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Indomethacin

产品号 DB00328 公司名称 DrugBank
CAS号 53-86-1 公司网站 http://www.ualberta.ca/
分子式 C19H16ClNO4 电 话 (780) 492-3111
分子量 357.78764 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 213

产品价格信息

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产品别名

标题
Indomethacin
IUPAC标准名
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
IUPAC传统名
[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid
商标名
Indo-Tablinen
Dolcidium
Miametan
Methazine
Arthrexin
Artrivia
Chibro-Amuno
Indameth
Indocid
Indocid Pda
Indocin
Indocin I.V
Indorektal
Metartril
Rheumacin La
Artracin
Artrinovo
Bonidin
Dolcidium Pl
Idomethine
Imbrilon
Indacin
Indmethacine
Indo-Rectolmin
Indo-Spray
Indocin Sr
Indomecol
Indomee
Lausit
Liometacen
Metacen
Mikametan
Mobilan
Novo-Methacin
Novomethacin
Tannex
Vonum
Indaflex
Amuno
Apo-Indomethacin
Argun
Bonidon
Bonidon Gel
Catlep
Chrono-Indicid
Chrono-Indocid
Confortid
Dolovin
Durametacin
Elmetacin
Flexin Continus
Hicin
Inacid
Indo-Lemmon
Indo-Phlogont
Indocid Sr
Indocin I.V.
Indolar Sr
Indomed
Indomethegan
Indomo
Indomod
Indoptic
Indoptol
Indoxen
Inflazon
Infrocin
Inteban Sp
Metindol
Nu-Indo
Reumacide
Rhemacin La
Sadoreum
别名
Indometicina
Indomethancin
Indomethazine
IMN
Indomethacinum
Indomethacine
Indometacyna
Indometacine
Indomethine
indomethacin

产品登记号

PubChem SID 46508291
CAS号 53-86-1
PubChem CID 3715

产品性质

疏水性(logP) 3.4
溶解度 0.937 mg/L

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved; investigational
Description Indomethacin is a non-steroidal antiinflammatory agent (NSAIA) with antiinflammatory, analgesic and antipyretic activity. Its pharmacological effect is thought to be mediated through inhibition of the enzyme cyclooxygenase (COX), the enzyme responsible for catalyzes the rate-limiting step in prostaglandin synthesis via the arachidonic acid pathway.
Indication For moderate to severe rheumatoid arthritis including acute flares of chronic disease, ankylosing spondylitis, osteoarthritis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis.
Pharmacology Indomethacin, a NSAIA, with analgesic and antipyretic properties exerts its pharmacological effects by inhibiting the synthesis of prostaglandins involved in pain, fever, and inflammation. Indomethacin inhibits the catalytic activity of the COX enzymes, the enzymes responsible for catalyzing the rate-limiting step in prostaglandin synthesis via the arachidonic acid pathway. Indomethacin is known to inhibit two well-characterized isoforms of COX, COX-1 and COX-2, with greater selectivity for COX-1. COX-1 is a constitutively expressed enzyme that is involved in gastric mucosal protection, platelet and kidney function. It catalyzes the conversion of arachidonic acid to prostaglandin (PG) G2 and PGG2 to PGH2. COX-1 is involved in the synthesis pathways of PGE2, PGD2, PDF2a, PGI2 (also known as prostacyclin) and thromboxane A2 (TXA2). COX-2 is constitutively expressed and highly inducible by inflammatory stimuli. It is found in the central nervous system, kidneys, uterus and other organs. It also catalyzes the conversion of arachidonic acid to PGG2 and PGG2 to PGH2. In the COX-2-mediated pathway, PGH2 is subsequently converted to PGE2 and PGI2 (also known as prostacyclin). PGE2 is involved in mediating inflammation, pain and fever. Decreasing levels of PGE2 leads to decreased inflammation.
Toxicity 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.
Affected Organisms
Humans and other mammals
Biotransformation Hepatic.
Absorption Bioavailability is approximately 100% following oral administration and 80–90% following rectal administration.
Half Life 4.5 hours
Protein Binding 97%
Elimination Indomethacin is eliminated via renal excretion, metabolism, and biliary excretion.
References
Akbarpour F, Afrasiabi A, Vaziri ND: Severe hyperkalemia caused by indomethacin and potassium supplementation. South Med J. 1985 Jun;78(6):756-7. [Pubmed]
HART FD, BOARDMAN PL: INDOMETHACIN: A NEW NON-STEROID ANTI-INFLAMMATORY AGENT. Br Med J. 1963 Oct 19;2(5363):965-70. [Pubmed]
Lum GM, Aisenbrey GA, Dunn MJ, Berl T, Schrier RW, McDonald KM: In vivo effect of indomethacin to potentiate the renal medullary cyclic AMP response to vasopressin. J Clin Invest. 1977 Jan;59(1):8-13. [Pubmed]
Phelan KM, Mosholder AD, Lu S: Lithium interaction with the cyclooxygenase 2 inhibitors rofecoxib and celecoxib and other nonsteroidal anti-inflammatory drugs. J Clin Psychiatry. 2003 Nov;64(11):1328-34. [Pubmed]
Ragheb M: The clinical significance of lithium-nonsteroidal anti-inflammatory drug interactions. J Clin Psychopharmacol. 1990 Oct;10(5):350-4. [Pubmed]
External Links
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参考文献

  • Akbarpour F, Afrasiabi A, Vaziri ND: Severe hyperkalemia caused by indomethacin and potassium supplementation. South Med J. 1985 Jun;78(6):756-7. Pubmed
  • HART FD, BOARDMAN PL: INDOMETHACIN: A NEW NON-STEROID ANTI-INFLAMMATORY AGENT. Br Med J. 1963 Oct 19;2(5363):965-70. Pubmed
  • Lum GM, Aisenbrey GA, Dunn MJ, Berl T, Schrier RW, McDonald KM: In vivo effect of indomethacin to potentiate the renal medullary cyclic AMP response to vasopressin. J Clin Invest. 1977 Jan;59(1):8-13. Pubmed
  • Phelan KM, Mosholder AD, Lu S: Lithium interaction with the cyclooxygenase 2 inhibitors rofecoxib and celecoxib and other nonsteroidal anti-inflammatory drugs. J Clin Psychiatry. 2003 Nov;64(11):1328-34. Pubmed
  • Ragheb M: The clinical significance of lithium-nonsteroidal anti-inflammatory drug interactions. J Clin Psychopharmacol. 1990 Oct;10(5):350-4. Pubmed