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Nisoldipine
drug data and news
Nisoldipine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Nisoldipine | ||
| 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 | ||
| Indication | Hypertension | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Nisoldipine News (When available) |
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 | ||
| Dosage Forms | Not Available | ||
| Drug_Category | Vasodilator Agents; Antihypertensive Agents; ATC:C08CA07 | ||
| 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. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | methyl2-methylpropyl2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate | ||
| Chemical Formula | C20H24N2O6 | ||
| Molecular Weight | 388.414 g/mol | ||
| Smiles String | CC1=C(C(C(=C(N1)C)C(=O)OCC(C)C)C2=CC=CC=C2[N+](=O)[O-])C(=O)OC | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 3.475 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Not Available | ||
| Half Life | 7-12 hours | ||
| Protein Binding [%] | 99% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Nisoldipine.html http://www.rxlist.com/cgi/generic/nisoldipine.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00635 | ||
| CAS Registry Number | 63675-72-9 | ||
| KEGG Compound ID | C07699 | ||
| PubChem ID | SID:184770 | ||
| PharmGKB ID | PA450634 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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