ivabradine hydrochloride

CLINICAL USE

Symptomatic treatment of chronic stable angina pectoris in patients with sinus rhythm, if beta-blockers are contraindicated

DOSE IN NORMAL RENAL FUNCTION

2.5–7.5 mg twice daily (dose is reduced if heart rate is consistently below 50 beats per minute)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :504.5

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :70

%Excreted unchanged in urine &nbsp &nbsp : 4

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :100 litres

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :2/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function15–20 Dose as in normal renal function<15 Dose as in normal renal function. Use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in GFR<15 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unlikely to be dialysed. Dose as in GFR<15 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR<15 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone and disopyramide

Antibacterials: concentration possibly increased by clarithromycin and telithromycin – avoid concomitant use; increased risk of ventricular arrhythmias with erythromycin – avoid concomitant use

Antifungals: concentration increased by ketoconazole – avoid concomitant use; concentration increased by fluconazole – reduce initial ivabradine dose; concentration possibly increased by itraconazole – avoid concomitant use

Antimalarials: increased risk of ventricular arrhythmias with mefloquine

Antipsychotics: increased risk of ventricular arrhythmias with pimozide or sertindole

Antivirals: concentration possibly increased by nelfinavir and ritonavir – avoid concomitant use

Beta-blockers: increased risk of ventricular arrhythmias with sotalol

Calcium-channel blockers: concentration increased by diltiazem and verapamil – avoid concomitant use

Grapefruit juice: ivabradine concentration increased

Pentamidine: increased risk of ventricular arrhythmiasSt John’s wort: ivabradine concentration reduced – avoid concomitant use

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–ivabradine hydrochloride

Tags: post-by-auto-php