Sitagliptin 100mg Tablets
It is used to help control blood sugar in people with type 2 diabetes.
Drug Class
Antidiabetic agent
Pharmacologic Class
Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
Pregnancy Category
Not available
FDA Approved
Oct 2006
DEA Schedule
Not Controlled
Overview
What is this medicine?
Sitagliptin is a medication used to help control blood sugar levels in adults with type 2 diabetes. It works by increasing the body's natural ability to lower high blood sugar after meals.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, as directed. It's essential to continue taking this medication as prescribed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
For all tablet products, store them at room temperature in a dry place, avoiding bathrooms.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, as directed. It's essential to continue taking this medication as prescribed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
For all tablet products, store them at room temperature in a dry place, avoiding bathrooms.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses.
Lifestyle & Tips
- Take sitagliptin exactly as prescribed by your doctor, usually once a day with or without food.
- Continue to follow your doctor's recommendations for diet and exercise while taking this medication.
- Monitor your blood sugar levels regularly as advised by your healthcare provider.
- Be aware of symptoms of low blood sugar (hypoglycemia) if you are taking sitagliptin with other diabetes medications like insulin or sulfonylureas. Carry a source of sugar (e.g., glucose tablets, juice) to treat low blood sugar.
- Report any unusual or severe abdominal pain, with or without vomiting, to your doctor immediately, as this could be a sign of pancreatitis.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
100 mg once daily
Dose Range:
100 - 100 mg
Condition-Specific Dosing:
monotherapy:
100 mg once daily
combination_therapy:
100 mg once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (safety and efficacy not established in patients <18 years of age)
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment (CrCl ≥50 mL/min)
Moderate:
50 mg once daily (CrCl ≥30 to <50 mL/min)
Severe:
25 mg once daily (CrCl <30 mL/min)
Dialysis:
25 mg once daily, administered without regard to timing of dialysis
Hepatic Impairment:
Mild:
No dose adjustment
Moderate:
No dose adjustment
Severe:
Not studied, caution advised
Pharmacology
Mechanism of Action
Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It works by inhibiting the enzyme DPP-4, which is responsible for the inactivation of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By preventing the breakdown of these incretins, sitagliptin increases their active concentrations, leading to enhanced glucose-dependent insulin secretion from pancreatic beta cells and decreased glucagon secretion from pancreatic alpha cells. This results in improved glycemic control.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 87%
Tmax:
1 to 4 hours
FoodEffect:
No clinically meaningful effect on pharmacokinetics
Distribution:
Vd:
Approximately 198 L
ProteinBinding:
Approximately 79%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 12.4 hours
Clearance:
Approximately 350 mL/min (renal clearance: 300 mL/min)
ExcretionRoute:
Renal (primarily unchanged drug)
Unchanged:
Approximately 79% (urine)
Pharmacodynamics
OnsetOfAction:
Within 24 hours (glucose-lowering effect)
PeakEffect:
Within 1-4 hours (plasma concentration), sustained effect on incretins throughout dosing interval
DurationOfAction:
24 hours (due to once-daily dosing)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Allergic Reaction: Rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Severe Skin Reaction (Stevens-Johnson Syndrome): Red, swollen, blistered, or peeling skin (with or without fever), red or irritated eyes, or sores in the mouth, throat, nose, or eyes.
Kidney Problems: Inability to urinate, changes in urine output, blood in the urine, or sudden weight gain. If you have a history of heart failure or kidney problems, inform your doctor.
Heart Failure: If you experience extreme fatigue, shortness of breath, sudden weight gain, or swelling in the arms or legs, contact your doctor immediately.
Low Blood Sugar: Dizziness, headache, feeling sleepy or weak, shaking, rapid heartbeat, confusion, hunger, or sweating. If you experience any of these symptoms, contact your doctor and follow their instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or consuming fruit juices.
Pancreatitis: Severe stomach pain, severe back pain, or severe nausea and vomiting. If you experience any of these symptoms, contact your doctor immediately.
Bullous Pemphigoid: Blisters or skin breakdown. If you notice any of these symptoms, contact your doctor immediately.
