a Center for Neurobiology and Behavior, Department of Psychiatry , University of Pennsylvania School of Medicine , Philadelphia , PA , USA.
b Assurex Health Inc ., Mason , OH , USA.
Am J Drug Alcohol Abuse. 2018;44(4):431-440. doi: 10.1080/00952990.2017.1420795. Epub 2018 Jan 15.
Currently, no pharmacogenetic tests for selecting an opioid-dependence pharmacotherapy have been approved by the US Food and Drug Administration.
Determine the effects of variants in 11 genes on dropout rate and dose in patients receiving methadone or buprenorphine/naloxone (ClinicalTrials.gov Identifier: NCT00315341).
Variants in six pharmacokinetic genes (CYP1A2, CYP2B6, CYP2C19, CYP2C9, CYP2D6, CYP3A4) and five pharmacodynamic genes (HTR2A, OPRM1, ADRA2A, COMT, SLC6A4) were genotyped in samples from a 24-week, randomized, open-label trial of methadone and buprenorphine/naloxone for the treatment of opioid dependence (n = 764; 68.7% male). Genotypes were then used to determine the metabolism phenotype for each pharmacokinetic gene. Phenotypes or genotypes for each gene were analyzed for association with dropout rate and mean dose.
Genotype for 5-HTTLPR in the SLC6A4 gene was nominally associated with dropout rate when the methadone and buprenorphine/naloxone groups were combined. When the most significant variants associated with dropout rate were analyzed using pairwise analyses, SLC6A4 (5-HTTLPR) and COMT (Val158Met; rs4860) had nominally significant associations with dropout rate in methadone patients. None of the genes analyzed in the study was associated with mean dose of methadone or buprenorphine/naloxone.
This study suggests that functional polymorphisms related to synaptic dopamine or serotonin levels may predict dropout rates during methadone treatment. Patients with the S/S genotype at 5-HTTLPR in SLC6A4 or the Val/Val genotype at Val158Met in COMT may require additional treatment to improve their chances of completing addiction treatment. Replication in other methadone patient populations will be necessary to ensure the validity of these findings.
目前,美国食品和药物管理局尚未批准任何用于选择阿片类药物依赖药物治疗的药物遗传学检测。
确定 11 个基因中的变异对接受美沙酮或丁丙诺啡/纳洛酮治疗的患者的脱落率和剂量的影响(ClinicalTrials.gov 标识符:NCT00315341)。
在一项为期 24 周的、随机、开放标签的美沙酮和丁丙诺啡/纳洛酮治疗阿片类药物依赖的试验中,对 764 名患者(68.7%为男性)的样本进行了六个药代动力学基因(CYP1A2、CYP2B6、CYP2C19、CYP2C9、CYP2D6、CYP3A4)和五个药效学基因(HTR2A、OPRM1、ADRA2A、COMT、SLC6A4)的变异检测。然后,使用基因分型来确定每个药代动力学基因的代谢表型。分析每个基因的表型或基因型与脱落率和平均剂量的关系。
SLC6A4 基因的 5-HTTLPR 基因型与美沙酮和丁丙诺啡/纳洛酮联合组的脱落率呈名义相关。当使用两两分析分析与脱落率最显著相关的变体时,美沙酮患者中 SLC6A4(5-HTTLPR)和 COMT(Val158Met;rs4860)与脱落率呈名义相关。在本研究中分析的基因均与美沙酮或丁丙诺啡/纳洛酮的平均剂量无关。
这项研究表明,与突触多巴胺或 5-羟色胺水平相关的功能多态性可能预测美沙酮治疗期间的脱落率。在 SLC6A4 中 5-HTTLPR 为 S/S 基因型或在 COMT 中 Val158Met 为 Val/Val 基因型的患者可能需要额外的治疗,以提高他们完成成瘾治疗的机会。在其他美沙酮患者群体中进行复制将是必要的,以确保这些发现的有效性。