Müller B, Wilsmann K
Arzneimittelforschung. 1984;34(4):430-3.
Cardio-hemodynamic and direct cardiac effects of 1-(m-methoxyphenyl)-2-(dimethylaminomethyl)- cyclohexan -1-ol (tramadol, Tramal ), and pentazocine were investigated in anaesthetized rabbits and in isolated guinea-pig atria and papillary muscles. Tramadol in anaesthetized rabbits at 1 and 4.64 mg/kg i.v. slightly increased arterial blood pressure and heart rate and at 10 mg/kg i.v. transiently decreased blood pressure, LV dp/dtmax and cardiac output and increased LV enddiastolic pressure. Pentazocine at 1 mg/kg i.v. increased blood pressure and peripheral vascular resistance, while with 2.15 and 4.64 mg/kg exerted dose-dependent cardiodepressive effects with initial fall of blood pressure, heart rate, LV dp/dtmax and cardiac output and increase of LV enddiastolic pressure. In spontaneously beating atria and electrically driven papillary muscles tramadol in the concentration range from 1 X 10(-6)-1 X 10(-4) mol/l showed concentration-dependent positive inotropic effects which where abolished and reversed to negative inotropic actions in catecholamine-depleted papillary muscles. In contrast, pentazocine in the same concentration range showed pure negative inotropic and negative chronotropic effects which were intensified in catecholamine-depleted papillary muscles. These in vitro results suggest that both tramadol and pentazocine interact with endogenous catecholamines in a way counteracting direct negative inotropic effects. While in the case of tramadol the sum of both properties leads to positive inotropic effects at least in vitro, with pentazocine negative inotropic action prevails.
研究了1-(间甲氧基苯基)-2-(二甲基氨基甲基)-环己醇(曲马多,曲马朵)和喷他佐辛对麻醉兔以及离体豚鼠心房和乳头肌的心脏血液动力学及直接心脏效应。在麻醉兔中,静脉注射1mg/kg和4.64mg/kg的曲马多可使动脉血压和心率略有升高,静脉注射10mg/kg时可使血压、左心室dp/dtmax和心输出量短暂下降,并使左心室舒张末期压力升高。静脉注射1mg/kg的喷他佐辛可使血压和外周血管阻力升高,而静脉注射2.15mg/kg和4.64mg/kg时则产生剂量依赖性的心脏抑制作用,导致血压、心率、左心室dp/dtmax和心输出量初始下降,左心室舒张末期压力升高。在自发搏动的心房和电驱动的乳头肌中,浓度范围为1×10(-6)-1×10(-4)mol/l的曲马多呈现浓度依赖性正性肌力作用,而在去甲肾上腺素耗竭的乳头肌中这种作用被消除并转变为负性肌力作用。相比之下,相同浓度范围内的喷他佐辛呈现纯粹的负性肌力和负性变时作用,在去甲肾上腺素耗竭的乳头肌中作用增强。这些体外实验结果表明,曲马多和喷他佐辛均以内源性去甲肾上腺素相互作用的方式抵消直接负性肌力作用。虽然就曲马多而言,这两种特性的总和至少在体外导致正性肌力作用,但喷他佐辛的负性肌力作用占主导。