| 张芹 唐辉 姬利红 张焕云 李乐.CYP3A5*3 基因多态性对癫痫患者卡马西平及其主要代谢物浓度的影响[J].,2016,16(27):5262-5265 |
| CYP3A5*3 基因多态性对癫痫患者卡马西平及其主要代谢物浓度的影响 |
| Effects of CYP3A5*3 Genetic Polymorphisms on SerumConcentrations in People with Epilepsy |
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| DOI： |
| 中文关键词: 卡马西平 CYP3A5*3 基因多态性 药物浓度监测 癫痫 清除率 个体差异 |
| 英文关键词: Carbamazepine CYP3A5 Polymorphism drug monitoring Epilepsy Clearance Individual variation |
| 基金项目:国家自然科学基金项目(81260627) |
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| 中文摘要: |
| 背景：卡马西平（carbamazepine, CMZP）主要由CYP3A酶家族代谢，其代谢酶主要包括CYP3A5。本研究探讨了CYP3A5基
因多态性与卡马西平血清浓度（CMZP）之间的关系，对个体化药物治疗的开展具有十分积极的意义。目的：CYP3A5 * 3的基因型
可以影响CYP3A 药物的药代动力学。本研究旨在评估CYP3A基因多态性对癫痫患者血清卡马西平稳态浓度及其代谢物水平的
影响。方法：研究共纳入278 例患者，检测个体卡马西平的血清浓度及CYP3A5 基因型，并探讨CYP3A5 基因型对卡马西平稳态
血药浓度的影响。结果：根据基因型分为成CYP3A5 表达组（CYP3A5*1/*1 和CYP3A5*1/*3）和非表达组（CYP3A5*3/*3）两组。
278 例患者中120 例为CYP3A5 表达组，158例患者为CYP3A5 非表达组。CYP3A5 非表达组的总卡马西平剂量和剂量标准化后
的卡马西平血清浓度均高于CYP3A5 表达组（P=0.608 和P=0.000）。CYP3A5 表达组中卡马西平环氧化物浓度更高（P=0.000），但
这两组间的血清药物浓度无显著差异（P=0.090）。结论：CYP3A5*3 基因多态性与卡马西平的血清浓度之间有密切的关系。
CYP3A5 基因影响了卡马西平血药浓度水平和代谢过程，其可能是导致卡马西平在癫痫患者中个体变异的一个重要因素。 |
| 英文摘要: |
| Objective:Carbamazepine (CMZP) mainly metabolize by CYP3A enzyme family, which includes enzyme CYP3A5.
This study investigated the relationship between CYP3A5 gene polymorphism and serum concentration of carbamazepine.
CYP3A5 * 3 genotype CYP3A can affect the pharmacokinetics of carbamazepine. This study aimed to assess the impact of CYP3A gene
polymorphism on the steady-state serum concentrations of carbamazepine and its metabolite levels in patients with epilepsy.Methods:A
total of 278 cases of patients, serum concentrations of carbamazepine and CYP3A5 genotype of individuals were collected, and the impact
of CYP3A5 genotype on steady-state plasma concentrations of carbamazepine were analysis.Results:According to the expression of
CYP3A5 genotype，we divided all patients into two groups，CYP3A5 expression group (CYP3A5 * 1 / * 1 and CYP3A5 * 1 / * 3) and
non-expression group (CYP3A5 * 3 / * 3) groups. 120 cases in CYP3A5 expression group, 158 cases of patients in CYP3A5 non-expressing
group. Carbamazepine serum concentrations and it's normalized dose in CYP3A5 expression group were higher than the
CYP3A5 non-expression group (P=0.608 and P=0.000). And the carbamazepine epoxide concentration in CYP3A5 expression group was
much higher (P=0.000), but no significance carbamazepine serum concentrations difference was detected between the two groups
(P=0.090).Conclusion:There is a close relationship between CYP3A5 * 3 polymorphism and serum concentrations of carbamazepine.
CYP3A5 gene can affects the plasma concentration of carbamazepine levels and metabolic processes, which may be an important factor
leading to carbamazepine individual variation in epilepsy patients. |
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