Sitagliptin 25mg Tablets

Manufacturer ZYDUS PHARMACEUTICALS (USA) Active Ingredient Sitagliptin Tablets(sit a GLIP tin) Pronunciation sit a GLIP tin
It is used to help control blood sugar in people with type 2 diabetes.
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Drug Class
Antidiabetic Agent
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Pharmacologic Class
Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
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Pregnancy Category
Category B
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FDA Approved
Oct 2006
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DEA Schedule
Not Controlled

Overview

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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 amount of natural substances in your body (called incretins) that help release insulin when your blood sugar is high and reduce the amount of sugar your liver makes. This helps lower your blood sugar.
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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 the bathroom.

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.
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Lifestyle & Tips

  • Follow a healthy diet plan as recommended by your doctor or dietitian.
  • Engage in regular physical activity as advised by your healthcare provider.
  • Monitor your blood sugar levels regularly as instructed.
  • Do not skip meals.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 100 mg once daily
Dose Range: 25 - 100 mg

Condition-Specific Dosing:

type2DiabetesMellitus: 100 mg orally once daily, with or without food.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Safety and effectiveness not established in pediatric patients under 18 years of age).
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Dose Adjustments

Renal Impairment:

Mild: No dosage adjustment required (CrCl â‰Ĩ 50 mL/min).
Moderate: 50 mg orally once daily (CrCl â‰Ĩ 30 to < 50 mL/min).
Severe: 25 mg orally once daily (CrCl < 30 mL/min, including end-stage renal disease requiring hemodialysis or peritoneal dialysis).
Dialysis: 25 mg orally once daily. May be administered without regard to timing of dialysis.

Hepatic Impairment:

Mild: No dosage adjustment required.
Moderate: No dosage adjustment required.
Severe: No dosage adjustment required (based on pharmacokinetic studies, no adjustment is needed for mild to moderate impairment; severe hepatic impairment has not been studied).

Pharmacology

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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 rapid degradation 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 levels. Increased active incretin levels enhance glucose-dependent insulin release from pancreatic beta cells and decrease glucagon secretion from pancreatic alpha cells. This leads to improved glycemic control in patients with type 2 diabetes.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 87%
Tmax: 1 to 4 hours
FoodEffect: No clinically meaningful effect of food on absorption.

Distribution:

Vd: Approximately 198 liters
ProteinBinding: Approximately 38%
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 12.4 hours
Clearance: Approximately 350 mL/min (renal clearance: 300 mL/min)
ExcretionRoute: Renal (primary), Fecal
Unchanged: Approximately 79% (renal)
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Pharmacodynamics

OnsetOfAction: Within 24 hours (glucose-lowering effects)
PeakEffect: Within 1-4 hours (plasma concentration), sustained effect on incretin levels throughout the dosing interval.
DurationOfAction: 24 hours (allows for once-daily dosing)

Safety & Warnings

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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 medical attention immediately:

Allergic Reaction: Rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble 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 pass urine, changes in urine output, blood in the urine, or significant weight gain.
Heart Failure: If you have a history of heart failure or kidney problems, inform your doctor. Seek immediate medical attention if you experience extreme fatigue, shortness of breath, significant weight gain, or swelling in the arms or legs.
Low Blood Sugar: Dizziness, headache, feeling sleepy or weak, shaking, fast heartbeat, confusion, hunger, or sweating. If you experience any of these symptoms, contact your doctor right away and follow your prescribed plan for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or some fruit juices.
Pancreatitis: Severe stomach pain, severe back pain, or severe nausea and vomiting. Seek medical help immediately if you experience any of these symptoms.
Bullous Pemphigoid: Blisters or skin breakdown. Contact your doctor right away if you notice any of these symptoms.
Joint Pain: Severe and disabling joint pain or persistent joint pain. Seek medical attention if you experience any of these symptoms.

Other Possible Side Effects

While many people may not experience side effects or may only have mild side effects, it's essential to be aware of the following:

Headache
Common cold symptoms
* Nose or throat irritation

If you experience any of these side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help.

Reporting 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe stomach pain that does not go away, with or without vomiting (signs of pancreatitis).
  • Allergic reactions such as swelling of the face, lips, tongue, or throat, difficulty breathing, or severe skin rash.
  • Blisters or skin erosions (signs of bullous pemphigoid).
  • Severe and disabling joint pain.
  • Signs of heart failure: unusual shortness of breath, rapid weight gain, or swelling in your feet or legs.
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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.
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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 can significantly increase your risk of being involved in an accident.

Monitor your blood sugar levels as directed by your doctor to ensure they remain within a healthy range. Additionally, have your blood work checked as recommended by your doctor and discuss the results with them.

Before consuming alcohol, consult with your doctor to understand any potential risks or interactions.

Adhere to the diet and exercise plan prescribed by your doctor to maintain optimal blood sugar control. Be aware that stress, such as fever, infection, injury, or surgery, can affect blood sugar levels, as can changes in physical activity, exercise, or diet.

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, inform your doctor, as they will need to discuss the benefits and risks of this medication with you to ensure the best possible outcome for both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Hypoglycemia (if co-administered with sulfonylurea or insulin)
  • Mild prolongation of QT interval (not considered clinically significant at therapeutic doses)
  • Other non-specific symptoms

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 gastrointestinal tract, employ clinical monitoring, and institute supportive treatment as dictated by the patient's clinical status). Sitagliptin is modestly dialyzable. Call 1-800-222-1222 (Poison Control Center) immediately.

