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| Mechanism of Action |
Nicardipine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
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| Pharmacology |
Nicardipine¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
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| Metabolism |
Nicardipine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)Cytochrome P450 2C9 (CYP2C9)Cytochrome P450 2C19 (CYP2C19)Cytochrome P450 2C8 (CYP2C8)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Nicardipine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ >95%
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| Half-life |
Nicardipine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 8.6 hours
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| Absorption |
Nicardipine¿¡ ´ëÇÑ Absorption Á¤º¸ 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.
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| Pharmacokinetics |
Nicardipine HClÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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- ´Ü¹é°áÇÕ : 95%
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- »ýü³»ÀÌ¿ëÀ² : 35% (absolutely)
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- ÃÖ°íÇ÷Áß³óµµ µµ´Þ½Ã°£ : 20-120ºÐ À̳»
- Ç÷¾ÐÇϰȿ°ú ¹ßÇö½Ã°£ : 20ºÐ À̳»
- ¼Ò½Ç : ´ë»çü·Î¼ ´¢¸¦ ÅëÇØ ¹è¼³µÊ.
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| Biotransformation |
Nicardipine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Nicardipine HCl is metabolized extensively by the liver.
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| Toxicity |
Nicardipine¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 Rat = 184 mg/kg, Oral LD50 Mouse = 322 mg/kg
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| Drug Interactions |
Nicardipine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Cyclosporine Nicardipine increases the effect and toxicity of cyclosporineQuinupristin This combination presents an increased risk of toxicityTerfenadine Increased risk of cardiotoxicity and arrhythmias
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Nicardipine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Nicardipine¿¡ ´ëÇÑ Description Á¤º¸ 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. [PubChem]
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| Drug Category |
Nicardipine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antiarrhythmic AgentsAntihypertensive AgentsCalcium Channel BlockersDihydropyridinesVasodilator Agents
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| Smiles String Canonical |
Nicardipine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1
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| Smiles String Isomeric |
Nicardipine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC(=O)C1=C(C)NC(C)=C([C@@H]1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1
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| InChI Identifier |
Nicardipine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C26H29N3O6/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19/h5-12,15,24,27H,13-14,16H2,1-4H3
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| Chemical IUPAC Name |
Nicardipine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ O5-methyl O3-[2-(methyl-(phenylmethyl)amino)ethyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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The database contains the following fields: The generic name of each chemical For module A10 (liver enzyme composite module): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the number of active and marginally active scores for each compound at the five individual endpoints (see research article for full description of method) Number of endpoints at which each compound is marginally active (M) Number of endpoints at which each compound is active (A) For modules A11 to A15 (alkaline phosphatase increased, SGOT increased, SGPT increased, LDH increased, and GGT increased, respectively): Overall activity category for each compound (A for active, M for marginally active, or I for inactive) based on the RI and ADR values (see the research article for full description of method) Number of ADR reports for each compound, given as <4 or ¡Ã4 Reporting Index value for each compound, except where no shipping units were available (NSU) Group 1 comprises of compounds for which ADR data were available for the first five years of marketing, so when no ADR reports were listed during this period the compounds were evaluated as inactive. Group 2 comprises of compounds for which a 'steady state' period of ADR data were available (1992-1996). In cases where no ADR reports were filed during this period, the compounds were scored as 'NA' (data not available) since they may have had one or more ADR reports during their first five years of marketing which should not be negated by a lack of ADR reports during the steady-state period. NICARDIPINE[GGT Increase][Composite Activity](Score) I(Marginal) 1(Active) 0[Alkaline Phosphatase Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 2[SGOT Increase](Activity Score) M(Number of Rpts) ¡Ã4(Index value) 3[SGPT Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 2.5[LDH Increase](Activity Score) I(Number of Rpts) ¡Ã4(Index value) 0.9[GGT Increase](Activity Score) I(Number of Rpts) <4(Index value) 0.4
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