Sitagliptin | Side Effects, Dosage, Uses & More
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Sitagliptin

Highlights

  1. Sitagliptin is an oral drug that’s used to treat high blood sugar levels caused by type 2 diabetes.
  2. Sitagliptin is used along with lifestyle changes and sometimes other medications.
  3. The standard starting dose is 100 mg taken by mouth once per day.
  4. This drug may increase your risk of inflammation of your pancreas. This can be severe and sometimes fatal.
  5. Common side effects include stomach problems, diarrhea, upper respiratory infections, stuffy or runny nose, and headaches.

IMPORTANT INFORMATION

Pancreatitis warning
Sitagliptin may increase your risk of inflammation of your pancreas (pancreatitis). This can be severe and sometimes fatal. Before you start taking this drug, tell your doctor if you’ve ever had:

  • pancreatitis
  • stones in your gallbladder (gallstones)
  • alcoholism
  • high triglyceride levels
  • kidney problems

Joint pain
This drug may cause severe and disabling joint pain. Tell your doctor right away if you have joint pain. Your doctor may switch you to another medicine to control your diabetes.


What is sitagliptin?

Sitagliptin is a prescription drug. It’s available as an oral tablet.

This drug may be used as part of a combination therapy. That means you need to take it with other drugs.

Why it's used

Sitagliptin is used to treat high blood sugar levels caused by type 2 diabetes. It’s used along with lifestyle changes (diet, exercise, and no smoking) and sometimes other medications.

How it works

Sitagliptin belongs to a class of drugs called dipeptidyl peptidate-4 (DPP-4) inhibitors. A class of drugs refers to medications that work similarly. They have a similar chemical structure and are often used to treat similar conditions.

Insulin is a chemical in your body that helps remove sugar from your blood and moves it to cells, where it can be used for energy. Hormones in your body called incretins regulate the production and release of insulin. Sitagliptin works by protecting incretin hormones so they aren’t broken down too quickly. This helps your body use insulin better and lowers your blood sugar.

Amlodipine side effects

More common side effects

The most common side effects that occur with sitagliptin include:

  • upset stomach
  • diarrhea
  • stomach pain
  • upper respiratory infection
  • stuffy or runny nose and sore throat
  • headache

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious side effects

If you experience any of these serious side effects, call your doctor right away. If your symptoms are potentially life-threatening or if you think you’re experiencing a medical emergency, call 9-1-1.

  • pancreatitis. Symptoms may include:
    • severe pain in your stomach that won’t go away, and that can be felt from your stomach through your back
    • vomiting
  • low blood sugar. Symptoms may include:
    • intense hunger
    • nervousness
    • shakiness
    • sweating, chills, and claminess
    • dizziness
    • fast heart rate
    • lightheadedness
    • sleepiness
    • confusion
    • blurred vision
    • headache
    • depression
    • irritability
    • crying spells
    • nightmares and crying out in your sleep
  • severe allergic reaction. Symptoms may include:
    • skin rash
    • hives
    • swelling of your face, lips, tongue, and throat
    • trouble breathing or swallowing
  • kidney problems. Symptoms may include:
    • swelling of your feet, ankles, or legs
    • drowsiness
    • tiredness
    • chest pain
    • nausea
    • shortness of breath
    • producing less urine than usual
Pharmacist's Advice
This drug will decrease your blood sugar levels. Sitagliptin can cause your blood sugar level to drop too low (hypoglycemia). If you have a low blood sugar reaction, you need to treat it.

For mild hypoglycemia (55–70 mg/dL), treatment is 15–20 grams of glucose (a type of sugar). You need to eat or drink one of the following:

• 3–4 glucose tablets
• a tube of glucose gel
• ½ cup of juice or regular, non-diet soda
• 1 cup of nonfat or 1% cow’s milk
• 1 tablespoon of sugar, honey, or corn syrup
• 8–10 pieces of hard candy, such as lifesavers

Test your blood sugar 15 minutes after you treat the low sugar reaction. If your blood sugar is still low, then repeat the above treatment.

Once your blood sugar level is back in the normal range, eat a small snack if your next planned meal or snack is more than 1 hour later.

Sitagliptin doesn’t cause drowsiness.

Sitagliptin may interact with other medications

Sitagliptin can interact with other medications, herbs, or vitamins you might be taking. That’s why your doctor should manage all of your medications carefully. If you’re curious about how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Note: You can reduce your chances of drug interactions by having all of your prescriptions filled at the same pharmacy. That way, a pharmacist can check for possible drug interactions.

Medications that might interact with this drug

Other diabetes medications

  • insulin
  • sulfonylureas
  • glipizide
  • glimepiride
  • glyburide

When you take sitagliptin with certain other diabetes drugs, your blood sugar can become too low. Your doctor will check your blood sugar more closely when you’re taking one of these drugs with sitagliptin.


SITAGLIPTIN WARNINGS

People with pancreatitis
Sitagliptin may increase your risk of inflammation of your pancreas (pancreatitis). If you have pancreatitis already, your doctor may choose another medication to treat your diabetes.

