Sitagliptin
Sitagliptin is a DPP-4 inhibitor used to treat type 2 diabetes in adults. It works by blocking the DPP-4 enzyme, which allows incretin hormones to remain active longer, stimulating the pancreas to release more insulin when blood sugar is high while also reducing glucagon secretion. This medication is typically prescribed alongside diet and exercise, either as monotherapy or in combination with other glucose-lowering drugs.
Sitagliptin is a diabetes medication that helps control blood sugar by enhancing the body's natural incretin hormone activity to boost insulin production.
Key facts at a glance
- ATC
- A10BH01
- Generic
- Sitagliptin
- Class
- dpp4-inhibitor
- Brands
- Januvia
- Availability
- rx
- Pregnancy
- B
- Lactation
- unknown
- Half-life (h)
- 12.5
- Onset (min)
- 60
- Duration (h)
- 24
- Routes
- oral
- Forms
- tablet
- Regions
- CN, US, EU, JP
- Monitoring
- renal-function, blood-glucose
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 100mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 50mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 100mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
8 groupspregnancy
generaluse lowest effective dose if benefits outweigh risks
use only if clearly needed, avoid in pregnancy unless potential benefits justify potential risks to fetus
regular prenatal monitoring
Use with caution and monitor for adverse effects.
lactation
generalconsider discontinuing breastfeeding or discontinuing drug
sitagliptin is excreted in breast milk in small amounts, use only if clearly needed
monitor infant for any adverse effects
Use with caution and monitor for adverse effects.
geriatric
elderly over 65no dose adjustment required based on age alone
use standard dosing but assess renal function before initiating therapy
monitor renal function periodically
pediatric_age
children under 18not recommended - safety and efficacy not established
not indicated for use in pediatric patients due to lack of studies
not applicable
renal_impairment
severereduce dose to 25 mg once daily
for patients with CrCl less than 30 mL/min including those with ESRD on dialysis, use 25 mg once daily
monitor renal function periodically
renal_impairment
moderatereduce dose to 50 mg once daily
for patients with CrCl 30 to less than 50 mL/min, use 50 mg once daily
monitor renal function periodically
hepatic_impairment
mild moderateno dose adjustment required
no dose adjustment needed for mild to moderate hepatic impairment
standard monitoring
hepatic_impairment
severeuse with caution
not studied in severe hepatic impairment, use only if benefits outweigh risks
close monitoring of liver function
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Drug class information for Sitagliptin
Common uses
Primary therapeutic indication
FDA approval year
Regulatory approval information
Mechanism of action
Pharmacological mechanism
Sitagliptin is FDA-approved for improving glycemic control in adults with type 2 diabetes mellitus. It may be used as monotherapy or in combination with other antidiabetic agents such as metformin, sulfonylureas, or thiazolidinediones when single-agent therapy is insufficient.
By inhibiting the DPP-4 enzyme, sitagliptin prevents the breakdown of incretin hormones GLP-1 and GIP. This prolongs their activity, leading to glucose-dependent insulin secretion from pancreatic beta cells and suppression of glucagon release, resulting in improved blood glucose control without causing significant hypoglycemia when used alone.
Sitagliptin is taken orally once daily with or without food. Common side effects include upper respiratory infections and headache. It should not be used in patients with type 1 diabetes or diabetic ketoacidosis. Rare cases of acute pancreatitis have been reported, and the medication should be discontinued if pancreatitis is suspected. Renal function monitoring may be needed as dose adjustment is required in patients with moderate to severe renal impairment.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 22, 2026. · Read our editorial policy