Silinor 25

Generic

Sitagliptin

 

Indications

Silinor is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. It is also indicated for use in combination with Metformin, Sulfonylurea or Thiazolidinediones when diet and exercise plus the single agent does not provide adequate glycemic control.

 

Pharmacology

Sitagliptin is a DPP4 inhibitor, which is thought to work in type 2 diabetes by slowing the inactivation of the hormone incretin. The concentration of active intact hormones is increased by sitagliptin, thereby increasing and prolonging the activity of these hormones. Stimulant hormones, including glucagon-like peptide1 (GLP1) and glucose-dependent non-gonadotropic polypeptide (GIP), are released from the gut throughout the day and levels increase in response to meals. These hormones are rapidly inactivated by the enzyme DPP4. Increasedtin is part of an 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 release from pancreatic beta cells via intracellular signaling pathways involving cyclic AMP. GLP1 also reduces glucagon secretion by the alpha cells of the pancreas, resulting in decreased hepatic glucose production. By increasing and prolonging the increase in activity, sitagliptin increases insulin release and decreases glucose-dependent circulating glucagon levels. Sitagliptin exhibits selectivity for DPP4 and does not inhibit the activity of DPP8 or DPP9 in vitro at concentrations close to those of 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

 

Interaction

Co-administration of Digoxin and Sitagliptin may slightly increase the mean peak drug concentration of Digoxin. But no dosage adjustment of Digoxin or Sitagliptin is recommended.

 

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 & Lactation

Pregnancy Category B. There are no adequate and well[1]controlled 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 & Warnings

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

Use in renal impairment: Dosage adjustment is recommended in patients with moderate or severe renal impairment and in patients with ESRD requiring hemodialysis or peritoneal dialysis.

Use with drugs known to cause hypoglycemia: When sitagliptin is used in combination, dose adjustment of the sulfonylurea or insulin may be necessary to reduce the risk of hypoglycemia.

Hypersensitivity Reactions: There have been post-marketing reports of serious hypersensitivity reactions in patients treated with sitagliptin. These reactions include anaphylaxis, angioedema, and exfoliative skin conditions, including StevensJohnson syndrome. If a hypersensitivity reaction is suspected, discontinue sitagliptin, investigate other potential causes of the phenomenon, and institute alternative therapy for diabetes.

 

Therapeutic Class

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

 

Storage Conditions

Store below 25°C in a dry place away from light. Keep the medicines in a safe place, out of the reach of children. Do not use later than the date of expiry. To be dispensed only on the prescription of a registered physician

 

Pharmaceutical Name

Healthcare Pharmaceuticals Ltd.