Sitagliptin and Metformin (Oral)

The drug combination of sitagliptin and metformin is used to treat patients with high blood sugar levels.

Overview

The drug combination of metformin and sitagliptin is used to treat Type 2 Diabetes sufferers who have high blood sugar levels. This medication is not effective in treating people who have insulin-dependent Type 1 Diabetes. This drug will most likely form part of a lifestyle change program that will include a change in your diet and an exercise regimen for you to adhere to.

Both of the constituents of the medication work by increasing the levels of incretins that the body naturally produces. Incretins help to control the amount of insulin produced by your body.

The metformin component of the drug causes a reduction of the sugar that is absorbed from food in the patient’s stomach. It also reduces the amount of stored sugar that is released from the liver. Both these functions enable the body to make more efficient use of the sugar it contains. Sitagliptin also works to control the levels of sugar in the blood by stimulating the production of insulin by the pancreas. When blood sugar levels become dangerously high, sitagliptin instructs the liver to stop releasing glucose into the bloodstream.

In the US, this medication is sold under the brand names Janumet and Janumet XR. Both these drugs are only available via a prescription from a medical professional. Metformin and sitagliptin combination are prescribed in either extended-release tablet or ordinary tablet form.

Conditions Treated

  • Type 2 Diabetes
  • High blood sugar

Type of medicine

  • Tablet
  • Extended-release tablet

Side Effects

There are some patients who do notice a few unpleasant side effects while being treated with metformin and sitagliptin combination. Not everyone experiences undesirable effects, but if you do notice anything out of the ordinary after you begin taking your medicine, you should consult your treating physician, as more medical attention might be needed.

The following effects are sometimes reported by patients taking metformin and sitagliptin combination. These effects must be mentioned to your doctor straight away:

  • White spots, ulcers or sores in the mouth or on the lips
  • Vomiting
  • Very painful joints
  • Unusual tiredness or weakness
  • Stomach pains, side pains, or pains in the abdomen, sometimes radiating round to your back
  • Slurred speech
  • Sleepiness
  • Skin rashes, hives, itching or welts
  • Shortness of breath
  • Shakiness
  • Seizures
  • Red skin lesions, sometimes with purple centers
  • Puffiness or swelling around the eyes, or eyelids, face, lips, or tongue
  • Poor appetite
  • Peeling, blisters, or patches of loose skin
  • Not thinking clearly
  • Nightmares
  • Nausea
  • Muscle pain or cramp
  • Loss of consciousness
  • Large swellings on the eyelids, face, lips, throat, tongue, legs, hands, feet, or genitalia
  • Jaundice
  • Increased hunger
  • Headache
  • General feeling of discomfort
  • Fast, shallow breathing
  • Fast heartbeat
  • Dizziness
  • Diarrhea
  • Depression
  • Decreased appetite
  • Dark urine
  • Cool, pale skin
  • Confusion
  • Cold sweats
  • Chills
  • Blurred vision
  • Anxiety
  • Abdominal or stomach pain

Some unpleasant side effects are quite common in people taking sitagliptin and metformin, but they will resolve naturally once the body gets used to the new drug. Your GP or nurse will give you some ideas on how you can manage these unwanted effects:

  • Vomiting
  • Stuffy or runny nose
  • Sore throat
  • Passing gas
  • Muscle aches
  • Lack or loss of strength
  • Indigestion
  • Excess air or gas in the stomach or intestines
  • Bloated or full feeling

There may be some other side effects that you experience that are not listed here. If the effects do not go away within a couple of weeks of taking the new drug, consult your doctor.

Serious allergic reactions to this drug are uncommon, however, you should be aware of the signs of anaphylaxis. Anaphylaxis is a potentially fatal condition and its symptoms include the following:

  • A skin rash
  • Itching or swelling sensations, especially of the tongue, face, or throat
  • Severe dizziness
  • Breathing problems

Usually, the symptoms of anaphylactic shock appear within a few minutes of the medication being taken. If you think that you or someone else is anaphylactic, call 911 immediately.

Dosage

When you receive your first supply of sitagliptin and metformin, you will be given a patient medication guide. Read this information thoroughly so that you understand how to use the drug. If there is anything that you do not understand, ask your GP or pharmacist for further information.

You must only use your prescription of sitagliptin and metformin as directed by your medical professional. Do not take more of the drug than you have been prescribed. Do not use the drug more often than your doctor has directed. Do not continue using the medicine for a longer duration than your GP tells you to. Exceeding the prescribed dose can exacerbate any side effects that you may experience.

The amount of this medicine and the frequency of use that you are prescribed will probably be different to that given to other patients. Follow your doctor’s directions or the instructions that are given on the product label. The following dosage information is the average for this drug. If the instructions that you have been given are different, do not change your dose unless your doctor tells you to.

If you forget your medication, you must try to take it as soon as possible. If the time of the next dose is nearly due, you should omit the dose that you missed and go back to your usual dosage schedule. Do not take twice the prescribed dose to make up for a dose that you have missed.

Do not share your prescription with another patient.

If you begin to feel worse or if you do not think there has been a significant improvement in your condition, consult your GP promptly.

