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8806433005009 |
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1) ÃâÇ÷(Ç÷¿ìº´, ¸ð¼¼Ç÷°ü Ãë¾àÁõ, µÎ°³³»ÃâÇ÷, »óºÎ¼ÒȰüÃâÇ÷, ¿ä·ÎÃâÇ÷, °´Ç÷, ÃÊÀÚüÃâÇ÷ µî) ¶Ç´Â ±×·¯ÇÑ ¼ÒÀÎ(Ȱµ¿¼º ¼Òȱ˾ç, ÃÖ±Ù 6°³¿ù À̳»¿¡ ÃâÇ÷¼º³úÁ¹Áß, 3°³¿ù À̳»¿¡ ¿Ü°ú¼ö¼ú, Áõ½Ä´ç´¢¸Á¸·º´Áõ, Á¶ÀýµÇÁö ¾Ê´Â °íÇ÷¾Ð)ÀÌ Àִ ȯÀÚ(ÃâÇ÷À» Á¶ÀåÇÒ ¿ì·Á°¡ ÀÖ´Ù)
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1) Áß´ëÇÑ ÀÌ»ó¹ÝÀÀ
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2) ±âŸÀÇ ÀÌ»ó¹ÝÀÀ
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4) CYP3A4³ª CYP2C19ÀÇ ±âÁúÀÌ µÇ´Â ¾à¹°(½Ã»çÇÁ¸®µå, ¹Ì´ÙÁ¹¶÷)°úÀÇ º´¿ë¿¡ ÀÇÇØ ÀÌ ¾àÀÇ Ç÷Áß ³óµµ°¡ »ó½ÂÇÏ¿© ÀÛ¿ëÀÌ Áõ°¡ÇÒ ¿ì·Á°¡ ÀÖ´Ù. º´¿ëÇÏ´Â °æ¿ì¿¡´Â °¨·® ¶Ç´Â Àú¿ë·®ºÎÅÍ ½ÃÀÛÇÏ´Â µî ÁÖÀÇÇØ¾ß ÇÑ´Ù.
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¡á Âü°í
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¡Û Comparison of TripleVersus Dual Antiplatelet Therapy After Drug-Eluting Stent Implantation (fromthe DECLARE-Long trial) Lee SW, Am J Cardiol. 2007 Oct 1;100(7):1103-8
¡Û Reduced 6-monthresource use and costs associated with cilostazol in patients after successfulcoronary stent implantation: Results from the Cilostazol for RESTenosis (CREST)trial Zefeng Zhang, Am Heart J 2006;152:770-6
¡Û Triple Versus Dual Antiplatelet Therapy after Coronary Stenting-Impact on stent Thrombosis
Seung-Whab Lee, J Am CollCardiol 2005;46:1833-7
¡Û Coronary stentrestenosis in patients treated with cilostazol. Douglas JS Jr, Circulation. 2005; 112:2826-2832.
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[Cilostazol]
> [Cilostazol] CAS number/73963-72-1 ATC code/? PubChem/2754 DrugBank/APRD00155 Formula/C20H27N5O2?/SUP> Mol. mass/369.46 g/mol Bioavailability/? Metabolism/Hepatic (CYP2C19- and CYP3A4-mediated) Excretion/renal Pregnancy cat./
C(US) Legal status/ Routes/Oral Protein binding/95?8%
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| Mechanism of Action |
Cilostazol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ The mechanism of the effects of cilostazol on the symptoms of intermittent claudication is not fully understood. Cilostazol and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
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| Pharmacology |
Cilostazol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cilostazol is a quinolinone derivative indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.
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| Metabolism |
Cilostazol¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C19 (CYP2C19)Cytochrome P450 3A4 (CYP3A4)
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| Protein Binding |
Cilostazol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 95-98%
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| Half-life |
Cilostazol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 11-13 hours.
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| Absorption |
Cilostazol¿¡ ´ëÇÑ Absorption Á¤º¸ Cilostazol is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known.
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| Pharmacokinetics |
CilostazolÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
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| Biotransformation |
Cilostazol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Two metabolites are active, with one metabolite appearing to account for at least 50% of the pharmacologic (PDE III inhibition) activity after administration of cilostazol.
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| Toxicity |
Cilostazol¿¡ ´ëÇÑ Toxicity Á¤º¸ Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.
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| Drug Interactions |
Cilostazol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Diltiazem Diltiazem increases the effect of cilostazolErythromycin Erythromycin increases the effect of cilostazolJosamycin Erythromycin increases the effect of cilostazolFluconazole Fluconazole decreases the effect of cilostazolFluoxetine Fluoxetine increases the effect of cilostazolFluvoxamine Fluvoxamine increases the effect of cilostazolItraconazole The imidazole increases the effect of cilostazolKetoconazole The imidazole increases the effect of cilostazolNefazodone Nefazodone increases the effect of cilostazolOmeprazole Omeprazole increases the effect of cilostazolSertraline Sertraline increases the effect of cilostazol
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Cilostazol¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take on an empty stomach, a lipid rich meal will increase absorption.Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Cilostazol¿¡ ´ëÇÑ Description Á¤º¸ Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal. Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease. [Wikipedia]
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| Drug Category |
Cilostazol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Bronchodilator AgentsFibrinolytic AgentsNeuroprotective AgentsPhosphodiesterase InhibitorsPlatelet Aggregation InhibitorsVasodilator Agents
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| Smiles String Canonical |
Cilostazol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ O=C1CCC2=C(N1)C=CC(OCCCCC1=NN=NN1C1CCCCC1)=C2
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| Smiles String Isomeric |
Cilostazol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ O=C1CCC2=C(N1)C=CC(OCCCCC1=NN=NN1C1CCCCC1)=C2
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| InChI Identifier |
Cilostazol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26)/f/h21H
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| Chemical IUPAC Name |
Cilostazol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
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ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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