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Ranolazine
General information
Ranolazine is a piperazine derivative approved for the treatment of chronic angina [ ]. It is thought to act by shifting myocardial energy metabolism away from free fatty acids and towards glucose as a substrate for production of adenosine triphosphate. It also has antidysrhythmic actions [ ].
Ranolazine is metabolized in the small intestine and liver to active metabolites, primarily by CYP3A4 and CYP3A5 and partly by CYP2D6; it is also a substrate of P glycoprotein.
Drug studies
Observational studies
In a survey of data from 746 patients with chronic angina treated in the ROLE (Ranolazine Open Label Experience) program, in which ranolazine was titrated to optimal dosages of 500–1000 mg bd, with mean follow-up for 2.82 years, 571 patients (77%) were still taking ranolazine 2 years after initial dosing and 72 patients (9.7%) stopped taking it because of adverse events [ ]. Among six factors evaluated, only age of at least 64 years predicted higher withdrawal rates. Patients with a history of congestive cardiac failure had lower withdrawal rates. The mean QT c interval was prolonged by 2.4 ms and prolongation of the QT interval did not result in withdrawals or episodes of torsade de pointes. There were 64 deaths during a total of 2102 patient-years (3.0% annually) during the program, fewer than would have been expected.
Comparative studies
In a retrospective cohort study of 393 consecutive patients undergoing CABG, amiodarone was compared with ranolazine in prevention of postoperative atrial fibrillation [ ]. The patients who took amiodarone were more likely to develop atrial fibrillation than those who took ranolazine (OR = 1.7; 95% CI = 1.01, 2.91). There was no difference in adverse events between the groups.
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