Saudan S, Habre W
Unité d'anesthésie pédiatrique, hôpital des enfants, hôpitaux universitaires de Genève, Genève, Switzerland.
Ann Fr Anesth Reanim. 2007 Jun;26(6):560-3. doi: 10.1016/j.annfar.2007.03.015. Epub 2007 May 23.
The recent studies focusing on the pharmacokinetics of tramadol in children contributed to the increase popularity of tramadol as an analgesic alternative in clinical practice. Tramadol is a racemic mixture of 2 enantiomers that have comparable pharmacokinetic profile and this lack of difference is also observed with their main active metabolite, O-demethyl tramadol (M1). The serum concentrations of this metabolite depend largely on the activity of the cytochrome P450 and particularly of the enzyme CYP2D6 which reaches its maturity in the newborn. Nevertheless, the interindividual variability observed in the pharmacokinetics of tramadol and consequently in the pharmacodynamic profile is mainly due to the genetic polymorphism of cytochrome P450.
近期针对曲马多在儿童体内药代动力学的研究，促使曲马多在临床实践中作为一种镇痛替代药物的受欢迎程度有所提高。曲马多是两种对映体的外消旋混合物，它们具有相似的药代动力学特征，其主要活性代谢物O-去甲基曲马多（M1）也存在这种差异缺失的情况。该代谢物的血清浓度在很大程度上取决于细胞色素P450的活性，尤其是在新生儿中已发育成熟的CYP2D6酶的活性。然而，曲马多药代动力学以及由此导致的药效学特征中观察到的个体间变异性，主要是由于细胞色素P450的基因多态性所致。