Drug Interactions

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Moderate Interactions

  • Digoxin (monitor digoxin levels, as sitagliptin may slightly increase digoxin concentrations)
  • Cyclosporine (co-administration with cyclosporine may increase sitagliptin exposure, but no dose adjustment is typically needed for sitagliptin)

Monitoring

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Baseline Monitoring

HbA1c

Rationale: To establish baseline glycemic control and guide treatment.

Timing: Prior to initiation of therapy.

Renal Function (e.g., eGFR, serum creatinine)

Rationale: To determine appropriate starting dose and identify need for dose adjustment.

Timing: Prior to initiation of therapy.

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Routine Monitoring

HbA1c

Frequency: Every 3-6 months

Target: Individualized, typically <7% for most adults.

Action Threshold: If target HbA1c is not met, consider dose adjustment or addition of other antidiabetic agents.

Renal Function (e.g., eGFR, serum creatinine)

Frequency: Periodically, especially in elderly or those with risk factors for renal impairment.

Target: Maintain within normal limits or stable for patient.

Action Threshold: If eGFR declines, adjust sitagliptin dose accordingly.

Signs/Symptoms of Pancreatitis

Frequency: Ongoing

Target: N/A

Action Threshold: If persistent severe abdominal pain (with or without vomiting) occurs, discontinue sitagliptin and evaluate for pancreatitis.

Signs/Symptoms of Hypersensitivity Reactions

Frequency: Ongoing

Target: N/A

Action Threshold: If severe allergic reactions (e.g., anaphylaxis, angioedema, exfoliative skin conditions) occur, discontinue sitagliptin immediately.

Signs/Symptoms of Bullous Pemphigoid

Frequency: Ongoing

Target: N/A

Action Threshold: If bullous pemphigoid develops, discontinue sitagliptin.

Signs/Symptoms of Severe Arthralgia

Frequency: Ongoing

Target: N/A

Action Threshold: If severe and disabling joint pain occurs, consider discontinuing sitagliptin.

Signs/Symptoms of Heart Failure

Frequency: Ongoing

Target: N/A

Action Threshold: Monitor for signs and symptoms of heart failure, especially in patients with a history of heart failure.

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Symptom Monitoring

  • Persistent severe abdominal pain (with or without vomiting) - possible pancreatitis
  • Swelling of face, lips, tongue, or throat; difficulty breathing or swallowing; severe rash or hives - possible hypersensitivity reaction
  • Blisters or erosions on the skin - possible bullous pemphigoid
  • Severe and disabling joint pain
  • Unusual tiredness, shortness of breath, rapid weight gain, swelling in ankles/feet - possible heart failure
  • Symptoms of hypoglycemia (if used with insulin or sulfonylurea): sweating, shakiness, dizziness, confusion, hunger, rapid heartbeat

Special Patient Groups

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Pregnancy

Sitagliptin is classified as Pregnancy Category B. Animal studies have shown no evidence of harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if clearly needed and the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Limited human data, animal studies show no teratogenicity.
Second Trimester: Limited human data.
Third Trimester: Limited human data. Poorly controlled diabetes during pregnancy increases risk of birth defects, pre-eclampsia, and other complications.
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Lactation

Sitagliptin is excreted into the milk of lactating rats. It is not known whether sitagliptin is excreted in human milk. Caution should be exercised when sitagliptin is administered to a nursing woman. Consider the benefits of breastfeeding, the risk of potential infant drug exposure, and the risk of untreated maternal condition.

Infant Risk: L3 (Moderate risk - no human data, but low molecular weight suggests possible excretion into milk. Monitor for hypoglycemia in breastfed infant if used.)
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Pediatric Use

Safety and effectiveness of sitagliptin have not been established in pediatric patients under 18 years of age. Not recommended for use in this population.

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Geriatric Use

No dosage adjustment is required based on age alone. However, because sitagliptin is substantially excreted by the kidney, and elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function in elderly patients.

Clinical Information

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Clinical Pearls

  • Sitagliptin is generally well-tolerated with a low risk of hypoglycemia when used as monotherapy or in combination with metformin or a TZD.
  • Dose adjustment is crucial for patients with renal impairment; always check renal function before initiating and periodically during treatment.
  • Educate patients on the symptoms of pancreatitis (severe, persistent abdominal pain) and instruct them to seek immediate medical attention if these occur.
  • Rare but serious adverse events include severe arthralgia, bullous pemphigoid, and hypersensitivity reactions.
  • Can be taken with or without food, at any time of day, but consistency is recommended.
  • Does not cause weight gain and may even lead to slight weight loss in some patients.
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Alternative Therapies

  • Other DPP-4 inhibitors (e.g., Saxagliptin, Linagliptin, Alogliptin)
  • Metformin
  • Sulfonylureas (e.g., Glipizide, Glyburide, Glimepiride)
  • Thiazolidinediones (TZDs) (e.g., Pioglitazone, Rosiglitazone)
  • GLP-1 Receptor Agonists (e.g., Liraglutide, Semaglutide, Dulaglutide)
  • SGLT2 Inhibitors (e.g., Canagliflozin, Dapagliflozin, Empagliflozin)
  • Insulin
  • Alpha-glucosidase inhibitors (e.g., Acarbose, Miglitol)
  • Meglitinides (e.g., Repaglinide, Nateglinide)
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Cost & Coverage

Average Cost: $100 - $500 per 30 tablets (generic)
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (preferred brand or generic)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure your safety and the effectiveness of your treatment, 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 that provides important information about your treatment. Please read this guide carefully when you first receive your medication and review it again each time your prescription is refilled. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, pharmacist, or other healthcare provider.

In the event of a suspected overdose, it is crucial to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication taken, the amount consumed, and the time it occurred. This information will help healthcare professionals provide you with the most effective treatment and care.