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Glimepiride

Generic Name
Glimepiride
Brand Names
Duetact, Tandemact
Drug Type
Small Molecule
Chemical Formula
C24H34N4O5S
CAS Number
93479-97-1
Unique Ingredient Identifier
6KY687524K

Overview

First introduced in 1995, glimepiride is a member of the second-generation sulfonylurea (SU) drug class used for the management of type 2 diabetes mellitus (T2DM) to improve glycemic control. Type 2 diabetes is a metabolic disorder with increasing prevalences worldwide; it is characterized by insulin resistance in accordance with progressive β cell failure and long-term microvascular and macrovascular complications that lead to co-morbidities and mortalities. Sulfonylureas are one of the insulin secretagogues widely used for the management of type 2 diabetes to lower blood glucose levels. The main effect of SUs is thought to be effective when residual pancreatic β-cells are present, as they work by stimulating the release of insulin from the pancreatic beta cells and they are also thought to exert extra-pancreatic effects, such as increasing the insulin-mediated peripheral glucose uptake. Glimepiride works by stimulating the secretion of insulin granules from pancreatic islet beta cells by blocking ATP-sensitive potassium channels (K channels) and causing depolarization of the beta cells. Compared to glipizide, another second SU drug, glimepiride has a longer duration of action. It is sometimes classified as a third-generation SU because it has larger substitutions than other second-generation SUs. Compared to other SUs, glimepiride was associated with a lower risk of developing hypoglycemia and weight gain in clinical trials as well as fewer cardiovascular effects than other SUs due to minimal effects on ischemic preconditioning of cardiac myocytes. It is effective in reducing fasting plasma glucose, postprandial glucose, and glycosylated hemoglobin levels and is considered to be a useful, cost-effective treatment option for managing type 2 diabetes mellitus. Glimepiride was approved by the Food and Drug Administration (FDA) in the United States in 1995 for the treatment of T2DM. It is commonly marketed under the brand name Amaryl as oral tablets and is typically administered once daily.

Background

First introduced in 1995, glimepiride is a member of the second-generation sulfonylurea (SU) drug class used for the management of type 2 diabetes mellitus (T2DM) to improve glycemic control. Type 2 diabetes is a metabolic disorder with increasing prevalences worldwide; it is characterized by insulin resistance in accordance with progressive β cell failure and long-term microvascular and macrovascular complications that lead to co-morbidities and mortalities. Sulfonylureas are one of the insulin secretagogues widely used for the management of type 2 diabetes to lower blood glucose levels. The main effect of SUs is thought to be effective when residual pancreatic β-cells are present, as they work by stimulating the release of insulin from the pancreatic beta cells and they are also thought to exert extra-pancreatic effects, such as increasing the insulin-mediated peripheral glucose uptake. Glimepiride works by stimulating the secretion of insulin granules from pancreatic islet beta cells by blocking ATP-sensitive potassium channels (K channels) and causing depolarization of the beta cells. Compared to glipizide, another second SU drug, glimepiride has a longer duration of action. It is sometimes classified as a third-generation SU because it has larger substitutions than other second-generation SUs. Compared to other SUs, glimepiride was associated with a lower risk of developing hypoglycemia and weight gain in clinical trials as well as fewer cardiovascular effects than other SUs due to minimal effects on ischemic preconditioning of cardiac myocytes. It is effective in reducing fasting plasma glucose, postprandial glucose, and glycosylated hemoglobin levels and is considered to be a useful, cost-effective treatment option for managing type 2 diabetes mellitus. Glimepiride was approved by the Food and Drug Administration (FDA) in the United States in 1995 for the treatment of T2DM. It is commonly marketed under the brand name Amaryl as oral tablets and is typically administered once daily.

Indication

Glimepiride is indicated for the management of type 2 diabetes in adults as an adjunct to diet and exercise to improve glycemic control as monotherapy. It may also be indicated for use in combination with metformin or insulin to lower blood glucose in patients with type 2 diabetes whose high blood sugar levels cannot be controlled by diet and exercise in conjunction with an oral hypoglycemic (a drug used to lower blood sugar levels) agent alone.

Associated Conditions

  • Type 2 Diabetes Mellitus

Clinical Trials

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Title
Posted
Study ID
Phase
Status
Sponsor
2012/01/25
Phase 2
Completed
2012/01/19
Phase 1
Completed
2012/01/18
Phase 2
Completed
2012/01/13
Phase 2
Completed
2012/01/12
Phase 4
Completed
2011/12/21
Phase 1
Completed
2011/12/19
Phase 3
Completed
2011/12/19
Phase 3
Completed
2011/11/29
Phase 3
Terminated
2011/11/23
Phase 3
Terminated

FDA Drug Approvals

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Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
NCS HealthCare of KY, Inc dba Vangard Labs
0615-8334
ORAL
4 mg in 1 1
4/30/2020
Takeda Pharmaceuticals America, Inc.
64764-302
ORAL
2 mg in 1 1
6/1/2020
REMEDYREPACK INC.
70518-3719
ORAL
1 mg in 1 1
3/28/2024
BluePoint Laboratories
68001-178
ORAL
2 mg in 1 1
2/21/2024
Bryant Ranch Prepack
71335-9657
ORAL
2 mg in 1 1
9/30/2018
Golden State Medical Supply, Inc.
60429-918
ORAL
1 mg in 1 1
2/21/2024
Carlsbad Technology, Inc.
61442-116
ORAL
2 mg in 1 1
10/27/2022
Micro Labs Limited
42571-103
ORAL
4 mg in 1 1
12/2/2021
Bryant Ranch Prepack
71335-1848
ORAL
1 mg in 1 1
1/16/2019
DIRECT RX
61919-250
ORAL
4 mg in 1 1
1/11/2023

EMA Drug Approvals

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HSA Drug Approvals

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NMPA Drug Approvals

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PPB Drug Approvals

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TGA Drug Approvals

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