[1]梁业飞.阿利吉仑的药理作用和临床应用研究进展[J].大众科技,2022,24(03):63-66.
 Research Progress Pharmacological Effects and Clinical Application of Aliskiren[J].Popular Science & Technology,2022,24(03):63-66.
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阿利吉仑的药理作用和临床应用研究进展()
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《大众科技》[ISSN:1008-1151/CN:45-1235/N]

卷:
24
期数:
2022年03
页码:
63-66
栏目:
医药与卫生
出版日期:
2022-03-20

文章信息/Info

Title:
Research Progress Pharmacological Effects and Clinical Application of Aliskiren
作者:
梁业飞 
(钦州市第一人民医院,广西 钦州 535000)
关键词:
阿利吉仑高血压直接肾素抑制剂药理作用临床应用
Keywords:
Aliskiren hypertension direct renin inhibitor pharmacological effects clinical application
文献标志码:
A
摘要:
高血压老年患者大多合并多种疾病,存在多种药物合用,达到降压目标依然面临着挑战,因此老年高血压的药物治疗一直是研究的热点。阿利吉仑是首个上市的口服直接肾素抑制剂,可直接降低肾素的活性,作用于肾素-血管紧张素系统。阿利吉仑作为抗高血压药物,起效快,降压效果确切,具有心血管和肾脏的保护作用。文章综合国内外文献,探讨阿利吉仑药理作用及其多样性和临床应用。
Abstract:
Most elderly patients with hypertension are complicated with a variety of diseases, and there are a variety of drugs in combination. Meeting the goal of reducing blood pressure is still facing challenges. Therefore, the drug treatment of elderly hypertension has always been a research hotspot. Aliskiren is the first listed oral direct renin inhibitor, which can directly reduce the activity of renin and act on the renin angiotensin system. As an antihypertensive drug, Aliskiren has rapid effect and definite antihypertensive effect. It has the protective effects of cardiovascular and kidney. The clinical application and research of aliskiren are less in China. This paper summarizes the literature at home and abroad to explore the pharmacological effects, diversity and clinical application of Aliskiren.

参考文献/References:

