Ivabradine (1 brand name, 1 dosage form, 1 route)
Available dosage forms: SOLUTION.
Routes of administration: ORAL.
Brand Names
- CORLANOR
Contraindications
Ivabradine is contraindicated in patients with: • Acute decompensated heart failure • Clinically significant hypotension • Sick sinus syndrome, sinoatrial block or 3rd degree AV block, unless a functioning demand pacemaker is present • Clinically significant bradycardia [see Warnings and Precautions (5.3)] • Severe hepatic impairment [see Use in Specific Populations (8.6)] • Pacemaker dependence (heart rate maintained exclusively by the pacemaker) [see Drug Interactions (7.3)] • Concomitant use of strong cytochrome P450 3A4 (CYP3A4) inhibitors [see Drug Interactions (7.1)]
Adverse Reactions
Clinically significant adverse reactions that appear in other sections of the labeling include: • Atrial Fibrillation [see Warnings and Precautions (5.2)] • Bradycardia and Conduction Disturbances [see Warnings and Precautions (5.3)]
Mechanism of Action
Ivabradine blocks the hyperpolarization-activated cyclic nucleotide-gated (HCN) channel responsible for the cardiac pacemaker I f current, which regulates heart rate. In clinical electrophysiology studies, the cardiac effects were most pronounced in the sinoatrial (SA) node, but prolongation of the AH interval has occurred as has PR interval prolongation. There was no effect on ventricular repolarization and no effects on myocardial contractility [see Clinical Pharmacology (12.2)]. Ivabradine can also inhibit the retinal current Ih. Ih is involved in curtailing retinal responses to bright light stimuli. Under triggering circumstances (e.g., rapid changes in luminosity), partial inhibition of Ih by ivabradine may underlie the luminous phenomena experienced by patients. Luminous phenomena (phosphenes) are described as a transient enhanced brightness in a limited area of the visual field [see Adverse Reactions (6.1)].
Overdosage
Overdose may lead to severe and prolonged bradycardia. In the event of bradycardia with poor hemodynamic tolerance, temporary cardiac pacing may be required. Supportive treatment, including intravenous (IV) fluids, atropine, and intravenous beta-stimulating agents such as isoproterenol, may be considered.