Ivabradine

Ivabradine Ivabradine has an active metabolite S-18982. Both ivabradine and S-18982 possess bradycardic activity, although the extent of the activity of both could not be determined from the data available. A multiple ligand PD model provided the best fit to the data. The model was assessed in terms of its posterior predictive performance and was able to describe the original data adequately when used for simulation purposes... 

Duffull, S.B. and Aarons, L., Development of a sequential linked pharmacokinetic and pharmacodynamic simulation model for ivabradine in healthy volunteers, Eur. J. Pharm. ScL, 10, 275-284, 2000. 

Ivabradine is used in the treatment of angina in patients in normal sinus rhythm. It acts on the sinus node resulting in a reduction of the heart rate. It is contraindicated in severe bradycardia (heart rate lower than 60 beats/ minute), cardiogenic shock, acute myocardial infarction, moderate-to-severe heart failure, immediately after a cerebrovascular accident, second and third-degree heart block and patients with unstable angina or a pacemaker. Side-effects include bradycardia, first-degree heart block, ventricular extrasystoles, headache, dizziness and visual disturbances, including blurred vision. 

Mulder P, Barbier S, Chagraoui A, et al. Long-term heart rate reduction induced by the selective 1(f) current inhibitor ivabradine improves left ventricular function and intrinsic myocardial structure in congestive heart failure. Circulation 1674 109 1674-9. 

So-called bradycardic drugs, relatively selective If sodium channel blockers (eg, ivabradine), reduce cardiac rate by inhibiting the hyperpolarization-activated sodium channel in the sinoatrial node. No other significant hemodynamic effects have been reported. Ivabradine appears to reduce anginal attacks with an efficacy similar to that of calcium channel blockers and 3 blockers. The lack of effect on gastrointestinal and bronchial smooth muscle is an advantage of ivabradine, and FDA approval is expected. 

Ivabradine Investigational inhibitor of sinoatrial pacemaker reduction of heart rate reduces oxygen demand ... 

Borer JS Clinical effect of pure heart rate slowing with a prototype If inhibitor placebo-controlled experience with ivabradine. Adv Cardiol 2006 43 54. [PMID 16936472]... 

AMIODARONE IVABRADINE Risk of arrhythmias Additive effect Monitor ECG closely... 

CALCIUM CHANNEL BLOCKERS IVABRADINE t levels with diltiazem and verapamil Uncertain Avoid co-administration... 

IVABRADINE ANTIBIOTICS 1. Risk of arrhythmias with eiythromycin 2. Possible T levels with clarithromycin and telithromycin 1. Additive effect 2. Uncertain Avoid co-administration... 

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