Tolmetin sodium

한글명:Tolmetin sodium

카스 번호35711-34-3

상품명:Tolmetin sodium

CBNumberCB6397353

분자식C15H14NNaO3

포뮬러 무게279.27

MOL 파일35711-34-3.mol

그림문자(GHS)

Tolmetin sodium 화학적 특성, 용도, 생산

용도
Tolmetin Sodium is a non-steroidal anti-inflammatory drug.
Pharmacokinetics
Tolmetin sodium is rapidly and almost completely absorbed on oral administration, with peak plasma levels being attained within the first hour of administration. It has a relatively short plasma half-life of approximately 1 hour because of extensive first-pass metabolism, involving hydroxylation of the p-methyl group to the primary alcohol, which is subsequently oxidized to the dicarboxylic acid.
Clinical Use
Tolmetin is synthesized straightforwardly from 1-methylpyrrole. It was introduced in the United States in 1976 and like other NSAIDs, inhibits prostaglandin biosynthesis. Tolmetin, however, also inhibits polymorph migration and decreases capillary permeability. Its anti-inflammatory activity, as measured in the carrageenan-induced rat paw edema and cotton pellet granuloma assays, is intermediate between those of phenylbutazone and indomethacin.
부작용
The most frequently adverse reactions are those involving the GI tract (e.g., abdominal pain, discomfort, and nausea) but appear to be less than those observed with aspirin. The CNS effects (e.g., dizziness and drowsiness) also are observed. Few cases of overdosage have been reported, but in such cases, recommended treatment includes elimination of the drug from the GI tract by emesis or gastric lavage and elimination of the acidic drug from the circulatory system by enhancing alkalinization of the urine with sodium bicarbonate.
신진 대사
This metabolite is inactive in standard in vivo anti-inflammatory assays. The free acid (pKa = 3.5) is highly bound to plasma proteins (99%), and excretion of tolmetin and its metabolites occurs primarily in the urine.Approximately 15 to 20% of an administered dose is excreted unchanged and 10% as the glucuronide conjugate of the parent drug. Conjugates of the dicarboxylic acid metabolite account for the majority of the remaining administered drug.

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