How does this medication work? What will it do for me?

This is a combination medication that contains 2 active ingredients: sitagliptin and metformin. They are used together, along with diet and exercise, to improve blood glucose (sugar) levels for adults with type 2 diabetes. Sitagliptin – metformin may be used in addition to other diabetes medications to reduce blood sugar levels, when other medications haven’t provided adequate control.

Sitagliptin belongs to the group of medications called DPP-4 inhibitors. It works by increasing the amount of incretin released by the intestine. Incretin is a hormone that raises insulin levels when blood glucose is high and decreases the amount of glucose made by the body. Metformin belongs to the group of medications called biguanides. It works by reducing the amount of glucose made by the liver and by making it easier for glucose to enter into the tissues of the body.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

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What form(s) does this medication come in?

50 mg/500 mg
Each light pink, capsule-shaped, film-coated tablet with "575" debossed on one side contains sitagliptin phosphate monohydrate 64.25 mg equivalent to sitagliptin 50 mg as free base, and metformin hydrochloride 500 mg. Nonmedicinal ingredients: microcrystalline cellulose, polyvinylpyrrolidone, sodium lauryl sulfate, and sodium stearyl fumarate; film coating: black iron oxide, polyvinyl alcohol, polyethylene glycol, red iron oxide, talc, and titanium dioxide.

50 mg/850 mg
Each pink, capsule-shaped, film-coated tablet with "515" debossed on one side contains sitagliptin phosphate monohydrate 64.25 mg equivalent to sitagliptin 50 mg as free base, and metformin hydrochloride 850 mg. Nonmedicinal ingredients: microcrystalline cellulose, polyvinylpyrrolidone, sodium lauryl sulfate, and sodium stearyl fumarate; film coating: black iron oxide, polyvinyl alcohol, polyethylene glycol, red iron oxide, talc, and titanium dioxide.

50 mg/1000 mg
Each red, capsule-shaped, film-coated tablet with "577" debossed on one side contains sitagliptin phosphate monohydrate 64.25 mg equivalent to sitagliptin 50 mg as free base, and metformin hydrochloride 1,000 mg. Nonmedicinal ingredients: microcrystalline cellulose, polyvinylpyrrolidone, sodium lauryl sulfate, and sodium stearyl fumarate; film coating: black iron oxide, polyvinyl alcohol, polyethylene glycol, red iron oxide, talc, and titanium dioxide.

How should I use this medication?

The initial dose of sitagliptin - metformin is based on the dose of each medication that is currently being taken. Your doctor will determine the dose that is appropriate for you. This medication should be taken twice a day with meals. The maximum dose of sitagliptin is 100 mg per day and the maximum dose of metformin is 2,000 mg per day.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important that this medication be taken exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

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Who should NOT take this medication?

Do not take sitagliptin - metformin if you:

  • are allergic to sitagliptin, metformin, or any ingredients of the medication
  • are breast-feeding
  • are pregnant or planning to become pregnant
  • are severely dehydrated
  • drink a lot of alcohol in a short term or on a regular basis
  • have cardiovascular collapse (sudden failure of blood circulation) or cardio-respiratory insufficiency (reduced oxygen supply to tissues)
  • have metabolic acidosis (including diabetic ketoacidosis) or a history of ketoacidosis or lactic acidosis (too much acid in the blood)
  • have or are recovering from a severe infection, trauma, or surgery
  • have poor blood glucose control or insulin-dependent (Type 1) diabetes mellitus
  • have reduced kidney function or kidney disease
  • have severely reduced liver function or liver disease
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What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • bloating
  • constipation
  • diarrhea
  • headache
  • loss of appetite
  • metallic taste in mouth
  • nausea
  • passing of gas
  • sore throat
  • stomach upset
  • stuffy or runny nose
  • vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • signs of kidney failure (e.g., decreased urine production, swelling, fatigue, abdominal pain, nausea, loss of appetite)
  • signs of pancreatitis (e.g., abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat, swollen abdomen)
  • symptoms of mildly low blood sugar (e.g., anxiety, difficulty concentrating, nausea, cold sweat, cool pale skin, headache, fast heartbeat, weakness, shakiness)

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • signs of lactic acidosis (e.g., nausea, vomiting, increased breathing rate, abdominal pain, unusual tiredness, dizziness, rapid heart rate, muscle pain or cramping, feeling cold)
  • symptoms of a severe allergic reaction (e.g., hives, difficulty breathing or swallowing, swelling of the face, lips, tongue, or throat)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

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Are there any other precautions or warnings for this medication?

Before you begin taking a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Alcohol intake: Large amounts of alcohol or regular use of alcohol increases the risk of developing lactic acidosis when taking metformin. People taking this medication should avoid excessive alcohol intake.

Blood glucose control: People taking this medication who have a fever, experience trauma, or have surgery may experience a temporary loss of blood glucose control. At such times, it may be necessary to stop this medication and temporarily inject insulin. This medication may be started again after the problem is resolved.

Congestive heart failure (CHF): Congestive heart failure can increase the risk of lactic acidosis caused by metformin. For this reason, this medication is not recommended for people with CHF. If you have CHF, speak to your doctor.

Diabetes complications: The use of this medication will not prevent the development of complications of diabetes mellitus (e.g., kidney disease, nerve disease, eye disease).

Dye or contrast agents: If you are going to have an X-ray procedure that uses dye or a contrast agent, you may need to stop taking this medication for a short time. Contact your doctor for instructions.

