Monotherapy And Combination Therapy: Saxagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Limitation Of Use: Saxagliptin is not indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis, as it would not be effective in these settings.

Dipeptidyl Peptidase-4 (DPP-4) inhibitor

Saxagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels. It elevates the circulating levels of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) which stimulates insulin secretion in pancreatic β-cells in a glucose dependent manner. It improves glycaemic control by reducing fasting and postprandial plasma glucose concentration in patients w/ type 2 DM.

Recommended Dosage: The recommended dosage of Saxagliptin is 2.5 mg or 5 mg once daily taken regardless of meals. Saxagliptin tablets must not be split or cut.

Dosage In Patients With Renal Impairment: No dosage adjustment for Saxagliptin is recommended for patients with mild renal impairment (CrCl >50 mL/min).

The dosage of Saxagliptin is 2.5 mg once daily (regardless of meals) for patients with moderate or severe renal impairment, or with end-stage renal disease (ESRD) requiring hemodialysis (CrCl ≤ 50 mL/min). Saxagliptin should be administered following hemodialysis. Saxagliptin has not been studied in patients undergoing peritoneal dialysis.

Because the dosage of Saxagliptin should be limited to 2.5 mg based upon renal function, assessment of renal function is recommended prior to initiation of Saxagliptin and periodically thereafter. Renal function can be estimated from serum creatinine using the Cockcroft-Gault formula or Modification of Diet in Renal Disease formula.

Dosage Adjustment With Concomitant Use Of Strong CYP3A4/5 Inhibitors: The dosage of Saxagliptin is 2.5 mg once daily when coadministered with strong cytochrome P450 3A4/5 (CYP3A4/5) inhibitors (e.g., ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin)

Concomitant Use With An Insulin Secretagogue (e.g., Sulfonylurea) Or With Insulin When Saxagliptin is used in combination with an insulin secretagogue (e.g., sulfonylurea) or with insulin, a lower dose of the insulin secretagogue or insulin may be required to minimize the risk of hypoglycemia

May be taken with or without food.

Increased risk of hypoglycaemia with concomitant sulfonylureas, dose reduction may be necessary. Increased serum levels with CYP3A4/5 inhibitors (e.g. atazanavir, ketoconazole, nefazodone, ritonavir). Concomitant CYP3A4 inducers (e.g. carbamazepine, phenobarbital) may reduce the glycaemic lowering effect of saxagliptin.

Type 1 diabetes, diabetic ketoacidosis.

The following serious adverse reactions are described below or elsewhere in the prescribing information: Pancreatitis, Heart Failure, Hypoglycemia with Concomitant Use of Sulfonylurea or Insulin, Hypersensitivity Reactions, Severe and disabling arthralgia, Bullous pemphigoid

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Moderate and severe renal impairment. Pregnancy and lactation.

Mild Renal Impairment: No dosage adjustment needed.

Moderate to Severe including with ESRD requiring hemodialysis: 2.5 mg once daily.

Hepatic Impairment No dosage adjustment.

Store between 20-25° C.