Saxagliptin

Generic Name

Saxagliptin

Other Names

• Onglyza

Drug Class

• Dipeptidyl peptidase-4 (DPP-4) inhibitor

Chemical Formula

C18H25N3O2

Molecular Weight

315.41 g/mol

Mechanism of Action

• Increases insulin secretion
• Decreases glucagon secretion

Indications

• Type 2 diabetes mellitus

Common Dosage Forms

• Tablet

Typical Dosage

• 2.5 mg or 5 mg once daily

Pediatric Dosage

• Not established

Geriatric Dosage

• Dose adjustment may be needed based on renal function

Side Effects

• Hypoglycemia
• Nasopharyngitis
• Upper respiratory tract infection
• Headache

Contraindications

• History of pancreatitis
• Severe renal impairment
• End-stage renal disease

Pregnancy Category

• Category B

Lactation Safety

• Not recommended

Drug Interactions

• CYP3A4 inhibitors and inducers
• Digoxin
• Insulin or insulin secretagogues

Overdose Symptoms

• Hypoglycemia

Antidote for Overdose

• Glucagon, intravenous dextrose

Storage Conditions

• Store at room temperature away from moisture and heat

Pharmacokinetics

• Absorption: Rapidly absorbed
• Distribution: Protein binding is approximately 99%
• Metabolism: Primarily metabolized by CYP3A4
• Excretion: Excreted in urine (75%) and feces (22%)

Precautions

• Monitor renal function periodically
• Avoid use in patients with heart failure

Warnings

• May increase the risk of heart failure exacerbation

Others

• May be taken with or without food