Tolmetin

Tolmetin

File:Tolmetin Structural Formulae.png
Systematic (IUPAC) name
[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetic acid
Clinical data
Routes of administration	oral
Pharmacokinetic data
Biological half-life	1-2 hours, next phase up to 5 hours
Identifiers
CAS Number	26171-23-3
ATC code	M01AB03 (WHO) M02AA21
PubChem	CID 5509
DrugBank	APRD01268
Chemical data
Formula	C15H15NO3
Molar mass	257.285 g/mol[[]]
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Tolmetin (pronounced /ˈtɒlmətɨn/) is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. It is used primarily to reduce hormones that cause pain, swelling, tenderness, and stiffness in conditions such as osteoarthritis and rheumatoid arthritis, including juvenile rheumatoid arthritis. In the United States it is marketed as Tolectin and comes as a tablet or capsule.

Tolmetin can increase the risk of heart or circulatory conditions such as heart attacks and strokes. It should not be taken shortly before or after coronary artery bypass surgery. Tolmetin can also increase the risk of gastrointestinal conditions such as perforation or bleeding, which is fatal. Antacids can be taken with tolmetin to relieve stomachaches that often occur. Overdose can result in drowsiness, nausea, epigastric pain, and vomiting.

When tested in rats tolmetin prevented experimentally stimulated polyarthritis and reduced inflammation. In patients with rheumatoid arthritis or osteoarthritis tolmetin restrained disease activity as efficiently as aspirin and indometacin, although the occurrence of mild gastrointestinal adverse effects and tinnitus was lower in patients treated with tolmetin than it was with aspirin-treated patients and the occurrence of adverse effects of the central nervous system was lower with tolmetin than it was with indometacin.

Although the mechanism of action of tolmetin is unknown, research involving humans and animals has shown that tolmetin does not achieve anti-inflammatory response by stimulation of the adrenal or pituitary gland, but it has shown tolmetin restrains prostaglandin synthetase in vitro and reduces plasma of prostaglandin E, possibly causing the anti-inflammatory response. 500px

http://dx.doi.org/10.1021/jm00289a026

References

es:Tolmetina