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Sitagliptin and metformin (Oral)

met-FOR-min hye-droe-KLOR-ide, sit-a-GLIP-tin FOS-fate

Oral route(Tablet;Tablet, Extended Release)

Postmarketing cases of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. Symptoms included malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Laboratory abnormalities included elevated blood lactate levels, anion gap acidosis, an increased lactate/pyruvate ratio, and metformin plasma levels generally greater than 5 mcg/mL. Risk factors include renal impairment, concomitant use of certain drugs (eg, carbonic anhydrase inhibitors), age 65 years old or greater, radiological studies with contrast, surgery and other procedures, hypoxic states, excessive alcohol intake, and hepatic impairment. If lactic acidosis is suspected, immediately discontinue metformin hydrochloride/sitagliptin phosphate and institute general supportive measures in a hospital setting; prompt hemodialysis is recommended .

Medically reviewed on June 7, 2018

Commonly used brand name(s)

In the U.S.

  • Janumet
  • Janumet XR

Available Dosage Forms:

  • Tablet, Extended Release
  • Tablet

Therapeutic Class: Antidiabetic

Pharmacologic Class: Sitagliptin

Chemical Class: Metformin

Uses For This Medicine

Metformin and sitagliptin combination is used to treat high blood sugar levels caused by type 2 diabetes. Metformin reduces the absorption of sugar from the stomach, reduces the release of stored sugar from the liver, and helps your body use sugar better. Sitagliptin helps to control blood sugar levels by increasing substances in the body that make the pancreas release more insulin. It also signals the liver to stop producing sugar (glucose) when there is too much sugar in the blood. Sitagliptin and metformin does not help patients who have insulin-dependent or type 1 diabetes.

Sitagliptin and metformin is available only with your doctor's prescription.

Before Using This Medicine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For sitagliptin and metformin, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to sitagliptin and metformin or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of metformin and sitagliptin combination in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of metformin and sitagliptin combination in the elderly. However, elderly patients are more likely to have age-related kidney problems, which may require caution and an adjustment in the dose for patients receiving metformin and sitagliptin combination.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking sitagliptin and metformin, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using sitagliptin and metformin with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Acetrizoic Acid
  • Diatrizoate
  • Ethiodized Oil
  • Iobenzamic Acid
  • Iobitridol
  • Iocarmic Acid
  • Iocetamic Acid
  • Iodamide
  • Iodipamide
  • Iodixanol
  • Iodohippuric Acid
  • Iodopyracet
  • Iodoxamic Acid
  • Ioglicic Acid
  • Ioglycamic Acid
  • Iohexol
  • Iomeprol
  • Iopamidol
  • Iopanoic Acid
  • Iopentol
  • Iophendylate
  • Iopromide
  • Iopronic Acid
  • Ioseric Acid
  • Iosimide
  • Iotasul
  • Iothalamate
  • Iotrolan
  • Iotroxic Acid
  • Ioxaglate
  • Ioxitalamic Acid
  • Ipodate
  • Metrizamide
  • Metrizoic Acid
  • Tyropanoate Sodium

Using sitagliptin and metformin with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Acarbose
  • Aspirin
  • Balofloxacin
  • Besifloxacin
  • Bupropion
  • Chlorpropamide
  • Ciprofloxacin
  • Dasabuvir
  • Dofetilide
  • Dolutegravir
  • Eliglustat
  • Enoxacin
  • Fleroxacin
  • Flumequine
  • Gatifloxacin
  • Gemifloxacin
  • Glimepiride
  • Glipizide
  • Glyburide
  • Ioversol
  • Lanreotide
  • Levofloxacin
  • Lomefloxacin
  • Metformin
  • Moxifloxacin
  • Nadifloxacin
  • Nateglinide
  • Norfloxacin
  • Octreotide
  • Ofloxacin
  • Ombitasvir
  • Paritaprevir
  • Pasireotide
  • Pazufloxacin
  • Pefloxacin
  • Pioglitazone
  • Prulifloxacin
  • Repaglinide
  • Ritonavir
  • Rufloxacin
  • Simeprevir
  • Sitagliptin
  • Sparfloxacin
  • Thioctic Acid
  • Tolazamide
  • Tolbutamide
  • Tosufloxacin
  • Vandetanib

Using sitagliptin and metformin with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Acebutolol
  • Atenolol
  • Betaxolol
  • Bisoprolol
  • Bitter Melon
  • Carteolol
  • Carvedilol
  • Celiprolol
  • Esmolol
  • Fenugreek
  • Furazolidone
  • Glucomannan
  • Guar Gum
  • Iproniazid
  • Isocarboxazid
  • Labetalol
  • Levobunolol
  • Linezolid
  • Methylene Blue
  • Metipranolol
  • Metoprolol
  • Moclobemide
  • Nadolol
  • Nebivolol
  • Nialamide
  • Oxprenolol
  • Patiromer
  • Penbutolol
  • Phenelzine
  • Pindolol
  • Practolol
  • Procarbazine
  • Propranolol
  • Psyllium
  • Ranolazine
  • Rasagiline
  • Rifampin
  • Safinamide
  • Selegiline
  • Sotalol
  • Timolol
  • Tranylcypromine
  • Verapamil

