Dosing and uses of Januvia (sitagliptin)
Adult dosage forms and strengths
tablet
- 25mg
- 50mg
- 100mg
Diabetes Mellitus, Type 2
100 mg PO qDay
Dosing Modifications
Renal impairment
- CrCl >50 mL/min: Dose adjustment not necessary
- CrCl 30-50 mL/min: 50 mg PO qDay
- CrCl <30 mL/min: 25 mg PO qDay
- ESRD: 25 mg PO qDay regardless of hemodialysis
Hepatic impairment
- Mild to moderate impairment: Dose adjustment not necessary
- Severe impairment: Not studied
Pediatric dosage forms and strengths
Safety and efficacy not established
Januvia (sitagliptin) adverse (side) effects
1-10%
Nasopharyngitis (5%)
Diarrhea (4%)
Headache (3.6%)
Constipation (3%)
Peripheral edema (2%)
Nausea (2%)
Pharyngitis (1%)
Osteoarthritis (1%)
URI (1%)
<1%
Hypersensitivity reactions such as 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
Constipation
Vomiting
Worsening renal function, including acute renal failure (sometimes requiring dialysis)
Severe and disabling arthralgia
Myalgia
Pain in extremity
Back pain
Postmarketing Reports
Pruritus
Warnings
Contraindications
Documented hypersensitivity
Cautions
Use with caution in hepatic impairment, or heart failure (due to an elevated overall risk of acute HF in those patients taking any dipeptidyl peptidase4 inhibitor)
Use with caution in renal failure; worsening of renal failure, including acute renal failure reported
Not for use in diabetic ketoacidosis patients; not effective
Not for use in type 1 diabetes mellitus; not effective
Combo treatment studied only with metformin and thiazolidinediones, not with insulin or sulfonylureas
Caution when coadministering with strong CYP3A4/5 inhibitors (may require dose adjustment)
May cause acute pancreatitis, including hemorrhagic and necrotizing pancreatitis; unknown if patients with history of pancreatitis are at increased risk
Concomitant use of insulin with secretagogues may increase risk of hypoglycemia
Angioedema reported with other dipeptidyl peptidase-4 (DPP-4) inhibitors; caution with history of angioedema
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
Pregnancy and lactation
Pregnancy category: B
Lactation: Not known whether excreted in breast milk: use caution
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 of Januvia (sitagliptin)
Mechanism of action
DPP-4 inhibitor; therefore, 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
Distribution
Protein bound: 38%
Vd: 198 L
Metabolism
Limited; primarily via CYP3A4 and CYP2C8
Elimination
Half-life, terminal: 12.4 hr
Excretion: Urine (87%), feces (13%)
Administration
Instructions
Take with or without food
Swallow tablet whole; do not chew, crush, or split
