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인드메타신

인드메타신
인드메타신 구조식 이미지
카스 번호:
53-86-1
한글명:
인드메타신
동의어(한글):
인도메타신;인드메타신
상품명:
Indometacin
동의어(영문):
Amuno;Vonum;Catlep;Tannex;Inacid;Lausit;INDOCIN;Bonidin;Mobilan;Dolovin
CBNumber:
CB1750267
분자식:
C19H16ClNO4
포뮬러 무게:
357.79
MOL 파일:
53-86-1.mol

인드메타신 속성

녹는점
155-162 °C
밀도
1.2135 (rough estimate)
굴절률
1.6800 (estimate)
저장 조건
Store at RT
용해도
ethanol: 50 mg/mL, clear, yellow-green
물리적 상태
White to off-white powder
산도 계수 (pKa)
4.5(at 25℃)
수용성
Soluble in acetone (40 mg/mL - clear, yellow solution), ethanol (20 mg/mL), ether, castor oil; Soluble in chloroform (50 mg/mL - clear, yellow, extremely viscous solution); decomposed by strong alkali but stable in neutral or slightly acidic media; insoluble in water.
감도
Light Sensitive
Merck
14,4968
BRN
497341
안정성
Stable. Incompatible with strong oxidizing agents.
InChIKey
CGIGDMFJXJATDK-UHFFFAOYSA-N
CAS 데이터베이스
53-86-1(CAS DataBase Reference)
NIST
Indomethacin(53-86-1)
EPA
1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy- 2-methyl-(53-86-1)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 T+,Xi,T
위험 카페고리 넘버 28-36/37/38-39/23/24/25-23/24/25
안전지침서 28-36/37-45-36-26
유엔번호(UN No.) UN 2811 6.1/PG 1
WGK 독일 3
RTECS 번호 NL3500000
F 고인화성물질 8-10
TSCA Yes
위험 등급 6.1
포장분류 I
HS 번호 29339900
유해 물질 데이터 53-86-1(Hazardous Substances Data)
독성 LD50 i.p. in rats: 13 mg/kg (Klaassen)
그림문자(GHS):
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H300 삼키면 치명적임 급성 독성 물질 - 경구 구분 1,2 위험 P264, P270, P301+P310, P321, P330,P405, P501
H341 유전적인 결함을 일으킬 것으로 의심됨 (노출되어도 생식세포 유전독성을 일으키지 않는다는 결정적인 증거가 있는 노출경로가 있다면 노출경로 기재) 생식세포 변이원성 물질 구분 2 경고 P201,P202, P281, P308+P313, P405,P501
예방조치문구:
P201 사용 전 취급 설명서를 확보하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P308+P313 노출 또는 접촉이 우려되면 의학적인 조치· 조언를 구하시오.
P405 밀봉하여 저장하시오.

인드메타신 MSDS


1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid

인드메타신 C화학적 특성, 용도, 생산

화학적 성질

Crystalline Solid

용도

antiinflammatory, antipyretic, analgesic

용도

Inhibits cyclooxygenase (IC50=0.1uM) selectively over liposygenases (IC50=100uM for 5-,12- and 15-LO). A clinically useful NAISD

Indications

Indomethacin (Indocin) is used in the treatment of acute gouty arthritis, rheumatoid arthritis, ankylosing spondylitis, and osteoarthritis. It is not recommended for use as a simple analgesic or antipyretic because of its potential for toxicity.While indomethacin inhibits both COX-1 and COX-2, it is moderately selective for COX- 1. It produces more CNS side effects than most of the other NSAIDs. Severe headache occurs in 25 to 50% of patients; vertigo, confusion, and psychological disturbances occur with some regularity. GI symptoms also are more frequent and severe than with most other NSAIDs. Hematopoietic side effects (e.g., leukopenia, hemolytic anemia, aplastic anemia, purpura, thrombocytopenia, and agranulocytosis) also may occur. Ocular effects (blurred vision, corneal deposits) have been observed in patients receiving indomethacin, and regular ophthalmological examinations are necessary when the drug is used for long periods. Hepatitis, jaundice, pancreatitis, and hypersensitivity reactions also have been noted.

정의

The antiinflammatory drug indomethacin.

상표명

Indocin (Merck);Argan.

