Sitagliptin (sitagliptin)
Also sold as: Januvia, Istavel, Zoryl-M (with metformin), Sitamet
Pregnancy
Cat B
Lactation
Unknown
Schedule
H
Forms
tablet 25mg +4
Indications
- Type 2 diabetes mellitus — as monotherapy (when metformin is not tolerated) or add-on to metformin, sulfonylurea, TZD, SGLT2 inhibitor, or insulin
- Type 2 diabetes in elderly patients (well-tolerated, low hypoglycemia risk, no titration required)
Adult Dosing
Type 2 diabetes mellitus (monotherapy or add-on)
100mg orally once daily
Once daily at any time of day, with or without food
No dose titration required. If combined with a sulfonylurea or insulin, consider reducing the dose of those agents to reduce hypoglycemia risk.
Pediatric Dosing
Safety and efficacy not established in paediatric populations.
Renal Dose Adjustment
| CrCl / eGFR | Dose Adjustment |
|---|---|
| CrCl ≥50 mL/min (eGFR ≥50) | 100mg once daily — no adjustment |
| CrCl 30–49 mL/min (eGFR 30–49) | 50mg once daily |
| CrCl <30 mL/min (eGFR <30) | 25mg once daily |
| ESRD (haemodialysis or peritoneal dialysis) | 25mg once daily (administered without regard to timing of dialysis session). Dose adjustment is essential — sitagliptin is renally cleared. |
Hepatic Adjustment
Mild-to-moderate hepatic impairment (Child-Pugh ≤9): no dose adjustment required. Severe hepatic impairment: limited clinical experience; use with caution.
Pregnancy & Lactation
Pregnancy: Category B
Animal studies show no teratogenicity. No adequate well-controlled studies in pregnant women. Use only if clearly needed; insulin remains preferred for T2DM management during pregnancy due to established safety profile.
Lactation: Unknown
Unknown whether sitagliptin is excreted in human breast milk. Excreted in rat milk. Caution advised; weigh risk-benefit. If breastfeeding, consider switching to insulin.
Top Drug Interactions
| Interacting Drug | Effect | Severity |
|---|---|---|
| Digoxin | Sitagliptin may slightly increase digoxin plasma exposure (AUC ~11%, Cmax ~18%). Monitor digoxin levels periodically in patients on concurrent therapy, especially at higher digoxin doses. | Minor |
| Insulin / Sulfonylureas | Additive insulin-secretory effect increases hypoglycemia risk. Reduce sulfonylurea dose (e.g., glimepiride, glibenclamide) when adding sitagliptin. Monitor blood glucose; adjust insulin dose if needed. | Moderate |
| Cyclosporine | Cyclosporine (P-gp inhibitor) increases sitagliptin Cmax by ~68% and AUC by ~29%. Monitor for sitagliptin-related adverse effects (GI, pancreatitis). | Moderate |
| Rifampicin | Rifampicin (P-gp and CYP inducer) slightly reduces sitagliptin AUC. Clinical significance is minor; no dose adjustment generally required. | Minor |
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Side Effects
Common
- Nasopharyngitis (upper respiratory tract infection — most common adverse effect)
- Headache
- Nausea (mild)
- Constipation
- Hypoglycemia (when combined with sulfonylurea or insulin)
- Arthralgia (joint pain — reported with class effect)
Serious / Discontinue If
- Acute pancreatitis — FDA class warning for all DPP-4 inhibitors; rare but reported. Stop immediately if suspected (severe abdominal pain, persistent vomiting). Do not restart after confirmed pancreatitis.
- Severe and disabling arthralgia (joint pain) — FDA safety communication 2015; may occur months to years after starting. Resolves on discontinuation.
- Serious hypersensitivity reactions (anaphylaxis, angioedema, Stevens-Johnson syndrome) — rare; discontinue and treat
- Bullous pemphigoid — rare skin blistering disorder reported with DPP-4 inhibitors; stop drug if diagnosed
- Acute kidney injury — rare; reported with class. Monitor renal function especially at dose initiation.
- Heart failure hospitalization — EXAMINE trial showed no benefit or harm vs placebo in T2DM with recent ACS; monitor for HF symptoms
Contraindications
- History of serious hypersensitivity reaction to sitagliptin (anaphylaxis, angioedema, severe skin reactions)
- Type 1 diabetes mellitus
- History of pancreatitis (relative contraindication — use with caution; some guidelines avoid)
- eGFR <30 without dose reduction (use 25mg OD if <30 or on dialysis)
Available Indian Brands
| Brand | Manufacturer | Price (approx) |
|---|---|---|
| Januvia 100mg | MSD (Merck Sharp & Dohme) | ₹185/14 tab |
| Istavel 100mg | Sun Pharma | ₹145/14 tab |
| Sitamet 50/500 | Cipla | ₹125/10 tab (with metformin 500mg) |
Monitoring Required
- HbA1c every 3 months until goal, then every 6 months
- Renal function (eGFR/serum creatinine) at baseline and at least annually — dose adjustment required for CrCl <50
- Blood glucose monitoring (especially if on concurrent sulfonylurea or insulin)
- Lipase and amylase if abdominal pain occurs (pancreatitis screening)
- Skin examination — report new blisters or skin erosions (bullous pemphigoid)
- Joint pain assessment at each visit (severe arthralgia is a class effect)
- Signs of hypersensitivity reactions (rash, urticaria, facial swelling)
- Body weight (DPP-4 inhibitors are weight-neutral — no expected weight change)
Patient Counseling Points
- Take sitagliptin once daily at any convenient time — morning, afternoon, or evening. It can be taken with or without food.
- No dose adjustment or titration needed — this is a "set it and forget it" medicine for daily diabetes control.
- This medicine rarely causes low blood sugar on its own. However, if you are also taking a sulfonylurea (like glimepiride or glibenclamide) or insulin, you may have hypoglycemia — know the symptoms (sweating, shaking, confusion, fast heartbeat) and how to treat it.
- ALERT: Stop the medicine and go to the emergency room if you develop severe, persistent abdominal pain — this could be pancreatitis.
- Report any new joint pain that is severe or disabling — this medicine can rarely cause serious joint pain that goes away when the medicine is stopped.
- Report any new skin blisters or erosions to your doctor (rare bullous pemphigoid).
- This medicine is weight-neutral — do not expect it to cause weight loss (unlike GLP-1 agonists) or weight gain (unlike sulfonylureas/insulin).
- If your kidney function changes (new diagnosis of CKD, or worsening of existing kidney disease), inform your doctor — the dose may need adjustment.
- If you develop any allergic reactions (swelling of face, lips, or throat; difficulty breathing; hives) — stop immediately and seek emergency care.
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Clinically reviewed by: Dr. Priya Menon, MD, DM Endocrinology, AIIMS New Delhi
Last reviewed: 2026-04-01
References
- White WB, et al. Alogliptin after Acute Coronary Syndrome in Patients with Type 2 Diabetes (EXAMINE — DPP-4 class reference). NEJM. 2013.
- MSD. Januvia (sitagliptin) Prescribing Information. 2024.
- FDA Drug Safety Communication: DPP-4 inhibitors may cause severe joint pain. August 2015.
- CDSCO. Sitagliptin Approval and Prescribing Guidelines. India.