术后病人静滴不同剂量盐酸反式曲马多后血清中母体药物及活性代谢物对映体监测

Mornitoring of the enantiomers of(±)-trans tramadol and its active metabolite in the serum of postoperative patients after different intravenous doses of(±)-trans tramadol hydrochloride injection

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。

Aim To investigate the relationship between the clinical actions and the serum concentrations of the enantiomers of (±)-trans tramadol and its active metabolite. Methods 20 postoperative patients were divided into two groups and given multiple intravenous doses of (±)-trans tramadol hydrochloride injection, 400 mg·d-1 (group A) or 300 mg·d-1 (group B). The blood samples were taken at 38 h after the initial dose. The concentrations of the enantiomers of (±)-trans tramadol and its active metabolite, (±)-trans O-demethyltramadal were determined with high performance capillary electrophoresis(HPCE). Results The concentrations of the enantiomers of (±)-trans tramadol, the frequency and serious level of adverse reactions were higher in group A than in group B. The concentrations of the enantiomers of (±)-trans O-demethyltramadal, the analgesic effect were similar between group A and group B. Conclusion There is much closer relation between the analgesic effect and the concentration of (+)-O-demethyltramadal. The frequency and serious level of adverse reactions may be attributed to the higher concentrations of the enantiomers of (±)-trans tramadol, which are caused by the saturated metabolism.