Generic

Sitagliptin

Indications

Monotherapy and combination therapy: Sitagliptin can be used as a supplement to diet and exercise to improve blood sugar control in adults with type 2 diabetes. Important limitation of
use: sitagliptin should not be used in patients with type 1 diabetes or in the treatment of diabetic ketoacidosis because it is not effective in these cases. Sitagliptin has not been studied in patients with a history of pancreatitis. It is not clear whether patients with a history of pancreatitis will increase the risk of pancreatitis when using sitagliptin.

Pharmacology

Sitagliptin is a DPP4 inhibitor that is believed to work in patients with type 2 diabetes by delaying the inactivation of incretin hormone. Sitagliptin increases the level of intact active hormones, thereby increasing and prolonging the effects of these hormones. Incretin hormones, including glucagon-like peptide 1 (GLP1) and glucose-dependent insulinotropic polypeptide (GIP), are released from the intestine throughout the day, and their levels increase with meals. These hormones are quickly inactivated by the DPP4 enzyme. Incretin is a part of the endogenous system involved in the physiological regulation of glucose homeostasis. When blood glucose levels are normal or elevated, GLP1 and GIP increase insulin synthesis and pancreatic β-cell release through intracellular signaling pathways involving cyclic AMP. GLP1 also reduces the secretion of glucagon from pancreatic alpha cells, resulting in a decrease in liver glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and reduces circulating glucagon levels in a glucose-dependent manner. Sitagliptin shows selectivity for DPP4 and does not inhibit the in vitro activity of DPP8 or DPP9 at concentrations close to the therapeutic dose.

Dosage & Administration

Take Silinor ® exactly as prescribed by physicians.

Usual dose:100 mg once daily by mouth with or without food.
● For patients with mild renal insufficiency (creatinine clearance, CrCl>–50ml/min), no dosage adjustment is required
● For patients with moderate renal insufficiency (CrCl > 30 to <50ml/min) the dose of Silinor is 50 mg once daily
● For patients with severe renal insufficiency (CrCl<–30 ml/min) or with End-Stage Renal Disease (ESRD) requiring hemodialysis or potential dialysis, the dose of Silinor is 25 mg once daily

Interactions

The effect of sitagliptin on other drugs: Sitagliptin did not significantly change the pharmacokinetics of metformin, glibenclamide, simvastatin, rosiglitazone, warfarin, or oral contraceptives.
Digoxin: Sitagliptin slightly increases mean digoxin concentration. However, it is not necessary to adjust the dose of either drug.

Contraindications

History of a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis or angioedema.

Side Effects

The most common adverse reactions are; upper respiratory tract infection, nasopharyngitis and headache.
Hypoglycemia may occur in patients treated with the combination of Sitagliptin and sulfonylurea and add-on to insulin.

Pregnancy

Pregnancy Category B. There are no adequate and wellcontrolled studies in pregnant women. Safety of Sitagliptin in pregnant women has not been established. Sitagliptin should be used during pregnancy only if the potential benefit justifies the potential risk of the fetus. It is unknown if Silinor is secreted in brest milk.

Precautions

If pancreatitis is suspected, sitagliptin should be discontinued immediately and appropriate treatment initiated.

for patients with renal impairment: Dosage adjustment is recommended for patients with moderate or severe renal impairment and ESRD patients requiring hemodialysis or peritoneal dialysis.
Used with drugs known to cause hypoglycaemia: When sitagliptin is used in combination therapy, the dose of sulfonylureas or insulin may need to be adjusted to reduce the risk of hypoglycaemia.
Hypersensitivity: There have been post-marketing reports of severe hypersensitivity in patients treated with sitagliptin. These reactions include allergic reactions, angioedema, and exfoliative skin diseases, including

Stevens-Johnson syndrome. If hypersensitivity is suspected, discontinue sitagliptin, evaluate other possible causes of the event, and develop an alternative treatment plan for diabetes.

Therapeutic Class

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Storage Conditions

Store at temperature not exceeding 30 ºC in a dry place. Protect from light.

Pharmaceutical Name

Healthcare Pharmaceuticals Ltd.