nicardipine

Nicardipine is a dihydropyridine calcium channel blocker used to treat hypertension and angina. It acts by inhibiting L-type calcium channels in vascular smooth muscle, resulting in arterial vasodilation and reduced peripheral vascular resistance. The effect is largely on the vasculature, with relatively modest direct effects on cardiac conduction at usual antihypertensive doses; reflex tachycardia may occur.

Nicardipine is available in oral and intravenous forms. Orally, it is used for chronic management of hypertension and for angina. Intravenous nicardipine is employed in hypertensive emergencies to rapidly lower blood pressure and is also used to manage cerebral vasospasm after subarachnoid hemorrhage or during neurosurgical procedures.

Pharmacokinetics and interactions: after oral administration, nicardipine is well absorbed but undergoes substantial first-pass metabolism; it is extensively metabolized in the liver, primarily by CYP3A4, and excreted in urine and feces. The elimination half-life is typically around 8–10 hours. Drug interactions are important to consider, particularly with CYP3A4 inhibitors or inducers, which can alter plasma levels.

Adverse effects and safety: common adverse effects include edema, headache, flushing, dizziness, palpitations, and gingival hyperplasia. Hypotension and reflex tachycardia can occur, and very rarely more serious events may arise. Contraindications include hypotension, known hypersensitivity to nicardipine or dihydropyridine calcium channel blockers, severe aortic stenosis, and cardiogenic shock. Caution is advised in patients with significant left ventricular dysfunction or other cardiovascular conditions.

Brand names and formulations: nicardipine is marketed under several names, including Cardene, and is available as oral tablets and as an intravenous infusion.