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目的探讨血清中反式曲马多 ((±)_transT)及其活性代谢物对映体浓度与临床效果的关系。方法20例术后病人静滴盐酸(±)_transT400mg·d -1(A组)或300mg·d -1(B组) ,38h后取静脉血 ,高效毛细管电泳法 (HPCE)分离测定血清中(±)_transT及其活性代谢物反式氧去甲基曲马多 ((±)_M1)对映体的浓度 ,并观察临床镇痛效果及不良反应。结果A组病人血清中(±)_transT对映体的浓度、不良反应的发生率和严重程度明显高于B组病人 ,而A、B两组病人血清中活性代谢物 (+)_M1浓度及镇痛效果无明显区别。结论血清中 (+)_M1 的浓度与镇痛效果密切相关 ;由于代谢饱和引起的血清中(±)_transT对映体浓度过高可能是不良反应明显增强的原因之一。
Objective To investigate the relationship between the enantiomeric concentrations of trans-tramadol (±) _transT and its active metabolites in serum and its clinical effect. Methods Twenty patients were treated with intravenous (±) _transT400 mg · d -1 or 300 mg · d -1 hydrochloric acid (hydrochloric acid) intravenously and plasma samples were collected by capillary electrophoresis (HPCE) ±) _transT and its active metabolite trans-deoxy-methyl tramadol ((±) _M1) enantiomer concentration, and observe the clinical analgesic effect and adverse reactions. Results The serum concentrations of (±) _transT enantiomers and the incidence and severity of adverse reactions in group A patients were significantly higher than those in group B patients. However, serum concentrations of active metabolites (+) _M1 and group A No significant difference in the effect of pain. Conclusions The concentration of (+) _M1 in serum is closely related to the analgesic effect. The high concentration of (+) _transT enantiomer in serum due to metabolic saturation may be one of the reasons for the significant increase of adverse reactions.