Ivabradine: a selective If current inhibitor in the treatment of stable angina.

Abstract

The role of heart rate reduction in the management of myocardial ischemia and chronic stable angina is pivotal. However, broad use and appropriate dosing of commonly used rate-slowing drugs is limited by their poor tolerability. Ivabradine is a selective inhibitor of the If currents of the sinoatrial node cells. If currents activity determines the slope of the depolarization curve towards the threshold level controlling heart rate in patients with sinus rhythm. Ivabradine, a compound of the benzocyclobutane (S 16257), exhibits a unique specificity for the If current and has a more favorable profile of adverse reactions compared to other If inhibitors. Accordingly, ivabradine has been used in the treatment of stable angina, where it presented anti-anginal and anti-ischemic effects equivalent to the effects of atenolol and amlodipine. Clinical studies proved the efficacy of ivabradine in patients with stable angina, while clinical data are awaited to verify its probable value in the treatment of atrial tachyarrhythmias and tachycardia due to ventricular dysfunction. Thus, the clinical value of ivabradine, which has completed clinical development for stable angina, is expected to exceed its role in the treatment of myocardial ischemia. In this context, ivabradine, promising efficacious and safe pharmacological management of heart rate, is a huge step in cardiovascular therapeutics.

• Authors: George Andrikopoulos, Chryssanthi Dasopoulou, Dimitris Sakellariou, Stylianos Tzeis, Spyridon Koulouris, Athanasios Kranidis, Kostas Kappos, Antonis S Manolis
• Journal: Recent patents on cardiovascular drug discovery (Recent Pat Cardiovasc Drug Discov) Vol. 1 Issue 3 Pg. 277-82 (Nov 2006) United Arab Emirates
• PMID: 18221092 (Publication Type: Journal Article, Review)

Chemical References

• Benzazepines
• Cyclic Nucleotide-Gated Cation Channels
• HCN4 protein, human
• Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels
• Ion Channels
• Muscle Proteins
• Potassium Channels
• Ivabradine

Topics

• Angina Pectoris (drug therapy)
• Animals
• Benzazepines (therapeutic use)
• Clinical Trials as Topic
• Cyclic Nucleotide-Gated Cation Channels (physiology)
• Humans
• Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels
• Ion Channels (antagonists & inhibitors)
• Ivabradine
• Muscle Proteins (physiology)
• Potassium Channels
• Sinoatrial Node (drug effects, physiology)