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Nicardipine
drug data and news
Nicardipine 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 | Nicardipine | ||
| Brand Names/Synonyms | Cardene; Cardene Sr; Nicardipine; Nicardipine Hcl; Nicardipino [Inn-Spanish]; Nicardipinum [Inn-Latin]; YC-93 | ||
| Indication | Used for the management of patients with chronic stable angina | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Nicardipine News (When available) |
Nicardipine Helps Restore Cerebral Oxygenation in Hypertensive ... Feb 27, 2006 Sustained Hypertension at Reperfusion of the Transplanted Kidneys ... Feb 21, 2006 Protein Design Labs Becomes PDL BioPharma Jan 9, 2006 Preserving Competition, FTC Requires Divestitures Before Allowing ... Jan 23, 2006 Obama against review of stress disorder cases Oct 2, 2005 Phenylephrine to increase blood flow in the radial artery used as ... Sep 30, 2005 Drugs to combat hypertension Apr 12, 2005 Medicines Co. halts drug trial over irregular heartbeat risk Mar 29, 2005 Medicines Company Suspends Clevelox Patient Enrollment Mar 28, 2005 The Medicines Company Voluntarily Suspends Enrollment In Clevelox ... Mar 28, 2005 The Medicines Company Voluntarily Suspends Enrollment In Clevelox ... Mar 28, 2005 Medicines Co. halts drug trial over irregular heartbeat risk Mar 29, 2005 Medicines Company Suspends Clevelox Patient Enrollment Mar 28, 2005 Protein Design Labs Announces Above Consensus Full-Year and Fourth ... Mar 14, 2005 The Medicines Company Voluntarily Suspends Enrollment In Clevelox ... 28 Mar 2005 | ||
| Dosage Forms | CAPSULE | ||
| Drug_Category | Antiarrhythmic Agents; Vasodilator Agents; Antihypertensive Agents; Dihydropyridines; ATC:C08CA04 | ||
| 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. | ||
| Interactions |
-->Interactions for Nicardipine: 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. | ||
| Toxicity | Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | methyl2-(benzyl-methyl-amino)ethyl2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate | ||
| Chemical Formula | C26H29N3O6 | ||
| Molecular Weight | 479.525 g/mol | ||
| Smiles String | CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)CC2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OC | ||
| Melting Point | 136-138 °C | ||
| Water Solubility | 2.2 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 3.967 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Nicardipine HCl is metabolized extensively by the liver. | ||
| Half Life | 8.6 hours | ||
| Protein Binding [%] | >95% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Nicardipine.html http://www.rxlist.com/cgi/generic/nicardipine.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00088 | ||
| CAS Registry Number | 55985-32-5 | ||
| KEGG Compound ID | C07264 | ||
| PubChem ID | SID:182381 | ||
| PharmGKB ID | PA450620 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2162733 |
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