| Generic name |
Gliclazide
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| Brand Names/Synonyms |
Glimicron (TN); Gliclazide (JAN); Diamicron; GLICLAZIDE; Gliclazida [INN-Spanish]; Gliclazide [BAN:DCF:INN:JAN]; Gliclazidum [INN-Latin]; Glimicron; Nordialex; 1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea; 1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea; N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea |
| Indication |
For the treatment of Diabetes mellitus |
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Description |
Not Available |
| Pharmacology |
Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates beta cells of the islet of Langerhans in the pancreas to release insulin. It also enhances peripheral insulin sensitivity. Overall it potentiates insulin release and improves insulin dynamics. |
| Mechanism Of Action |
Gliclazide binds to the beta cell sulfonyl urea receptor (SUR1). This binding subsequently blocks the ATP sensitive potassium channels. The binding results in closure of the channels and leads to a resulting decrease in potassium efflux leads to depolarization of the beta cells. This opens voltage-dependent calcium channels in the beta cell resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules. |
Gliclazide News
(When available) |
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| Dosage Forms |
TABLET |
| Drug_Category |
Hypoglycemic Agents; Sulfonylureas; ATC:A10BB09 |
| Absorption |
Rapidly and well absorbed but may have wide inter- and intra-individual variability. |
| Interactions |
Not Available |
| Toxicity |
Oral LD50=3000 mg/kg (Mouse) |
| Organisms Affected |
Humans and other mammals |
| Chemical IUPAC Name |
N-(7-azabicyclo[3.3.0]oct-7-yl)methanamide |
| Chemical Formula |
C15H21N3O3S |
| Molecular Weight |
323.412 g/mol |
| Smiles String |
CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2CC3CCCC3C2 |
| Melting Point |
181 °C |
| Water Solubility |
Not Available |
| State |
Solid |
| LogP/Hphobicity |
2.418 |
| Isoelectric Point |
5.98 (Doucet J et al.,Drug Invest;8(4):219-24) |
| Biotransformation |
Hepatic |
| Half Life |
11 hours (Campbell DB et al.,Diabetes Res Clin Pract.;14:S21-36) |
| Protein Binding [%] |
Not Available |
| RxList Link |
Not Available>RXlist |
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| Drug Reference |
http://www.drugs.com/cons/Gliclazide.html |
| Drug Type |
Approved Drug |
| Accession No |
APRD00460 |
| CAS Registry Number |
21187-98-4 |
| KEGG Compound ID |
C13059 |
| PubChem ID |
SID:585123 |
| PharmGKB ID |
PA10892 |
| SwissProt ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
2248453
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