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Related Concept Videos

Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

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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...
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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.
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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...
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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...
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Oral Hypoglycemic Agents: Sulfonylureas01:17

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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...
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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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Sitagliptin for Type 2 diabetes: a 2015 update.

Maria Lee1, Mary K Rhee

  • 1Emory University School of Medicine, Medicine/Endocrinology, 1303 Woodruff Memorial Research Building,101 Woodruff Circle, Suite 1303, Atlanta, GA 30322, USA.

Expert Review of Cardiovascular Therapy
|May 23, 2015
PubMed
Summary

Sitagliptin, a DPP-4 inhibitor, effectively treats type 2 diabetes with a low hypoglycemia risk and neutral weight effect. It is suitable for patients with chronic kidney disease, offering a well-tolerated therapeutic option.

Keywords:
Type 2 diabetesdiabetes mellitusdipeptidyl peptidase 4 inhibitorincretin-based therapysitagliptin

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Area of Science:

  • Pharmacology and Endocrinology
  • Metabolic Diseases

Background:

  • Sitagliptin, a dipeptidyl peptidase 4 (DPP-4) inhibitor, was the first in its class approved by the US FDA in 2006 for type 2 diabetes mellitus.
  • It has demonstrated favorable characteristics as an antidiabetic agent in numerous clinical trials.

Purpose of the Study:

  • To provide an up-to-date discussion on sitagliptin.
  • To cover its pharmacokinetics/pharmacodynamics, clinical efficacy, safety, and tolerability.

Main Methods:

  • Review of clinical trials and scientific literature on sitagliptin.
  • Analysis of pharmacokinetic and pharmacodynamic data.
  • Evaluation of safety and tolerability profiles.

Main Results:

  • Sitagliptin exhibits a low risk of hypoglycemia.
  • It has a neutral effect on body weight.
  • The drug is a viable option for patients with chronic kidney disease.

Conclusions:

  • Sitagliptin is a well-established and effective treatment for type 2 diabetes mellitus.
  • Its pharmacokinetic and pharmacodynamic properties support its clinical efficacy and favorable safety profile.
  • Sitagliptin offers a valuable therapeutic option with good tolerability and specific advantages for certain patient populations.