Amtolmetin guacil
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amtolmetin guacil a NSAID.
Prodrug of tolmetin sodium.
Background of molecule:
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
General Information
Nomenclature: 2-Methoxyphenyl-1-Methyl-5p-Methylbenzoyl-pyrrol-2-Acetamido acetate
CAS No: 87344-06-7
Molecular Formula: C24H24N2O5
Molecular Weight: 420.458 g/mole
Physical description: White or almost white crystal or crystalline powder. Pharmacology:
v Almost is absorbed on oral administration. It is concentrated maximum in internal the gastric wall, and highest concentration reached in 2 hours after administration. v Amtolmetin guacil hydrolysed in to following metabolites Tolmetin, MED5 and Guiacol. v Elimination will complete in 24 hours. Happens mostly with urine in shape of gluconides products (77%), faecal (7.5 %). v It is advised to take the drug on empty stomach. v 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 vanilic moiety and also releases NO which is gastro protective. It also inhibits prostaglandin synthesis and Cyclooxygenase (COX).
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