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替米沙坦:用于心血管疾病预防的综述。

Telmisartan: a review of its use in cardiovascular disease prevention.

机构信息

Adis, a Wolters Kluwer Business, Auckland, New Zealand.

出版信息

Drugs. 2011 Apr 16;71(6):651-77. doi: 10.2165/11206710-000000000-00000.

DOI:10.2165/11206710-000000000-00000
PMID:21504246
Abstract

Telmisartan (Micardis®, Pritor®), a well established angiotensin type 1 receptor antagonist, is indicated in the EU for the reduction of cardiovascular morbidity in patients with manifest atherothrombotic cardiovascular disease (CVD) or type 2 diabetes mellitus with documented target organ damage, as well as for the treatment of hypertension. In the pivotal ONTARGET trial, which enrolled ACE inhibitor-tolerant patients at high vascular risk, telmisartan 80 mg once daily added to existing, proven therapy was noninferior to ramipril 10 mg once daily (the gold standard cardioprotective ACE inhibitor) in terms of CVD prevention. Moreover, telmisartan was better tolerated than ramipril, as reflected in, for example, lower incidences of permanent treatment discontinuations due to cough and angioedema. The placebo-controlled TRANSCEND and PRoFESS studies provided supporting evidence for the (time-dependent) effectiveness of telmisartan in preventing cardiovascular events, although the drug appeared to have neither a beneficial nor a harmful impact on cardiovascular mortality. The TRANSCEND trial also demonstrated that telmisartan was well tolerated in ACE inhibitor-intolerant patients at high vascular risk. On the basis of these findings, telmisartan can be considered an effective treatment option for CVD prevention in patients at high vascular risk. Consideration may be given to prescribing the drug as an alternative to ramipril in patients who are able to tolerate ACE inhibitors and, potentially, instead of ramipril in patients who are unable to tolerate ACE inhibitors.

摘要

替米沙坦(美卡素 ® 、必洛斯 ® ),一种成熟的血管紧张素 1 型受体拮抗剂,在欧盟被批准用于减少有明显动脉粥样硬化性心血管疾病(CVD)或有明确靶器官损害的 2 型糖尿病患者的心血管发病率,以及治疗高血压。在关键性 ONTARGET 试验中,该试验招募了血管风险高的能耐受 ACE 抑制剂的患者,替米沙坦 80mg 每日一次联合现有、已证实的治疗方案与雷米普利 10mg 每日一次(金标准的心脏保护 ACE 抑制剂)在预防 CVD 方面非劣效。此外,替米沙坦的耐受性优于雷米普利,例如,因咳嗽和血管水肿导致永久停药的发生率较低。安慰剂对照的 TRANSCEND 和 PRoFESS 研究提供了支持替米沙坦(时间依赖性)有效性的证据,尽管该药物对心血管死亡率似乎既没有有益影响也没有有害影响。TRANSCEND 试验还表明,替米沙坦在血管风险高的不能耐受 ACE 抑制剂的患者中耐受性良好。基于这些发现,替米沙坦可被视为高血管风险患者预防 CVD 的有效治疗选择。对于能够耐受 ACE 抑制剂的患者,可以考虑将该药物作为雷米普利的替代药物进行处方,对于不能耐受 ACE 抑制剂的患者,也可以考虑将其替代雷米普利。

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Telmisartan: a review of its use in cardiovascular disease prevention.替米沙坦:用于心血管疾病预防的综述。
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Telmisartan prevents cardiovascular events in a broad group of at-risk patients.替米沙坦可预防广泛高危患者的心血管事件。
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Renal outcomes with telmisartan, ramipril, or both, in people at high vascular risk (the ONTARGET study): a multicentre, randomised, double-blind, controlled trial.替米沙坦、雷米普利或二者联用对高血管风险人群的肾脏结局影响(ONTARGET研究):一项多中心、随机、双盲、对照试验
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Am Heart J. 2004 Jul;148(1):52-61. doi: 10.1016/j.ahj.2004.03.020.
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本文引用的文献

