Sitagliptin (Oral)

Sitagliptin is an antihyperglycemic medicine, often prescribed on its own, or in conjunction with other drugs in aiding patients suffering from Type 2 diabetes.


Sitagliptin was once marketed as a phosphate salt and is an antihyperglycemic drug (that is, a form of antidiabetic medication) known as a DPP-4 inhibitor, due to its impact of restricting the production of dipeptidyl peptidase-4 enzymes in the body.

Sitagliptin can be prescribed by itself, or in conjunction with other antihyperglycemic treatments, such as thiazolidinedione, pioglitazone, insulin, glimepiride, or metformin to assist in treating patients suffering from Type 2 diabetes mellitus.

As well as combining with other medications sitagliptin is usually prescribed alongside a course of exercise and a healthy diet to treat hyperglycemia (high levels of sugar in the blood) caused by the patient's diabetes. Sitagliptin increases the production of certain substances in a patient's body that enables the pancreas to release higher levels of insulin, thus controlling levels of sugar in the blood. It also sends a signal to the liver, causing it to cease producing glucose (sugar) when there is already too much in the patient's blood.

Because of its area of impact, sitagliptin is not an appropriate form of treatment for those patients who suffer from Type 1 or insulin-dependent diabetes.

Sitagliptin is only available under prescription from a doctor. It is available in the following dosage forms:

  • Tablet

Conditions Treated

Type of Medicine

  • Antihyperglycemic (antidiabetic)
  • DPP-4 (dipeptidyl peptidase-4) inhibitor class

Side Effects

In addition to any desired and expected effects, your medication can result in less desirable outcomes. Whilst it is not certain that any or all of those listed here will occur, if any of them should, it might be necessary for you to seek attention from a medical expert.

Should any of these side effects listed exhibit themselves during your course of treatment with Sitagliptin, you ought to consult your examining doctor as a matter of urgency.

  • White spots, ulcers, or sores to the lips, or in the mouth
  • Vomiting
  • Unusual weakness or tiredness
  • Swelling or puffiness to the tongue, lips, face, around the eyes, or the eyelids
  • Slurred speech
  • Skin rash, itching, welts, or hives
  • Shakiness
  • Severe pain in the joints
  • Seizures
  • Reddening of the skin
  • Pains to the abdomen, side, or stomach, perhaps radiating around to the patient's back
  • Nightmares
  • Nausea
  • Loss or lack of appetite
  • Losing consciousness
  • Loosening, peeling, or blistering to the skin
  • Lesions to the skin, usually red and often containing a purplish center
  • Large swellings, being hive-like in appearance, to the sex organs, feet, legs, hands, throat, tongue, lips, eyelids, or face
  • Increased hunger
  • Headache
  • Fast heartbeat
  • Dizziness
  • Diarrhea
  • Depression
  • Cool, pale skin
  • Confusion
  • Cold sweats
  • Chills
  • Blurred vision
  • Anxiety

Though the above-listed side effects could require a doctor's attention, there are other side impacts of this drug, which likely would not. These effects tend to disappear during your treatment, as your body starts to become acclimatized to the drug. In addition, your doctor can sometimes recommend alternative methods by which you can prevent or reduce many of the negative side effects. If you present with any of these impacts during your treatment, and you find them becoming bothersome, you should speak to your examining doctor.

  • Body pains or aches
  • Runny or stuffy nose
  • Sore throat
  • Sneezing
  • Muscle aches
  • Loss or lack of voice
  • Fever
  • Ear congestion
  • Difficulty whilst breathing
  • Diarrhea
  • Cough
  • Stomach or abdominal pain

These negative effects are not an exhaustive list, and other negative symptoms can present themselves during your course of Sitagliptin. If you become aware of any negative effects during your course of treatment with Sitagliptin, make sure that you consult your doctor.


The dosage recommended of Sitagliptin can differ between patients. You should ensure that you follow your prescribing doctor's instructions or the specific dosage instructions on the medication's label. The information listed below indicates the average dosages of Sitagliptin, and you should not infer any professional medical advice from them. If your prescribing doctor recommends a different dosage from those described below, do not change them, unless subsequently recommended to do so by an expert.

The amount of Sitagliptin you take is determined by the strength of the medication. Additionally, the time you should allow to elapse between doses, the amount of doses that you take every day, and how long your course of Sitagliptin lasts is based on your specific medical condition and the efficacy of the drug to combat it.

For oral dosage tablets:

For type 2 diabetes:

  • Adults: 100 milligrams (mg) dosage, once per day
  • Children: the use and dosage of Sitagliptin must be decided upon by your prescribing doctor

If you happen to miss a dosage of Sitagliptin, it is advisable to take it again as soon as you can, unless it is almost the time for your next dosage, in which case it is best if you skip your missed dosage, returning to the normal schedule of medication at the earliest opportunity. Under no circumstances should you double the dose.


