Ranolazine

ATC code

C01EB18

Therapeutic class

Other cardiac preparations · Late sodium current (INa) inhibitor

Forms

prolonged-release tablet

Brand names

Ranexa (EU) · Latixa (EU (previous name))

Overall confidence

high

Regulatory sources consulted

Add-on therapy for the symptomatic treatment of patients with stable angina pectoris who are inadequately controlled or intolerant to first-line anti-anginal therapies (such as beta-blockers and / or calcium antagonists).

Hypersensitivity to the active substance.
Severe renal impairment (creatinine clearance < 30 ml/min).
Moderate or severe hepatic impairment.
Concomitant administration of potent CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin).
Concomitant administration of Class Ia (e.g., quinidine) or Class III (e.g., dofetilide, sotalol) antiarrhythmics.

Major warning · QT interval prolongation: Ranolazine prolongs the QTc interval in a dose-dependent manner. Use with caution in patients with congenital long QT syndrome, a family history thereof, or on concomitant therapy with other QT-prolonging drugs. — EMA

HighKetoconazoleJ02AB02
Mechanism: Potent inhibition of CYP3A4, the main metabolic pathway for ranolazine, drastically increasing its exposure (AUC) and the risk of QTc prolongation.
Recommendation: Concomitant administration is contraindicated.
EMA SPC
ModerateDiltiazemC08DB01
Mechanism: Moderate inhibition of CYP3A4 by diltiazem, increasing ranolazine plasma concentrations by 1.5- to 2.4-fold.
Recommendation: Careful dose titration of ranolazine is recommended in patients treated with moderate CYP3A4 inhibitors such as diltiazem. A dose reduction of ranolazine may be required.
EMA SPC

dizziness · headache · constipation · vomiting · nausea · asthenia

QTc prolongation · angioedema · acute renal failure

FDA category: Not assigned

Ranolazine should not be used during pregnancy unless clearly necessary. It should not be used during breast-feeding.