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ranolazine + metoprolol
- Development stage
- Unknown
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ranolazine + metoprolol is a combination of two small molecule drugs used primarily in the management of chronic stable angina and heart failure. Ranolazine acts mainly by inhibiting the cardiac late sodium current (late INa), which reduces intracellular sodium and calcium overload, thereby improving myocardial relaxation, reducing diastolic tension, and enhancing coronary blood flow. Metoprolol is a selective beta-1 adrenergic receptor antagonist (beta-blocker) that decreases heart rate, contractility, and cardiac output by blocking sympathetic stimulation to the heart. The combination may be used when monotherapy with either agent does not adequately control symptoms or as part of a multi-drug regimen for angina or heart failure. Clinical studies have shown that this combination can prevent progressive left ventricular dysfunction and remodeling in heart failure models[2][4]. Caution is advised due to pharmacokinetic interactions; ranolazine can increase plasma concentrations of metoprolol via CYP2D6 inhibition[1][3][5].
- Other names
- ranolazine + metoprolol
02
Targets
SCN5A (Sodium channel protein type 5 subunit alpha)ADRB1 (β1)
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