Certain medications should never be taken at the same time as one another. However, there are other occasions under which two or more different drugs can be taken in unison, despite the likelihood of a negative interaction taking place. In a situation like this, it is expected that your doctor will adjust the dosage of either medicine, or suggest alternative precautions. Whilst taking Sitagliptin, you must ensure that your doctor knows that you're taking any other kinds of medication, especially if you're taking any of these listed here. These interactions are listed here based on the likelihood of their occurrence and potential significance. This list is not necessarily exhaustive.

Using Sitagliptin in unison with the following medicines is usually not something to be recommended. However, it might be necessary in some circumstances. Should both medications be prescribed at the same time, your prescribing doctor might amend the dosage of Sitagliptin, or perhaps adjust the regularity with which the doses ought to be taken.

  • Balofloxacin
  • Tosufloxacin
  • Thioctic Acid
  • Sparfloxacin
  • Simeprevir
  • Rufloxacin
  • Prulifloxacin
  • Pefloxacin
  • Pazufloxacin
  • Pasireotide
  • Ofloxacin
  • Octreotide
  • Norfloxacin
  • Nadifloxacin
  • Moxifloxacin
  • Lomefloxacin
  • Levofloxacin
  • Lanreotide
  • Gemifloxacin
  • Gatifloxacin
  • Flumequine
  • Fleroxacin
  • Enoxacin
  • Eliglustat
  • Ciprofloxacin
  • Besifloxacin

Using Sitagliptin at the same tame as taking any of the drugs below can produce an increased chance of you exhibiting particular negative symptoms, but can occasionally be the best way to treat your specific medical condition. If your doctor prescribes both of them together, they may well decide that an adjustment to the dosage, or to the frequency of said dosage, whether that be in reference to sitagliptin alone, or to both drugs at once.

  • Acebutolol
  • Timolol
  • Sotalol
  • Propranolol
  • Practolol
  • Pindolol
  • Penbutolol
  • Oxprenolol
  • Nebivolol
  • Nadolol
  • Metoprolol
  • Metipranolol
  • Levobunolol
  • Labetalol
  • Esmolol
  • Celiprolol
  • Carvedilol
  • Carteolol
  • Bisoprolol
  • Betaxolol
  • Atenolol

Some drugs shouldn't be taken at or around the time when you are eating; or shouldn't be taken when eating certain kinds of food, as negative interactions are known to occur. Such interactions may also present themselves if certain medications are taken whilst using tobacco and/or alcohol products. If concerned about your use of tobacco, alcohol, or food during your course of treatment with Sitagliptin, consult your prescribing doctor.


Whenever you choose to use a certain medicine you need to consider the risk of its usage, compared to the benefits it will bring. This is something to be discussed through consultation with your examining doctor. When prescribed Sitagliptin you ought to consider the following:

Inform your prescribing doctor should you have suffered an allergic, or any other kind of unusual reaction to Sitagliptin, or indeed to any other medication. Your prescribing doctor should also be advised of any other negative or allergic reactions you suffer from. This can include reactions to animals, dyes, foods, or preservatives.

There have been no appropriate studies conducted to determine the relationship between age and the impact of Sitagliptin among the pediatric population. Your prescribing doctor will decide if Sitagliptin is the correct choice for a juvenile patient.

Whilst studies have not shown any problems specific to the geriatric population that would preclude or limit the use of Sitagliptin amongst elderly patients, there is evidence that older patients are often more susceptible to developing kidney problems as a consequence of their age. This could necessitate extra caution, or might require the prescribing doctor to adjust the dosage of Sitagliptin for elderly patients.

No studies have been conducted among women that have demonstrated a risk in the use of Sitagliptin to the fetus during pregnancy.

There have not been sufficient adequate studies conducted among women to determine any risk to the nursing infant whilst using Sitagliptin during breastfeeding. You must always weigh the possible benefits of the medication against its possible risks to your child before deciding to take Sitagliptin whilst breastfeeding.

Take Sitagliptin precisely as your prescribing doctor recommends. You must not take a larger dosage, nor should you take your medication more regularly, nor should you extend your course of treatment with the drug.

Your prescribing doctor will advise just how much sitagliptin you ought to use and how frequently. Your dosage might have to be altered a number of times before your doctor is satisfied with the amount that works best in your situation.

Sitagliptin is normally accompanied by a leaflet that provides the patient with information. Be sure that you read these instructions and that you follow them carefully. Should you have any concerns or questions, be sure to consult your doctor.

Be sure that you follow the specific meal plan that your prescribing doctor will have provided you. This is easily the most significant aspect of controlling the impact of your diabetes, and is essential if you intend the sitagliptin to work as it should. Partake in regular exercise, and take blood and/or urine sugar tests, as directed by your examining doctor.

