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Pharmacology of Ivabradine ; Overview, Pharmacokinetics, Mechanism of action, Uses, Effects
Ivabradine is a heart rate-lowering medication used to treat chronic heart failure and stable angina pectoris. Here's a brief overview of its pharmacology:
Mechanism of Action
Ivabradine selectively inhibits the funny current (If) in the sinoatrial (SA) node of the heart. This current is responsible for regulating the heart rate2. By inhibiting the If current, ivabradine reduces the heart rate without affecting myocardial contractility or ventricular repolarization.
Administration Routes
Ivabradine is taken orally, usually in tablet form.
Pharmacokinetics
Absorption: Ivabradine is well absorbed from the gastrointestinal tract, with a bioavailability of about 40%.
Distribution: It has a volume of distribution of approximately 100 L and is about 70% protein-bound.
Metabolism: Ivabradine is metabolized in the liver by the enzyme CYP3A4.
Excretion: It is excreted mainly through urine (4% as unchanged drug) and feces.
Half-Life: The elimination half-life is about 2 hours, with an effective half-life of around 6 hours.
Indications
Ivabradine is indicated for the treatment of:
Chronic heart failure in patients with a left ventricular ejection fraction (LVEF) of 35% or less, who are in sinus rhythm with a resting heart rate of 70 beats per minute (bpm) or higher, and who are either on maximally tolerated doses of beta-blockers or have a contraindication to beta-blocker use.
Stable angina pectoris in patients who cannot be treated with beta-blockers or in combination with beta-blockers when they are insufficiently controlled.
Adverse Effects
Common side effects include:
Visual disturbances (e.g., phosphenes)
Bradycardia (slow heart rate)
Dizziness
Headache
More serious side effects can include:
Severe bradycardia
Heart block
Does this cover what you were looking for, or is there something more specific you'd like to know about ivabradine?
#Ivabradine
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