Aravindan Lakshmi, Velu Sanjana, Sivam Inesh, Sivam Sahana, Tallapaneni Pooja S, Ressler Ruthie, Marks Michael, Venkataramanan Raman, Radhakrishnan Rupa, Sadhasivam Senthilkumar
Department of Biosciences, Rice University, Houston, TX, USA.
Pre-medical Medical Program, Pennsylvania State University, University Park, PA, USA.
Pharmacogenomics. 2025 May-Jun;26(7-9):263-270. doi: 10.1080/14622416.2025.2546770. Epub 2025 Sep 5.
Buprenorphine, a semi-synthetic opioid, is used to treat Opioid Use Disorder (OUD) and as an analgesic. Buprenorphine's benefits over other opioids include longer duration of action, lower abuse potential, and a ceiling effect to serious adverse effects such as respiratory depression. This is a literature review of gene variants affecting the pharmacokinetics and pharmacodynamics of buprenorphine from databases, such as PubMed. Genetic polymorphisms related to metabolism and receptor binding of buprenorphine can alter the pharmacokinetics and response to buprenorphine. Specifically, genetic variants in , and may affect metabolism and clinical response to buprenorphine. There is strong evidence linking polymorphism in Cytochrome P450 3A4 () and UDP-Glucuronosyltransferase-2B7 (), enzymes involved in buprenorphine metabolism, with dosing requirements, treatment of OUD, and pain relief. Response to buprenorphine, an effective treatment for opioid use disorder and pain management, differs significantly based on several human genetic variations. However, there is currently insufficient evidence for the clinical significance of individualized treatment of buprenorphine based on genetic variants. Therefore, it is crucial that future research should prioritize evaluating the feasibility and clinical significance of individualized risk predictions and personalized dosing of buprenorphine.
丁丙诺啡是一种半合成阿片类药物，用于治疗阿片类物质使用障碍（OUD）并作为镇痛药。丁丙诺啡相对于其他阿片类药物的优势包括作用时间更长、滥用可能性更低，以及对呼吸抑制等严重不良反应有封顶效应。这是一篇从PubMed等数据库对影响丁丙诺啡药代动力学和药效学的基因变异进行的文献综述。与丁丙诺啡代谢和受体结合相关的基因多态性可改变其药代动力学和对丁丙诺啡的反应。具体而言，某些基因变异可能会影响丁丙诺啡的代谢和临床反应。有强有力的证据表明，参与丁丙诺啡代谢的细胞色素P450 3A4（CYP3A4）和尿苷二磷酸葡萄糖醛酸基转移酶-2B7（UGT2B7）的基因多态性与给药要求、OUD治疗及疼痛缓解有关。基于几种人类基因变异，丁丙诺啡作为阿片类物质使用障碍和疼痛管理的有效治疗方法，其反应存在显著差异。然而，目前基于基因变异的丁丙诺啡个体化治疗的临床意义证据不足。因此，未来研究应优先评估丁丙诺啡个体化风险预测和个性化给药的可行性及临床意义，这一点至关重要。
