Saxagliptin

Saxagliptin is a prescription drug and should be used under medical supervision. In trials the common adverse effects were headache, nasopharyngitis, and upper-respiratory and urinary-tract infections; it is generally weight-neutral with low hypoglycemia risk on its own, though that risk rises when combined with sulfonylureas or insulin ^[4][5]. The SAVOR-TIMI 53 cardiovascular outcome trial found an increased rate of hospitalization for heart failure, a notable class-relevant signal ^[1]. Dose reduction is advised in significant kidney impairment and with strong CYP3A4/5 inhibitors. Rare pancreatitis and joint-pain reports exist for the class. Not medical advice.

Saxagliptin is metabolized by CYP3A4 and CYP3A5 to an active metabolite, so inhibitors of those enzymes raise its exposure roughly two and a half fold. Ketoconazole is the studied example, and clarithromycin, itraconazole, ritonavir, atazanavir, nelfinavir, indinavir, telithromycin and nefazodone are expected to behave the same way; the prescribing information restricts the saxagliptin dose whenever a strong inhibitor is on board. Strong inducers such as rifampin cut exposure substantially and blunt the glucose lowering effect.

The frequent interaction is simpler. Saxagliptin rarely causes hypoglycemia on its own, but combined with insulin or a sulfonylurea it lowers glucose enough that hypoglycemia becomes common, and it is usually the secretagogue that gets adjusted.

DPP-4 inhibitors also slow the breakdown of bradykinin and substance P, so adding one to an ACE inhibitor raises the risk of angioedema; cases have been described with this class.

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