Ranolazine inhibits persistent or late inward sodium current ( I Na) in heart muscle in a variety of voltage-gated sodium channels. ĭrugs that are metabolized by CYP2D6, such as tricyclic antidepressants, may need to be given at reduced doses when administered with ranolazine. įor drugs that are moderate CYP3A inhibitors, such as diltiazem, verapamil, and erythromycin, the dose of ranolazine should be reduced. Ranolazine should not be used with drugs such as ketoconazole, clarithromycin, and nelfinavir that strongly inhibit CYP3A, nor with drugs that activate CYP3A, such as rifampin and phenobarbital. For this reason, the doses of ranolazine and drugs that interact with those enzymes need to be adjusted when they are used by the same patient. It also inhibits another metabolizing enzyme, cytochrome CYP2D6. Ranolazine is metabolized mainly by the CYP3A enzyme. Other side effects include headache and nausea. The most common side effects are dizziness (11.5%) and constipation (10.9%). The drug's effect on the QT interval is increased in the setting of liver dysfunction thus it is contraindicated in persons with mild to severe liver disease. Additionally, in clinical trials ranolazine slightly increased QT interval in some patients and the FDA label contains a warning for doctors to beware of this effect in their patients. Some contraindications for ranolazine are related to its metabolism and are described under Drug Interactions.
Its use is not recommended in Scotland as of 2019. It is also effective at preventing atrial fibrillation, and has been studied as monotherapy as well as in combination with other medications against irregular heartbeat. It may be used concomitantly with β blockers, nitrates, calcium channel blockers, antiplatelet therapy, lipid-lowering therapy, ACE inhibitors, and angiotensin receptor blockers.
Ranolazine is used to treat chronic angina.
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