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A New Option for Therapeutic Management of Patients with Cardiovascular Disease : A Closer Look at the ONTARGET Study.
High Blood Press Cardiovasc Prev. 2008 Apr;15(2):47-51. doi: 10.2165/00151642-200815020-00002. Epub 2013 Jan 3.
2
Cardiovascular and renal outcomes with telmisartan, ramipril, or both in people at high renal risk: results from the ONTARGET and TRANSCEND studies.替米沙坦、雷米普利或两者联合用于高危肾脏人群的心血管和肾脏结局:ONTARGET 和 TRANSCEND 研究结果。
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3
ONTARGET still OFF-TARGET?是“在靶点上”还是“脱靶”?
Telmisartan increases systemic exposure to rosuvastatin after single and multiple doses, and in vitro studies show telmisartan inhibits ABCG2-mediated transport of rosuvastatin.
替米沙坦单次及多次给药后均会增加瑞舒伐他汀的全身暴露量,且体外研究表明替米沙坦可抑制ABCG2介导的瑞舒伐他汀转运。
Eur J Clin Pharmacol. 2016 Dec;72(12):1471-1478. doi: 10.1007/s00228-016-2130-1. Epub 2016 Sep 20.
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Comparative effectiveness of angiotensin-receptor blockers for preventing macrovascular disease in patients with diabetes: a population-based cohort study.血管紧张素受体阻滞剂预防糖尿病患者大血管疾病的效果比较:基于人群的队列研究。
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Telmisartan improves insulin resistance in patients with low cytokine levels.替米沙坦可改善细胞因子水平低的患者的胰岛素抵抗。
J Investig Med. 2011 Mar;59(3):602-5. doi: 10.2310/JIM.0b013e31820bf26b.
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Clinical effectiveness of telmisartan alone or in combination therapy for controlling blood pressure and vascular risk in the elderly.替米沙坦单药或联合治疗对控制老年患者血压和血管风险的临床效果。
Clin Interv Aging. 2010 Dec 3;5:403-16. doi: 10.2147/CIA.S6709.
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Antihypertensive drugs and risk of cancer: network meta-analyses and trial sequential analyses of 324,168 participants from randomised trials.降压药物与癌症风险:来自随机试验的 324168 名参与者的网络荟萃分析和试验序贯分析。
Lancet Oncol. 2011 Jan;12(1):65-82. doi: 10.1016/S1470-2045(10)70260-6. Epub 2010 Nov 29.
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From evidence to rationale: cardiovascular protection by angiotensin II receptor blockers compared with angiotensin-converting enzyme inhibitors.从证据到理论依据:与血管紧张素转换酶抑制剂相比,血管紧张素II受体阻滞剂对心血管的保护作用
Cardiology. 2010;117(3):163-73. doi: 10.1159/000320094. Epub 2010 Nov 4.
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Effects of telmisartan on insulin resistance in Japanese type 2 diabetic patients.替米沙坦对日本2型糖尿病患者胰岛素抵抗的影响。
Intern Med. 2010;49(17):1843-7. doi: 10.2169/internalmedicine.49.3189. Epub 2010 Sep 1.
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Effects of telmisartan on arterial stiffness assessed by the cardio-ankle vascular index in hypertensive patients.替米沙坦对高血压患者中心血管踝指数评估的动脉僵硬度的影响。
Kidney Blood Press Res. 2010;33(4):304-12. doi: 10.1159/000316724. Epub 2010 Jul 24.
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Effects of suboptimal doses of the AT1 receptor blocker, telmisartan, with the angiotensin-converting enzyme inhibitor, ramipril, on cerebral arterioles in spontaneously hypertensive rat.替米沙坦与血管紧张素转换酶抑制剂雷米普利联合应用于自发性高血压大鼠脑小动脉时,低于最佳剂量的 AT1 受体阻滞剂的作用。
J Hypertens. 2010 Jul;28(7):1566-73. doi: 10.1097/hjh.0b013e328339f1f3.