Sitagliptin; Uses, Dosage, Side Effects, Drug Interactions

Last updated: February 7, 2026Reviewed date: February 7, 2026Reading time: 8 min read
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Sitagliptin is a Dipeptidyl Peptidase 4 Inhibitor. The mechanism of action of sitagliptin is as a Dipeptidyl Peptidase 4 Inhibitor. Sitagliptin is an orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis. Sitagliptin is a...

For severe symptoms, danger signs, pregnancy, child illness, or sudden worsening, seek urgent medical care.

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Article Summary

Sitagliptin is a Dipeptidyl Peptidase 4 Inhibitor. The mechanism of action of sitagliptin is as a Dipeptidyl Peptidase 4 Inhibitor. Sitagliptin is an orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis. Sitagliptin is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. This enzyme-inhibiting drug is to...

Key Takeaways

  • This article explains Mechanism of Action of Sitagliptin in simple medical language.
  • This article explains Indications of Sitagliptin in simple medical language.
  • This article explains Contra-Indications of Sitagliptin in simple medical language.
  • This article explains Dosage of Sitagliptin in simple medical language.
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Sitagliptin is a Dipeptidyl Peptidase 4 Inhibitor. The mechanism of action of sitagliptin is as a Dipeptidyl Peptidase 4 Inhibitor. Sitagliptin is an orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis.
Definition

Sitagliptin is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. This enzyme-inhibiting drug is to be used either alone or in combination with metformin or a thiazolidinedione for control of type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), the reduced amount of release of glucagon (diminishes its release) and increased release of insulin.

Mechanism of Action of Sitagliptin

Sitagliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones released in response to a meal. By preventing GLP-1 and GIP inactivation, they are able to increase the secretion of insulin and suppress the release of glucagon by the alpha cells of the pancreas. This drives blood glucose levels towards normal. As the blood glucose level approaches normal, the amounts of insulin released and glucagon suppressed diminishes, thus tending to prevent an “overshoot” and subsequent low blood sugar (hypoglycemia) which is seen with some other oral hypoglycemic agents. Sitagliptin has been shown to lower HbA1c level by about 0.7% points versus placebo. It is slightly less effective than metformin when used as a monotherapy. It does not cause weight gain and has less hypoglycemia compared to sulfonylureas. Sitagliptin is recommended as a second line drug (in combination with other drugs) after the combination of diet/exercise and metformin fails.

or

Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by Januvia, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, Januvia increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

Indications of Sitagliptin

  • Type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">Diabetes Mellitus
  • As an adjunct to diet and exercise to improve glycemic control in patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus.
  • For use as an adjunct to diet and exercise to improve glycemic control in patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus.
  • Also for use in patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus to improve glycemic control in combination with metformin or a PPARγ agonist (e.g., thiazolidinediones) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
  • For adult patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus, is indicated to improve glycaemic control
  • As monotherapy in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance.
  • As dual oral therapy in combination with metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.
  • A sulphonylurea when diet and exercise plus maximally tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance.
  • A peroxisome proliferator-activated receptor gamma (PPARy) agonist (i.e. a thiazolidinedione) when use of a PPARy agonist is appropriate and when diet and exercise plus the PPARy agonist alone do not provide adequate glycaemic control.
  • As triple oral therapy in combination with sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
  • a PPARy agonist and metformin when use of a PPARy agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
  • TESAVEL is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.
    For adult patients with type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes mellitus, Xelevia is indicated to improve glycaemic control
  • As monotherapy in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance.
  • As dual oral therapy in combination with metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.
  • Sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance.
  • A peroxisome proliferator-activated receptor gamma (PPAR) agonist (i.e. a thiazolidinedione) when use of a PPAR agonist is appropriate and when diet and exercise plus the PPAR agonist alone do not provide adequate glycaemic control.
  • As triple oral therapy in combination with a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.a PPAR agonist and metformin when use of a PPAR agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.

Contra-Indications of Sitagliptin

  • Infection
  • Low blood sugar
  • Pituitary hormone deficiency
  • Decreased function of the adrenal gland
  • Inadequate vitamin B12
  • Excess body acid
  • Extreme loss of body water
  • Habit of drinking too much alcohol
  • Alcohol intoxication
  • Heart attack
  • Suddenly serious symptoms of heart failure
  • Liver problems
  • Recent operation
  • Fever
  • Shock
  • Severe vomiting
  • Severe diarrhea
  • Serious lack of oxygen in the blood
  • Weakened patient
  • Injury
  • Sepsis syndrome
  • X-Ray Study with intravenous iodine contrast agent
  • Kidney disease with likely reduction in kidney function
  • Acute infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation of the pancreas
  • Chronic infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation of the pancreas
  • Moderate to Severe kidney impairment