[1] WHO. Report on cardiovascular diseases[R]. Geneva: World Health Organization, 2017. [2] Jagadeesh G, Balakumar P, Stockbridge N. How well do aliskirens purported mechanisms track its effects on cardiovascular and renal disorders?[J]. Cell Signal, 2012, 24(8): 1583-1591. [3] 治疗高血压的药物阿利吉仑在华获准上市[J]. 中国执业药师,2010,7(9): 54. [4] 朱依谆,殷明. 药理学[M]. 人民卫生出版社,2011. [5] Imanishi T, Tsujioka H, Ikejima H, et al. Renin inhibitor aliskiren improves impaired nitric oxide bioavailability and protects against atherosclerotic changes[J]. Hypertension, 2008, 52(3): 563-572. [6] Whaley-Connell A, Nistala R, Habibi J, et al. Comparative effect of direct renin inhibition and AT1R blockade on glomerular filtration barrier injury in the transgenic Ren2 rat[J]. American Journal of Physiology-Renal Physiology, 2009, 298(3): 655-661. [7] Singh V P, Le B, Khode R, et al. Intracellular angiotensin II production in diabetic rats is correlated with cardiomyocyte apoptosis, oxidative stress, and cardiac fibrosis[J]. Diabetes, 2008, 57(12): 3297-3306. [8] Habibi J, Whaley-Connell A, Hayden M R, et al. Renin inhibition attenuates insulin resistance, oxidative stress, and pancreatic remodeling in the transgenic Ren2 rat[J]. Endocrinology, 2008, 149(11): 5643-5653. [9] Solomon S D, Appelbaum E, Manning W J, et al. Effect of the direct renin inhibitor aliskiren, the angiotensin receptor blocker losartan, or both on left ventricular mass in patients with hypertension and left ventricular hypertrophy[J]. Circulation, 2009, 119(4): 530-537. [10] Schmerbach K, Pfab T, Zhao Y, et al. Effects of aliskiren on stroke in rats expressing human renin and angiotensinogen genes[J]. PLoS ONE, 2010, 5(11): e15052. [11] Miao J, Wang L, Zhang X, et al. Protective effect of aliskiren in experimental ischemic stroke: up-regulated p-PI3K, p-AKT, Bcl-2 expression, attenuated bax expression[J]. Neurochemical Research, 2016, 41(9): 2300-2310. [12] Wiggins K J, Kelly D J. Aliskiren: a novel renoprotective agent or simply an alternative to ACE inhibitors?[J]. Kidney International, 2009, 76(1): 23-31. [13] Pimenta E, Oparil S. Role of aliskiren in cardio-renal protection and use in hypertensives with multiple risk factors[J]. Vascular Health and Risk Management, 2009, 5(1): 453-463. [14] Fisher N D, Jan D A H, Nussberger J, et al. Renal and hormonal responses to direct renin inhibition with aliskiren in healthy humans[J]. Circulation, 2008, 117(25): 3199-3205. [15] 陆婉杏,蒙兰青,黄晓华. 阿利吉仑对氧糖剥夺损伤的SH-SY5Y细胞的保护作用及可能机制[J]. 中国病理生理杂志,2019,35(9): 1630-1634. [16] 李晓青,陈云茹,张曦,等. 阿利吉仑对大鼠急性肝衰竭的保护作用及机制研究[J]. 医学研究杂志,2021,50(6): 31-35,40. [17] 吴冰璇,黄淑芬,吴文超,等. 阿利吉仑通过抑制炎症和凋亡反应改善小鼠心肌缺血再灌注损伤[J]. 中南医学科学杂志,2021,49(4): 397-401. [18] 古钎林,吴冰璇,黄振华,等. 阿利吉仑通过调控线粒体介导的凋亡通路改善心肌缺血再灌注损伤[J]. 中国动脉硬化杂志,2020,28(7): 559-565. [19] Mohamed E Nashwa B, Ahmed E, et al. Functional and molecular evaluation of using aliskiren during acute and chronic partial ureteral obstruction in rat solitary kidney[J]. Life Sciences, 2021, 265: 118811. [20] Choi D E, Jeong J Y, Lim B J, et al. Aliskiren ameliorates renal inflammation and fibrosis induced by unilateral ureteral obstruction in mice[J]. Journal of Urology, 2011, 186: 694-701. [21] Ahmed A T, Azad K A, Hassan O H, et al. The anti-inflammatory effect of different doses of aliskiren in rat models of inflammation[J]. Drug Design Development and Therapy, 2020, 14: 2841-2851. [22] Yan K, Shen Y. Aliskiren has chondroprotective efficacy in a rat model of osteoarthritis through suppression of the local renin-angiotensin system[J]. Molecular Medicine Reports, 2017, 16: 3965-3973. [23] Azouz A A, Esraa A, Abo-Saif A A. Aliskiren, tadalafil, and cinnamaldehyde alleviate joint destruction biomarkers MMP-3 and RANKL in complete Freunds adjuvant arthritis model: Downregulation of IL-6/JAK2/STAT3 signaling pathway[J]. Saudi Pharmaceutical Journal, 2020, 28: 1101-1111. [24] Saeed A. Aliskiren-A promising antioxidant agent beyond hypertension reduction[J]. Chemico-Biological Interactions, 2020, 326: 109145. [25] Mohammad A, Hale T M, Czubryt P. Targeting the renin-angiotensin-aldosterone system in fibrosis[J]. Matrix Biology, 2020(91-92): 