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¾ÆÀ̵ð°Ö¿¬°í [Indomethacin]
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µå·°ÀÎÆ÷¿¡¼´Â ÀǾàǰ ÀÎÅÍ³Ý ÆÇ¸Å¸¦ ÇÏÁö ¾Ê½À´Ï´Ù. |
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À¯·áÁ¤º¸¸ñ·ÏÀº Àü¹®È¸¿øÀ¸·Î
·Î±×ÀÎ ÇϽøé È®ÀÎ °¡´ÉÇÕ´Ï´Ù.
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[A06702341]
[º¸ÇèÄڵ忡 µû¸¥ ¾àǰ±âº»Á¤º¸ Á÷Á¢Á¶È¸]
\0 ¿ø/1g(2006.02.01)(ÇöÀç¾à°¡)
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| º¸°ü»ó ÁÖÀÇ |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
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Indomethacin¿¡ ´ëÇÑ µ¶¼ºÁ¤º¸ : Á¤º¸º¸±â
Ãâó: ±¹¸³µ¶¼º°úÇпø µ¶¼º¹°ÁúÁ¤º¸DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Indomethacin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Antiinflammatory effects of Indomethacin are believed to be due to inhibition of cylooxygenase in platelets which leads to the blockage of prostaglandin synthesis. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
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| Pharmacology |
Indomethacin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Indomethacin, a nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain.
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| Metabolism |
Indomethacin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C19 (CYP2C19)UDP-glucuronosyltransferase 1-9 (UGT1A9)
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| Protein Binding |
Indomethacin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 97%
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| Half-life |
Indomethacin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 4.5 hours
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| Absorption |
Indomethacin¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is approximately 100% following oral administration and 80??0% following rectal administration.
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| Pharmacokinetics |
IndomethacinÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- ÀÛ¿ë¹ßÇö½Ã°£ : 30ºÐ À̳»
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4-6 ½Ã°£
- Èí¼ö : ½Å¼ÓÇϰÔ, ¸¹Àº ¾çÀÌ Èí¼öµÊ
- ºÐÆ÷ : ºÐÆ÷¿ëÀû : 0.34-1.57 L/kg. ÅÂ¹Ý Åë°ú, À¯Áó ºÐºñ
- ´Ü¹é°áÇÕ : 90%
- ´ë»ç : °£´ë»ç, Àå°£¼øÈ¯
- ¹Ý°¨±â : 4.5 ½Ã°£. ½Å»ý¾Æ¿¡¼´Â ¿¬ÀåµÊ
- Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ : °æ±¸ : 3-4 ½Ã°£ À̳»
- ¼Ò½Ç : Àå°£¼øÈ¯ Å. ÁÖ·Î glucuronide Æ÷ÇÕü·Î¼ ½Å¹è¼³
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| Biotransformation |
Indomethacin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
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| Toxicity |
Indomethacin¿¡ ´ëÇÑ Toxicity Á¤º¸ The following symptoms may be observed following overdosage: nausea, vomiting, intense headache, dizziness, mental confusion, disorientation, or lethargy. There have been reports of paresthesias, numbness, and convulsions. The oral LD50 of indomethacin in mice and rats (based on 14 day mortality response) was 50 and 12 mg/kg, respectively.
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| Drug Interactions |
Indomethacin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol Risk of inhibition of renal prostaglandinsAtenolol Risk of inhibition of renal prostaglandinsBetaxolol Risk of inhibition of renal prostaglandinsBevantolol Risk of inhibition of renal prostaglandinsBisoprolol Risk of inhibition of renal prostaglandinsCarteolol Risk of inhibition of renal prostaglandinsCarvedilol Risk of inhibition of renal prostaglandinsMethotrexate The NSAID increases the effect and toxicity of methotrexateDiflunisal Diflunisal increases the effect and toxicity of indomethacinEsmolol Risk of inhibition of renal prostaglandinsLabetalol Risk of inhibition of renal prostaglandinsMetoprolol Risk of inhibition of renal prostaglandinsNadolol Risk of inhibition of renal prostaglandinsLosartan Indomethacin decreases the effect of losartanLithium The NSAID increases serum levels of lithiumOxprenolol Risk of inhibition of renal prostaglandinsPenbutolol Risk of inhibition of renal prostaglandinsPindolol Risk of inhibition of renal prostaglandinsPractolol Risk of inhibition of renal prostaglandinsProbenecid Probenecid increases the effect/toxicity of indomethacinSotalol Risk of inhibition of renal prostaglandinsPropranolol Risk of inhibition of renal prostaglandinsTimolol Risk of inhibition of renal prostaglandinsWarfarin The NSAID increases the anticoagulant effectAcenocoumarol The NSAID increases the anticoagulant effectDicumarol The NSAID increases the anticoagulant effectAnisindione The NSAID increases the anticoagulant effectTorasemide The NSAID decreases the diuretic and antihypertensive effects of the loop diureticBumetanide The NSAID decreases the diuretic and antihypertensive effects of the loop diureticFurosemide The NSAID decreases the diuretic and antihypertensive effects of the loop diureticEthacrynic acid The NSAID decreases the diuretic and antihypertensive effects of the loop diureticCyclosporine Monitor for nephrotoxicityAlendronate Increased risk of gastric toxicityTriamterene Risk of acute renal impairment with this combination
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Indomethacin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Avoid alcohol.Take with food or antacids to reduce irritation.