Dosage of Sitagliptin

Strengths: 50 mg; 25 mg; 100 mg

Diabetes Type 2

  • Usual dose: 100 mg orally once a day

Side Effects of Sitagliptin

Most common

More common

Less common

  • Abnormal stools
  • bad, unusual, or unpleasant (after) taste
  • change in taste
  • difficulty with moving
  • discoloration of the fingernails or toenails
  • flu-like symptoms
  • joint pain
  • rash
  • runny nose
  • sneezing
  • stuffy nose
  • swollen joints

Drug Interactions of Sitagliptin

Sitagliptin may interact with following drugs, supplements & may decrease the efficacy of drug

Pregnancy & Lactation of Sitagliptin

FDA Pregnancy Category B

Pregnancy

This medication is not recommended for use during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding

It is not known if sitagliptin passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

References

Sitagliptin; Uses, Dosage, Side Effects, Drug Interactions

 

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What to tell the doctor

  • Write when the problem started and how it changed.
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Questions to ask

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  • Basic physical examination by a clinician
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  • Do not delay emergency care when danger signs are present.

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Safe first steps

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OTC medicine safety

  • For mild back pain, pain-relief medicine may be discussed with a doctor or pharmacist.
  • Avoid repeated painkiller use if you have kidney disease, stomach ulcer, uncontrolled blood pressure, or are taking blood thinners.

Avoid these mistakes

  • Do not start antibiotics without a proper medical decision.
  • Do not use steroid tablets or injections casually for quick relief.
  • Do not delay emergency care because of home remedies.

Get urgent help if

  • Back pain with leg weakness, numbness around private area, loss of urine/stool control, fever, cancer history, or major injury needs urgent care.
Medicine names, dose, and timing must be decided by a qualified clinician or pharmacist after checking age, pregnancy, allergy, other diseases, and current medicines.

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Write your symptoms, medicines already taken, test results, and questions before visiting a doctor. This note stays on your device unless you print or copy it.

Doctor to discuss: Medicine doctor / pediatrician for children / qualified clinician
Tests to discuss with doctor
  • Temperature chart and hydration assessment
  • CBC with platelet count if fever persists or dengue/other infection is possible
  • Urine test, malaria/dengue tests, chest evaluation, or blood culture only when clinically indicated
Questions to ask
  • What is the most likely cause of my symptoms?
  • Which warning signs mean I should go to emergency care?
  • Which tests are really needed now?
  • Which medicines are safe for my age, pregnancy status, allergy, kidney/liver/stomach condition, and current medicines?
  • Do I need antibiotics, or is this more likely viral?

Emergency warning signs such as chest pain, severe breathing difficulty, sudden weakness, confusion, severe dehydration, major injury, or loss of bladder/bowel control need urgent medical care. Do not wait for online information.

Safe pathway to proper treatment

Care roadmap for: Sitagliptin; Uses, Dosage, Side Effects, Drug Interactions

Use this simple roadmap to understand the next safe steps. It is educational and does not replace examination by a doctor.

Go to emergency care if you notice:
  • Severe or rapidly worsening symptoms
  • Breathing difficulty, chest pain, fainting, confusion, severe weakness, major injury, or severe dehydration
Doctor / service to discuss: Qualified healthcare provider; specialist depends on symptoms and examination.
  1. Step 1

    Check danger signs first

    If danger signs are present, seek emergency care and do not wait for online information.

  2. Step 2

    Record the symptom story

    Write when symptoms started, severity, medicines already taken, allergies, pregnancy status, and test results.

  3. Step 3

    Visit a qualified clinician

    A doctor, nurse, or qualified healthcare provider can examine you and decide which tests or treatment are needed.

  4. Step 4

    Do only useful tests

    Do tests after clinical assessment. Avoid unnecessary tests, random antibiotics, or repeated medicines without diagnosis.

  5. Step 5

    Follow up and return early if worse

    If symptoms worsen, new warning signs appear, or treatment is not helping, return for review quickly.

Rural patient practical tips
  • Take a written symptom diary and all previous prescriptions/test reports.
  • Do not hide medicines already taken, even herbal or over-the-counter medicines.
  • Ask which warning signs mean urgent referral to hospital.

This roadmap is for education. A real diagnosis and treatment plan requires history, examination, and clinical judgment.

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Frequently Asked Questions

Is this article a replacement for a doctor?

No. It is educational content only. Patients should consult a qualified clinician for diagnosis and treatment.

When should I seek urgent care?

Seek urgent care for severe symptoms, rapidly worsening condition, breathing difficulty, severe pain, neurological changes, or any emergency warning sign.

References

Add references, clinical guidelines, textbooks, journal articles, or trusted medical sources here. You can edit this area from the RX Article Professional Blocks panel.

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