Gliclazide is an oral hypoglycemic drug used to treat type 2 diabetes. It works by binding to receptors on pancreatic beta cells, blocking potassium channels and stimulating the release of insulin. It is well absorbed orally but exhibits inter-individual variability, extensively metabolized in the liver, and primarily eliminated through urine and feces. Gliclazide may have increased effects when taken with other antidiabetic drugs, beta-blockers, ACE inhibitors, and NSAIDs, while its effect may be reduced with danazol.
Gliclazide is an oral hypoglycemic drug used to treat type 2 diabetes. It works by binding to receptors on pancreatic beta cells, blocking potassium channels and stimulating the release of insulin. It is well absorbed orally but exhibits inter-individual variability, extensively metabolized in the liver, and primarily eliminated through urine and feces. Gliclazide may have increased effects when taken with other antidiabetic drugs, beta-blockers, ACE inhibitors, and NSAIDs, while its effect may be reduced with danazol.
Gliclazide is an oral hypoglycemic drug used to treat type 2 diabetes. It works by binding to receptors on pancreatic beta cells, blocking potassium channels and stimulating the release of insulin. It is well absorbed orally but exhibits inter-individual variability, extensively metabolized in the liver, and primarily eliminated through urine and feces. Gliclazide may have increased effects when taken with other antidiabetic drugs, beta-blockers, ACE inhibitors, and NSAIDs, while its effect may be reduced with danazol.
Gliclazide is an oral hypoglycemic drug used to treat type 2 diabetes. It works by binding to receptors on pancreatic beta cells, blocking potassium channels and stimulating the release of insulin. It is well absorbed orally but exhibits inter-individual variability, extensively metabolized in the liver, and primarily eliminated through urine and feces. Gliclazide may have increased effects when taken with other antidiabetic drugs, beta-blockers, ACE inhibitors, and NSAIDs, while its effect may be reduced with danazol.
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Gliclazide
GENERAL DRUG CLASSIFICATION: CNS-Neurogenerative disease drugs-Cholinesterase inhibitor
CHEMICAL NAME: 1-(4-methylbenzenesulfonyl)-3-{octahydrocyclopenta[c]pyrrol-2-yl}urea [1]
GENERIC NAME: Gliclazide[1]
BRAND NAME: Azukon MR [2] INDICATIONS: For the treatment of NIDDM in conjunction with diet and exercise. (2) PHARMACOKINETICS: 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. [1]
Distribution: plasma protein binding approximately 94-95 %. [2]
Metabolism: 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. [1]
Excretion: Metabolites and conjugates are eliminated primarily by the
kidneys (60-70%) and also in the feces (10-20%).[1] PHARMACODYNAMICS: 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 resulting in calmodulin activation, which in turn leads to exocytosis of insulin containing secretorty granules. [1] DRUG INTERACTIONS: May increase hypoglycaemic effect w/ phenylbutazone. [2]
Potentiation of blood glucose lowering effect w/ other antidiabetics
(e.g. acarbose, insulins, metformin), β-blockers, ACE inhibitors, H 2- receptor antagonists, MAOIs, sulfonamides, clarithromycin and NSAIDs. [2]
Chlorpromazine, glucocorticoids, ritodrine, salbutamol may cause
increases in blood glucose levels. [2]
Terbutaline may cause increases in blood glucose levels. [2]
May diminish hypoglycaemic effect w/ danazol. May increase
anticoagulant effect of warfarin. [2] LABORATORY INTERFERENCES: No data available [1] REFERENCES: Gliclazide - DrugBank. Drugbank.ca. https://www.drugbank.ca/drugs/DB01120. Published 2018. Accessed November 24, 2018. [2] Gliclazide: Indication, Dosage, Side Effect, Precaution | MIMS.com Philippines. Mims.com. https://www.mims.com/philippines/drug/info/gliclazide?mtype=generic. Published 2018. Accessed 2018.
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