If you or someone else has taken an overdose of sitagliptin and metformin, they may lose consciousness, or complain of breathing difficulties and a shortness of breath. If you think that an overdose has occurred, call 911 immediately or contact your local poison control centre.

The medication should be taken at meal times in order to reduce the likelihood of you suffering a stomach upset. The extended-release tablets should be taken in the evenings. When taking either form of tablet, do not crush, chew or break them first; try to swallow them in one piece.

You must follow the diet plan that your treating physician gave you. This is necessary to control your diabetes and also ensures that the medication works properly. Take regular exercise, and remember to carry out blood or urine tests as instructed by your GP so that you can keep a check on your blood sugar levels.

If you are prescribed Janumet XR, you may notice tablets in your stools. If you notice this has happened a few times, tell your doctor immediately.

Do not suddenly stop taking the medication unless you are instructed to do so by your doctor.

For the treatment of type 2 diabetes (extended-release tablets) metformin alone:

  • Adults: to begin with, take 100 mg of sitagliptin once daily, in addition to the dose of metformin that you are already taking. This dose may be increased until your doctor is happy that your blood sugar is under control. Patients taking 850 mg or 1000 mg of immediate-release metformin twice daily may begin with two 50 mg sitagliptin tablets and 100 mg of metformin as once treatment, taken once daily.
  • Children: The use and dose of this drug is to be determined by your GP.

For the treatment of type 2 diabetes sitagliptin alone:

  • Adults: to begin with, take 100 mg of sitagliptin and 1000 mg of metformin once daily. This dose may be increased until your doctor is happy that your blood sugar is under control. The maximum dose does generally not exceed 100 mg sitagliptin and 2000 mg of metformin once daily.
  • Children: The use and dose of this drug is to be determined by your GP.

For the treatment of type 2 diabetes Janumet immediate-release tablets:

  • Adults: the dose you are currently taking will remain the same. This dose may be increased until your doctor is happy that your blood sugar is under control. The maximum dose does not generally exceed 100 mg of sitagliptin and 2000 mg of metformin once daily.
  • Children: The use and dose of this drug is to be determined by your GP.

For the treatment of type 2 diabetes (immediate-release tablets) metformin alone:

  • Adults: to begin with, take 50 mg of sitagliptin, in addition to the dose of metformin that you are already taking, twice daily. This dose may be increased until your doctor is happy that your blood sugar is under control. Patients taking 850 mg of metformin twice daily may begin with two 50 mg sitagliptin tablets and 1000 mg of metformin as one treatment, taken once daily.
  • Children: The use and dose of this drug is to be determined by your GP.

For the treatment of type 2 diabetes sitagliptin alone:

  • Adults: to begin with, take 50 mg of sitagliptin and 500 mg of metformin twice daily. This dose may be increased until your doctor is happy that your blood sugar is under control. The maximum dose does generally not exceed 50 mg sitagliptin and 1000 mg of metformin twice daily.
  • Children: The use and dose of this drug is to be determined by your GP.

For the treatment of type 2 diabetes metformin and sitagliptin as separate tablets but taken together:

  • Adults: the dose remains the same as your current dose. This dose may be increased until your doctor is happy that your blood sugar is under control.
  • Children: The use and dose of this drug is to be determined by your GP.

Interactions

Some medicines cannot be used together because this could change the way in which or the other drug works. There may also be an increased risk of you experiencing unpleasant or serious side effects. However, in some cases, your GP may decide to use two different drugs at the same time, even though an interaction may occur. In these circumstances, your GP may suggest altering the dose of one or both of your drugs.

There are a number of commonly used drugs that may interact with sitagliptin and metformin. It is not usually advisable to use following drugs with sitagliptin and metformin, although your doctor may decide to do so if appropriate and beneficial to your course of treatment:

  • Vandetanib
  • Tyropanoate Sodium
  • Tosufloxacin
  • Thioctic Acid
  • Sparfloxacin
  • Simeprevir
  • Rufloxacin
  • Ritonavir
  • Prulifloxacin
  • Pefloxacin
  • Pazufloxacin
  • Pasireotide
  • Paritaprevir
  • Ombitasvir
  • Ofloxacin
  • Octreotide
  • Norfloxacin
  • Nadifloxacin
  • Moxifloxacin
  • Metrizoic Acid
  • Metrizamide
  • Lomefloxacin
  • Levofloxacin
  • Lanreotide
  • Ipodate
  • Ioxitalamic Acid
  • Ioxaglate
  • Ioversol
  • Iotroxic Acid
  • Iotrolan
  • Iothalamate
  • Iotasul
  • Iosimide
  • Ioseric Acid
  • Iopronic Acid
  • Iopromide
  • Iophendylate
  • Iopentol
  • Iopanoic Acid
  • Iopamidol
  • Iomeprol
  • Iohexol
  • Ioglycamic Acid
  • Ioglicic Acid
  • Iodoxamic Acid
  • Iodopyracet
  • Iodohippuric Acid
  • Iodixanol
  • Iodipamide
  • Iodamide
  • Iocetamic Acid
  • Iocarmic Acid
  • Iobitridol
  • Iobenzamic Acid
  • Gemifloxacin
  • Gatifloxacin
  • Flumequine
  • Fleroxacin
  • Ethiodized Oil
  • Enoxacin
  • Eliglustat
  • Dolutegravir
  • Dofetilide
  • Diatrizoate
  • Dasabuvir
  • Ciprofloxacin
  • Bupropion
  • Besifloxacin
  • Balofloxacin
  • Aspirin
  • Acetrizoic Acid

Sitagliptin and metformin combination, when used with any of the following drugs, can increase the risk of some side effects. However, your GP may decide to do so if this is the best course of treatment for you. The dose and frequency of one or more of the drugs may be altered, depending on how your body reacts to the treatment.

