Januvia Indication:

For use as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Also for use in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin or a PPARγ agonist (e.g., thiazolidinediones) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.

Januvia Mechanism Of Action:

Januvia is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Januvia demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

Januvia Drug Interactions:

Not Available

Januvia Food Interactions:

Not Available

Januvia Generic Name:

Synonyms:

  • MK-0431
  • Sitagliptin phosphate
  • Sitagliptan

Drug Type:

Small Molecule; Approved

Absorption:

Rapidly absorbed following oral administration, with an absolute bioavailability of 87%.

Toxicity (Overdose):

Not Available

Protein Binding:

The fraction of sitagliptin reversibly bound to plasma proteins is low (38%).

Biotransformation:

Hepatic. In vitro studies indicated that the primary enzyme responsible for the limited metabolism of sitagliptin was CYP3A4, with contribution from CYP2C8.

Half Life:

12.4 hours

Dosage Forms of Januvia:

Tablet, film coated Oral

Chemical IUPAC Name:

(3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[3,4-c]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one

Organisms Affected:

Humans and other mammals

Januvia to general, pharmacology

General, pharmacology..
diabetes