Tolmetin sodium is an approved NSAID, marketed for the treatment of rheumatoid arthritis, osteoarthritis and juvenile rheumatoid arthritis.[2] In humans, tolmetin sodium is absorbed rapidly with peak plasma levels observed 30 minutes after administration. It is eliminated rapidly with a mean plasma elimination t½ of approximately 1 hour. 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 NSAID properties similar to tolmetin with additional analgesic, antipyretic, and gastro protective properties. Amtolmetin is formed by amidation of tolmetin by glycine.
Pharmacologyedit
Most is absorbed on oral administration. It is concentrated in the gastric wall. Highest concentration is reached 2 hours after administration.
Amtolmetin guacil can be hydrolysed to produce the metabolites Tolmetin, MED5 and Guiacol.
Elimination completes in 24 hours. This 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 continues up to 72 hours, with single administration.
Mechanism of actionedit
Amtolmetin guacil stimulates capsaicin receptors present on gastrointestinal walls, because of presence of vanillic moiety and also releases NO which is gastro protective. It also inhibits prostaglandin synthesis and cyclooxygenase (COX).
Referencesedit
^Tsvetkova E, Denisov L, Nasonov E (2017). "AB0798 Amtolmetin guacil-effective and good safe nonsteroidal anti-inflammatory drug in knee osteoarthritis patients with dyspepsia". Annals of the Rheumatic Diseases. 76 (Suppl 2): 1337.2–1337. doi:10.1136/annrheumdis-2017-eular.5253.
^Garg A, Shoeb A, Moodahadu LS, Sharma A, Gandhi A, Akku S (2016). "Amtolmetin: A Reappraisal of NSAID with Gastroprotection". Arthritis. 2016: 7103705. doi:10.1155/2016/7103705. PMC4820613. PMID 27092274.
January 01, 1970
amtolmetin, guacil, this, article, needs, additional, citations, verification, please, help, improve, this, article, adding, citations, reliable, sources, unsourced, material, challenged, removed, find, sources, news, newspapers, books, scholar, jstor, march, . This article needs additional citations for verification Please help improve this article by adding citations to reliable sources Unsourced material may be challenged and removed Find sources Amtolmetin guacil news newspapers books scholar JSTOR March 2019 Learn how and when to remove this message Amtolmetin guacil is a non steroidal anti inflammatory drug NSAID It is a prodrug of tolmetin sodium 1 Amtolmetin guacilClinical dataOther namesST 679ATC codenoneIdentifiersIUPAC name 2 methoxyphenyl 2 2 1 methyl 5 4 methylbenzoyl pyrrol 2 yl acetyl amiCAS Number87344 06 7 NPubChem CID65655ChemSpider59091 YUNII323A00CRO9KEGGD07453 YChEMBLChEMBL1766570 NCompTox Dashboard EPA DTXSID50236291ECHA InfoCard100 207 038Chemical and physical dataFormulaC 24H 24N 2O 5Molar mass420 465 g mol 13D model JSmol Interactive imageSMILES O C c1ccc n1C CC O NCC O Oc2ccccc2OC c3ccc cc3 CInChI InChI 1S C24H24N2O5 c1 16 8 10 17 11 9 16 24 29 19 13 12 18 26 19 2 14 22 27 25 15 23 28 31 21 7 5 4 6 20 21 30 3 h4 13H 14 15H2 1 3H3 H 25 27 YKey CWJNMKKMGIAGDK UHFFFAOYSA N Y N Y what is this verify Contents 1 Background 2 Pharmacology 3 Mechanism of action 4 ReferencesBackground editTolmetin sodium is an approved NSAID marketed for the treatment of rheumatoid arthritis osteoarthritis and juvenile rheumatoid arthritis 2 In humans tolmetin sodium is absorbed rapidly with peak plasma levels observed 30 minutes after administration It is eliminated rapidly with a mean plasma elimination t of approximately 1 hour 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 NSAID properties similar to tolmetin with additional analgesic antipyretic and gastro protective properties Amtolmetin is formed by amidation of tolmetin by glycine Pharmacology editMost is absorbed on oral administration It is concentrated in the gastric wall Highest concentration is reached 2 hours after administration Amtolmetin guacil can be hydrolysed to produce the metabolites Tolmetin MED5 and Guiacol Elimination completes in 24 hours This 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 continues up to 72 hours with single administration Mechanism of action editAmtolmetin guacil stimulates capsaicin receptors present on gastrointestinal walls because of presence of vanillic moiety and also releases NO which is gastro protective It also inhibits prostaglandin synthesis and cyclooxygenase COX References edit Tsvetkova E Denisov L Nasonov E 2017 AB0798 Amtolmetin guacil effective and good safe nonsteroidal anti inflammatory drug in knee osteoarthritis patients with dyspepsia Annals of the Rheumatic Diseases 76 Suppl 2 1337 2 1337 doi 10 1136 annrheumdis 2017 eular 5253 Garg A Shoeb A Moodahadu LS Sharma A Gandhi A Akku S 2016 Amtolmetin A Reappraisal of NSAID with Gastroprotection Arthritis 2016 7103705 doi 10 1155 2016 7103705 PMC 4820613 PMID 27092274 Retrieved from https en wikipedia org w index php title Amtolmetin guacil amp oldid 1182071910, wikipedia, wiki, book, books, library,
