Drug insight: If inhibitors as specific heart-rate-reducing agents.

Heart rate is determined primarily by spontaneously repeating net inward current carried by sodium ions and potassium ions through hyperpolarization-activated cyclic-nucleotide-gated channels. Within the heart, these channels are found most abundantly in sinoatrial cardiomyocytes. The channels open in response to membrane hyperpolarization, modulated by local cAMP concentrations. They permit activation of the I(f) current, which can be blocked specifically by molecules characterized by linked benzazepinone and benzocyclobutane rings, and which are devoid of effects on cardiac conduction, inotropy or peripheral vascular tone. The resulting heart-rate reduction has been effective in angina prevention in clinical trials involving 4,000 patients, using the prototype I(f) inhibitor, ivabradine. No serious adverse events have been attributed to the treatment; the most prominent side-effect is dose-related, always reversible and often transient visual symptoms that seldom result in voluntary drug discontinuation.

作 者：

Borer JS

刊 名：

Nature clinical practice. Cardiovascular medicine 

年，卷(期)：

2004vol.1(no.2) 

分类号：

 

关键词：

Angina Pectoris  Benzazepines  Cardiotonic Agents  Heart  Heart Rate  Ion Channels  心绞痛  苯丙氮|ZHUO|类  强心药  心脏  心率  离子通道  窦房结

正文语种：

eng 

基金项目：