Kidney function: Kidney disease or reduced kidney function may cause metformin or sitagliptin to build up in the body, causing side effects. If you have reduced kidney function or kidney disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Sitagliptin may cause decreased kidney function, including kidney failure. Your doctor may recommend regular testing to check your kidney function while you are taking this medication. This medication is not recommended for people with reduced kidney function.

Lactic acidosis: Lactic acidosis is a rare but serious problem that occurs due to metformin accumulation (i.e., the body doesn't get rid of the medication fast enough) during treatment. People with severe kidney disease, heart failure, or dehydration are at higher risk of developing lactic acidosis. Since alcohol may increase the risk of lactic acidosis, do not drink a lot of alcohol over the short or long term while taking this medication. When it does occur (very rarely), it is fatal in 50% of cases. If you experience symptoms of lactic acidosis (e.g., weakness; tiredness; drowsiness; unusual muscle pain; trouble breathing; stomach pain with nausea, vomiting, or diarrhea; feeling cold; dizziness; lightheadedness; slow or irregular heartbeat), stop taking this medication and get immediate medical attention.

Liver function: This medication is not recommended for people with severely reduced liver function. If you have moderately reduced liver function, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Low blood glucose: Under usual circumstances, low blood glucose does not occur for people who take this medication. Low blood glucose could occur when not enough food is eaten, especially when strenuous exercise is undertaken at the same time or when large amounts of alcohol have been consumed. If you experience low blood sugar (e.g., headache, drowsiness, weakness, dizziness, confusion, irritability, hunger, fast heartbeat, sweating, and feeling jittery) while taking this medication, contact your doctor.

Pancreatitis: This medication may cause pancreatitis (inflammation of the pancreas). If you have a history of pancreatitis, gallstones, alcoholism, or high triglycerides you may be more at risk of experiencing this. If you experience prolonged and severe abdominal pain with or without vomiting while taking this medication, contact your doctor immediately.

Reduced response: Over a period of time, people may become progressively less responsive to a particular treatment for diabetes because their diabetes worsens. If your blood glucose control worsens or you are not staying within your target levels, talk to your doctor.

Surgery: This medication should be stopped temporarily for surgery (except for minor surgery where food and fluid intake is not restricted). You will be restarted on this medication once you are eating and drinking and your kidney function has been tested and is normal. Talk to your doctor for specific instructions.

Vitamin B12 levels: This medication may decrease vitamin B12 levels. Your doctor will monitor your B12 levels with blood tests while you are taking this medication.

Pregnancy: This medication is not recommended for use during pregnancy or for women who are planning to become pregnant. If you become pregnant while taking this medication, contact your doctor immediately. Insulin is usually used during pregnancy to control blood glucose levels.

Breast-feeding: It is not known if sitagliptin - metformin passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. This medication should not be used by women who are breast-feeding.

Children: The safety and effectiveness of this medication have not been established for children less than 18 years of age.

Seniors: Kidney function often decreases with age. As a result, seniors may be more likely to experience side effects of this medication.

What other drugs could interact with this medication?

There may be an interaction between sitagliptin - metformin and any of the following:

  • abiraterone
  • acetazolamide
  • alcohol
  • amiodarone
  • angiotensin converting enzyme inhibitors (ACEIs; captopril, enalapril, ramipril)
  • "azole" antifungals (e.g., fluconazole, itraconazole, ketoconazole, voriconazole)
  • β2-agonists (e.g., salbutamol, formoterol)
  • birth control pills
  • bupropion
  • carbamazepine
  • carvedilol
  • cephalexin
  • cimetidine
  • inhaled corticosteroids (e.g., budesonide, ciclesonide, fluticasone)
  • oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
  • crizotinib
  • cyclosporine
  • danazol
  • darunavir
  • other diabetes medications (e.g., chlorpropamide, glipizide, glyburide, insulin, metformin, nateglinide, rosiglitazone)
  • digoxin
  • dipyridamole
  • diuretics (water pills; e.g., hydrochlorothiazide, furosemide, amiloride, triamterene)
  • dofetilide
  • doxorubicin
  • dronedarone
  • estrogens (e.g., conjugated estrogen, estradiol, ethinyl estradiol)
  • everolimus
  • goserelin
  • glycopyrrolate
  • grapefruit juice
  • HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
  • iodinated contrast material
  • isoniazid
  • lamotrigine
  • leuprolide
  • macrolide antibiotics (e.g., clarithryomycin, erythromycin)
  • mefloquine
  • methyltestosterone
  • monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
  • nefazodone
  • nandrolone
  • nicotinic acid
  • nilotinib
  • octreotide
  • phenothiazines (e.g., chlorpromazine, promethazine)
  • phenytoin
  • progesterone
  • propanolol
  • quinidine
  • quinine
  • quinolone antibiotics (e.g., ciprofloxacin, levofloxacin, moxifloxacin)
  • reserpine
  • rifampin
  • St. John's wort
  • salicylates (e.g., ASA)
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
  • somatropin
  • "statin" anti-cholesterol medications (e.g., atorvastatin, lovastatin, simvastatin)
  • sulfonamides (e.g., sulfamethoxazole)
  • sulfonylureas (e.g., glyburide, gliclazide)
  • sympathomimetics (e.g., phenylephrine, pseudoephedrine)
  • tacrolimus
  • tamoxifen
  • telaprevir
  • tenofovir
  • testosterone
  • topiramate
  • trazodone
  • trimethoprim
  • verapamil
  • vinblastine

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.