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Amtolmetin guacil

Amtolmetin guacil
Systematic (IUPAC) name
(2-methoxyphenyl) 2-[ [2-[1-methyl-5-(4-methylbenzoyl)pyrrol-2-yl]acetyl]ami


CAS number 87344-06-7
ATC code  ?
PubChem 65655
Chemical data
Formula C24H24N2O5 
Mol. mass 420.458 g/mol
Synonyms ST-679
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.


Legal status
Routes  ?

Amtolmetin guacil a NSAID which is a prodrug of tolmetin sodium.


Tolmetin sodium is an effective NSAID approved and marketed for the treatment of rheumatoid arthritis, osteoarthritis and juvenile rheumatoid arthritis. In humans, tolmetin sodium is absorbed rapidly with peak plasma levels observed 30 min after p.o. administration, but it is also eliminated rapidly with a mean plasma elimination t½ of approximately 1 hr. The preparation of slow release formulations or chemical modification of NSAIDs to form prodrugs has been suggested as a method to reduce the gastrotoxicity of these agents.

Amtolmetin guacil is a non-acidic prodrug of tolmetin, having similar NSAID properties like tolmetin with additional analgesic, antipyretic, and gastro protective properties. Amtolmetin is formed by amidation of tolmetin by glycine


  • Almost is absorbed on oral administration. It is concentrated maximum in internal the gastric wall, and highest concentration reached in 2 hours after administration.
  • Amtolmetin guacil hydrolysed in to following metabolites Tolmetin, MED5 and Guiacol.
  • Elimination will complete in 24 hours. Happens mostly with urine in shape of gluconides products (77%), faecal (7.5 %).
  • It is advised to take the drug on empty stomach.
  • Permanent anti-inflammatory action is continued up to 72 hours, with single administration.

Mechanism of action

Amtolmetin guacil stimulates capsaicin receptors present on gastro intestinal walls, because of presence of vanillic moiety and also releases NO which is gastro protective. It also inhibits prostaglandin synthesis and cyclooxygenase (COX).

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Amtolmetin_guacil". A list of authors is available in Wikipedia.
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