Sitagliptin Phosphate (10 brand names, 2 dosage forms, 2 routes)
Available dosage forms: TABLET, TABLET, EXTENDED RELEASE.
Routes of administration: ORAL, FILM COATED.
Brand Names
- JANUMET
- JANUMET XR
- JANUVIA
- JUVISYNC
- METFORMIN HYDROCHLORIDE AND SITAGLIPTIN PHOSPHATE
- SITAGLIPTIN
- SITAGLIPTIN AND METFORMIN HYDROCHLORIDE
- SITAGLIPTIN PHOSPHATE
- SITAGLIPTIN PHOSPHATE; METFORMIN HYDROCHLORIDE
- STEGLUJAN
Indications and Usage
Sitagliptin tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitations of Use Sitagliptin tablets should not be used in patients with type 1 diabetes. Sitagliptin tablets have not been studied in patients with a history of pancreatitis. It is unknown whether patients with a history of pancreatitis are at increased risk for the development of pancreatitis while using sitagliptin tablets. [See Warnings and Precautions (5.1).]
Contraindications
History of a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis or angioedema. [SeeWarnings and Precautions ( 5.5 ); Adverse Reactions (6.2).]
Adverse Reactions
The following adverse reactions are also discussed elsewhere in the labeling: •Pancreatitis [see Warnings and Precautions (5.1)] •Heart Failure [see Warnings and Precautions (5.2)] •Acute Renal Failure [see Warnings and Precautions (5.3)] •Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues [see Warnings and Precautions (5.4)] •Hypersensitivity Reactions [see Warnings and Precautions (5.5)] •Severe and Disabling Arthralgia [see Warnings and Precautions (5.6)] •Bullous Pemphigoid [see Warnings and Precautions (5.7)]
Mechanism of Action
Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus 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. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.
Overdosage
In the event of an overdose with sitagliptin, contact the Poison Control Center. In the event of an overdose, it is reasonable to employ supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy as dictated by the patient’s clinical status. Sitagliptin is modestly dialyzable. In clinical studies, approximately 13.5% of the dose was removed over a 3- to 4-hour hemodialysis session. Prolonged hemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialyzable by peritoneal dialysis.