Saxagliptin
Indications
Saxagliptin is used for:
Type 2 diabetes
Adult Dose
Oral
Type 2 diabetes mellitus
Adult: 2.5 or 5 mg once daily.
Combination therapy: May need to reduce dosage of sulfonylurea or other insulin secretagogues when administered in combination
Coadministration with strong CYP450 3A4/5 inhibitors: Not to exceed 2.5 mg PO qDay
Elderly: No dosage adjustment.
Hepatic Impairment No dosage adjustment.
Child Dose
<18 years: Safety and efficacy not established
Renal Dose
Renal impairment
CrCl >50 mL/min: No dose adjustment required
CrCl <50 mL/min: Not to exceed 2.5 mg PO qDay
ESRD requiring hemodialysis: Not to exceed 2.5 mg PO qDay administered postdialysis
ESRD requiring peritoneal dialysis: Not studied
Administration
May be taken with or without food.
Contra Indications
Documented hypersensitivity (eg, anaphylaxis, angioedema, exfoliative skin conditions)
Precautions
Renal impairment
Decrease dose with strong CYP450 3A4/5 inhibitors
Coadministration with thiazolidinediones (eg, rosiglitazone, pioglitazone) increases risk for peripheral edema
Pancreatitis reported with saxagliptin; monitor for signs and symptoms and discontinue if pancreatitis suspected
Serious hypersensitivity reactions with saxagliptin reported (typically within the first 3 months of therapy)
History of angioedema
Coadministration with a sulfonylurea or with insulin may increase hypoglycemia; monitor closely and adjust sulfonylurea and/or insulin dose accordingly
Congestive heart failure (CHF) risks. Observe patients for signs and symptoms of heart failure during therapy;
Lactation: Not known whether distributed in breast milk; caution advised
Pregnancy-Lactation
Interactions
Strong CYP3A4/5 inhibitors (eg ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir & telithromycin).
Adverse Effects
Side effects of Saxagliptin :
1-10% (selected)
Urinary tract infection (7%),Headache (7%),Hypersensitivity-related events (<4%; eg, urticaria, facial edema),Peripheral edema (<4%; increased incidence when coadministered with thiazolidinediones),Upper respiratory tract infection (3%),Gastroenteritis (2%),Hypoglycemia (1.6%)
Frequency Not Defined
Increased creatinine phosphokinase,Increased creatinine,Idiopathic thrombocytopenic purpura rash
Mechanism of Action
Dipeptidyl peptidase IV (DPP-4) inhibition that results in increased incretin hormones and enhanced glycemic control.