Joint Pain: Severe and disabling joint pain or persistent joint pain. If you experience any of these symptoms, contact your doctor immediately.
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms or any other unusual effects, contact your doctor:
Headache
Common cold symptoms
* Nose or throat irritation
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Allergic Reaction: Rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Severe Skin Reaction (Stevens-Johnson Syndrome): Red, swollen, blistered, or peeling skin (with or without fever), red or irritated eyes, or sores in the mouth, throat, nose, or eyes.
Kidney Problems: Inability to urinate, changes in urine output, blood in the urine, or sudden weight gain. If you have a history of heart failure or kidney problems, inform your doctor.
Heart Failure: If you experience extreme fatigue, shortness of breath, sudden weight gain, or swelling in the arms or legs, contact your doctor immediately.
Low Blood Sugar: Dizziness, headache, feeling sleepy or weak, shaking, rapid heartbeat, confusion, hunger, or sweating. If you experience any of these symptoms, contact your doctor and follow their instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or consuming fruit juices.
Pancreatitis: Severe stomach pain, severe back pain, or severe nausea and vomiting. If you experience any of these symptoms, contact your doctor immediately.
Bullous Pemphigoid: Blisters or skin breakdown. If you notice any of these symptoms, contact your doctor immediately.
Joint Pain: Severe and disabling joint pain or persistent joint pain. If you experience any of these symptoms, contact your doctor immediately.
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms or any other unusual effects, contact your doctor:
Headache
Common cold symptoms
* Nose or throat irritation
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe, persistent abdominal pain (possible pancreatitis)
- Signs of allergic reaction (e.g., rash, hives, swelling of face/lips/tongue/throat, difficulty breathing)
- Blisters or erosions on the skin (possible bullous pemphigoid)
- Severe and disabling joint pain
- Symptoms of kidney problems (e.g., swelling in legs/feet, decreased urination)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have type 1 diabetes, as this medication is not intended to treat this condition.
This medication may interact with other medications or health conditions. Therefore, it is crucial to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your health problems, including any medical conditions or diseases
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have type 1 diabetes, as this medication is not intended to treat this condition.
This medication may interact with other medications or health conditions. Therefore, it is crucial to provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your health problems, including any medical conditions or diseases
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
If you experience low blood sugar, do not operate a vehicle, as this increases your risk of being involved in an accident. Monitor your blood sugar levels as directed by your doctor to ensure timely detection and management of any fluctuations.
Regular blood tests, as scheduled by your doctor, are crucial to assess your overall health and adjust your treatment plan accordingly. Discuss any concerns or questions you may have with your doctor.
Before consuming alcohol, consult with your doctor to understand the potential risks and interactions with your medication. Adhere to the personalized diet and exercise plan recommended by your doctor to maintain optimal blood sugar control.
Be aware that stress, such as fever, infection, injury, or surgery, can impact your blood sugar levels, making them more challenging to manage. Additionally, changes in physical activity, exercise, or diet can also affect your blood sugar control.
Kidney problems are a potential side effect of this medication, and in severe cases, may require hospitalization or dialysis.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
If you experience low blood sugar, do not operate a vehicle, as this increases your risk of being involved in an accident. Monitor your blood sugar levels as directed by your doctor to ensure timely detection and management of any fluctuations.
Regular blood tests, as scheduled by your doctor, are crucial to assess your overall health and adjust your treatment plan accordingly. Discuss any concerns or questions you may have with your doctor.
Before consuming alcohol, consult with your doctor to understand the potential risks and interactions with your medication. Adhere to the personalized diet and exercise plan recommended by your doctor to maintain optimal blood sugar control.
Be aware that stress, such as fever, infection, injury, or surgery, can impact your blood sugar levels, making them more challenging to manage. Additionally, changes in physical activity, exercise, or diet can also affect your blood sugar control.
Kidney problems are a potential side effect of this medication, and in severe cases, may require hospitalization or dialysis.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Limited experience with overdose. In clinical trials, single doses up to 800 mg were well tolerated. Higher doses (e.g., 600 mg/day for 10 days) did not result in increased adverse events.
