What Is Sitagliptin and How Does It Work?

Sitagliptin is a prescription medication used with a proper diet and exercise program and possibly with other medications to control high blood sugar. It is used in people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems. Proper control of diabetes may also lessen your risk of a heart attack or stroke.

Sitagliptin is an anti-diabetic drug that works by increasing levels of natural substances called incretins. Incretins help to control blood sugar by increasing insulin release, especially after a meal. They also decrease the amount of sugar your liver makes.

Sitagliptin is available under the following different brand names: Januvia.

Dosages of Sitagliptin


  • 25 mg
  • 50 mg
  • 100 mg

Dosage Considerations – Should be Given as Follows:

Diabetes Mellitus, Type 2

  • 100 mg orally once daily

Dosing Modifications

Renal impairment

  • Creatinine clearance over 50 ml/minute: dose adjustment not necessary
  • Creatinine clearance 30-50 ml/minute: 50 mg orally once daily
  • Creatinine clearance under 30 ml/minute: 25 mg orally once daily
  • ESRD: 25 mg orally once daily regardless of hemodialysis

Hepatic impairment

  • Mild to moderate impairment: dose adjustment not necessary
  • Severe impairment: not studied


  • Safety and efficacy not established

What Are Side Effects Associated with Using Sitagliptin?

Common side effects of sitagliptin include:

  • runny or stuffy nose
  • diarrhea
  • headache
  • constipation
  • swelling of extremities
  • nausea
  • sore throat
  • osteoarthritis
  • upper respiratory tract infection
  • hypersensitivity reactions (severe allergic reaction, skin swelling, rash, hives, inflamed blood vessels under the skin, and exfoliative skin conditions [including Stevens-Johnson syndrome])
  • liver enzyme elevations
  • acute pancreatitis
  • constipation
  • vomiting
  • worsening renal function, including acute kidney failure
  • severe and disabling joint pain
  • muscle pain
  • pain in extremities
  • back pain
  • low blood sugar

Postmarketing side effects of sitagliptin reported include:

  • itching
  • large, fluid-filled blisters
  • severe allergic reaction (anaphylaxis)
  • skin swelling
  • rash
  • hives
  • inflammation of small and medium-sized vessels in the skin
  • Stevens-Johnson syndrome
  • liver enzyme elevations
  • acute pancreatitis
  • worsening kidney function
  • acute kidney failure
  • severe and disabling joint pain
  • constipation
  • vomiting
  • headache
  • muscle pain
  • pain in extremity
  • back pain

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

What Other Drugs Interact with Sitagliptin?

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Sitagliptin has no known severe interactions with other drugs.

Serious interactions of sitagliptin include:

Sitagliptin has moderate interactions with at least 67 different drugs.

Sitagliptin has mild interactions with at least 81 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

What Are Warnings and Precautions for Sitagliptin?


This medication contains sitagliptin. Do not take Januvia if you are allergic to sitagliptin or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.


  • Documented hypersensitivity.

Effects of Drug Abuse

  • None

Short-Term Effects

  • See "What Are Side Effects Associated with Using Sitagliptin?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Sitagliptin?"


  • Use with caution in liver impairment, or heart failure (due to an elevated overall risk of acute heart failure in those patients taking any dipeptidyl peptidase inhibitor).
  • Use with caution in kidney failure; worsening of kidney failure, including acute kidney 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.
  • Cases of bullous pemphigoid requiring hospitalization reported with DPP-4 inhibitor use; in reported cases, patients typically recovered with topical or systemic immunosuppressive treatment and discontinuation of DPP-4 inhibitor; tell patients to report development of blisters or erosions while receiving therapy; if bullous pemphigoid is suspected, discontinue therapy and consider making referral to dermatologist, for diagnosis and appropriate treatment.

Pregnancy and Lactation

  • Use of sitagliptin during pregnancy may be acceptable. Either animal studies show no risk but human studies are not available or animal studies showed minor risks and human studies were done and showed no risk.
  • It is unknown whether excreted breast milk contains sitagliptin; use caution if breastfeeding. Consult your physician.
Medscape. Sitagliptin.
RxList. Januvia Side Effects Center.

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