Schedule H

Oral

• Tablets: 25 mg, 50 mg, 100 mg

Note: Available as monotherapy and in fixed-dose combinations (FDCs) with metformin.

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Type 2 Diabetes Mellitus (T2DM) — Monotherapy

(When metformin is contraindicated or not tolerated)

Parameter Recommendation

Starting dose 100 mg once daily

Titration Not required

Usual maintenance dose 100 mg once daily

Maximum dose 100 mg once daily

Key Clinical Notes:

• Suitable for patients with mild hyperglycaemia, particularly elderly

• Weight-neutral with low hypoglycaemia risk

• Expected HbA1c reduction: 0.5–0.8%

1. Type 2 Diabetes Mellitus — Add-on to Metformin (Dual Therapy)

Parameter Recommendation

Starting dose 100 mg once daily

Titration Not required

Usual maintenance dose 100 mg once daily

Maximum dose 100 mg once daily

Key Clinical Notes:

• First-line add-on when metformin monotherapy inadequate

• Expected additional HbA1c reduction: 0.6–0.8%

• FDC with metformin available for improved compliance

1. Type 2 Diabetes Mellitus — Triple Therapy

(Add-on to metformin + sulfonylurea OR metformin + pioglitazone)

Parameter Recommendation

Starting dose 100 mg once daily

Titration Not required

Usual maintenance dose 100 mg once daily

Maximum dose 100 mg once daily

Key Clinical Notes:

• When combined with sulfonylurea, hypoglycaemia risk increases — consider reducing sulfonylurea dose

• Monitor glucose more frequently during initial combination period

1. Type 2 Diabetes Mellitus — Add-on to Insulin (± Metformin)

Parameter Recommendation

Starting dose 100 mg once daily

Titration Not required

Usual maintenance dose 100 mg once daily

Maximum dose 100 mg once daily

Key Clinical Notes:

• Consider reducing insulin dose by 10–20% to minimize hypoglycaemia risk

• Requires frequent glucose monitoring during initial weeks

Secondary Indications – Adults Only (Off-label)

Indication Dose Duration Notes

Suspected MODY-3 (HNF-1α mutation) 100 mg once daily Chronic OFF-LABEL; Specialist endocrinologist only; Based on Indian endocrinology practice in non-obese young diabetics with suspected monogenic diabetes

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Type 2 Diabetes Mellitus (Age ≥10 years)

Parameter Recommendation

Starting dose 50 mg once daily

Titration May increase to 100 mg once daily after 1–2 weeks if tolerated and glycaemic control inadequate

Usual maintenance dose 50–100 mg once daily

Maximum dose 100 mg once daily

Key Clinical Notes:

• Use only under paediatric endocrinologist supervision

• Indicated as add-on when metformin monotherapy insufficient

• Adjust dose based on renal function

Safety Monitoring:

• Renal function at baseline and periodically

• Blood glucose (fasting and postprandial)

• HbA1c every 3 months

• Growth parameters

• Signs of pancreatitis

Secondary Indications – Paediatric Doses (Off-label)

Not applicable — No established off-label paediatric indications.

Minimum age limit: Not recommended below 10 years of age due to lack of safety and efficacy data.

Additional Notes:

• Sitagliptin is minimally dialyzable; no supplemental dose required post-haemodialysis

• May be administered without regard to timing of dialysis

Impairment Level Recommendation

Mild (Child-Pugh A) No dose adjustment required

Moderate (Child-Pugh B) No dose adjustment required

Severe (Child-Pugh C) Use with caution; limited data available; not routinely recommended

• Type 1 Diabetes Mellitus

• Diabetic ketoacidosis

• Known hypersensitivity to sitagliptin or any DPP-4 inhibitor

• History of serious hypersensitivity reaction to sitagliptin (anaphylaxis, angioedema, Stevens-Johnson syndrome)

• History of pancreatitis (increased risk; monitor for symptoms; discontinue if suspected)

• Renal impairment (dose adjustment required based on eGFR)

• Concurrent use with sulfonylureas or insulin (increased hypoglycaemia risk — consider dose reduction of secretagogue/insulin)

• Elderly patients with reduced renal reserve (monitor renal function regularly)

• History of angioedema with ACE inhibitors (potential additive risk)

• Heart failure (cardiovascular safety established but monitor clinically)

Parameter Recommendation

Safety status Not recommended; insufficient human data

Preferred alternatives Insulin (standard of care for diabetes in pregnancy including GDM)

When it may be used Only if benefit clearly outweighs risk and insulin not feasible; specialist input required

Monitoring Maternal glucose levels; fetal growth assessment; amniotic fluid volume

Parameter Recommendation

Compatibility Not recommended; no human data on excretion in breast milk

Preferred alternatives Insulin; Metformin (compatible with breastfeeding)

