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| 독성정보 |
Indomethacin에 대한 독성정보 : 정보보기
출처: 국립독성과학원 독성물질정보DB : http://www.nitr.go.kr/nitr/contents/m134200/view.do |
| Mechanism of Action |
Indomethacin에 대한 Mechanism_Of_Action 정보
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 |
Indomethacin에 대한 Pharmacology 정보
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 |
Indomethacin에 대한 Metabolism 정보
# Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C19 (CYP2C19)UDP-glucuronosyltransferase 1-9 (UGT1A9)
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| Protein Binding |
Indomethacin에 대한 단백결합 정보
97%
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| Half-life |
Indomethacin에 대한 반감기 정보
4.5 hours
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| Absorption |
Indomethacin에 대한 Absorption 정보
Bioavailability is approximately 100% following oral administration and 80??0% following rectal administration.
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| Pharmacokinetics |
Indomethacin의 약물동력학자료
- 작용발현시간 : 30분 이내
- 작용지속시간 : 4-6 시간
- 흡수 : 신속하게, 많은 양이 흡수됨
- 분포 : 분포용적 : 0.34-1.57 L/kg. 태반 통과, 유즙 분비
- 단백결합 : 90%
- 대사 : 간대사, 장간순환
- 반감기 : 4.5 시간. 신생아에서는 연장됨
- 혈중최고농도 도달시간 : 경구 : 3-4 시간 이내
- 소실 : 장간순환 큼. 주로 glucuronide 포합체로서 신배설
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| Biotransformation |
Indomethacin에 대한 Biotransformation 정보
Hepatic.
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| Toxicity |
Indomethacin에 대한 Toxicity 정보
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 |
Indomethacin에 대한 Drug_Interactions 정보
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 Table직접조회]
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| Food Interaction |
Indomethacin에 대한 Food Interaction 정보
Avoid alcohol.Take with food or antacids to reduce irritation.
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| Drug Target |
[Drug Target]
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| Description |
Indomethacin에 대한 Description 정보
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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| Dosage Form |
Indomethacin에 대한 Dosage_Form 정보
Capsule OralPowder, for solution IntravenousSuppository Rectal
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| Drug Category |
Indomethacin에 대한 Drug_Category 정보
Anti-Inflammatory Agents, Non-SteroidalAnti-inflammatory AgentsCardiovascular AgentsCyclooxygenase InhibitorsGout SuppressantsNonsteroidal Antiinflammatory Agents (NSAIDs)Tocolytic Agents
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| Smiles String Canonical |
Indomethacin에 대한 Smiles_String_canonical 정보
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 |
Indomethacin에 대한 Smiles_String_isomeric 정보
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 |
Indomethacin에 대한 InChI_Identifier 정보
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 |
Indomethacin에 대한 Chemical_IUPAC_Name 정보
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid
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| Drug-Induced Toxicity Related Proteins |
INDOMETHACIN 의 Drug-Induced Toxicity Related Protein정보
Replated Protein:Tumor necrosis factor receptor superfamily member 1A (TNF-R1)
Drug:indomethacin
Toxicity:gastric damage and granulocyte infiltration.
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Replated Protein:Plasma kallikrein
Drug:indomethacin
Toxicity:enterocolitis.
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Replated Protein:Heat shock 70 kDa protein
Drug:indomethacin
Toxicity:denatured proteins.
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Replated Protein:c-myc oncogene
Drug:indomethacin
Toxicity:apoptosis by indomethacin.
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Replated Protein:Acetylcholinesterase
Drug:indomethacin
Toxicity:enhance contractility of the small intestine.
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Replated Protein:G1/S-specific cyclin-D1
Drug:indomethacin
Toxicity:arrests endothelial cell proliferation.
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Replated Protein:Acetylcholinesterase
Drug:indomethacin
Toxicity:enhance contractility of the small intestine.
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Replated Protein:P-selectin
Drug:indomethacin
Toxicity:Indomethacin induced gastropathy.
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Replated Protein:B2 bradykinin receptor
Drug:indomethacin
Toxicity:enterocolitis.
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Replated Protein:Nitric oxide synthase, inducible
Drug:indomethacin
Toxicity:gastric damage and granulocyte infiltration.
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Replated Protein:Intercellular adhesion molecule 1
Drug:indomethacin
Toxicity:Indomethacin induced gastropathy.
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Replated Protein:Plasma kallikrein
Drug:indomethacin
Toxicity:enterocolitis.
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Replated Protein:Integrin alpha-M
Drug:indomethacin
Toxicity:experimental dystonia.
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Replated Protein:Tumor necrosis factor
Drug:indomethacin
Toxicity:gastric damage and granulocyte infiltration.
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Replated Protein:Cytochrome b5
Drug:indomethacin
Toxicity:selective effect of a p-chlorophenyl moiety.
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Replated Protein:NADH-cytochrome b5 reductase
Drug:indomethacin
Toxicity:selective effect of a p-chlorophenyl moiety.
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Replated Protein:Epoxide hydrolase
Drug:indomethacin
Toxicity:selective effect of a p-chlorophenyl moiety.
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