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| Systematic (IUPAC) name | |
|---|---|
| 3-ethyl-4-methyl-N-(4-[N-((1r,4r)-4-methylcyclohexylcarbamoyl)sulfamoyl]phenethyl)-2-oxo-2,5-dihydro-1H-pyrrole-1-carboxamide | |
| Identifiers | |
| CAS number | 93479-97-1 |
| ATC code | A10BB12 |
| PubChem | 3476 |
| DrugBank | APRD00381 |
| Chemical data | |
| Formula | C24H34N4O5S |
| Mol. mass | 490.617 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | >99.5% |
| Metabolism | ? |
| Half life | 5 Hours |
| Excretion | Urine & Fecal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | Oral |
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Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. It is marketed as Amaryl by Sanofi-Aventis and Glyree by Ipca. Glimepiride is the first third-generation sulfonylurea, and is very potent.
It is sometimes classified as third-generation,[1] and sometimes classified as second-generation.[2]
Contents |
Indications
Type 2 diabetes (NIDDM).
Adverse effects
GI disturbance, rarely thrombocytopenia , leukopenia, hemolytic anemia, occasionally allergic reactions occur. In the initial weeks of treatment, the risk of hypoglycemia may be increased.
Contraindications
-Hypersensitivity to glimepiride or other sulfonylureas.
-Pregnancy
Interactions
With NSAIDs like Salicylates, Sulphonamides, Chloramphenicol, coumadin and probencid may potentiate the hypoglycemic action of glimepiride. Thiazides, other diuretic, phothiazides, thyroid products, oral contraceptives, phenytoin tend to produce hyperglycemia.
Pharmacology
With glimepiride GI absorption is complete, with no interference of meals. Significant absorption of glimepiride was seen within 1 hour, and distributed throughout the body, bound to the plasma protein to an extent of 99.5% and it is metabolized by oxidative biotransformation and 60% is excreted in the urine, the remaining being excreted in the feces.
Mechanism of action
Glimepiride lowers the blood glucose level by stimulating pancreatic beta cells to produce more insulin and by inducing increased activity of intracellular insulin receptors.
It is considered a secretagogue.[3]
References
- ^ Hamaguchi T, Hirose T, Asakawa H, et al. (December 2004). "Efficacy of glimepiride in type 2 diabetic patients treated with glibenclamide". Diabetes Res. Clin. Pract. 66 Suppl 1: S129–32. doi:. PMID 15563963. http://linkinghub.elsevier.com/retrieve/pii/S0168-8227(04)00148-2.
- ^ Davis SN (2004). "The role of glimepiride in the effective management of Type 2 diabetes". J. Diabetes Complicat. 18 (6): 367–76. doi:. PMID 15531188. http://linkinghub.elsevier.com/retrieve/pii/S1056-8727(04)00078-9.
- ^ Nissen SE, Nicholls SJ, Wolski K, et al. (April 2008). "Comparison of pioglitazone vs glimepiride on progression of coronary atherosclerosis in patients with type 2 diabetes: the PERISCOPE randomized controlled trial". JAMA 299 (13): 1561–73. doi:. PMID 18378631. http://jama.ama-assn.org/cgi/pmidlookup?view=long&pmid=18378631.
External links
- http://www.drugdigest.org/DD/DVH/Uses/1,3915,298|Amaryl%2BTablets|2805,00.html*
- http://www.theodora.com/drugs/amaryl_tablets_sanofi_aventis.html
- http://www.rxlist.com/cgi/generic/glimepiride.htm
- http://www.pharmgkb.org/do/serve?objId=213&objCls=DrugProperties
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