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QuickView for Gliclazide (compound)

Name: Gliclazide
PubChem Compound ID: 3475
Description: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.
Molecular formula: C15H21N3O3S
Molecular weight: 323.412 g/mol
KBio2_007094; Gliclazide [BAN:DCF:INN:JAN]; CHEBI:31654; Gliclazida [INN-Spanish]; Nordialex; N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea; DivK1c_006966; SE 1702; SpecPlus_000870; Spectrum3_001862.
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Name: Gliclazide
Name (isomeric): DB01120
Drug Type: small molecule
Description: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.
1-(Hexahydrocyclopenta(c)pyrrol-2(1H)-yl)-3-(p-tolylsulfonyl)urea; Gliclazida [INN-Spanish]; Gliclazidum [INN-Latin]; N-(4-Methylbenzenesulfonyl)-N'-(3-azabicyclo(3.3.0)oct-3-yl)urea; 1-(3-Azabicyclo(3.3.0)oct-3-yl)-3-(p-tolylsulfonyl)urea
Brand: Glimicron, Diamicron, Mylan-Gliclazide, Diamicron MR, Nordialex, PMS-Gliclazide
Category: Hypoglycemic Agents, Sulfonylureas, Antidiabetic
CAS number: 21187-98-4
Indication: For the treatment of NIDDM in conjunction with diet and exercise.
Pharmacology: Gliclazide is a second generation sulphonylurea which acts as a hypoglycemic agent. It stimulates β 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 β 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 β cells. This opens voltage-dependent calcium channels in the β cell r...
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Absorption: Rapidly and well absorbed but may have wide inter- and intra-individual variability. Peak plasma concentrations occur within 4-6 hours of oral administration.
Protein binding: 94%, highly bound to plasma proteins
Biotransformation: Extensively metabolized in the liver. Less than 1% of the orally administered dose appears unchanged in the urine. Metabolites include oxidized and hydroxylated derivates, as well as glucuronic acid conjugates.
Route of elimination: Metabolites and conjugates are eliminated primarily by the kidneys (60-70%) and also in the feces (10-20%).
Half Life: 10.4 hours. Duration of action is 10-24 hours.
Toxicity: LD50=3000 mg/kg (orally in mice). Gliclazide and its metabolites may accumulate in those with severe hepatic and/or renal dysfunction. Symptoms of hypoglycemia include: dizziness, lack of energy, drowsiness, headache and sweating.
Affected organisms: Humans and other mammals
Food interaction:
Avoid alcohol.
Take without regard to meals. A consistent diet is recommended to reduce the risk of hypoglycemia.
Drug interaction:
Somatropin recombinantSomatropin may antagonize the hypoglycemic effect of gliclazide. Monitor for changes in fasting and postprandial blood sugars.
OxprenololThe beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
BevantololThe beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
EsmololThe beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
MetoprololThe beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.
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