Ezetimibe:回顾其新陈代谢,药物动力学和药物的相互作用。
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Kosoglou T, Statkevich P, Johnson-Levonas AO,保利的摩根富林明,伯格曼AJ,奥尔顿KB
Ezetimibe:回顾其新陈代谢,药物动力学和药物的相互作用。
Pharmacokinet。2005; 44 (5): 467 - 94。
- PubMed ID
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15871634 (在PubMed]
- 文摘
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Ezetimibe是第一降脂药物,抑制肠道吸收的膳食和胆汁胆固醇而不影响脂溶性营养素的吸收。口服后,ezetimibe迅速广泛吸收和代谢药物活性ezetimibe-glucuronide (> 80%)。总ezetimibe(“父”ezetimibe之和加上ezetimibe-glucuronide) post-administration浓度达到最大值1 - 2小时,其次是肝肠循环和缓慢的消除。ezetimibe的半衰期估计终端和ezetimibe-glucuronide大约是22小时。符合ezetimibe的消除半衰期,近似2倍积累观察在重复每日一次。ezetimibe 10毫克/天的推荐剂量可以管理在早上或者晚上不考虑食物。没有临床显著影响的年龄、性别或种族ezetimibe药物动力学和轻度肝损害患者的剂量的调整是必要的或轻微到严重肾功能不全。ezetimibe的主要代谢途径由glucuronidation 4-hydroxyphenyl组的尿苷5 ' -diphosphate-glucuronosyltransferase同功酶形成ezetimibe-glucuronide在小肠和肝脏。大约78%的剂量是在粪便中排出ezetimibe为主,与之相平衡的尿液中主要是ezetimibe-glucuronide。总的来说,ezetimibe有利的药物之间交互配置文件,可以在缺乏临床相关ezetimibe之间的相互作用和各种药物患者常用的血胆甾醇过多。 Ezetimibe does not have significant effects on plasma levels of HMG-CoA reductase inhibitors commonly known as statins (atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin), fibric acid derivatives (gemfibrozil, fenofibrate), digoxin, glipizide, warfarin and triphasic oral contraceptives (ethinylestradiol and levonorgestrel). Concomitant administration of food, antacids, cimetidine or statins had no significant effect on ezetimibe bioavailability. Although coadministration with gemfibrozil and fenofibrate increased the bioavailability of ezetimibe, the clinical significance is thought to be minor considering the relatively flat dose-response curve of ezetimibe and the lack of dose-related increase in adverse events. In contrast, coadministration with the bile acid binding agent colestyramine significantly decreased ezetimibe oral bioavailability (based on area under the plasma concentration-time curve of total ezetimibe). Hence, ezetimibe and colestyramine should be administered several hours apart to avoid attenuating the efficacy of ezetimibe. Finally, higher ezetimibe exposures were observed in patients receiving concomitant ciclosporin, and ezetimibe caused a small but statistically significant effect on plasma levels of ciclosporin. Because treatment experience in patients receiving ciclosporin is limited, physicians are advised to exercise caution when initiating ezetimibe in the setting of ciclosporin coadministration, and to carefully monitor ciclosporin levels.
DrugBank数据引用了这篇文章
- 药物
- 药物酶
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药物 酶 类 生物 药理作用 行动 Ezetimibe 细胞色素P450 2 c8 蛋白质 人类 未知的抑制剂细节 Ezetimibe 细胞色素P450 3 a4 蛋白质 人类 未知的抑制剂细节 Ezetimibe UDP-glucuronosyltransferase 1 - 1 蛋白质 人类 未知的底物细节 Ezetimibe UDP-glucuronosyltransferase 1 - 3 蛋白质 人类 未知的底物细节 Ezetimibe UDP-glucuronosyltransferase 2去往b15 蛋白质 人类 未知的底物细节 Ezetimibe UDP-glucuronosyltransferase 2 b7 蛋白质 人类 未知的底物细节 - 药物反应
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反应 细节 细节 细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