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| Drug Target |
[Drug Target]
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| Description |
Indomethacin¿¡ ´ëÇÑ Description Á¤º¸ A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes. [PubChem]
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| Drug Category |
Indomethacin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Inflammatory Agents, Non-SteroidalAnti-inflammatory AgentsCardiovascular AgentsCyclooxygenase InhibitorsGout SuppressantsNonsteroidal Antiinflammatory Agents (NSAIDs)Tocolytic Agents
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| Smiles String Canonical |
Indomethacin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COC1=CC2=C(C=C1)N(C(=O)C1=CC=C(Cl)C=C1)C(C)=C2CC(O)=O
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| Smiles String Isomeric |
Indomethacin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COC1=CC2=C(C=C1)N(C(=O)C1=CC=C(Cl)C=C1)C(C)=C2CC(O)=O
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| InChI Identifier |
Indomethacin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C19H16ClNO4/c1-11-15(10-18(22)23)16-9-14(25-2)7-8-17(16)21(11)19(24)12-3-5-13(20)6-4-12/h3-9H,10H2,1-2H3,(H,22,23)/f/h22H
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| Chemical IUPAC Name |
Indomethacin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid
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| Drug-Induced Toxicity Related Proteins |
INDOMETHACIN ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Tumor necrosis factor receptor superfamily member 1A (TNF-R1) Drug:indomethacin Toxicity:gastric damage and granulocyte infiltration. [¹Ù·Î°¡±â] Replated Protein:Plasma kallikrein Drug:indomethacin Toxicity:enterocolitis. [¹Ù·Î°¡±â] Replated Protein:Heat shock 70 kDa protein Drug:indomethacin Toxicity:denatured proteins. [¹Ù·Î°¡±â] Replated Protein:c-myc oncogene Drug:indomethacin Toxicity:apoptosis by indomethacin. [¹Ù·Î°¡±â] Replated Protein:Acetylcholinesterase Drug:indomethacin Toxicity:enhance contractility of the small intestine. [¹Ù·Î°¡±â] Replated Protein:G1/S-specific cyclin-D1 Drug:indomethacin Toxicity:arrests endothelial cell proliferation. [¹Ù·Î°¡±â] Replated Protein:Acetylcholinesterase Drug:indomethacin Toxicity:enhance contractility of the small intestine. [¹Ù·Î°¡±â] Replated Protein:P-selectin Drug:indomethacin Toxicity:Indomethacin induced gastropathy. [¹Ù·Î°¡±â] Replated Protein:B2 bradykinin receptor Drug:indomethacin Toxicity:enterocolitis. [¹Ù·Î°¡±â] Replated Protein:Nitric oxide synthase, inducible Drug:indomethacin Toxicity:gastric damage and granulocyte infiltration. [¹Ù·Î°¡±â] Replated Protein:Intercellular adhesion molecule 1 Drug:indomethacin Toxicity:Indomethacin induced gastropathy. [¹Ù·Î°¡±â] Replated Protein:Plasma kallikrein Drug:indomethacin Toxicity:enterocolitis. [¹Ù·Î°¡±â] Replated Protein:Integrin alpha-M Drug:indomethacin Toxicity:experimental dystonia. [¹Ù·Î°¡±â] Replated Protein:Tumor necrosis factor Drug:indomethacin Toxicity:gastric damage and granulocyte infiltration. [¹Ù·Î°¡±â] Replated Protein:Cytochrome b5 Drug:indomethacin Toxicity:selective effect of a p-chlorophenyl moiety. [¹Ù·Î°¡±â] Replated Protein:NADH-cytochrome b5 reductase Drug:indomethacin Toxicity:selective effect of a p-chlorophenyl moiety. [¹Ù·Î°¡±â] Replated Protein:Epoxide hydrolase Drug:indomethacin Toxicity:selective effect of a p-chlorophenyl moiety. [¹Ù·Î°¡±â]
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
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¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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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. INDOMETHACIN[GGT Increase][Composite Activity](Score) NA(Marginal) 2(Active) 0[Alkaline Phosphatase Increase](Activity Score) M(Number of Rpts) ¡Ã4(Index value) 3.1[SGOT Increase](Activity Score) M(Number of Rpts) ¡Ã4(Index value) 3.8[SGPT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[LDH Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA[GGT Increase](Activity Score) NA(Number of Rpts) NA(Index value) NA
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