Sitagliptin

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Information about Sitagliptin

Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other oral hypoglycemic agents.

Liver safety of Sitagliptin

Only rare isolated reports of liver injury due to sitagliptin have been published.

Mechanism of action of Sitagliptin

Sitagliptin (sit" a glip' tin) is an inhibitor of dipeptidyl peptidase-4, which is the major enzyme responsible for the degradation of glucagon-like peptide-1 (GLP-1), an important gastrointestinal hormone (incretin) that increases glucose dependent insulin secretion by the pancreas. By prolonging the effect of GLP-1, sitagliptin increases insulin levels and lowers blood glucose and helps in glycemic control in patients with type 2 diabetes. Sitagliptin

FDA approval information for Sitagliptin

Sitagliptin was approved for use in the United States in 2006 and was the first DPP-4 inhibitor introduced into clinical practice. The current indications are for management of glycemic control in type 2 diabetes used in combination with diet and exercise, with or without other oral hypoglycemic agents or insulin.

Dosage and administration for Sitagliptin

Sitagliptin is available in tablets of 25, 50 and 100 mg under the brand name Januvia and in fixed combinations with metformin under the name Janumet. The typical dose of sitagliptin in adults is 100 mg once daily.

Side effects of Sitagliptin

Adverse reactions to sitagliptin are not common, but may include headache, nausea, arthralgia and rash. Hypoglycemia is uncommon with sitagliptin alone (<1%), but occurs in higher rates when it is combined with other oral hypoglycemic agents. Sitagliptin has also been linked to rare instances of bullous pemphigoid and acute pancreatitis that can be severe and even fatal.

Antidiabetics

•  Alpha-Glucosidase Inhibitors
  • Acarbose
  • Miglitol
• Incretin-Based Drugs
  • Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
    • Alogliptin
    • Linagliptin
    • Saxagliptin
    • Sitagliptin
  • Glucagon-Like Peptide-1 (GLP-1) Analogues
    • Albiglutide
    • Dulaglutide
    • Exenatide
    • Liraglutide
    • Lixisenatide
•  Insulin
• Metformin
• Metiglinide Analogues
  • Nateglinide
  • Repaglinide
• Pramlintide
• Sodium Glucose Cotransporter-2 (SGLT-2) Inhibitors
  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin
• Sulfonylureas
  • First Generation Sulfonylureas
    • Acetohexamide
    • Chlorpropamide
    • Tolazamide
    • Tolbutamide
  • Second Generation Sulfonylureas
    • Gliclazide
    • Glimepiride
    • Glipizide
    • Glyburide (Glibenclamide)
• Thiazolidinediones
  • Pioglitazone
  • Rosiglitazone
  • Troglitazone

• Dailymed label info on Sitagliptin
• FDA Sitagliptin

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  Sitagliptin chemical structure
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  3D model of Sitagliptin