Pharmacologic class: Dipeptidyl peptidase-4 (DPP-4) inhibitor
Therapeutic class: Hypoglycemic
Pregnancy risk category B
Inhibits DPP-4 and slows inactivation of incretin hormones, thereby increasing blood concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus
Tablets: 2.5 mg, 5 mg
➣ Adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus
Adults: 2.5 to 5 mg P.O. daily
• Moderate, severe, or end-stage renal disease
• Concurrent use of strong CYP450 inhibitors
• History of serious hypersensitivity to drug (such as anaphylaxis, angioedema, or exfoliative skin conditions)
Use cautiously in:
• renal impairment, history of pancreatitis
• concurrent use of insulin secretagogues or strong CYP450 and CYP3A4/5 inhibitors
• pregnant or breastfeeding patients
• children (safety and efficacy not established).
• Assess renal function before starting therapy.
☞ Before starting drug, identify possible risk factors for pancreatitis, such as history of pancreatitis, alcoholism, gallstones, or hypertriglyceridemia.
• Administer without regard to meals.
• Be aware that drug shouldn't be used for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.
CNS: headache
EENT: sinusitis
GI: vomiting, abdominal pain, gastroenteritis, acute pancreatitis
GU: urinary tract infection
Metabolic: hypoglycemia
Respiratory: upper respiratory tract infection
Skin: urticaria, exfoliative skin conditions
Other: peripheral edema, facial edema, hypersensitivity (including anaphylaxis and angioedema)
Drug-drug. Insulin secretagogues (such as sulfonylureas): possible increased risk of hypoglycemia
Strong CYP3A4/5 inhibitors (such as atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin): significantly increased saxagliptin effect
Drug-diagnostic tests. Lymphocytes: decreased count
Drug-food. Any food: increased saxagliptin area under the curve
• Monitor blood glucose and hemoglobin A1C levels and renal function tests periodically during therapy.
• Monitor CBC with differential, particularly lymphocyte count, in patients with unusual or prolonged infection.
☞ Observe patient carefully for signs and symptoms of pancreatitis. If pancreatitis is suspected, promptly discontinue drug and initiate appropriate management.
• Tell patient to take drug with or without food. Tell patient not to split or cut tablet.
• Teach patient about signs and symptoms of hypoglycemia (blurred vision, confusion, tremor, diaphoresis, excessive hunger, drowsiness, increased heart rate) and how to treat it, especially if taking saxagliptin with other drugs that may cause hypoglycemia.
☞ Instruct patient to discontinue drug and immediately report signs and symptoms of hypersensitivity reaction (such as hives, rash, or swelling of face, lips, or throat) or pancreatitis (persistent severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting).
• Instruct patient to routinely monitor blood glucose level at home.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, and food mentioned above.