Tolmetin

한글명:Tolmetin

카스 번호26171-23-3

상품명:Tolmetin

CBNumberCB2875183

분자식C15H15NO3

포뮬러 무게257.28

MOL 파일26171-23-3.mol

화학적 성질

녹는점	156 °C
끓는 점	400.53°C (rough estimate)
밀도	1.1391 (rough estimate)
굴절률	1.5200 (estimate)
저장 조건	2-8°C
용해도	클로로포름(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	pKa 3.5(H2O t undefined I undefined) (Uncertain)
색상	황백색에서 연한 노란색
수용성	222mg/L
NIST	Tolmetin(26171-23-3)
EPA	1H-Pyrrole-2-acetic acid, 1-methyl-5-(4-methylbenzoyl)- (26171-23-3)

위험 및 안전 성명

유해 물질 데이터

26171-23-3(Hazardous Substances Data)

그림문자(GHS)

Tolmetin MSDS

Tolmetin 화학적 특성, 용도, 생산

개요
An antiinflammatory, analgesic, and antipyretic that is as efficacious as moderate doses of aspirin and better tolerated. Tolmetin produces a number of adverse effects including epigastric pain, dyspepsia, nausea, and vomiting. Tolmetin is approximately 99% plasma protein bound, yet does not interfere with concurrent treatment with oral hypoglycemics. Tolmetin has been found to be effective in the treatment of osteoarthritis and rheumatoid arthritis.
용도
Tolmetine is an NSAID.
Indications
Tolmetin (Tolectin) is indicated for the relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and moderate pain. It is ineffective in gouty arthritis for unknown reasons.Tolmetin can inhibit both COX-1 and COX-2 but has a moderate selectivity for COX-1. The most frequently reported side effects are GI disturbance and CNS reactions (e.g., headache, asthenia, and dizziness). These effects are less frequently observed than after aspirin or indomethacin use. Blood pressure elevation, edema, and weight gain or loss have been associated with tolmetin administration. Tolmetin metabolites in urine have been found to produce pseudoproteinuria in some laboratory tests.
정의
ChEBI: A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug.
Biological Functions
Tolmetin (Tolectin) is an antiinflammatory, analgesic, and antipyretic agent that produces the usual gastric distress and ulceration observed with NSAIDs. However, tolmetin is better tolerated than aspirin and produces less tinnitus and vertigo. Tolmetin is a substitute for indomethacin in indomethacin-sensitive patients and is unique among such drugs in that it can be used to treat juvenile arthritis.
일반 설명
Tolmetin sodium (Tolectin), is an arylacetic acid derivativewith a pyrrole as the aryl group. This drug is well absorbed and has a relatively short plasma half-life (1 hour). It is recommendedfor use in the management of acute and chronicRA. Its efficacy is similar to aspirin and indomethacin, butwith less frequency of the adverse effects and tinnitus associatedwith aspirin. It does not potentiate coumarin-likedrugs nor alter the blood levels of sulfonylureas or insulin.However, tolmetin, and especially its closely related drug,zomepirac (i.e., with a p-chlorobenzoyl group and an additionalmethyl group on the pyrrole ring), can produce a rarebut fatal anaphylactic reaction because of irreversible bindingof their unstable acyl glucuronides. Zomepirac waswithdrawn from market because it is eliminated only via theester-type, acyl glucuronide. It is possible that tolmetin isless toxic in this regard because it undergoes additional hepaticbenzylic hydroxylation via its p-methyl group and isexcreted as its stable ether glucuronide.
상품명
Artrocaptin (Estedi, Spain), Tolectin (Cilag, Belgium; Janssen-Cilag, Austria; McNeil, USA).

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