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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

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

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 Inhibitors01:19

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: Sulfonylureas01:17

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),...
Oral Hypoglycemic Agents: Biguanides and Glitazones01:26

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...

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Related Experiment Videos

Saxagliptin.

Sohita Dhillon1, Juliane Weber

  • 1Adis, Auckland, New Zealand. demail@adis.co.nz

Drugs
|October 2, 2009
PubMed
Summary
This summary is machine-generated.

Saxagliptin, a dipeptidyl peptidase-4 inhibitor, effectively lowers blood sugar in type 2 diabetes. It shows significant improvements in glycosylated hemoglobin (HbA1c) levels when used alone or with other oral diabetes medications.

Related Experiment Videos

Area of Science:

  • Endocrinology
  • Pharmacology
  • Metabolic Diseases

Background:

  • Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor.
  • It enhances incretin hormone levels, improving glucose regulation.
  • DPP-4 inhibitors are a key class of oral antihyperglycemic agents.

Purpose of the Study:

  • To evaluate the efficacy and safety of saxagliptin in type 2 diabetes mellitus.
  • To assess saxagliptin as monotherapy and in combination with other oral agents.
  • To determine the impact on glycemic control, specifically HbA1c levels.

Main Methods:

  • 24-week clinical trials involving treatment-naive and treatment-experienced patients.
  • Monotherapy with saxagliptin (2.5 or 5 mg once daily).
  • Combination therapy with saxagliptin plus metformin, glyburide, or a thiazolidinedione.

Main Results:

  • Saxagliptin monotherapy significantly improved HbA1c compared to placebo in treatment-naive patients.
  • Combination therapy with saxagliptin and metformin showed significant HbA1c reduction versus monotherapy.
  • Adding saxagliptin to existing therapies significantly improved HbA1c in treatment-experienced patients.
  • Saxagliptin was generally well-tolerated with mild to moderate adverse events.
  • No increased cardiovascular event risk was observed.
  • Saxagliptin had a weight-neutral effect.

Conclusions:

  • Saxagliptin effectively improves glycemic control in type 2 diabetes.
  • It is a viable monotherapy and combination treatment option.
  • The drug is well-tolerated and has a neutral effect on body weight.