Uses of Sigtil: - Type 2 diabetes mellitus Type 2 diabetes mellitus Hypersensitivity reactions such as anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome can occur. Type 1 diabetes. Diabetic ketoacidosis.

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

The DPP-4 inhibitors are a class of agents that act as incretin enhancers. By inhibiting the DPP-4 enzyme, Sitagliptin increases the levels of two known active incretin hormones, 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. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. This mechanism is unlike the mechanism seen with sulfonylureas; sulfonylureas cause insulin release even when glucose levels are low, which can lead to sulfonylurea-induced hypoglycemia in patients with type ll diabetes and in normal subjects. Sitagliptin demonstrates high selectivity for DPP-4 and does not inhibit closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations.

How to use Sitagliptin: Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Sitagliptin may be taken with or without food, but it is better to take it at a fixed time. Administration: May be taken with or without food. Adult Dose: Oral Type 2 diabetes mellitus Adult: 100 mg once daily. Hepatic impairment Mild to moderate impairment: Dose adjustment not necessary Severe impairment: Not studied Child Dose: Safety and efficacy not established Renal Dose: Renal impairment CrCl >50 mL/min: Dose adjustment not necessary CrCl 30-50 mL/min: 50 mg PO qDay CrCl <30 mL/min: 25 mg PO qDay ESRD: 25 mg PO qDay regardless of hemodialysis

Increased risk of hypoglycaemia when used in combination w/ sulfonylureas or insulin.

Hypersensitivity reactions such as anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome can occur. Type 1 diabetes. Diabetic ketoacidosis.

Common - Headache - Hypoglycaemia (low blood sugar level) in combination with insulin or sulphonylurea - Upper respiratory tract infection - Nasopharyngitis (inflammation of the throat and nasal passages) 1-10% Nasopharyngitis (5%),Diarrhea (4%),Headache (3.6%),Constipation (3%),Peripheral edema (2%),Nausea (2%),Pharyngitis (1%),Osteoarthritis (1%),URI (1%) <1% Hypersensitivity reactions such as anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions (including Stevens-Johnson syndrome) Hepatic enzyme elevations,Acute pancreatitis, including fatal and nonfatal hemorrhagic and necrotizing pancreatitis.Constipation.Vomiting.Worsening renal function, including acute renal failure (sometimes requiring dialysis),Severe and disabling arthralgia,Myalgia,Pain in extremity,Back pain

Pregnancy: Pregnancy Category B. 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.Nursing Mothers: It is not known whether Sitagliptin is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Sitagliptin is administered to a nursing woman.

Precaution: Patient w/ type 1 diabetes, history of angioedema. Not intended for the treatment of diabetic ketoacidosis. Moderate and severe renal impairment. Pregnancy and lactation. Monitoring Parameters Monitor glycosylated Hb (HbA1c), serum glucose. Assess renal function prior to initiation of therapy and periodically thereafter. Lactation: Not known whether excreted in breast milk: use caution

During controlled clinical trials in healthy subjects, single doses of up to 800 mg Sitagliptin were administered. Maximal mean increases in QTc of 8.0 msec were observed in one study at a dose of 800 mg Sitagliptin, a mean effect that is not considered clinically important. There is no experience with doses above 800 mg in clinical studies. In Phase I multiple-dose studies, there were no dose-related clinical adverse reactions observed with Sitagliptin with doses of up to 600 mg per day for periods of up to 10 days and 400 mg per day for up to 28 days. In the event of an overdose, it is reasonable to employ the usual 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.

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

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV), resulting in prolonged active incretin levels. Incretin hormones increases insulin synthesis and release from pancreatic beta-cells and reduces glucagon secretion from pancreatic beta-cells. Reduced glucagon secretion leads to decreased hepatic glucose production.

Pregnancy Category B. Reproduction studies have been performed in rats and rabbits. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Sitagliptin is secreted in the milk of lactating rats at milk to plasma ratio of 4:1. It is not known whether sitagliptin is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when sitagliptin is administered to a nursing woman.