目的:评估细胞色素P450 2D6*10基因多态性,对汉族人群术后吗啡自控镇痛效果的影响。方法:美国麻醉医师协会(American Society of Anesthesiologists,ASA)Ⅰ～Ⅱ级患者共64名被纳入此实验,56名患者完成实验。根据CYP2D6基因型,患者分为3...目的:评估细胞色素P450 2D6*10基因多态性,对汉族人群术后吗啡自控镇痛效果的影响。方法:美国麻醉医师协会(American Society of Anesthesiologists,ASA)Ⅰ～Ⅱ级患者共64名被纳入此实验,56名患者完成实验。根据CYP2D6基因型,患者分为3组:野生型纯合子组(w/w组,n=19),杂合子组(m/w组,n=21)和突变型纯合子组(m/m组,n=16)。在手术结束前10 min给予复合剂量吗啡(静脉注射,0.1 mg/kg)后,患者可通过吗啡(单次给药1 mg)自控输注泵进行自控镇痛(patient-controlled analgesia,PCA)。全身麻醉诱导后采集血样。采用聚合酶链反应-限制性片段长度多态性(PCR-RFLP)进行CYP2D6*10基因分型。记录并比较术后72 h各组间的吗啡用量及视觉模拟评分(visual analogue score,VAS)。结果:与m/m组相比,m/w组吗啡在T0.5～4 h的累积量显著升高(P<0.05)。3组中各时间段的VAS评分对比差异无统计学意义。结论:在全麻术后0.5 h至4 h急性疼痛治疗中,CYP2D6*10 m/w组所需吗啡的量比m/m组高,以此推测m/w组产生的内源性阿片肽比m/m组低。展开更多
Several preclinical and clinical studies suggested that tramadol has a multi-mechanistic analgesic action. Upon in vitro evaluation, tramadol parent drug was determined to have only very weak affinity for opioid recep...Several preclinical and clinical studies suggested that tramadol has a multi-mechanistic analgesic action. Upon in vitro evaluation, tramadol parent drug was determined to have only very weak affinity for opioid receptors. Metabolism via CYP2D6, though, yields the O-desmethyl metabolite (M1), which has much greater opioid receptor affinity. In tests in animals and human volunteers, tramadol’s analgesic effect is only partially blocked by the opioid antagonist naloxone. Yet the contribution of parent drug to analgesia is still debated. Observance of good analgesic response to tramadol in Japanese and other Asian populations that express the CYP2D6*10 genotype suggests that parent drug accounts for the majority of tramadol’s analgesic effect in most clinical settings. Understanding of tramadol’s multi-mechanistic action continues to form the basis for understanding its clinical attributes.展开更多
文摘Several preclinical and clinical studies suggested that tramadol has a multi-mechanistic analgesic action. Upon in vitro evaluation, tramadol parent drug was determined to have only very weak affinity for opioid receptors. Metabolism via CYP2D6, though, yields the O-desmethyl metabolite (M1), which has much greater opioid receptor affinity. In tests in animals and human volunteers, tramadol’s analgesic effect is only partially blocked by the opioid antagonist naloxone. Yet the contribution of parent drug to analgesia is still debated. Observance of good analgesic response to tramadol in Japanese and other Asian populations that express the CYP2D6*10 genotype suggests that parent drug accounts for the majority of tramadol’s analgesic effect in most clinical settings. Understanding of tramadol’s multi-mechanistic action continues to form the basis for understanding its clinical attributes.
