From the Guidelines
Ranolazine is an antianginal medication that inhibits the late inward sodium current, reducing the deleterious effects of intracellular sodium and calcium overload that accompany myocardial ischemia, and is currently indicated for the treatment of chronic angina. The mechanism of action of ranolazine is unique in that it improves oxygen efficiency without significantly affecting heart rate or blood pressure, making it a useful option for patients who cannot tolerate the hemodynamic effects of other anti-anginal medications 1. Some key points about ranolazine include:
- It is typically started at a dose of 500 mg orally twice daily, which can be uptitrated to a maximum of 1000 mg orally twice daily based on clinical response 1.
- Common side effects include constipation, nausea, dizziness, and headache 1.
- Ranolazine prolongs the QTc interval in a dose-related manner, but the risk of QTc prolongation requiring dose reduction is comparable to placebo 1.
- It is generally used as an add-on therapy rather than first-line treatment for angina, and is particularly useful for patients who have not responded to standard antianginal therapy 1. The use of ranolazine has been studied in several trials, including the MERLIN-TIMI 36 trial, which examined the efficacy and safety of ranolazine in patients with non-ST-elevation acute coronary syndromes (NSTE-ACS) 1. While the primary endpoint of the trial was not met, subgroup analyses suggested that ranolazine may be associated with a reduced incidence of recurrent ischemia and improved exercise duration in patients with prior chronic angina 1. Overall, ranolazine is a useful option for the treatment of chronic angina, particularly in patients who cannot tolerate traditional anti-anginal medications or have not responded to standard therapy.
From the FDA Drug Label
Ranolazine is a racemic mixture, chemically described as 1-piperazineacetamide, N (2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-, (±)-. What is RANOLAZINE EXTENDED-RELEASE TABLETS? Ranolazine Extended-Release Tablets is a prescription medicine used to treat angina that keeps coming back (chronic angina).
Ranolazine is a prescription medicine used to treat chronic angina. It is a racemic mixture with a specific chemical description. 2 2
From the Research
Definition and Mechanism of Action
- Ranolazine is a novel antianginal and anti-ischemic agent 3.
- Its exact mechanism of action is unknown, but it is believed to exert its antiischemic effect through antagonism of the late sodium current and other cardiac ion channels 4.
- Unlike other available antianginal drugs, ranolazine has no significant effect on either heart rate or blood pressure 3.
Therapeutic Uses
- Ranolazine is currently approved for the treatment of angina pectoris, either as monotherapy or added to beta-blockers, nitrates, and calcium channel blockers 3.
- It is also used as an adjunctive treatment for chronic stable angina 4.
- Ranolazine may be considered the first choice in presence of comorbidities that difficult the use of traditional therapies 5.
Adverse Effects and Interactions
- The most common adverse effects reported in clinical trials during ranolazine treatment are dizziness, headaches, constipation, and nausea 3.
- Ranolazine prolongs the QT interval in a dose-dependent manner, exposing patients to the risk of torsades de pointes 6.
- There is a high risk of pharmacokinetic interactions due to ranolazine's metabolism by cytochrome P450 isoenzymes CYP 3A4 and CYP 2D6, as well as its status as a P-glycoprotein substrate 6.