92-108. [26] Ames M K, Atkins C E, Pitt B. The renin-angiotensin- aldosterone system and its suppression[J]. Journal of Veterinary Internal Medicine, 2019, 33(2): 363-382. [27] Vaimes E A, Galceran J M, Raij L. Angiotensin II induces superoxide anion production by mesangial cells[J]. Kidney International, 1998, 54 (3): 775-784. [28] Jones M R, Sealey J E, Laragh J H. Effects of angiotensin receptor blockers on ambulatory plasma renin activity in healthy, normal subjects during unrestricted sodium intake[J]. American Journal of Hypertension, 2007, 20: 907. [29] Mori Y, Ogawa Y, Mochizuki A, et al. Design and discovery of new (3S, 5R)-5-[4-(2-chlorophenyl)-2, 2-dimethyl-5-oxopiperazin-1-yl] piperidine-3-carboxamides as potent renin inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2012, 22(24): 7677-7682. [30] Nakamura Y, Fujimoto T, Ogawa Y, et al. Discovery of DS-8108b, a novel orally bioavailable renin inhibitor[J]. ACS Medicinal Chemistry Letters, 2012, 3(9): 754-758. [31] Ferrario C M, Strawn W B. Role of the renin- angiotensin-aldosterone system and proinflammatory mediators in cardiovascular disease[J]. American Journal of Cardiology, 2006, 98(1): 121-128. [32] Barrios V, Escobar C. Aliskiren: a new drug for an old problem[J]. Cardiovascular and Hematological Agents in Medicinal Chemistry, 2010, 8(1): 1-10. [33] Wang G M, Li L J, Tang W, et al. Renin inhibitors versus angiotensin converting enzyme (ACE) inhibitors for primary hypertension[J]. Cochrane Database of Systematic Reviews, 2020, 10: CD012569. [34] 刘娟,梁珍玲,谢晓华. 阿利吉仑联合血管紧张素Ⅱ受体拮抗剂对老年高血压性心肌病患者血压控制及左心室功能的影响[J]. 中国处方药,2020,18(7): 108-109.[35] Carmine S, Carolina D C, Anna P, et al. Effect of direct renin inhibition on vascular function after long-term treatment with aliskiren in hypertensive and diabetic patients[J]. Journal of Hypertension, 2021, 39: 169-180. [36] 郭妍,曾葭,李强,等. 直接肾素抑制剂阿利吉仑治疗重型新型冠状病毒肺炎合并高血压患者的初步临床研究[J]. 中华高血压杂志,2021,29(6): 600-602. [37] Bourgonje A R, Abdulle A E, Wim T, et al. Angiotensin-converting enzyme 2 (ACE2), SARS-CoV-2 and the pathophysiology of coronavirus disease 2019 (COVID-19)[J]. Journal of Pathology, 2020, 251: 228-248. [38] Solomon S D, Shin S H, Amil S, et al. Effect of the direct renin inhibitor aliskiren on left ventricular remodelling following myocardial infarction with systolic dysfunction[J]. European Heart Journal, 2011, 32: 1227-1234. [39] Krum H, McMurray J J, Abraham W T, et al. The Aliskiren Trial to Minimize Outcomes in Patients with Heart failure trial (ATMOSPHERE): revised statistical analysis plan and baseline characteristics[J]. European Journal of Heart Failur,. 2015, 17(10): 1075-1083. [40] Bjerre H L, Christensen J B, Henrik N, et al. The role of aliskiren in the management of hypertension and major cardiovascular outcomes: a systematic review and meta-analysis[J]. Journal of Human Hypertension, 2019, 33: 795-806. [41] Zhao Q, Shen J, Lu J, et al. Clinical efficacy, safety and tolerability of Aliskiren Monotherapy (AM): an umbrella review of systematic reviews[J]. BMC Cardiovascular Disorders, 2020, 20: 179. [42] White W B, Bresalier R, Kaplan A P, et al. Safety and tolerability of the direct renin inhibitor aliskiren: a pooled analysis of clinical experience in more than 12,000 patients with hypertension[J]. Journal of Clinical Hypertension, 2010, 12(10): 765-775. [43] 国家心血管病中心国家基本公共卫生服务项目基层高血压管理办公室,国家基层高血压管理专家委员会. 国家基层高血压防治管理指南2020版[J]. 中国医学前沿杂志(电子版),2021,13(4): 26-37. [44] 中华医学会,中华医学会临床药学分会,中华医学会杂志社,中华医学会全科医学分会,中华医学会《中华全科医师杂志》编辑委员会,基层医疗卫生机构合理用药指南编写专家组. 高血压基层合理用药指南[J]. 中华全科医师杂志,2021,20(1): 21-28. [45] Lakshmanan L, Briget K B, Sakeena M, et al. Mechanistic insights on nsSNPs on binding site of renin and cytochrome P450 proteins: A computational perceptual study for pharmacogenomics evaluation[J]. Journal of Cellular Biochemistry, 2021, 122(4): 30069. [46] 何杜娟,郭子宏. 阿利吉仑降压疗效及对血尿酸的影响[J]. 中国老年保健医学,2020,18(6): 125-128.

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备注/Memo

备注/Memo:
【收稿日期】2021-12-22 【基金项目】青年基金项目“硫酸镁复合罗哌卡因腹横肌平面阻滞在腹腔镜直肠癌患者的术后镇痛研究”(Z20200219)。 【作者简介】梁业飞(1980-),男,广西钦州人,钦州市第一人民医院临床药学科副主任药师,研究方向为临床药学。
更新日期/Last Update: 2022-06-21