Ivabradine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Chronic stable angina pectoris in coronary artery disease patients w/ normal sinus rhythm Initial: ≤5 mg bid. Increase if necessary to 7.5 mg bid after 3-4 wk. Titrate downward to as low as 2.5 mg bid, if resting heart rate is <50 beats/min or patient experiences symptoms of bradycardia. Chronic heart failure Initial: 5 mg bid. After 2 wk, adjust dose to achieve resting heart rate between 50-60 beats/min. Max: 7.5 mg bid.
Dosage Details
Oral
Chronic stable angina pectoris in coronary artery disease patients with normal sinus rhythm
Adult: Initially, should not exceed 5 mg bid. Increase if necessary to 7.5 mg bid after 3-4 wk. Titrate downward to as low as 2.5 mg bid, if patient develops bradycardia symptoms (e.g. dizziness, fatigue) or resting heart rate is persistently <50 beats/min.
Elderly: ≥75 yr Initiate treatment at 2.5 mg bid. Titrate up if necessary.

Oral
Chronic heart failure
Adult: Initially, 5 mg bid. After 2 wk, increase to 7.5 mg bid if resting heart rate is persistently >60 beats/min or decrease to 2.5 mg bid if resting heart rate is persistently <50 beats/min. If heart rate is between 50-60 beats/min, maintain 5 mg bid. Max: 7.5 mg bid.
Elderly: ≥75 yr Initiate treatment at 2.5 mg bid. Titrate up if necessary.
Renal Impairment
CrCl (mL/min Dosage
<15 Use w/ caution.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food. Avoid excessive consumption of grapefruit juice.
Contraindications
Resting heart rate <70 beats/min prior to treatment, cardiogenic shock, acute MI, severe hypotension (<90/50 mmHg), sick sinus syndrome, SA block, unstable or acute heart failure, pacemaker dependent, unstable angina, 3rd degree AV block. Severe hepatic impairment. Pregnancy and lactation. Concurrent use w/ potent CYP3A4 inhibitors (e.g. azole antifungals, macrolides, HIV protease inhibitors or nefazodone), moderate CYP3A4 inhibitors (e.g. verapamil or diltiazem).
Special Precautions
Patient w/ retinitis pigmentosa, 2nd degree AV block, congenital QT prolongation, AF or other cardiac arrhythmias that interfere w/ sinus node function. Severe renal impairment (CrCl <15 mL/min).
Adverse Reactions
Luminous phenomena in the visual field (phosphenes), blurred vision, bradycardia, other cardiac arrhythmias, syncope, hypotension, asthenia, fatigue, headache, dizziness, nausea, constipation, diarrhoea, dyspnoea, muscle cramps, skin reactions, angioedema, hyperuricaemia, eosinophilia, elevated blood-creatinine concentrations.
MonitoringParameters
Monitor heart rate prior to initiation of treatment, prior to increasing dose or after decreasing dose; BP, cardiac rhythm.
Overdosage
Symptoms: Severe and prolonged bradycardia. Management: Treat severe bradycardia symptomatically. In case of bradycardia w/ poor haemodynamic tolerance, IV β-stimulating medicines e.g. isoprenaline may be used. If necessary, may institute temporary cardiac electrical pacing.
Drug Interactions
QT prolongation may be exacerbated by heart rate reduction w/ QT-prolonging drugs (e.g. quinidine, disopyramide, pimozide, ziprasidone). Concentration may be reduced w/ CYP3A4 inducers (e.g. rifampicin, barbiturates, phenytoin) and may require ivabradine dose adjustment.
Potentially Fatal: Increased serum concentration w/ potent CYP3A4 inhibitors (e.g. azole antifungals, macrolides, HIV protease inhibitors or nefazodone), moderate CYP3A4 inhibitors (e.g. verapamil or diltiazem).
Food Interaction
Food delays absorption but increases exposure by 20-30%. Increased serum concentration w/ grapefruit juice. Decreased serum concentration w/ St John's wort.
Action
Description: Ivabradine is a heart rate lowering agent that works through selective and specific inhibition of the cardiac pacemaker If current that controls the spontaneous diastolic depolarisation in the sinus node and regulates heart rate.
Pharmacokinetics:
Absorption: Almost completely absorbed from GI tract. Food delays absorption by approx 1 hr and increases exposure by 20-30%. Absolute bioavailability: Approx 40%. Time to peak plasma concentration: Approx 1 hr.
Distribution: Volume of distribution: Approx 100 L. Plasma protein binding: Approx 70%.
Metabolism: Extensively metabolised in the liver and gut via oxidation by CYP3A4 isoenzyme to form major active metabolite N-desmethyl-ivabradine (S-18982).
Excretion: Approx 4% as unchanged drug via urine; metabolites are excreted to a similar extent via urine and faeces. Plasma elimination half-life: 2 hr.
Chemical Structure

Click on icon to see table/diagram/image
Storage
Store at 25°C.
MIMS Class
ATC Classification
C01EB17 - ivabradine ; Belongs to the class of other cardiac preparations.
Disclaimer: This information is independently developed by MIMS based on Ivabradine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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