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Other Medical Problems

The presence of other medical problems may affect the use of sitagliptin and metformin. Make sure you tell your doctor if you have any other medical problems, especially:

  • Alcohol, excessive use or
  • Congestive heart failure, acute or unstable or
  • Dehydration, severe or
  • Heart attack, acute or
  • Heart or blood vessel problems or
  • Hypoxemia (decreased oxygen in the blood) or
  • Liver disease or
  • Poorly nourished condition or
  • Sepsis (severe infection) or
  • Shock (low blood pressure, poor blood circulation) or
  • Weakened physical condition—Use with caution. May increase risk of serious side effects.
  • Anemia (low blood cells) or
  • Kidney disease or
  • Vitamin B12 deficiency—Use with caution. May make these conditions worse.
  • Angioedema (swelling of the face, lips, tongue, throat, arms, or legs), history with this medication or other dipeptidyl peptidase-4 (DPP-4) inhibitors—Use with caution. May increase the risk of this condition occurring again.
  • Diabetic ketoacidosis or metabolic acidosis (high ketones and acid in the blood) or
  • Kidney disease, severe or
  • Type 1 diabetes—Should not be used in patients with these conditions.
  • Fever or
  • Infection of any type or
  • Surgery (major) or
  • Trauma—These conditions may cause temporary problems with blood sugar control and your doctor may treat you with insulin.
  • Heart failure, history of or
  • Kidney damage, history of—May increase risk for heart failure.
  • Hypercholesterolemia (high cholesterol in the blood) or
  • Hypertriglyceridemia (high triglycerides and fats in the blood) or
  • Obesity or
  • Pancreas problems, history of—Use with caution. May increase risk for pancreatitis (swelling of the pancreas).
  • Radiologic procedures (eg, X-rays, CT scans, and MRIs) that require dyes to be injected into your vein—Sitagliptin and metformin should be stopped before you have one of these procedures.

Proper Use of This Medicine

Take sitagliptin and metformin exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects.

Sitagliptin and metformin should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

Metformin and sitagliptin combination should be taken with meals to help reduce any stomach upset. Take the extended-release tablets as directed in the evening.

Swallow the extended-release tablet or immediate-release tablet whole. Do not crush, break, or chew it.

Carefully follow the special meal plan your doctor gave you. This is the most important part of controlling your diabetes, and is necessary if the medicine is to work properly. Exercise regularly and test for sugar in your blood or urine as directed.

While taking Janumet® XR, you may see tablets in your stools. If you see tablets in your stool several times, tell your doctor right away. Do not stop taking sitagliptin and metformin without checking first with your doctor.

Dosing

The dose of sitagliptin and metformin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of sitagliptin and metformin. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For type 2 diabetes:
    • For oral dosage form (extended-release tablets):
      • For patients taking metformin alone:
        • Adults—At first, 100 milligrams (mg) of sitagliptin, plus the dose of metformin already being taken once a day. Your doctor may gradually increase your dose until your blood sugar is controlled. If you are taking 850 or 1000 mg of immediate-release metformin 2 times per day, you may start with two 50 mg sitagliptin tablets and 1000 mg of metformin taken together once a day.
        • Children—Use and dose must be determined by your doctor.
      • For patients taking sitagliptin alone:
        • Adults—At first, 100 milligrams (mg) of sitagliptin and 1000 mg of metformin once a day. Your doctor may gradually increase your dose until your blood sugar is controlled. However, the dose is usually not more than 100 mg of sitagliptin and 2000 mg of metformin once a day.
        • Children—Use and dose must be determined by your doctor.
      • For patients using Janumet® immediate-release tablets:
        • Adults—The dose is the same as the dose you are already taking. Your doctor may gradually increase your dose until your blood sugar is controlled. However, the dose is usually not more than 100 mg of sitagliptin and 2000 mg of metformin once a day.
        • Children—Use and dose must be determined by your doctor.
    • For oral dosage form (immediate-release tablets):
      • For patients taking metformin alone:
        • Adults—At first, 50 milligrams (mg) of sitagliptin, plus the dose of metformin already being taken, 2 times per day. Your doctor may gradually increase your dose until your blood sugar is controlled. If you are taking 850 mg of metformin 2 times per day, you may start with 50 mg of sitagliptin and 1000 mg of metformin 2 times per day.
        • Children—Use and dose must be determined by your doctor.
      • For patients taking sitagliptin alone:
        • Adults—At first, 50 milligrams (mg) of sitagliptin and 500 mg of metformin two times per day. Your doctor may gradually increase your dose until your blood sugar is controlled. However, the dose is usually not more than 50 mg of sitagliptin and 1000 mg of metformin two times per day.
        • Children—Use and dose must be determined by your doctor.
      • For patients using metformin and sitagliptin together as separate tablets:
        • Adults—The dose is the same as the dose you are already taking. Your doctor may gradually increase your dose until your blood sugar is controlled.
        • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of sitagliptin and metformin, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine

It is very important that your doctor check your progress at regular visits, especially during the first few weeks that you take sitagliptin and metformin. Blood and urine tests may be needed to check for unwanted effects.

