Saxagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Dipeptidyl Peptidase-4 (DPP-4) inhibitor
Saxagliptin is an orally-active inhibitor of the DPP4 enzyme. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus.
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.
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).
In a controlled clinical trial, once-daily, orally-administered Saxagliptin in healthy subjects at doses up to 400 mg daily for 2 weeks (80 times the MRHD) had no dose-related clinical adverse reactions and no clinically meaningful effect on QTc interval or heart rate. In the event of an overdose, appropriate supportive treatment should be initiated as dictated by the patient's clinical status. Saxagliptin and its active metabolite are removed by hemodialysis (23% of dose over 4 hours).
Store at (at 20-25°C). Protect from light and moisture. Keep out of the reach of the children.
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