Department of Anesthesia, Riley Hospital for Children at Indiana University Health, Indianapolis, IN 46202, USA.
Department of Anesthesia, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Pharmacogenomics. 2021 Apr;22(5):275-290. doi: 10.2217/pgs-2020-0143. Epub 2021 Mar 17.
Oxycodone is a semisynthetic μ- and κ-opioid receptor with agonist with a broad scope of use including postoperative analgesia as well as control of neuropathic and cancer pain. Advantages over other opioids include prolonged duration of action, greater potency than morphine and lack of histamine release or ceiling effect. Individual responses to oxycodone can vary due to genetic differences. This review article aims to summarize the oxycodone literature and provide context on its pharmacogenomics and pharmacokinetics. The evidence for clinical effect of genetic polymorphisms on oxycodone is conflicting. There is stronger evidence linking polymorphic genetic enzymes CYP2D6 and CYP3A with therapeutic outcomes. Further, research is needed to discern all of oxycodone's metabolites and their contribution to the overall analgesic effect.
羟考酮是一种半合成的 μ-和 κ-阿片受体激动剂，具有广泛的用途，包括术后镇痛以及控制神经性疼痛和癌症疼痛。与其他阿片类药物相比，羟考酮具有作用持续时间长、比吗啡效力更大以及不释放组胺或无天花板效应等优点。个体对羟考酮的反应可能因遗传差异而有所不同。本文综述了羟考酮的相关文献，讨论了其药物基因组学和药代动力学特征。遗传多态性对羟考酮临床疗效的影响证据相互矛盾。与治疗结果相关的证据更强有力地表明，多态性遗传酶 CYP2D6 和 CYP3A 与治疗结果相关。此外，还需要进一步研究以确定羟考酮的所有代谢物及其对整体镇痛效果的贡献。
