Ranexa

Active ingredient: Ranolazine 500mg prolonged release tablets

MOA: inhibits late sodium current in cardiac cells, hence, reduces sodium accumulation in cells, and
consequently decrease intracellular Ca overload via Na+-Ca2+ exchange. Reduce ventricular tension
and myocardial oxygen consumption.
Does not reduce heart rate or blood pressure.

Use: Add-on therapy in patients with stable angina pectoris who are not adequately controlled or
cannot use first-line therapies (BB, CCB)

Administration: not to be crushed, broken or chewed, taken without regards to meals

Dosing:
375mg BD (initial)
500mg BD (2-4 wks later)
750mg BD (max dose)

Adverse effects: dizziness, headache, constipation, n/v, weakness and fatigue

Prolong QTc interval

Impact on patients:
 Increase exercise duration
 Increase time to onset of angina
 Decrease number of angina episodes and use of NTG tabs

Contraindicated in: CrCl <30 ml/min, moderate and severe hepatic impairment, concurrent use of
strong CYP3A4 inhibitors (itraconazole, ketoconazole, voriconazole, HIV protease inhibitors,
clarithromycin etc) and inducers, concurrent use of class Ia or III AADs (amiodarone is safe)

Pregnancy: only if benefit to mother outweighs risk to fetus, should not be used
Breastfeeding: weigh benefit of breastfeeding vs infant’s potential adverse effects, should not be
used

Drug interactions: avoid taking with strong CYP3A4 inhibitors/inducers, PGP inhibitors, CYP2D6
inhibitors, digoxin

Ranolazine moderate-potent inhibitor of P-gp, mild inhibitor of CYP3A4, CYP2D6 inhibitor (?), OCT-2
 Limit dose of simvastatin to 20mg OD in pts taking any dose of Ranexa
 Consider limiting dose of atorvastatin
 ≤500mg BD of ranolazine does not need alteration of metformin doses

Source of information: Ranexa PIL from HSA website, Uptodate, Micromedex, Dipiro 10th Edition