nisoldipine

Nisoldipine is a dihydropyridine calcium channel blocker used to treat hypertension and chronic stable angina. It works by inhibiting L-type calcium channels in vascular smooth muscle, leading to vasodilation and reduced peripheral resistance. The resulting drop in blood pressure can relieve anginal symptoms by lowering myocardial oxygen demand.

The drug is available in immediate-release and extended-release formulations, with the extended-release form designed for once-daily dosing. Nisoldipine is typically taken orally and is metabolized mainly in the liver. It is processed by cytochrome P450 3A4, and its plasma levels can be affected by strong CYP3A4 inhibitors or inducers. Grapefruit juice can also influence its metabolism.

Common adverse effects include edema (particularly of the ankles and feet), headache, flushing, dizziness, palpitations, and gingival hyperplasia. Hypotension and reflex tachycardia can occur, and less frequently patients may experience nausea or fatigue. The drug’s vasodilatory effects mean it should be used with caution in patients who may not tolerate significant drops in blood pressure.

Contraindications include hypersensitivity to nisoldipine and clinically significant hypotension. Caution is advised in patients with heart failure, hepatic impairment, or other conditions that may be exacerbated by hypotension. Nisoldipine is contraindicated or used with care when other medications that markedly affect CYP3A4 activity are involved due to potential drug interactions.

Brand names include Sular in some markets, and nisoldipine is available as a generic in many places. It is one of several long-acting dihydropyridine calcium channel blockers used for cardiovascular disease management.