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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...
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...
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: 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...
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),...

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Related Experiment Videos

Sitagliptin.

Katherine A Lyseng-Williamson1

  • 1Wolters Kluwer Health | Adis, Auckland, New Zealand, an editorial office of Wolters Kluwer Health, Conshohocken, Pennsylvania, USA. demail@adis.co.nz

Drugs
|March 14, 2007
PubMed
Summary

Sitagliptin, a DPP-4 inhibitor, effectively lowers blood sugar in type 2 diabetes patients. This oral medication demonstrated significant improvements in HbA1c levels and was well-tolerated, offering a safe treatment option.

Area of Science:

  • Endocrinology
  • Pharmacology
  • Metabolic Diseases

Background:

  • Type 2 diabetes mellitus (T2DM) is a global health concern requiring effective glycemic control.
  • Incretin hormones play a crucial role in glucose homeostasis.
  • Dipeptidyl peptidase-4 (DPP-4) inhibitors offer a therapeutic strategy for T2DM management.

Purpose of the Study:

  • To evaluate the efficacy and tolerability of sitagliptin, a DPP-4 inhibitor, in patients with T2DM.
  • To assess sitagliptin's impact on glycemic control, insulin response, and beta-cell function.
  • To compare sitagliptin's effects with placebo and other antihyperglycemic agents.

Main Methods:

  • Phase III clinical trials involving patients with T2DM.
  • Administration of sitagliptin (100 or 200 mg once daily) as monotherapy or combination therapy.

Related Experiment Videos

  • Assessment of glycosylated hemoglobin (HbA1c), insulin response, beta-cell function, and adverse events.

    • Main Results:

    • Sitagliptin significantly improved glycemic control (HbA1c) compared to placebo in monotherapy and as add-on therapy.
    • Add-on sitagliptin to metformin or pioglitazone showed greater HbA1c reduction than placebo.
    • Sitagliptin demonstrated a favorable safety profile, with similar adverse events and hypoglycemia incidence to placebo.

    Conclusions:

    • Sitagliptin is an effective and well-tolerated oral DPP-4 inhibitor for improving glycemic control in T2DM.
    • It offers significant benefits as both monotherapy and add-on therapy, with a neutral effect on body weight.
    • Sitagliptin represents a valuable therapeutic option for managing type 2 diabetes mellitus.