People with kidney problems
Your dose of this medicine will depend on your kidney function. If your kidneys don’t work as well as they should, you may need a lower dose of this drug so that you don’t experience side effects.

People with diabetic ketoacidosis
You shouldn’t use sitagliptin to treat diabetic ketoacidosis.

Pregnant women
Sitagliptin is a pregnancy category B drug. That means two things:

  1. Studies of the drug in pregnant animals haven’t shown risk to the fetus.
  2. There aren’t enough studies done in pregnant women to show the drug poses a risk to the fetus.

Tell your doctor if you’re pregnant or plan to become pregnant. Sitagliptin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Women who are breast-feeding
It isn’t known if sitagliptin passes through breast milk. It isn’t known whether sitagliptin causes side effects in a breastfeeding child.

You and your doctor may need to decide if you’ll take sitagliptin or breastfeed. If your doctor decides that it’s okay for you to take sitagliptin while you’re breastfeeding, your infant should be monitored for side effects of the medication.

For seniors
As you age, your kidneys may not work as well as they did when you were younger. Your doctor should monitor your kidney function before starting and during treatment with this medication to limit your risk of side effects.

For children
The safety and effectiveness of sitagliptin in people younger than 18 years old haven’t been established.

Allergies
Sitagliptin can cause a severe allergic reaction. Symptoms include:

  • skin rash
  • hives
  • swelling of your face, lips, tongue, and throat
  • trouble breathing or swallowing

Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal.


How to take sitagliptin

All possible dosages and forms may not be included here. Your dose, form, and how often you take it will depend on:

  • your age
  • the condition being treated
  • how severe your condition is
  • other medical conditions you have
  • how you react to the first dose

What are you taking this medication for?

Type 2 diabetes

Form: Oral tablet
Strengths: 25 mg, 50 mg, and 100 mg

Adult Dosage (ages 18-64 years)
The standard dose is 100 mg taken by mouth once per day.

Child Dosage (ages 0-17 years)
This medicine hasn’t been studied in children and shouldn’t be used in people younger than 18 years old.

Senior Dosage (ages 65 years and older)
As you age, your kidneys may not work as well as they once did. Your dose of sitagliptin will depend on your kidney function. Your doctor will check your kidneys before starting and regularly during treatment with this medication.

Special considerations

Kidney problems:

  • mild kidney impairment (creatinine clearance greater than or equal to 50 mL/min or serum creatinine levels of less than 1.7 mg/dL in men or less than 1.5 mg/dL in women): 100 mg per day
  • moderate kidney impairment (creatinine clearance greater than 30 but less than 50 mL/min or serum creatinine levels greater than 1.7 but equal to or less than 3 mg/dL in men or greater than 1.5 but less than or equal to 2.5 mg/dL in women): 50 mg per day
  • severe kidney impairment (creatinine clearance greater than 30 mL/min or serum creatinine levels of greater than 3 mg/dL in men or greater than 2.5 mg/dL in women): 25 mg per day
  • end-stage kidney disease (requiring dialysis): 25 mg per day
Pharmacist's Advice
Sitagliptin comes with serious risks if you don’t take it as prescribed.

If you don't take it at all
If you don’t take this drug at all, your symptoms of type 2 diabetes may not improve or may even get worse.

If you stop taking it suddenly
If your condition improved while you were taking sitagliptin and then you suddenly stop taking it, your symptoms of type 2 diabetes may come back.

If you take too much
If you double up your dose or take it too close to your next scheduled time, you may be at higher risk of experiencing serious side effects such as severe gastrointestinal problems or a low blood sugar reaction. If you think you’ve taken too much, call your doctor.

What to do if you miss a dose
If you forget to take your dose, take it as soon as you remember. If it’s just a few hours before the time for your next dose, then only take one dose at that time.

Never try to catch up by taking two doses at once. This could result in toxic side effects.

How to tell if the drug is working
You may be able to tell if this drug is working if your blood sugar is near your target range as determined by your doctor. Your symptoms of diabetes may also get better.

Sitagliptin is a long-term drug treatment.

Important considerations for taking this drug

Sitagliptin can be taken with or without food

Store sitagliptin at room temperature
Keep it at 68–77°F (20–25°C). This medication can be stored briefly from 59–86°F (15–30°C).

Keep the drug away from light and high temperature.

Keep your drugs away from areas where they could get wet, such as bathrooms. Store this drug away from moisture and damp locations.

Prescription is refillable

Travel
When traveling with your medication:

  • Always carry your medication with you or in your carry-on bag.
  • Don’t worry about airport X-ray machines. They can’t hurt this medication.
  • You may need to show your pharmacy’s label to clearly identify the medication. Keep the original prescription label with you when traveling.
  • Don’t leave this medicine in the car, especially when the temperature is hot or freezing.

Self-management
Your doctor may have you regularly test your blood sugar levels at home.

Ask your doctor or pharmacist how to use your blood glucose monitoring machine. You need to know how to use this device to test your blood sugar.

