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Oral Hypoglycemic Agents: Glinides

Oral Hypoglycemic Agents: Glinides

Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively manages...

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are typically...

Oral Hypoglycemic Agents: Biguanides and Glitazones

Oral Hypoglycemic Agents: Biguanides and Glitazones

Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood glucose levels...

Oral Hypoglycemic Agents: Sulfonylureas

Oral Hypoglycemic Agents: Sulfonylureas

Sulfonylureas are oral hypoglycemic agents utilized in treating type 2 diabetes. They are characterized by their unique sulfonylurea chemical structure. The family of sulfonylureas is divided into generations. First-generation sulfonylureas, including tolbutamide (Orinase), chlorpropamide (Diabinese), and tolazamide (Tolinase), trigger insulin release from pancreatic β cells and enhance peripheral tissues' insulin sensitivity. The second-generation members, such as glipizide (Glucotrol),...

Glucagon-like Receptor Agonists

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...

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An In Ovo Model for Testing Insulin-mimetic Compounds

An In Ovo Model for Testing Insulin-mimetic Compounds

Published on: April 23, 2018

Antidiabetic agents: past, present and future.

Ahmed Mehanna¹

¹Department of Pharmaceutical Sciences School of Pharmacy, Boston MCPHS University (Formerly Massachusetts College of Pharmacy & Health Sciences) 179 Longwood Avenue, Boston, MA 02115, USA. ahmed.mehanna@mcphs.edu

Future Medicinal Chemistry

|March 19, 2013

Summary

This review categorizes antidiabetic drugs by development era, from early 20th-century medications to recent innovations. It also explores future targets for safer diabetes mellitus treatments.

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A Zebrafish Model of Diabetes Mellitus and Metabolic Memory

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A Zebrafish Model of Diabetes Mellitus and Metabolic Memory

A Zebrafish Model of Diabetes Mellitus and Metabolic Memory

Published on: February 28, 2013

Area of Science:

Pharmacology and Endocrinology
Drug Development
Metabolic Diseases

Background:

Diabetes mellitus treatment often necessitates pharmacological intervention.
Understanding the evolution of antidiabetic medications is crucial for current and future therapeutic strategies.

Observation:

Antidiabetic agents are classified into three parts based on their historical development.
Part I includes early 20th-century drugs like insulin, sulfonylureas, and biguanides.
Part II covers newer agents from the early 21st century, such as GLP-1 analogs and SGLT2 inhibitors.

Findings:

The review details the properties of established antidiabetic medications.
It highlights emerging drug classes including GLP-1 receptor agonists, DPP-IV inhibitors, amylin analogs, and SGLT2 inhibitors.
Potential targets for novel antidiabetic agents with improved safety profiles are identified.

Implications:

This classification aids in understanding the progression of diabetes pharmacotherapy.
Identifying new targets may lead to the development of more effective and safer treatments for diabetes mellitus.
The review provides a foundation for future research in antidiabetic drug discovery.