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Gliclazide

Generic Name
Gliclazide
Brand Names
Diamicron
Drug Type
Small Molecule
Chemical Formula
C15H21N3O3S
CAS Number
21187-98-4
Unique Ingredient Identifier
G4PX8C4HKV

Overview

Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It has been classified differently according to its drug properties in which based on its chemical structure, gliclazide is considered a first-generation sulfonylurea due to the structural presence of a sulfonamide group able to release a proton and the presence of one aromatic group. On the other hand, based on the pharmacological efficacy, gliclazide is considered a second-generation sulfonylurea which presents a higher potency and a shorter half-life. Gliclazide belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%).

Background

Gliclazide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It has been classified differently according to its drug properties in which based on its chemical structure, gliclazide is considered a first-generation sulfonylurea due to the structural presence of a sulfonamide group able to release a proton and the presence of one aromatic group. On the other hand, based on the pharmacological efficacy, gliclazide is considered a second-generation sulfonylurea which presents a higher potency and a shorter half-life. Gliclazide belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Gliclazide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Gliclazide is extensively metabolized by the liver; its metabolites are excreted in both urine (60-70%) and feces (10-20%).

Indication

For the treatment of NIDDM in conjunction with diet and exercise.

Associated Conditions

  • Type 2 Diabetes Mellitus

FDA Approved Products

No FDA products found for this drug

Singapore Approved Products

DIAPRO TABLET 80 mg
Manufacturer:BEXIMCO PHARMACEUTICALS LTD
Form:TABLET
Strength:80 mg
Online:Yes
Approved: 2005/04/12
Approval:SIN13085P
DIANORM TABLET 80 mg
Manufacturer:MICRO LABS LTD
Form:TABLET
Strength:80 mg
Online:Yes
Approved: 1998/10/02
Approval:SIN10123P
DIAMICRON MR TABLET 60mg
Manufacturer:LES LABORATOIRES SERVIER INDUSTRIE, SERVIER (IRELAND) INDUSTRIES LTD, Kotra Pharma (M) Sdn Bhd
Form:TABLET, FILM COATED, EXTENDED RELEASE
Strength:60mg
Online:Yes
Approved: 2010/09/22
Approval:SIN13868P
DIAMICRON TABLET 80 mg
Manufacturer:LES LABORATOIRES SERVIER INDUSTRIE
Form:TABLET
Strength:80 mg
Online:Yes
Approved: 1990/04/20
Approval:SIN04316P
DIAMICRON MR TABLET 30 mg
Manufacturer:LES LABORATOIRES SERVIER INDUSTRIE
Form:TABLET
Strength:30 mg
Online:Yes
Approved: 2002/01/10
Approval:SIN11761P

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