If your doctor decides that you need to test your blood sugar at home, you’ll need the following:

  • sterile alcohol wipes
  • lancing device and lancets (a needle used to obtain drops of blood from your finger to test your blood sugar)
  • blood sugar test strips
  • blood glucose monitoring machine
  • needle container for safe disposal of lancets

Clinical monitoring
Before starting and during treatment with sitagliptin, your doctor may check your:

  • blood sugar levels
  • glycosylated hemoglobin (A1C) levels. This test measures your blood sugar control over the last 2–3 months.
  • cholesterol
  • kidney function

Your diet
Sitagliptin, when combined with lifestyle changes (diet, exercise, and not smoking), can help lower your blood sugar. Follow the nutrition plan that your doctor, registered dietician, or diabetes educator recommended.

Hidden costs

If your doctor decides that you need to test your blood sugar at home, you’ll need the following:

  • sterile alcohol wipes
  • lancing device and lancets (a needle used to obtain drops of blood from your finger to test your blood sugar)
  • blood sugar test strips
  • blood glucose monitoring machine
  • needle container for safe disposal of lancets

Insurance
Many insurance companies will require a prior authorization before they approve the prescription and pay for sitagliptin.

Are there any alternatives?

There are other drugs available to treat your condition. Some may be more suitable for you than others. Talk to your doctor about possible alternatives.

Sitagliptin (Januvia) professional information

Brand name

Januvia

Indications for use

Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Sitagliptin can be used alone or in combination.

Do not use in patients with Type I diabetes.

Contraindications

History of serious hypersensitivity reaction such as anaphylaxis or angioedema.

Warnings/precautions

Pancreatitis: Acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis, may occur. If pancreatitis is suspected, promptly discontinue sitagliptin.

Renal impairment: Acute renal failure, sometimes requiring dialysis, may occur. Dosage adjustment is recommended in patients with moderate or severe renal insufficiency and in patients with end-stage renal disease requiring hemodialysis or peritoneal dialysis.

Hypoglycemia: There is an increased risk of hypoglycemia when sitagliptin is added to an insulin secretagogue (e.g., sulfonylurea) or insulin therapy. A lower dose of sulfonylurea or insulin may be required to reduce the chance for hypoglycemia.

Hypersensitivity: Serious allergic and hypersensitivity reactions in patients treated with sitagliptin, such as anaphylaxis, angioedema, and exfoliative skin conditions, including Stevens-Johnson syndrome, are reported.

Arthralgia: Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors.

Mechanism of action

Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones.

Dosing in adults

Administer 100 mg of sitagliptin once per day. May be given without regards to meals.

When sitagliptin is combined with a sulfonylurea or with insulin, a lower dose of the sulfonylurea or insulin should be considered to reduce the risk of hypoglycemia.

Dosing in children

Safety and effectiveness of sitagliptin has not been established in patients younger than 18 years of age.

Dosing in elderly

There is no overall difference in safety and effectiveness in the elderly. However, because renal function is decreased in the elderly, care should be taken when choosing a dose of sitagliptin in elderly patients.

Dosing in renal impairment

For patients with mild renal insufficiency (CrCl ≥ 50 mL/min ), no dosage adjustment for sitagliptin is required.

For patients with moderate renal insufficiency (CrCl ≥ 30 to < 50 mL/min), the dose of sitagliptin is 50 mg once daily.

For patients with severe renal insufficiency (CrCl < 30 mL/min) or end-stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dose of sitagliptin is 25 mg once daily. Sitagliptin may be administered without regard to the timing of dialysis.

Dosing in hepatic impairment

NA

Drug interactions

There was a slight increase in the area under the curve and mean peak drug concentration of digoxin with the co-administration of 100 mg sitagliptin for 10 days. Patients receiving digoxin should be monitored appropriately. No dosage adjustment of digoxin or sitagliptin is recommended.

Adverse drug reactions

(Occurred in > 5% of patients) Hypoglycemia, nasopharyngitis, headache, peripheral edema

Monitoring parameters

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 (including obtaining an electrocardiogram), and institute supportive therapy as dictated by the patient's clinical status.

Sitagliptin is modestly dialyzable. In clinical studies, approximately 13.5% of the dose was removed over a three- to four-hour hemodialysis session. Prolonged hemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialyzable by peritoneal dialysis.

Pregnancy risk factor

Pregnancy category B: Reproduction studies have been performed in rats and rabbits. Doses of sitagliptin up to 125 mg/kg (approximately 12 times the human exposure at the maximum recommended human dose) did not impair fertility or harm the fetus. There are, however, no adequate and well-controlled studies in pregnant women. Sitagliptin administered to pregnant female rats and rabbits from gestation day six to 20 was not teratogenic at oral doses up to 250 mg/kg (rats) and 125 mg/kg (rabbits), or approximately 30- and 20-times human exposure at the maximum recommended human dose (MRHD) of 100 mg/day based on AUC comparisons. Higher doses increased the incidence of rib malformations in offspring at 1000 mg/kg, or approximately 100 times human exposure at the MRHD. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Preparation of suspension

NA


Disclaimer: Healthline has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. The drug information contained herein is for informational purposes only. Data sources include the drug manufacturer’s prescribing information and package insert.

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