Drug/Small Molecule:
tolmetin

2D structure

Overview

Generic Names: Tolmetin Sodium; Tolmetina [DCIT]; Tolmetine [INN-French]; Tolmetino [INN-Spanish]; Tolmetinum [INN-Latin]
Trade Names: Tolectin; Tolectin DS
PharmGKB Accession Id: PA451721

Description

A non-steroidal anti-inflammatory agent (anti-inflammatory agents, NON-steroidal) similar in mode of action to indomethacin. PubChem (source: Drug Bank)

Indication

For the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis, including the treatment of acute flares long-term management. Also for treatment of juvenile rheumatoid arthritis. (source: Drug Bank)

ATC Therapeutic Categories

  • M01AB:Acetic acid derivatives and related substances
  • M02AA:Antiinflammatory preparations, non-steroids for topical use

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

The mode of action of tolmetin is not known. However, studies in laboratory animals and man have demonstrated that the anti-inflammatory action of tolmetin is not due to pituitary-adrenal stimulation. Tolmetin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action. Tolmetin does not appear to alter the course of the underlying disease in man. (source: Drug Bank)

Pharmacology

Tolmetin is a nonsteroidal anti-inflammatory agent. Studies in animals have shown tolmetin to possess anti-inflammatory, analgesic and antipyretic activity. In the rat, tolmetin prevents the development of experimentally induced polyarthritis and also decreases established inflammation. In patients with either rheumatoid arthritis or osteaoarthritis, tolmetin is as effective as aspirin and indomethacin in controlling disease activity, but the frequency of the milder gastrointestinal adverse effects and tinnitus was less than in aspirin-treated patients, and the incidence of central nervous system adverse effects was less than in indomethacin-treated patients. In patients with juvenile rheumatoid arthritis, tolmetin is as effective as aspirin in controlling disease activity, with a similar incidence of adverse reactions. tolmetin has produced additional therapeutic benefit when added to a regimen of gold salts and, to a lesser extent, with corticosteroids. Tolmetin should not be used in conjunction with salicylates since greater benefit from the combination is not likely, but the potential for adverse reactions is increased. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Essentially all of the administered dose is recovered in the urine in 24 hours either as an inactive oxidative metabolite or as conjugates of tolmetin. (source: Drug Bank)

Absorption

Rapidly and almost completely absorbed with peak plasma levels being reached within 30-60 minutes after an oral therapeutic dose. (source: Drug Bank)

Toxicity

Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain. (source: Drug Bank)

Isomeric SMILES Code:

Cc1ccc(cc1)C(=O)c2ccc(n2C)CC(=O)O (source: Drug Bank)

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
PTGS1 Uncurated Annotation (source: Drug Bank)
PTGS2 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00500
KEGG Compound ID:
C02328
PubChem Compound ID:
5509
PubChem Substance ID:
7849414

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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