Niludipine

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A calcium channel blocker used in the treatment of hypertension


Niludipine
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Niludipine is a calcium channel blocker used primarily in the management of hypertension. It belongs to the dihydropyridine class of calcium channel blockers, which are known for their ability to selectively inhibit the influx of calcium ions through L-type calcium channels in the vascular smooth muscle, leading to vasodilation and a subsequent reduction in blood pressure.

Pharmacology

Mechanism of Action

Niludipine works by blocking the L-type calcium channels in the smooth muscle of the blood vessels. This action prevents calcium ions from entering the cells, which is necessary for muscle contraction. As a result, the vascular smooth muscle relaxes, leading to vasodilation and a decrease in systemic vascular resistance. This ultimately lowers blood pressure.

Pharmacokinetics

Niludipine is absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. It is highly protein-bound and has a relatively short half-life, necessitating multiple daily doses to maintain therapeutic levels. The drug is primarily excreted in the urine as inactive metabolites.

Clinical Use

Niludipine is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. The drug is particularly useful in patients with isolated systolic hypertension and in those who require additional cardiovascular protection.

Side Effects

Common side effects of niludipine include headache, flushing, dizziness, and peripheral edema. These effects are generally mild and tend to diminish with continued use. Rarely, more serious adverse effects such as hypotension and tachycardia may occur.

Contraindications

Niludipine is contraindicated in patients with known hypersensitivity to dihydropyridines. Caution is advised in patients with severe aortic stenosis, heart failure, or hepatic impairment.

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Contributors: Prab R. Tumpati, MD