Under certain conditions, too much metformin can cause lactic acidosis. The symptoms of lactic acidosis are severe and appear quickly. It usually occurs when other serious health problems are present, such as a heart attack or kidney failure. Symptoms of lactic acidosis include: abdominal or stomach discomfort, decreased appetite, diarrhea, fast, shallow breathing, a general feeling of discomfort, muscle pain or cramping, and unusual sleepiness, tiredness, or weakness. If you have more than one of these symptoms together, you should get emergency medical help right away.

Sitagliptin and metformin may cause hypoglycemia (low blood sugar). This is more common when sitagliptin and metformin is taken together with certain medicines. Low blood sugar must be treated before it causes you to pass out (unconsciousness). People feel different symptoms of low blood sugar. It is important that you learn which symptoms you usually have so you can treat it quickly. Talk to your doctor about the best way to treat low blood sugar.

Hyperglycemia (high blood sugar) may occur if you do not take enough or skip a dose of your medicine, overeat or do not follow your meal plan, have a fever or infection, or do not exercise as much as usual. High blood sugar can be very serious and must be treated right away. It is important that you learn which symptoms you have in order to treat it quickly. Talk to your doctor about the best way to treat high blood sugar.

There may be a time when you need emergency help for a problem caused by your diabetes. You need to be prepared for these emergencies. It is a good idea to wear a medical identification (ID) bracelet or neck chain at all times. Also, carry an ID card in your wallet or purse that says you have diabetes and a list of all your medicines.

Pancreatitis may occur while you are using sitagliptin and metformin. Check with your doctor right away if you have a sudden and severe stomach pain, chills, constipation, nausea, vomiting, loss of appetite, fever, or lightheadedness.

Check with your doctor right away if you have more than one of these symptoms: chest pain, decreased urine output, dilated neck veins, extreme fatigue, irregular breathing, irregular heartbeat, shortness of breath, swelling of the face, fingers, feet, or lower legs, tightness in the chest, trouble breathing, or weight gain. These may be signs of heart failure.

Sitagliptin and metformin may cause serious allergic reactions, including anaphylaxis, angioedema, or certain skin conditions (Stevens-Johnson syndrome). These reactions can be life-threatening and require immediate medical attention. Call your doctor right away if you have a rash, itching, blistering, peeling, or loosening of the skin, fever or chills, trouble breathing or swallowing, or any swelling of your hands, face, mouth, or throat while you are using sitagliptin and metformin.

Sitagliptin and metformin may cause severe and disabling joint pain. Call your doctor right away if you have severe joint pain while using sitagliptin and metformin.

Sitagliptin and metformin may cause bullous pemphigoid. Tell your doctor if you have large, hard skin blisters while using sitagliptin and metformin.

Let your doctor or dentist know that you are taking sitagliptin and metformin. Your doctor may advise you to temporarily stop taking sitagliptin and metformin before you have major surgery or diagnostic tests, including procedures that use contrast dye.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

This Medicine Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common

  • Anxiety
  • blurred vision
  • chills
  • cold sweats
  • confusion
  • cool, pale skin
  • depression
  • dizziness
  • fast heartbeat
  • headache
  • increased hunger
  • loss of consciousness
  • mental cloudiness
  • nausea
  • nightmares
  • not thinking clearly
  • seizures
  • shakiness
  • slurred speech
  • unusual tiredness or weakness

Rare

  • Decreased appetite
  • diarrhea
  • fast, shallow breathing
  • general feeling of discomfort
  • muscle pain or cramping
  • sleepiness
  • stomach discomfort

Incidence not known

  • Blistering, peeling, or loosening of the skin
  • darkened urine
  • hives or welts, itching, or skin rash
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • loss of appetite
  • pains in the stomach, side, or abdomen, possibly radiating to the back
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • red skin lesions, often with a purple center
  • severe joint pain
  • sores, ulcers, or white spots in the mouth or on the lips
  • vomiting
  • yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Bloated or feeling of fullness
  • excess air or gas in the stomach or intestines
  • indigestion
  • lack or loss of strength
  • muscle aches
  • passing gas
  • sore throat
  • stuffy or runny nose
  • vomiting

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Side effects (in more detail)

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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