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ALIMENTARY TRACT AND METABOLISM › DRUGS USED IN DIABETES › BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS › Dipeptidyl peptidase 4 (DPP-4) inhibitors
sitagliptin
A10BH01
Forms & Strengths
- Oral tablet: 25 mg
- Oral tablet: 50 mg
- Oral tablet: 100 mg
Adult Dosing
- Type 2 diabetes mellitus: 100 mg orally once daily
- Renal impairment eGFR 30 to <45 mL/min/1.73m2: 50 mg orally once daily
- Renal impairment eGFR <30 mL/min/1.73m2: 25 mg orally once daily
Pediatric Dosing
- Type 2 diabetes mellitus (Children 10 years and older): 100 mg orally once daily
- Safety and efficacy not established in children under 10 years of age
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
Mechanism of Action
- Dipeptidyl peptidase-4 (DPP-4) inhibitor
- Inhibits degradation of incretin hormones GLP-1 and GIP
- Increases insulin synthesis and release in a glucose-dependent manner
- Decreases glucagon secretion and hepatic glucose production
Contraindications
- History of a serious hypersensitivity reaction to sitagliptin, such as anaphylaxis or angioedema
Adverse Reactions
- Nasopharyngitis
- Upper respiratory tract infection
- Headache
- Hypoglycemia (when used with insulin or secretagogues)
- Acute pancreatitis
- Severe and disabling arthralgia
- Hypersensitivity reactions including anaphylaxis, angioedema, and exfoliative skin conditions
Drug Interactions
- Insulin or insulin secretagogues (e.g., sulfonylureas): Increased risk of hypoglycemia, lower doses may be required
- Strong CYP3A4/5 inducers (theoretical minor effect, generally no dose adjustment required)
Curated Content: Needs Vetting Before Put to Clinical Use