Cardene - General Information
A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
Pharmacology of Cardene
Cardene, 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. Cardene is similar to other peripheral vasodilators. Cardene 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.
Cardene for patients
In controlled clinical studies, adrenergic beta-receptor blockers have been frequently administered concomitantly with nicardipine HCl. The combination is well tolerated.
Cimetidine increases nicardipine HCl plasma levels. Patients receiving the two drugs concomitantly should be carefully monitored.
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.
Coadministration of Maalox TC had no effect on nicardipine HCl absorption.
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.
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.
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.
Additional information about Cardene
Cardene Indication: Used for the management of patients with chronic stable angina and for the treatment of hypertension.
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.
Drug Interactions: Cyclosporine Cardene increases the effect and toxicity of cyclosporine
Quinupristin This combination presents an increased risk of toxicity
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Food Interactions: Not Available
Generic Name: Nicardipine
Synonyms: Nicardipino [Inn-Spanish]; Nicardipine HCl; Nicardipinum [Inn-Latin]
Drug Category: Antiarrhythmic Agents; Vasodilator Agents; Antihypertensive Agents; Dihydropyridines
Drug Type: Small Molecule; Approved
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 (Overdose): Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg
Protein Binding: >95%
Biotransformation: Nicardipine HCl is metabolized extensively by the liver.
Half Life: 8.6 hours
Dosage Forms of Cardene: Capsule Oral
Chemical IUPAC Name: O5-methyl O3-[2-(methyl-(phenylmethyl)amino)ethyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Chemical Formula: C26H29N3O6
Nicardipine on Wikipedia: https://en.wikipedia.org/wiki/Nicardipine
Organisms Affected: Humans and other mammals