Name: | Nicardipine |
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PubChem Compound ID: | 197067 |
Description: | 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. |
Molecular formula: | C21H27ClN2O3 |
Molecular weight: | 390.903 g/mol |
Synonyms: |
EINECS 228-279-6; NSC 407307; 20alpha-Yohimban-16beta-carboxylic acid, 17alpha-hydroxy-, methyl ester, monohydrochloride (8CI); Rauwolscine hydrochloride; alpha-Yohimbine hydrochloride; alpha-Yohimbin hydrochloride; Methyl (16beta,17alpha,20alpha)-17-hydroxyyohimban-16-carboxylate hydrochloride; EU-0101093; Yohimban-16-carboxylic acid, 17-hydroxy-, methyl ester, monohydrochloride, (16beta,17alpha,20alpha)- (9CI); 20-alpha-Yohimban-16-beta-carboxylic acid, 17-alpha-hydroxy-, methyl ester, hydrochloride.
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Name: | Nicardipine |
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Name (isomeric): | DB00622 |
Drug Type: | small molecule |
Description: | 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. |
Synonyms: |
Nicardipine HCl; Nicardipinum [INN-Latin]; Nicardipino [INN-Spanish]
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Brand: | Cardene SR, Cardene, Cardene IV |
Category: | Vasodilator Agents, Antiarrhythmic Agents, Calcium Channel Blockers, Antihypertensive Agents, Dihydropyridines |
CAS number: | 55985-32-5 |
Indication: | Used for the management of patients with chronic stable angina and for the treatment of hypertension. |
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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...
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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 m...
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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. |
Protein binding: | >95% |
Biotransformation: | Nicardipine HCl is metabolized extensively by the liver. |
Route of elimination: | Nicardipine has been shown to be rapidly and extensively metabolized by the liver. |
Half Life: | 8.6 hours |
Clearance: | 0.4 L/hr∙kg [Following infusion] |
Toxicity: | Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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