ivabradine hydrochloride
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                           :504.5 %Protein binding                           :70 %Excreted unchanged in urine     : 4 Volume of distribution (L/kg)       :100 litreshalf-life – normal/ESRD (hrs)      :2/Unchanged DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
20 to 50     : 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                :Unlikely to be dialysed. Dose as in GFR<15 mL/min HD                     :Unlikely to be dialysed. Dose as in GFR<15 mL/minHDF/high flux   :Unknown dialysability. Dose as in GFR<15 mL/minCAV/VVHD      :Unknown dialysability. Dose as in normal renal function IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugsAnti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone and disopyramideAntibacterials: 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 useAntimalarials: increased risk of ventricular arrhythmias with mefloquineAntipsychotics: increased risk of ventricular arrhythmias with pimozide or sertindoleAntivirals: concentration possibly increased by nelfinavir and ritonavir – avoid concomitant useBeta-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
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