Expected milk levels Unknown

Infant monitoring If used — monitor infant for feeding difficulties, weight gain, hypoglycaemia signs

Parameter Recommendation

Starting dose 25–50 mg once daily (if eGFR reduced); 100 mg if renal function normal

Titration Conservative; based on renal function and glycaemic response

Extra risks Hypoglycaemia (especially with sulfonylureas/insulin); renal accumulation; polypharmacy interactions; dehydration

Special considerations Assess renal function before initiation and periodically; preferred agent due to weight-neutral and low hypoglycaemia profile

Drug/Class Effect Management

Sulfonylureas (glimepiride, gliclazide) Increased risk of hypoglycaemia Reduce sulfonylurea dose when initiating sitagliptin

Insulin Increased risk of hypoglycaemia Consider reducing insulin dose by 10–20%

Digoxin May increase digoxin plasma levels (mechanism unclear) Monitor digoxin levels and clinical response; particularly at higher digoxin doses

Rifampicin CYP3A4 induction may reduce sitagliptin efficacy Monitor glycaemic control; alternative antidiabetic may be considered

Drug/Class Effect Management

ACE inhibitors (enalapril, ramipril) Additive risk of angioedema (rare) Monitor for angioedema signs; counsel patient

Loop/Thiazide diuretics May alter glucose tolerance Monitor glycaemic control

Corticosteroids (prednisolone, dexamethasone) Antagonize glucose control Adjust antidiabetic regimen; monitor glucose

Atypical antipsychotics (olanzapine, clozapine) Antagonize glucose control Monitor glucose; may need intensification of diabetes therapy

Beta-blockers May mask hypoglycaemia symptoms Counsel patient; monitor glucose

• Headache

• Nasopharyngitis

• Upper respiratory tract infections

• Nausea

• Flatulence

• Constipation

• Peripheral oedema (especially when combined with pioglitazone)

• Arthralgia

Adverse Effect Clinical Action

Acute pancreatitis Discontinue immediately; hospitalize; supportive management; do not rechallenge

Anaphylaxis / Angioedema Discontinue immediately; emergency management; contraindicated for future use

Stevens-Johnson syndrome / Toxic epidermal necrolysis Discontinue immediately; hospitalize; specialist dermatology referral

Bullous pemphigoid Discontinue; dermatology referral; more common in elderly

Severe arthralgia Consider discontinuation if severe and disabling; symptoms may resolve after stopping

Severe hypoglycaemia (with secretagogues/insulin) Treat hypoglycaemia; adjust concomitant drug doses

After initiation (4–12 weeks) Fasting and postprandial glucose; symptoms of pancreatitis; hypoglycaemia episodes

Long-term HbA1c every 3 months until stable, then every 6 months; annual eGFR; periodic LFTs; monitor for signs of hypersensitivity or pancreatitis

• Januvia® (MSD)

• Istavel® (Sun Pharma)

• Zita® (Glenmark)

• Sitafirst® (Mankind)

• Jalra® (Novartis) — Note: This is vildagliptin, not sitagliptin

FDCs Available:

• Janumet® (Sitagliptin + Metformin)

• Istamet® (Sitagliptin + Metformin)

• Zitamet® (Sitagliptin + Metformin)

• Under NLEM 2022: No (DPP-4 inhibitors excluded)

• NPPA price control: Not applicable

• Government supply: Limited; primarily available in private sector

• Renal dosing is critical: Always check eGFR before initiating and adjust dose accordingly — one of the few oral antidiabetics usable in CKD stages 4–5.

• Weight-neutral and low hypoglycaemia: Preferred in elderly and patients where weight gain or hypoglycaemia is a concern (when not combined with SU/insulin).

• Sulfonylurea dose reduction: When adding sitagliptin to sulfonylurea, preemptively reduce SU dose to prevent hypoglycaemia.

• Pancreatitis vigilance: Counsel patients to report persistent severe abdominal pain; discontinue if pancreatitis suspected.

• Not for Type 1 DM: Ineffective and contraindicated in Type 1 diabetes; do not use.

• Do not combine with GLP-1 agonists: Both act on incretin pathway; no additional benefit and increased cost.

sitagliptin; DPP-4 inhibitor; type 2 diabetes; T2DM; renal-adjusted; weight-neutral; elderly-safe; pancreatitis-risk; hypoglycaemia-low; NLEM-excluded

RxIndia v1.0 — 28 May 2025

• CDSCO Product Information – Sitagliptin

• Indian Pharmacopoeia / National Formulary of India (NFI)

• ICMR Guidelines for Management of Type 2 Diabetes (2018)

• API Textbook of Medicine, 11th Edition

• AIIMS Antidiabetic Protocol

• NLEM 2022 (excluded class)

• Manufacturer Product Inserts (MSD – Januvia®, Sun Pharma – Istavel®)

• Indian Endocrine Society Practice Guidelines