What to Do:
In the event of an overdose, it is reasonable to employ the usual supportive measures (e.g., remove unabsorbed material from the GI tract, employ clinical monitoring, and institute supportive treatment as dictated by the patient’s clinical status). Sitagliptin is modestly dialyzable (approximately 13.5% removed over 3-4 hours of hemodialysis). Call 1-800-222-1222 (Poison Control Center).
Drug Interactions
Moderate Interactions
- Digoxin (monitor digoxin levels, as sitagliptin may slightly increase digoxin concentrations)
Monitoring
Baseline Monitoring
HbA1c
Rationale: To establish baseline glycemic control and assess treatment efficacy
Timing: Prior to initiation of therapy
Renal function (e.g., serum creatinine, eGFR)
Rationale: To determine appropriate dosing adjustments for patients with renal impairment
Timing: Prior to initiation of therapy
Routine Monitoring
HbA1c
Frequency: Every 3-6 months
Target: Individualized, typically <7% for most adults
Action Threshold: If target not met, consider dose adjustment or addition of other agents
Renal function (e.g., eGFR)
Frequency: At least annually, or more frequently in patients with known renal impairment or risk factors for kidney disease
Target: Maintain appropriate eGFR for dose
Action Threshold: If eGFR declines, adjust sitagliptin dose accordingly
Signs/symptoms of pancreatitis
Frequency: As needed, if symptoms arise
Target: N/A
Action Threshold: Discontinue sitagliptin immediately if pancreatitis is suspected
Symptom Monitoring
- Symptoms of hypoglycemia (e.g., sweating, tremor, dizziness, confusion, hunger)
- Symptoms of pancreatitis (e.g., severe, persistent abdominal pain, radiating to the back, with or without vomiting)
- Symptoms of severe hypersensitivity reactions (e.g., rash, urticaria, facial edema, anaphylaxis)
- Symptoms of bullous pemphigoid (e.g., blisters or erosions on the skin)
- Severe and disabling arthralgia (joint pain)
Special Patient Groups
Pregnancy
Limited data on sitagliptin use in pregnant women are insufficient to determine a drug-associated risk for major birth defects or miscarriage. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Insufficient data to assess risk.
Second Trimester:
Insufficient data to assess risk.
Third Trimester:
Insufficient data to assess risk.
Lactation
Sitagliptin is excreted in the milk of lactating rats. It is not known whether sitagliptin is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in breastfed infants, 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.
Infant Risk:
Potential for unknown adverse effects; caution advised.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients under 18 years of age.
Geriatric Use
No dose adjustment is required based on age alone. However, dose adjustment is recommended for elderly patients with moderate to severe renal impairment (based on eGFR). Renal function should be assessed more frequently in elderly patients.
Clinical Information
Clinical Pearls
- Sitagliptin is generally well-tolerated with a low risk of hypoglycemia when used as monotherapy or in combination with metformin.
- Dose adjustment is crucial for patients with renal impairment; always check eGFR before prescribing and periodically thereafter.
- Educate patients on the symptoms of pancreatitis and instruct them to seek immediate medical attention if these occur.
- While rare, severe hypersensitivity reactions and bullous pemphigoid have been reported; discontinue sitagliptin if these occur.
- Consider the cost and availability of generic sitagliptin, which became available in 2024, potentially improving access and affordability.
Alternative Therapies
- Other DPP-4 inhibitors (e.g., Saxagliptin, Linagliptin, Alogliptin)
- GLP-1 Receptor Agonists (e.g., Liraglutide, Semaglutide)
- SGLT2 Inhibitors (e.g., Canagliflozin, Dapagliflozin, Empagliflozin)
- Sulfonylureas (e.g., Glipizide, Glyburide, Glimepiride)
- Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone)
- Insulin
- Metformin
Cost & Coverage
Average Cost:
$400 - $600 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (preferred brand or non-preferred brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a valuable resource for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, we encourage you to discuss them with your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount, and the time it occurred.