Dosing & Uses
Dosage Forms & Strengths
tablet
- 25mg
- 50mg
- 100mg
Type 2 Diabetes Mellitus
Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (T2DM)
100 mg PO qDay
Dosage Modifications
Renal impairment
- eGFR ≥45 to <90 mL/min/1.73 m2: No dosage adjustment necessary
- eGFR 30 to <45 mL/min/1.73 m2: 50 mg PO qDay
- eGFR <30 mL/min/1.73 m2: 25 mg PO qDay
- End-stage renal disease requiring hemodialysis or peritoneal dialysis: 25 mg PO qDay regardless of timing of dialysis
Hepatic impairment
- Mild to moderate impairment: Dose adjustment not necessary
- Severe impairment: Not studied
Dosing Considerations
Limitations of use
- Should not be used in patients with type 1 diabetes
- Not studied in patients with a history of pancreatitis; unknown whether these patients are at increased risk for development of pancreatitis while using sitagliptin
Safety and efficacy not established
Three double-blind, placebo-controlled studies evaluated the efficacy and safety of sitagliptin in patients (n=410) aged 10-17 years with uncontrolled T2DM, with or without insulin therapy; results showed effects of patients treated with sitagliptin were not significantly different from placebo
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Combination with insulin with or without metformin
- Hypoglycemia (15.5%)
Combination with glimepiride with or without metformin
- Hypoglycemia (12.2%)
1-10%
Monotherapy
- Nasopharyngitis (5.2%)
- Upper respiratory tract infection (4.5%)
- Headache (1.1%)
Combination with pioglitazone
- Upper respiratory tract infection (6.3%)
- Headache (5.1%)
Combination with metformin
- Nasopharyngitis (6.2%)
- Upper respiratory tract infection (5.9%)
Combination with metformin and rosiglitazone
- Nasopharyngitis (6.1%)
- Upper respiratory tract infection (5.5%)
Combination with glimepiride with or without metformin
- Nasopharyngitis (6.3%)
- Upper respiratory tract infection (5.9%)
Postmarketing Reports
Hypersensitivity reactions including anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions including Stevens-Johnson syndrome
Hepatic enzyme elevations; acute pancreatitis, including fatal and nonfatal hemorrhagic and necrotizing pancreatitis
Worsening renal function, including acute renal failure (sometimes requiring dialysis)
Severe and disabling arthralgia
Constipation, vomiting
Headache, myalgia, pain in extremity, back pain
Rhabdomyolysis
Pruritus
Bullous pemphigoid
Mouth ulceration; stomatitis
Warnings
Contraindications
Serious hypersensitivity to sitagliptin (eg, anaphylaxis, angioedema)
Cautions
Acute pancreatitis reported, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis; if pancreatitis suspected, discontinue promptly
Acute renal failure reported, sometimes requiring dialysis; assess renal function before initiation and periodically thereafter
Serious allergic and hypersensitivity reactions (eg, anaphylaxis, angioedema, exfoliative skin conditions including Stevens-Johnson syndrome) reported; promptly stop treatment and assess for other potential causes; appropriately monitor and treat
Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate
Heart failure observed with other DPP-4 inhibitors; consider risks and benefits in patients with risk factors for heart failure; monitor for signs and symptoms; if heart failure develops, manage accordingly to standard of care and consider interrupting treatment
Bullous pemphigoid reported with DPP-4 inhibitor use, which required hospitalization; in reported cases, patients recovered with topical or systemic immunosuppressive treatment and discontinuation of DPP-4 inhibitor; advise to report any developing blisters/erosions; discontinue DPP-4 therapy and consult a dermatologist if bullous pemphigoid suspected
Drug interaction overview
- Sitagliptin is a P-gp and organic anion transporter-3 substrate; weak CYP3A4 and CYP2C8 substrates
-
Insulin or insulin secretagogues
- Increased risk of hypoglycemia when concomitantly used with insulin and/or an insulin secretagogue; consider lowering dose of insulin or insulin secretagogue
Pregnancy & Lactation
Pregnancy
Limited available data in pregnant females are not sufficient to inform a drug-associated risk for major birth defects and miscarriage
Pregnancy registry
- Monitors pregnancy outcomes in females exposed to drug during pregnancy
- Encourage patients to report any prenatal exposure to drug by calling 1-800-986-8999
Animal data
- No adverse developmental effects were observed when administered to pregnant rats and rabbits during organogenesis at oral doses up to 30x and 20x, respectively, the 100-mg clinical dose, based on AUC
Clinical considerations
- Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, still birth, and delivery complications
- Poorly controlled diabetes increases fetal risk for major birth defects, stillbirth, and macrosomia related morbidity
Lactation
There is no information regarding presence of drug in human milk, effects on breastfed infants, or on milk production
Present in rat milk and therefore possibly present in human
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Dipeptyl peptidase-IV (DPP-4) inhibitor; increases and prolongs incretin hormone activity, which is inactivated by DPP-4 enzyme
Incretins increase insulin release and synthesis from pancreatic beta cells and reduce glucagon secretion from pancreatic alpha cells
Absorption
Bioavailability: 87%
Peak plasma time: 1-4 hr
Peak plasma concentration: 950 nM (single oral 100-mg dose)
AUC: 8.52 microM·hr (single oral 100-mg dose)
Distribution
Protein bound: 38%
Vd: 198 L
Metabolism
Limited; primarily via CYP3A4 and CYP2C8
Elimination
Renal clearance: 350 mL/min
Half-life, terminal: 12.4 hr
Excretion: Urine (87% [79% unchanged]), feces (13%)
Administration
Oral Administration
Take with or without food
Swallow tablet whole; do not chew, crush, or split
Storage
Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)
Images
Patient Handout
Formulary
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