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US Previously Marketed

2

US Approved Rx

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Primary Target

Sulfonylurea receptor 1, Kir6.2

3

K-ATP channels, Rattus norvegicus

2

Acyl coenzyme A:cholesterol acyltransferase

1

Cytochrome P450 2C9

1

Cytochrome P450 3A4

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Highest Phase

Approved

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Approval Year

1957

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1984

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Condition

Type 2 diabetes mellitus

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Treatment Modality

Primary

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CNS Activity

CNS Penetrant

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Originator

Upjohn

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Hoechst

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Chemical

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Code System

CAS

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ChEMBL

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DRUG BANK

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EPA CompTox

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EVMPD

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ATC Level 1

ALIMENTARY TRACT AND METABOLISM

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VARIOUS

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DRUGS USED IN DIABETES

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DIAGNOSTIC AGENTS

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ATC Level 3

BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS

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OTHER DIAGNOSTIC AGENTS

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ATC Level 4

Sulfonamides, urea derivatives

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Tests for diabetes

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Showing 1 - 3 of 3 results

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GLYBURIDE

SX6K58TVWC

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Status:

US Approved Rx (2002)

First approved in 1984

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Sulfonylurea receptor 1, Kir6.2

Sulfonylurea receptor 1

Cytochrome P450 2C9

Sulfonylurea receptor 2

Cytochrome P450 3A4

Acyl coenzyme A:cholesterol acyltransferase

Conditions:

Type 2 diabetes mellitus

Glyburide, a second-generation sulfonylurea antidiabetic agent, lowers blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administratio...

n in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glibenclamide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, glyburide produces a mild diuresis by enhancement of renal free water clearance. Glyburide is twice as potent as the related second-generation agent glipizide. Sulfonylureas such as glyburide bind to ATP-sensitive potassium channels on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin. Glyburide is indicated as an adjunct to diet to lower the blood glucose in patients with NIDDM whose hyperglycemia cannot be satisfactorily controlled by diet alone. Glyburide is available as a generic, is manufactured by many pharmaceutical companies and is sold in doses of 1.25, 2.5 and 5 mg under many brand names including Gliben-J, Daonil, Diabeta, Euglucon, Gilemal, Glidanil, Glybovin, Glynase, Maninil, Micronase and Semi-Daonil. It is also available in a fixed-dose combination drug with metformin that is sold under various trade names, e.g. Bagomet Plus, Benimet, Glibomet, Gluconorm, Glucored, Glucovance, Metglib and many others.

TOLBUTAMIDE

982XCM1FOI

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Status:

US Previously Marketed

First approved in 1957

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Sulfonylurea receptor 1, Kir6.2

K-ATP channels, Rattus norvegicus

Conditions:

Type 2 diabetes mellitus

Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secr...

etagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose.

TOLBUTAMIDE SODIUM

E830VC49W5

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Status:

US Previously Marketed

First approved in 1957

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Sulfonylurea receptor 1, Kir6.2

K-ATP channels, Rattus norvegicus

Conditions:

Type 2 diabetes mellitus

Tolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It is structurally similar to acetohexamide, chlorpropamide and tolazamide and belongs to the sulfonylurea class of insulin secr...

etagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas lower blood glucose in patients with NIDDM by directly stimulating the acute release of insulin from functioning beta cells of pancreatic islet tissue by an unknown process that involves a sulfonylurea receptor (receptor 1) on the beta cell. Sulfonylureas inhibit the ATP-potassium channels on the beta cell membrane and potassium efflux, which results in depolarization and calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis, an effect similar to that of glucose.

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