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ALIMENTARY TRACT AND METABOLISM › DRUGS USED IN DIABETES › BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS › Combinations of oral blood glucose lowering drugs
sitagliptin and dapagliflozin
A10BD29
Forms & Strengths
- Fixed-dose combination tablet: 100 mg sitagliptin / 5 mg dapagliflozin
- Fixed-dose combination tablet: 100 mg sitagliptin / 10 mg dapagliflozin
Adult Dosing
- One tablet (100 mg sitagliptin / 10 mg dapagliflozin or 100 mg sitagliptin / 5 mg dapagliflozin) orally once daily in the morning with or without food
- Assess renal function prior to initiation and periodically thereafter; avoid use if eGFR is persistently <45 mL/min/1.73 m²
Pediatric Dosing
- Safety and efficacy in pediatric patients (<18 years of age) have not been established
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both sitagliptin and dapagliflozin is appropriate
Mechanism of Action
- Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that slows the inactivation of incretin hormones, increasing insulin release and decreasing glucagon levels in a glucose-dependent manner
- Dapagliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor that blocks renal glucose reabsorption, increasing urinary glucose excretion and osmotic diuresis
Contraindications
- History of a serious hypersensitivity reaction to sitagliptin or dapagliflozin (e.g., anaphylaxis, angioedema)
- Severe renal impairment (eGFR <30 mL/min/1.73 m²), end-stage renal disease, or patients on dialysis
- History of diabetic ketoacidosis
Adverse Reactions
- Upper respiratory tract infection
- Nasopharyngitis
- Hypoglycemia (especially when combined with insulin or secretagogues)
- Urinary tract infections and genital mycotic infections
- Volume depletion, hypotension, and dizziness
- Acute kidney injury
- Severe and disabling arthralgia
- Acute pancreatitis
- Hypersensitivity reactions including anaphylaxis, angioedema, and severe cutaneous adverse reactions
- Fournier's gangrene
Drug Interactions
- Insulin or insulin secretagogues (e.g., sulfonylureas): Increased risk of hypoglycemia; dose reduction of insulin or secretagogue may be required
- Diuretics: Dapagliflozin may additive-enhance diuretic effects, increasing the risk of hypovolemia and hypotension
- Strong CYP enzyme inducers (e.g., rifampin): May decrease exposure of dapagliflozin
- Lithium: SGLT2 inhibitors may increase renal lithium clearance, leading to decreased serum lithium concentrations
Curated Content: Needs Vetting Before Put to Clinical Use