Drug reference

Sitagliptin

DPP-4 Inhibitor · Antidiabetic

Also known as Sitagliptin phosphate

START

100 mg PO once daily

TYPICAL MAX

100 mg/day

STOP IF

Pancreatitis history · severe renal impairment without dose-cut

WATCH

Pancreatitis signs · joint pain · bullous pemphigoid (rare)

CDSCO approvedSchedule HJan AushadhiNPPA price-controlledATC A10BH01

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · DPP-4 inhibition
PEAK: 2h · Cmax
t½: 12h · plasma t½
DURATION: 1d · once-daily dosing window

EXCRETION

79% renal unchanged · minimal CYP

route + CYP

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

Category B — insulin preferred

FDA category + note

Top interactionssee all 6 →

BexaroteneSevereDatabaseDDInter
GatifloxacinSevereDatabaseDDInter

Available in India

112 branded formulations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4), an enzyme that degrades incretin hormones like glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By preventing DPP-4 from breaking down incretins, sitagliptin increases their active levels, leading to enhanced glucose-dependent insulin secretion from pancreatic beta cells and reduced glucagon secretion from alpha cells, thereby lowering blood glucose concentrations.

Indications

Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (monotherapy)Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus in combination with metformin, sulfonylurea, thiazolidinedione, or insulin (combination therapy)Treatment of type 2 diabetestype 2 diabetes mellitus (adjunctive to metformin/SUs/pioglitazone or insulin)type 2 diabetes mellitus (monotherapy when metformin cannot be used)

Dosing

Adult: 100 mg orally once daily, regardless of food.
Pediatric: Not recommended for use in pediatric patients younger than 18 years due to insufficient data on safety and efficacy.
Renal adjustment: eGFR ">= 45 mL/min/1.73 m^2: 100 mg once daily; eGFR >= 30 to < 45 mL/min/1.73 m^2: 50 mg once daily; eGFR < 30 mL/min/1.73 m^2 (including ESRD requiring dialysis): 25 mg once daily. For patients on dialysis, sitagliptin may be administered without regard to the timing of dialysis.…
Max dose: 100 mg/day

Pharmacokinetics

Onset

Rapid

Peak effect

1 to 4 hours

Duration

Approximately 24 hours

Half-life

Approximately 12.4 hours

Bioavailability

Approximately 87%

Protein binding

Approximately 38%

Metabolism

Primarily via CYP3A4 and CYP2C8, but metabolism is limited. The major metabolites are minimally active and do not contribute significantly to the plasma DPP-4 inhibitory activity.

Excretion

Approximately 79% excreted unchanged in urine, with active tubular secretion contributing to renal excretion. A small portion is excreted in feces.

Contraindications

History of serious hypersensitivity reaction to sitagliptin (e.g., anaphylaxis, angioedema, exfoliative skin conditions)
Type 1 diabetes mellitus
Diabetic ketoacidosis

Side effects

Common

NasopharyngitisHeadacheUpper respiratory tract infectionDiarrheaNauseaConstipationArthralgialoose stoolsrashesallergic reactionsedemacough

Serious

Pancreatitis (acute)
Severe hypersensitivity reactions (e.g., anaphylaxis, angioedema, exfoliative skin conditions including Stevens-Johnson syndrome)
Bullous pemphigoid
Acute renal failure (sometimes requiring dialysis)
Severe and disabling arthralgia
Heart failure (rare, in patients with pre-existing cardiovascular risk factors)
Increased hospitalization for heart failure (with saxagliptin, other DPP-4s neutral on CV events, but this is a class effect warning)
Severe joint pain (rarely associated)
pancreatitis (rare)

Pregnancy & lactation

Pregnancy

Category B — insulin preferred

Lactation

Sitagliptin is excreted in the milk of lactating rats. It is not known whether sitagliptin is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother and the potential risks to the infant.