Small molecule
PubChem CID 39186
Diltiazem
Cardizem
- Mechanism of action
- Non-dihydropyridine calcium channel blocker
- In plain language
- Relaxes and widens blood vessels, and slows the heart's electrical signals, by blocking calcium from entering heart and blood vessel muscle cells.
- How it works
- Diltiazem is a benzothiazepine-class calcium channel blocker that inhibits the influx of extracellular calcium through L-type calcium channels in cardiac and vascular smooth muscle during membrane depolarization. In vascular smooth muscle, this produces relaxation of coronary and peripheral arterial smooth muscle, decreased peripheral vascular resistance, and dilation of coronary arteries. In cardiac tissue, diltiazem slows conduction through the sinoatrial and atrioventricular nodes, prolonging AV nodal refractoriness, which reduces ventricular rate in supraventricular tachyarrhythmias. Because it produces coronary vasodilation and reduces myocardial oxygen demand with minimal negative inotropic effect at therapeutic doses, it relieves ischemia in angina while lowering blood pressure in hypertension.
- Therapeutic applications
- FDA-indicated for management of chronic stable angina and angina due to coronary artery vasospasm; treatment of hypertension, alone or in combination with other antihypertensives (extended-release formulations); and, intravenously, temporary control of rapid ventricular rate in atrial fibrillation or atrial flutter and rapid conversion of paroxysmal supraventricular tachycardia (PSVT) to sinus rhythm.
- Class
- Small molecule
- Therapeutic area
- Cardiovascular
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