Discipline of Pharmacology, School of Medical Sciences, Faculty of Health Sciences, University of Adelaide, Adelaide, Australia; Centre for Personalised Cancer Medicine, University of Adelaide, Adelaide, Australia; Department of Clinical Pharmacology, Royal Adelaide Hospital, Adelaide, Australia.
Clin Pharmacol Ther. 2015 Feb;97(2):125-7. doi: 10.1002/cpt.23. Epub 2014 Dec 9.
For opioids requiring CYP2D6 O-demethylation to active metabolites, poor metabolizers have reduced metabolite formation and minimal pain reduction. Clinically, this has only reliably been shown for tramadol. Ultra-rapid metabolizers have an increased risk of toxicity especially for codeine. ABCB1 genetics show no consistent findings. In Asian populations, the high OPRM1 118A>G frequency associates with higher opioid dosage requirements. Clinical translation of opioid genetics is premature because many important pain and addiction phenotype factors contribute.
对于需要 CYP2D6 O-去甲基化生成活性代谢物的阿片类药物，弱代谢者的代谢物生成减少，疼痛缓解最小。临床上，这仅在曲马多中可靠地显示。超快代谢者的毒性风险增加，特别是对可待因。ABCB1 遗传学没有一致的发现。在亚洲人群中，高 OPRM1 118A>G 频率与更高的阿片类药物剂量需求相关。阿片类药物遗传学的临床转化还不成熟，因为许多重要的疼痛和成瘾表型因素都有贡献。
