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Nisoldipine: profile and news
First Horizon Announces Results for the First Quarter Ended March ... Apr 28, 2005 First Horizon Announces Results for the First Quarter Ended March ... 29 Apr 2005 Drugs to combat hypertension Apr 12, 2005 Other information Indication Hypertension Pharmacology Nisoldipine, 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. Nisoldipine is similar to other peripheral vasodilators. Nisoldipine 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, Nisoldipine 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 Category Vasodilator Agents; Antihypertensive Agents; ATC:C08CA07 Brand Names/Synonyms Bay K 5552; Bay-K 5552; Baymycard; CHEMBANK2652; Nisocor; Nisoldipin; Nisoldipine; Nisoldipine [Usan:Ban:Inn:Jan]; Nisoldipino [Inn-Spanish]; Nisoldipinum [Inn-Latin]; Norvasc; Sular; Syscor; Zadipina Dosage Forms Not Available Absorption Not Available Interactions Interactions for Nisoldipine: A 30 to 45% increase in AUC and Cmax of nisoldipine was observed with concomitant administration of cimetidine 400 mg twice daily. Ranitidine 150 mg twice daily did not interact significantly with nisoldipine (AUC was decreased by 15-20 %). No pharmacodynamic effects of either histamine H2 receptor antagonist were observed. Coadministration of phenytoin with 40 mg SULAR tablets in epileptic patients lowered the nisoldipine plasma concentrations to undetectable levels. Coadministration of SULAR with phenytoin or any known CYP3A4 inducer should be avoided and alternative antihypertensive therapy should be considered. Pharmacokinetic interactions between nisoldipine and beta-blockers (atenolol, propranolol) were variable and not significant. Propranolol attenuated the heart rate increase following administration of immediate release nisoldipine. The blood pressure effect of SULAR tended to be greater in patients on atenolol than in patients on no other antihypertensive therapy. Quinidine at 648 mg bid decreased the bioavailability (AUC) of nisoldipine by 26%, but not the peak concentration. The immediate release, but not the coat-core formulation of nisoldipine increased plasma quinidine concentrations by about 20%. This interaction was not accompanied by ECG changes and its clinical significance is not known. No significant interactions were found between nisoldipine and warfarin or digoxin. Chemical IUPAC Name methyl2-methylpropyl2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Chemical Formula C20H24N2O6 Half Life 7-12 hours Drug Type Approved Drug # Accession No APRD00635 CAS Registry Number 63675-72-9 |
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