of tramadol on KCl-induced myometrial contractility.
  3. These results suggest that tramadol inhibits KCl-induced contractility of isolated human myometrium. They also suggest that tramadol relaxes the myometrium due to stimulation of ß1 adrenoceptors. However, the concentrations of tramadol required to relax the myometrium were high and likely to be attained at toxic doses, rather than therapeutic doses, of tramadol.
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