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Glucagon-like Receptor Agonists01:24

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...
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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...
Oral Hypoglycemic Agents: Glinides01:06

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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 Inhibitors01:19

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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.
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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: Sulfonylureas01:17

Oral Hypoglycemic Agents: Sulfonylureas

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Incretin-based therapies.

Anthony H Stonehouse1, Tamara Darsow, David G Maggs

  • 1Amylin Pharmaceuticals, Inc., San Diego, California 92121, USA. anthony.stonehouse@gmail.com

Journal of Diabetes
|June 29, 2011
PubMed
Summary
This summary is machine-generated.

Incretin-based therapies, including DPP-4 inhibitors and GLP-1 receptor agonists, offer improved glycemic control and weight management for Type 2 diabetes (T2D). These treatments target the attenuated incretin effect observed in T2D, showing potential benefits beyond glucose regulation.

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Area of Science:

  • Endocrinology and Metabolism
  • Pharmacology

Background:

  • Incretin-based therapies, such as dipeptidyl peptidase-4 (DPP-4) inhibitors and glucagon-like peptide-1 (GLP-1) receptor agonists, are now integral to diabetes management.
  • The incretin effect, crucial for postprandial glucose homeostasis, is diminished in Type 2 diabetes (T2D).

Purpose of the Study:

  • To review the characteristics of current and emerging incretin-based therapies for T2D.
  • To highlight the role of these therapies in addressing weight and hypoglycemia concerns.

Main Methods:

  • Literature review and synthesis of existing research on incretin-based therapies.
  • Analysis of clinical guidelines and consensus algorithms for T2D management.

Main Results:

  • Incretin-based therapies effectively improve glycemic control and aid in body weight management in T2D patients.
  • These therapies address the pathophysiology of T2D by targeting the reduced incretin effect.
  • Emerging data suggest benefits for inflammation, cardiovascular health, and the central nervous system.

Conclusions:

  • Incretin-based therapies represent a significant advancement in T2D treatment, offering multifaceted benefits.
  • Future research should continue to explore the full therapeutic potential of these agents.