SPECIFICATION
Requires Prescription (YES/NO)
Yes
Generics
Sitagliptin
Used For
Diabetes
How it works
Sitagliptin 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, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). 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 cyclicAMP. GLP1 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.
USAGE AND SAFETY
Dosage
Sitagliptin
Side Effects
Upper respiratory-tract infections, headache and nasopharyngitis.
Drug Interactions
Digoxin : Sitagliptin has a small effect on plasma digoxin concentrations. No dosage adjustment of digoxin is recommended. However, patients at risk of digoxin toxicity should be monitored for this when sitagliptin and digoxin are administered concomitantly.
Indication
Sitagliptin is indicated in patients with type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control as: - Monotherapy- Dual Therapy : In combination with metformin HCl or with a sulphonylurea or with a PPAR? agonist (i.e., thiazolidinediones) when the treatment with the single agent alone with diet and exercise does not provide adequate glycemic control.- Triple Therapy : In combination with metformin HCl and a sulphonylurea or with metformin HCl and a PPAR? (i.e., thiazolidinediones) when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control. - Combination with Insulin.
When not to Use
Sitagliptin is contraindicated in: - Patients with known hypersensitivity to sitagliptin or any of the components of the product. - Patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. - Children below 18 years of age.
PRECAUTIONS
Precaution
After initiation of sitagliptin, patients should be observed carefully for signs and symptoms of pancreatitis. If pancreatitis is suspected, sitagliptin should promptly be discontinued and appropriate management should be initiated.
WARNINGS
Warning 1
When sitagliptin is used in combination with a sulphonylurea or with insulin, medications known to cause hypoglycemia the incidence of hypoglycemia increases when used in combination with a sulphonylurea or with insulin. Therefore, a lower dose of sulphonylurea or insulin may be required to reduce the risk of hypoglycemia.
Warning 2
An association between dipeptidyl peptidase-4 (DPP-4) inhibitor treatment and heart failure has been observed in trials for two other members of the DPP-4 inhibitor class. Consider the risks and benefits of Sitagliptin prior to initiating treatment in patients at risk for heart failure, such as those with a prior history of heart failure and a history of renal impairment, and observe these patients for signs and symptoms of heart failure during therapy. Advise patients of the characteristic symptoms of heart failure and to immediately report such symptoms. If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation.
Warning 3
If a hypersensitivity reaction is suspected, discontinue this medicine, assess for other potential causes for the event, and institute alternative treatment for diabetes. Angioedema has also been reported with other DPP-4 inhibitors. Use caution in a patient with a history of angioedema with another DPP-4 inhibitor because it is unknown whether such patients will be predisposed to angioedema with sitagliptin.
ADDITIONAL INFORMATION
Pregnancy category
Always consult your physician before using any medicine.
Storage (YES/NO)
Store this medicine at room temperature, away from direct light and heat.
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