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中国临床药理学与治疗学 ›› 2000, Vol. 5 ›› Issue (2): 134-137.

• 论著 • 上一篇    下一篇

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

刘会臣, 杨燕燕, 侯艳宁, 王亚丽   

  1. 白求恩国际和平医院临床药理室, 石家庄 050082
  • 收稿日期:1999-12-07 修回日期:2000-05-04 出版日期:2000-06-26 发布日期:2020-12-01
  • 作者简介:刘会臣, 男, 36岁, 医学硕士, 副主任药师, 主要从事药代动力学研究。

Mornitoring of the enantiomers of (±)-trans tramadol andits active metabol ite in the serum of postoperative patients after differentintravenous doses of (±)-trans tramadol hydrochloride injection

LIU Hui-Chen, YANG Yan-Yan, HOU Yan-Ning, WANG Ya-Li   

  1. Department of Clinical Pharmacology, Bethune International Peace Hospital, Shijiazhuang 050082
  • Received:1999-12-07 Revised:2000-05-04 Online:2000-06-26 Published:2020-12-01

摘要: 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。

关键词: 反式曲马多, 反式氧去甲基曲马多, 镇痛效果, 不良反应, 高效毛细管电泳

Abstract: Aim To investig ate therelationship between the clinical actions and the serum concentrations of the enantiomers of (±)-trans tramadol andits active metabolite.Methods 20 postoperative patients weredividedinto two groups and given multiple intraveno us doses of (±)-trans tramadol hydrochloride injection, 400 mg·d-1 (group A)or 300 mg·d-1 (group B).The blood samples weretaken at 38 h after the initial dose.The concentrations of the enantiomers of (±)-trans tramadol andits active metabolite, (±)-trans O-demethy ltramadal weredetermined with high performance capillary electrophoresis(HPCE).Results The concentrations of the enantiomers of (±)-trans tramadol, the f requencyand serious level of adversereactions werehigher in group A than in group B.The concentrations of the enantiomers of (±)-trans O-d emethy ltramadal, the analgesic Effect weresimilarbetween group A and group B.Conclusion Thereis much closer relation between the analgesic Effect and the concentration of (+)-O-d emethy ltramadal.The f reque ncyand serious level of adversereactions may be at tributed to the higher concentrations of the enantiomers of (±)-trans tramadol, which arecaused by the saturated metabolism.

Key words: (±)-trans tramadol, (±)-trans O-demethy ltramadol, analg esic effect, adversereaction, high performance capillary electrophoresis

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