Saxagliptin Dosage & Rx Info | Uses, Side Effects

Saxagliptin Generic Name & Formulations

Legal Class

General Description

Saxagliptin 2.5mg, 5mg; tabs.

Pharmacological Class

Dipeptidyl peptidase-4 (DPP-4) inhibitor.

How Supplied

Contact supplier

Manufacturer

Various generic manufacturers

Mechanism of Action

Saxagliptin is a competitive DPP-4 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.

Saxagliptin Indications

Indications

Adjunct to diet and exercise to improve glycemic control in type 2 diabetes, as monotherapy or combination therapy.

Limitations of Use

Not for treatment of type 1 diabetes or diabetic ketoacidosis.

Saxagliptin Dosage and Administration

Adult

Swallow whole. 2.5mg or 5mg once daily. Moderate or severe renal impairment or ESRD requiring hemodialysis (eGFR <45mL/min/1.73m²), or concomitant strong CYP3A4/5 inhibitors: 2.5mg once daily. Give dose after hemodialysis session. Peritoneal dialysis: not studied.

Children

<18yrs: not established.

Saxagliptin Contraindications

Not Applicable

Saxagliptin Boxed Warnings

Not Applicable

Saxagliptin Warnings/Precautions

Warnings/Precautions

Assess renal function before starting therapy and periodically thereafter. Monitor for signs/symptoms of pancreatitis, serious hypersensitivity reactions, severe joint pain, or bullous pemphigoid; discontinue if suspected or occurs. Consider risks/benefits in patients with known risk factors for heart failure; monitor for signs/symptoms; evaluate and consider discontinuing if develops. History of angioedema to other DPP4 inhibitors. Pregnancy. Nursing mothers.

Saxagliptin Pharmacokinetics

Absorption

Median time to maximum concentration: 2 hours.

Metabolism

Hepatic (CYP3A4/5).

Elimination

Renal (75%), fecal (22%). Half-life: 2.5 hours. Average renal clearance: ~230 mL/min.

Saxagliptin Interactions

Interactions

Potentiated by strong CYP3A4/5 inhibitors (eg, ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin). May need lower dose of concomitant sulfonylurea or insulin to reduce risk of hypoglycemia.

Saxagliptin Adverse Reactions

Adverse Reactions

Upper respiratory tract infection, UTI, headache, peripheral edema (with thiazolidinediones); hypoglycemia (with sulfonylureas or insulin), hypersensitivity reactions (eg, anaphylaxis, angioedema, exfoliative skin conditions), pancreatitis, heart failure, severe and disabling arthralgia, bullous pemphigoid.

Saxagliptin Clinical Trials

See Literature

Saxagliptin Note

Notes

Formerly known under the brand name Onglyza.

Saxagliptin Patient Counseling