曲马多抑制离体羊逼尿肌的收缩力

A. Kumar, R. Prabha, T. Paul, F. X. Margaret Shanthi, J. George, J. Peedicayil, K. Ernest
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引用次数: 7

摘要

非典型阿片类镇痛药曲马多已被证明对逼尿肌过度活动患者提供有益的临床和尿动力学效果。曲马多对离体逼尿肌的作用尚未见研究。本研究考察了曲马多对乙酰胆碱(ACh)诱导的离体山羊逼尿肌收缩的抑制作用。研究了3种浓度(30、100和300 μm)曲马多对添加100、200和400 μm乙酰胆碱收缩的10只山羊逼尿肌条的影响。研究了曲马多诱导的乙酰胆碱反应抑制对β-肾上腺素受体拮抗剂心得安(1 μm)和阿片受体拮抗剂纳洛酮(100 μμ m)的敏感性。曲马多引起乙酰胆碱诱导的逼尿肌收缩的浓度依赖性抑制,这种抑制通过提高乙酰胆碱浓度而逆转。心得安而非纳洛酮逆转了曲马多诱导的逼尿肌对乙酰胆碱的抑制作用。这些结果表明曲马多抑制乙酰胆碱诱导的离体逼尿肌收缩。他们还认为曲马多是通过间接的抗胆碱能机制,包括刺激β-肾上腺素受体。曲马多可用于治疗需要放松逼尿肌的临床情况。虽然曲马多松弛逼尿肌所需的浓度相对较高,但这些浓度可以通过膀胱内给药在临床上达到。
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Tramadol inhibits the contractility of isolated caprine detrusor muscle

1 The atypical opioid analgesic tramadol has been shown to provide beneficial clinical and urodynamic effects in patients with detrusor overactivity. The effect of tramadol on isolated detrusor muscle has not been studied. This study investigated the ability of tramadol to inhibit acetylcholine (ACh)-induced contractility of the isolated caprine (goat) detrusor muscle. The effect of three concentrations (30, 100 and 300 μm) of tramadol on 10 caprine detrusor strips contracted by the addition of 100, 200 or 400 μm ACh was studied. The sensitivity of tramadol-induced inhibition of ACh responses to treatment with the β-adrenoceptor antagonist propranolol (1 μm) and the opioid receptor antagonist naloxone (100 μμ) was also studied.

2 Tramadol caused a concentration-dependent inhibition of ACh-induced detrusor contraction that was reversed by raising the concentration of ACh. Propranolol, but not naloxone, reversed the tramadol-induced inhibition of contractions to ACh in the detrusor.

3 These results suggest that tramadol inhibits ACh-induced contractility of the isolated detrusor. They also suggest that tramadol does so by an indirect anticholinergic mechanism involving the stimulation of β-adrenoceptors. Tramadol may be useful in managing clinical conditions requiring relaxation of the detrusor muscle. Although the concentrations of tramadol needed to relax the detrusor were relatively high, these could be clinically attained via intravesical administration.

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Issue Information Autonomic and Autacoid Pharmacology: Goodbye and thank you Attenuation of the anti-contractile effect of cooling in the rat aorta by perivascular adipose tissue Retraction: Dopamine receptor immunohistochemistry in the rat choroid plexus. Issue Information
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