World Health Organization (WHO)

Indometacin was introduced in 1963 and it is one of the first NSAIDs. Convulsions are rarely reported in relation with the use of this group of agents. Indometacin farnesil is a pro-drug of indometacin, and the occurrence of gastro-intestinal adverse effects could be expected. See also under nonsteroidal antiinflammatory agents.

Biological Functions

Indomethacin (Indocin) is an acetic acid derivative related functionally to sulindac (Clinoril), a prodrug with a long half-life, and etodolac (Lodine).They are metabolized in the liver and excreted as metabolites in the bile and via the kidney. They are potent inhibitors of COX and thus extremely effective antiinflammatory agents.

일반 설명

From the time of its introduction in 1965, indomethacin(Indocin) has been widely used as an analgesic to relieve inflammatorypain associated with RA, OA and ankylosingspondylitis, and, to a lesser extent, in gout. Although both itsanalgesic and anti-inflammatory activities are well established,its use is often limited because of frequent GI distressand potential drug interactions, especially with warfarinfurosemide, and lithium (i.e., it elevates blood levels oflithium as a result of reducing renal blood flow and thereforeincreases lithium toxicities).
Following oral administration, indomethacin is rapidlyabsorbed and is 90% protein bound at therapeutic plasmaconcentrations. The drug has a biological half-life ofabout 5 to 10 hours and a plasma clearance of 1 to 2.5 ml/kgper minute. It is metabolized to its inactive, O-desmethyl,N-deschlorobenzoyl-, and O-desmethyl, N-deschlorobenzoylindomethacinmetabolites.

일반 설명

Crystals.

공기와 물의 반응

Practically insoluble in water. Decomposes in alkali.

반응 프로필

A weak organic acid.

화재위험

Non-combustible, substance itself does not burn but may decompose upon heating to produce corrosive and/or toxic fumes. Some are oxidizers and may ignite combustibles (wood, paper, oil, clothing, etc.). Contact with metals may evolve flammable hydrogen gas. Containers may explode when heated.

Pharmaceutical Applications

Indomethacin is a nonsteroidal anti-inflammatory agent used in pain and moderate to severe inflammation in rheumatic diseases and other musculoskeletal disorders. It is a COX (cyclooxygenase) inhibitor and therefore interrupts the production of prostaglandins.
A series of new silicon compounds, based on the structure of indomethacin, have been synthesised and are under investigation as novel anticancer agents. The carboxyl group of indomethacin was reacted with a series of amino-functionalised silanes. The resulting products have been shown to be significantly more lipophilic and more selective to COX-2. Furthermore, in vitro testing has shown an increased uptake of the new compounds at the tumour site. The silane-functionalised indomethacin derivatives exhibited a 15-fold increased antiproliferative effect when tested against pancreatic cancer .

Pharmaceutical Applications

Indomethacinis a nonsteroidal anti-inflammatory agent used in pain and moderate to severe inflammation in rheumatic diseases and other musculoskeletal disorders. It is a COX (cyclooxygenase) inhibitor and therefore interrupts the production of prostaglandins.

생물학적 활성

Cyclooxgenase (COX) inhibitor; displays selectivity for COX-1 (IC 50 values are 230 and 630 nM for human COX-1 and COX-2 respectively). Widely used anti-inflammatory agent.

부작용

All of these drugs produce analgesic effects, antipyresis, and antiinflammatory effects.Due to the high incidence of gastric irritation, headache, nausea, and other side effects, including hematological effects and coronary vasoconstriction, they are not useful as an initial treatment for pain. GI irritation and ulceration occur to a lesser extent with etodolac. Indomethacin is useful in the treatment of acute gout, osteoarthritis, ankylosing spondylitis, and acceleration of the closure of the ductus arteriosus in premature infants. The tocolytic effects of indomethacin to prevent preterm labor are the result of its effects on prostaglandin synthesis. However, the toxicity of the drug limits such application, since it increases fetal morbidity. Indomethacin is contraindicated in pregnancy, in asthmatics, and in those with gastric ulcers or other ulceration of the GI tract. Indomethacin may increase the symptoms associated with depression or other psychiatric disturbances and those associated with epilepsy and Parkinson’s disease. The drug should be used with caution in such patients.

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