Sitagliptin may be taken alongside food, or without it.

You should only use the specific brand of Sitagliptin that has been prescribed by your doctor. A different brand might not have the same effect on your condition.

Do not stop taking or interrupt your course of Sitagliptin before consulting your doctor.

It is of the utmost is very important that you have your progress checked by your prescribing doctor on a regular basis. Urine and blood tests might be required at these tests, in order for you doctor to determine any unwanted effects of your medication. The purpose of the test is to ensure that your prescription is correct for your medical need, and whether you ought to continue on this course. Blood and urine tests may be needed to check for unwanted effects.

Sitagliptin can cause any of a number of serious allergic reactions such as anaphylaxis, or angioedema. Likewise, it has been known to induce unwelcome skin conditions, such as Stevens-Johnson syndrome. Such reactions have been known to become life-threatening in some cases, and medical attention should be sought immediately. Consult your doctor as soon as possible, should you develop any of these symptoms during your course of treatment with sitagliptin: swelling of your throat, hands, face, or mouth; difficulty whilst breathing and swallowing; developing chills or a fever; having skin that is itching, loose, peeling, or blistering, or which has come out in a rash.

Pancreatitis (that is, an inflammation or swelling of your pancreas) might present itself during your course of treatment with sitagliptin. Be sure to consult your prescribing doctor as soon as you can should you exhibit light-headedness, fever, loss or lack of appetite, vomiting, nausea, constipation, chills, or severe and sudden pains to the stomach during your course of treatment with sitagliptin.

Using sitagliptin can sometimes cause hypoglycemia (being low levels of blood-sugar). This can occur as well should you miss or delay your meals, indulge in more exercise that normal, consume alcohol, take particular medications, or use sitagliptin alongside other kinds of diabetes medication.

If you start exhibiting reactions that are symptomatic of low blood sugar levels, you must treat the condition quickly, so that you do not lapse into unconsciousness. Since some patients show reactions that are different to others when their blood sugar drops, it becomes important to know precisely what your reaction to a hypoglycemic attack is, so that an onset of symptoms may be treated swiftly.

If you do exhibit the symptoms of hypoglycemia, you must check the level of your blood sugar. If your levels are low, you should drink a sugar/water solution, some fruit juice, or a non-diet soda. Alternatively, you can eat some honey, sugar cubes, or corn syrup, or commercially available glucose tablets, or gel. A glucagon kit is recommended should you suffer from extreme symptoms (including convulsions (seizures) or loss of consciousness. Glucagon is used for emergency situations, and is administered via a needle and syringe. Be sure that a family member is aware of how to us the glucagon kit correctly, in case such symptoms should present themselves.

Certain medical issues sometimes affect the efficacy of Sitagliptin. Your prescribing doctor should always be aware of any other medical complaints you might have, particularly if they belong to the list below.

Sitagliptin should only be used with caution in patients who suffer from the conditions listed below:

  • Excessive use of alcohol
  • Gallbladder stones
  • Hypercholesterolemia (high levels of cholesterol in a patient's blood)
  • Hypertriglyceridemia (high levels or fats or triglycerides in a patient's blood)
  • History of pancreas problems.

This is because its use can increase the risk of contracting pancreatitis (that is, a painful inflammation and swelling of the pancreas).

Sitagliptin should also be used with caution in patients who has a history of angioedema (that is, a swelling to the legs, arm, throat, tongue, lips, or face) when using Sitagliptin, or any other type of DPP4 (dipeptidyl peptidase-4) inhibitor, as its used can increase the possibility of the condition recurring in the patient.

Sitagliptin should not be prescribed under any circumstances to patients who suffer from any of the conditions listed below:

  • Diabetic ketoacidosis (that is, high acid and ketones in a patient's blood)
  • Type 1 Diabetes

The effects of Sitagliptin might be increased among patients suffering from severe or moderate kidney disease, owing to the reduced rate at which it is removed from the body. As such, it is recommended that sitaglipin is only use with caution.


Sitagliptin ought to be kept in a secure container. It should be kept from freezing at all times, and stored at room temperature. Ensure that you keep your supply of Sitagliptin out of the way of direct light, heat, and moisture. Sitagliptin should never be kept within the reach of children.

If you no longer require your Sitagliptin solution, or should it be out of date, please dispose of it.
Before disposing of your sitagliptin solution, speak to your prescribing doctor on how best to do so safely.


Sitagliptin is an antihyperglycemic drug (that is, a form of antidiabetic medication) and DPP-4 inhibitor that promotes greater levels of insulin production in the patient's pancreas, as well as a reduction of glucose production in the patient's liver. It can be prescribed on its own, or concurrently with other diabetes treatments, alongside a wellness plan of good diet and regular exercise to combat the impact of Type 2 diabetes.


Last Reviewed:
January 30, 2018
Last Updated:
February 10, 2018