内分泌
词汇介绍
拓展阅读
解析
Repaglinide
释 义 瑞格列奈
例 句 Objective: To observe the clinical efficacy and safety of combined treatment of repaglinide and acarbose in aged patients with diabetes type 2. 目的：观察瑞格列奈、阿卡波糖联合治疗老年性2型糖尿病患者的临床疗效及安全性。
概述
概述
瑞格列奈是一种抗糖尿病药，称为美格替尼，于1983年发明，瑞格列奈是一种口服药物，除饮食和运动外，可用于控制2型糖尿病的血糖。瑞格列奈的作用机制涉及促进胰腺β胰岛细胞释放胰岛素。像其他抗糖尿病药一样，主要的副作用是低血糖症。
机制
瑞格列奈可通过刺激胰腺β胰岛细胞释放胰岛素来降低血糖，它通过关闭β细胞膜中ATP依赖性钾离子通道来实现，这使β细胞去极化，打开细胞的钙通道，并且所产生的钙内流诱导胰岛素分泌。
吸收：瑞格列奈从胃肠道吸收时具有56%的生物利用度。与食物一起服用会降低生物利用度，最大浓度降低20%。
分布：瑞格列奈与白蛋白的蛋白结合率大于98%。
代谢：瑞格列奈主要由肝脏代谢-特别是CYP450 2C8和3A4-并通过葡萄糖醛酸化程度较小。瑞格列奈的代谢产物是无活性的，并且不表现出降低葡萄糖的作用。
排泄：瑞格列奈在粪便中排泄90%，在尿中排泄8%。
临床应用
瑞格列奈可单独使用或与其他药物一起使用，以控制高血糖以及适当的饮食和锻炼计划，它用于2型糖尿病患者，控制高血糖有助于预防肾脏损害，失明，神经问题，四肢感觉异常和性功能问题。正确控制糖尿病也可以减少心脏病发作或中风的风险。它通过刺激人体产生更多的胰岛素而起作用。
不良反应
常见的不良事件包括：低血糖症（31%）；上呼吸道感染（16%）；鼻窦炎（6%）；鼻炎（3%）；恶心（5%）；腹泻（5%）；便秘（3%）；呕吐（3%）；关节痛（6%）；背痛（5%）；头痛（11%）；感觉异常（3%）等。
严重的不良事件包括：心脏缺血（2%）；心绞痛（1.8%）；心血管事件导致的死亡（0.5%）。
禁忌症
瑞格列奈禁用于以下人群：糖尿病性酮症酸中毒，伴或不伴昏迷；1型糖尿病；与吉非贝齐共同给药；已知对药物或非活性成分过敏。
注意事项
瑞格列奈是CYP3A4的主要底物，不应与吉非贝齐，克拉霉素或伊曲康唑或酮康唑等唑类抗真菌药同时使用，瑞格列奈和一种或多种这些药物的给药会导致瑞格列奈的血浆浓度升高，并可能导致低血糖症。瑞格列奈和氯吡格雷（一种CYP2C8抑制剂）的共同给药可能导致由于药物相互作用而使血糖水平显着下降。实际上，即使将这些药物一起使用一天也可能导致瑞格列奈水平升高5倍以上，并可能导致严重的低血糖症。瑞格列奈不宜与磺酰脲类药物合用，因为它们具有相同的作用机理。
复制标题瑞格列奈与塞来昔布代谢药物相互作用的药代动力学评价生物分析HPLC法同时荧光检测
发表时间：2019-08-02
影响指数：4.8
作者： Dong-Gyun Han
期刊：Pharmaceutics
Arthritis and diabetes mellitus are highly prevalent diseases with a total of over 350 million patients worldwide. The most common types of arthritis and diabetes mellitus are osteoarthritis (OA) and type 2 diabetes mellitus (T2DM), respectively. OA affects 14% of adults aged ≥25 years, and 34% of these patients are aged >65 years; similarly, T2DM affects 12% of adults aged ≥20 years, and 26% of these are aged >65 years. A recent survey estimated that the prevalence of OA was higher in individuals with T2DM than in those without T2DM. Thus, T2DM is generally recognized as a comorbidity of arthritis, while some previous studies have focused on diabetes as a risk factor of arthritis. Anyway, it is evident that T2DM is closely associated with an increased incidence and prevalence of OA, though the reasons remain unclear.Because T2DM frequently co-exists with OA, there is a possibility of concurrent administration of REP and CEL. Hence, a bioanalytical method of simultaneous determination of REP and CEL could be useful and efficient for further pharmaceutical development and therapeutic optimization. To date, several bioanalytical methods have been developed and validated for quantitative determination of REP or CEL individually using HPLC with UV/Vis detection or using liquid chromatography with tandem mass spectrometry (LC-MS/MS) systems. However, these methods are associated with a few limitations, such as an insufficient sensitivity, relatively large sample volume, and/or time-consuming liquid–liquid extraction procedures with volatile solvents that are potentially hazardous to health. Moreover, LC-MS/MS methods require relatively complex and/or expensive instrumentation, which may not be affordable for small-sized laboratories and companies in resource-limited settings. To the best of our knowledge, there have been no reported methods of simultaneous quantification of REP and CEL in biological samples using HPLC coupled with a fluorescence detector (HPLC-FL). Furthermore, a previous in vitro study reported that CEL inhibited REP metabolism in pooled human liver microsomes (HLM) with a Ki of 3.1 μM. This suggests the possibility of pharmacokinetic drug interaction between REP and CEL, but no information is currently available regarding this issue.
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