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氨氯地平与其他药物的相互作用研究进展
引用本文:陈沈珏,;匡泽民,;袁洪,;黄志军,;左笑丛.氨氯地平与其他药物的相互作用研究进展[J].中国临床药理学与治疗学,2014(6):701-706.
作者姓名:陈沈珏  ;匡泽民  ;袁洪  ;黄志军  ;左笑丛
作者单位:[1]中南大学湘雅三医院; [2]中南大学药学院; [3]中南大学药物临床评价研究中心,湖南长沙410013
基金项目:重大基础研究前期研究专项(973前期专项)(201ICB512001);国家“重大新药创制”科技重大专项(2012ZX09303014001);国家自然科学基金(81273594);湖南省自然科学基金重点项目(11JJ2054)
摘    要:氨氯地平属于第三代钙离子拮抗剂(CCB),主要用于心脑血管疾病的治疗。近期的研究发现,氨氯地平与多种药物存在相互作用,这些相互作用主要体现在药动学和药效学两个方面。药动学相互作用主要与肝药酶CYP450以及转运体P-gP(P-糖蛋白)有关。氨氯地平是CYP450和P-gp的底物,影响肝药酶或P-gp活性的药物,如抗病毒药物利托那韦、抗真菌药物伊曲康唑以及大环内酯内抗生素他克莫司等均可改变氨氯地平的药动学特征。药效学相互作用主要表现办疗效的改变,他汀类药物、血管紧张素转化酶抑制剂(ACEI)药物以及血管紧张素Ⅱ受体拮抗剂(ARB)等与氨氯地平具有协同作用,而氯吡格雷等其他药物与氨氯地平合用时,氨氯地平的疗效降低甚至失效。本文就近年来关于氨氯地平的相互作用研究做一综述。

关 键 词:氨氯地平  药动学  药效学  相互作用

Advances in research on interactions between amlodipine and other drugs
Institution:CHEN Shen-jue, KUANG Ze-min, YUAN Hong, HUANG Zhi-jun, ZUO Xiao-cong( 1 The third Xiangya Hospital of Central South University ; 2 Department of Pharmacy, Central South University ; 3 Drug clinical evaluation research center, Central South University, Changsha 410013, Hunan , China)
Abstract:Amlodipine is a third-generation calcium antagonists, which is mainly used in thetreatment of cardio-cerebrovascular diseases. Recent research demonstrated that there existedinteractions between amlodipine and other drugs. These interactions mainly reflect in the aspects of pharmacokinetics and pharmacodynamics. Pharmacokinetics interactions is primarily related with hepatic drug metabolizing en- zyme CYP450 and transporter P-gp (P-glycoprotein). Amlodipine is a substrate of CYP450 and P-gp. Drugs that affect the activity of CYP450 or P-gp may change the profile of the pharmaco- kinetics of amlodipine, such as antivirals ritona- vir, antifungal agents itraconazole and antibiot- ics tacrolimus and so on. However, pharmacodynamic interactions can be mainly reflected bythe change 0f th6rapeutlc effect or side effect. The statins, the Angiotensin-converting enzyme inhibitors (ACEI) and Angiotensin Ⅱ receptor blocker (ARB) have synergistic effect with amlodipine, but other drugs such as clopidogrel will reduce the efficacy of amlodipine, even make amlodipine loss its efficacy. Studies on the interactions between amlodipine and other drugs in recent years are reviewed in this paper.
Keywords:amlodipine  pharmacokinetics  pharmacodynamics  interaction
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