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用伊伐布雷定选择性且特异性地抑制 If,以治疗冠状动脉疾病或心力衰竭。

Selective and specific inhibition of If with ivabradine for the treatment of coronary artery disease or heart failure.

机构信息

UCSF School of Medicine, San Francisco, CA, USA,

出版信息

Drugs. 2013 Sep;73(14):1569-86. doi: 10.1007/s40265-013-0117-0.

DOI:10.1007/s40265-013-0117-0
PMID:24065301
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3786091/
Abstract

Heart rate is an important contributor in the pathophysiology of both coronary artery disease (CAD) and heart failure (HF). Ivabradine is an anti-anginal and anti-ischaemic agent, which selectively and specifically inhibits the I f current in the sino-atrial node and provides pure heart rate reduction without altering other cardiac parameters, including conduction, and without directly affecting other haemodynamic parameters. It is approved for the treatment of CAD and HF. This article summarises the pharmacological properties, pharmacokinetics, clinical efficacy and tolerability of ivabradine in the treatment of CAD and HF, and presents evidence demonstrating that the pharmacological and clinical properties and clinical efficacy of ivabradine make it an important therapeutic choice for patients with stable CAD or HF. The positive effect of ivabradine on angina pectoris symptoms and its ability to reduce myocardial ischemia make it an important agent in the management of patients with stable CAD or chronic HF. Further studies are underway to add to the already robust evidence of ivabradine for the prevention of cardiovascular events in patients with CAD but without clinical HF. The SIGNIFY (Study assessInG the morbidity-mortality beNefits of the I f inhibitor ivabradine in patients with coronarY artery disease) trial includes patients with stable CAD and an LVEF above 40 %, with no clinical sign of HF, and is investigating the long-term effects (over a period of 48 months) of ivabradine in a large study population. So far, this study has included more than 19,000 patients from 51 countries.

摘要

心率是冠状动脉疾病 (CAD) 和心力衰竭 (HF) 病理生理学的重要因素。伊伐布雷定是一种抗心绞痛和抗缺血药物,它选择性和特异性地抑制窦房结中的 If 电流,提供纯粹的心率降低,而不改变其他心脏参数,包括传导,也不直接影响其他血液动力学参数。它被批准用于治疗 CAD 和 HF。本文总结了伊伐布雷定在 CAD 和 HF 治疗中的药理学特性、药代动力学、临床疗效和耐受性,并提供了证据表明,伊伐布雷定的药理学和临床特性以及临床疗效使其成为稳定型 CAD 或 HF 患者的重要治疗选择。伊伐布雷定对心绞痛症状的积极影响及其减少心肌缺血的能力使其成为稳定型 CAD 或慢性 HF 患者管理的重要药物。正在进行进一步的研究,以增加伊伐布雷定在预防 CAD 患者心血管事件方面的已有强有力证据,但这些患者没有临床 HF。SIGNIFY(研究评估 If 抑制剂伊伐布雷定对冠状动脉疾病患者的发病率和死亡率的益处)试验纳入了稳定型 CAD 和 LVEF 高于 40%、无心力衰竭临床迹象的患者,并正在研究伊伐布雷定在大样本人群中的长期效果(超过 48 个月)。到目前为止,这项研究已经包括了来自 51 个国家的超过 19000 名患者。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/9c7ca241b4b6/40265_2013_117_Fig7_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/9c7ca241b4b6/40265_2013_117_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/3ecfac2f416e/40265_2013_117_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/99ac5cfe8ab3/40265_2013_117_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/8f313cdb1c7d/40265_2013_117_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/aebaab3a7be8/40265_2013_117_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0539/3786091/56b5670a3982/40265_2013_117_Fig5_HTML.jpg
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