Active ingredient: Nicardipine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Antiarrhythmic Agents
• Vasodilator Agents
• Antihypertensive Agents
• Dihydropyridines

Dosage Forms

• Capsule

Brands / Synonyms

Cardene; Cardene SR; Nicardipine; Nicardipine HCl; Nicardipino [Inn-Spanish]; Nicardipinum [Inn-Latin]

Indications

Used for the management of patients with chronic stable angina and for the treatment of hypertension.

Pharmacology

Nicardipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Mechanism of Action

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Absorption

While nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.

Toxicity

Oral LD₅₀ Rat = 184 mg/kg, Oral LD₅₀ Mouse = 322 mg/kg

Biotrnasformation / Drug Metabolism

Nicardipine HCl is metabolized extensively by the liver.

Contraindications

Nicardipine HCl is contraindicated in patients with hypersensitivity to the drug.

Because proof of the effect of nicardipine HCl is secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.

Drug Interactions

Beta-Blockers

In controlled clinical studies, adrenergic beta-receptor blockers have been frequently administered concomitantly with nicardipine HCl. The combination is well tolerated.

Cimetidine

Cimetidine increases nicardipine HCl plasma levels. Patients receiving the two drugs concomitantly should be carefully monitored.

Digoxin

Some calcium blockers may increase the concentration of digitalis preparations in the blood. Nicardipine HCl usually does not alter the plasma levels of digoxin, however, serum digoxin levels should be evaluated after concomitant therapy with nicardipine HCl is initiated.

Maalox®*

Coadministration of Maalox TC had no effect on nicardipine HCl absorption.

Fentanyl Anesthesia

Severe hypotension has been reported during fentanyl anesthesia with concomitant use of a beta-blocker and a calcium channel blocker. Even though such interactions were not seen during clinical studies with nicardipine HCl, an increased volume of circulating fluids might be required if such an interaction were to occur.

Cyclosporine

Concomitant administration of nicardipine and cyclosporine levels. Plasma concentrations of cyclosporine should therefore be closely monitored, and its dosage reduced accordingly, in patients treated with nicardipine.

When therapeutic concentrations of furosemide, propranolol, dipyridamole, warfarin, quinidine, or naproxen were added to human plasma (in vitro), the plasma protein binding of nicardipine HCl was not altered.