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

Some drugs can interact with certain types of food, with tobacco products, or with alcohol. Check with your doctor if any of these interactions apply when using sitagliptin and metformin.

Warnings

While you are taking sitagliptin and metformin, you must see your GP regularly for progress checks. These visits are important as they allow your doctor to make sure that your treatment is working, and to make any necessary adjustments to the dose of medicine that you are taking. You can also use these appointments to talk about any unpleasant effects that you may be experiencing. You will also be required to have blood and urine tests so that your GP can check your blood sugar levels.

Before you your course of treatment with sitagliptin and metformin combination, you must tell your GP if you are already using any other forms of medication. This includes herbal remedies, non-prescription drugs, and vitamin supplements. You should also tell your GP if you have any known allergies to particular foodstuffs, preservatives, food colorings, or animal derivatives.

Some existing and historical health conditions can affect the use of sitagliptin and metformin combination. Be sure to tell your doctor about any other health conditions you have.

Sitagliptin and metformin should be used with caution in patients who have the following medical conditions or have a history of them as to do so could increase the risk of serious side effects:

  • Weakened condition
  • Unstable or acute congestive heart failure
  • Severe dehydration
  • Sepsis
  • Poor blood circulation
  • Malnourishment
  • Low blood pressure
  • Liver disease
  • Hypoxemia
  • Heart attack
  • Blood vessel problems
  • Alcoholism

Using sitagliptin and metformin combination in patients with anemia or vitamin B12 deficiency could make these conditions worse.

Patients with a history of angioedema, who have received treatment with sitagliptin and metformin combination or dipeptidyl peptidase-(DPP-4) inhibitors may have an increased risk of this condition recurring if treated with sitagliptin and metformin combination.

People who suffer from metabolic acidosis or diabetic ketoacidosis, severe kidney disease, or type 1 diabetes should not be treated with sitagliptin and metformin combination.

Fever, major surgery, infection, or trauma cause temporarily cause problems with controlling blood sugar. In this case, patients should be treated with insulin, rather than sitagliptin and metformin combination.

Sitagliptin and metformin combination can cause pancreatitis and must, therefore, be used with caution in patients who have suffered from:

  • Pancreas problems
  • Obesity
  • High levels of fats or triglycerides in the blood
  • High cholesterol

If you are due to have any form of radiologic procedure, including MRI, CT scans, or X-rays, or any other procedure that necessitates having dye injected into your veins, you must stop taking sitagliptin and metformin combination.

Excess amounts of metformin can cause a condition called lactic acidosis. If you experience any of the following symptoms of lactic acidosis, summon emergency medical help immediately:

  • Unusual sleepiness, tiredness, or weakness
  • Muscle pain or cramping
  • Fast, shallow breathing
  • Diarrhea
  • Decreased appetite
  • Abdominal discomfort
  • A general feeling of discomfort

Sitagliptin and metformin combination can cause low blood sugar. This can also happen if you miss a meal or eat later than usual. Exercising more than usual, vomiting, drinking alcohol, or taking another form of diabetes medication can also cause this condition. Low blood sugar can cause loss of consciousness. If you experience any of the following signs, your blood sugar could have fallen to dangerously low levels:

  • Unusual tiredness or weakness.
  • Slurred speech
  • Shakiness
  • Restless sleep
  • Nightmares
  • Nervousness
  • Nausea
  • Headaches that continue
  • Fast heartbeat
  • Excessive hunger
  • Drowsiness
  • Difficulty thinking
  • Cool, pale skin
  • Confusion
  • Cold sweats
  • Blurred vision
  • Behavior changes, for example, appearing to be drunk
  • Anxiety

If you think that your blood sugar has fallen too low, eat sugar cubes, glucose tablets, corn syrup, honey, fruit juice, non-diet soda, or sugar dissolved in water. Make sure that you have a glucagon kit on hand for use in emergencies, and be sure to check your blood sugar regularly. You should make sure that you and your family know how to use your glucagon kit.

If you miss a dose of sitagliptin and metformin combination, it is possible that you could develop high blood sugar. Failure to follow your diet plan, over-eating, lack of exercise, and fever or infection can all cause your blood sugar levels to become too high. The following signs could indicate that you are suffering from high blood sugar levels:

  • Unusual thirst.
  • Unconsciousness
  • Troubled breathing (rapid and deep)
  • Tiredness
  • Stomach ache
  • Sleepiness
  • Nausea or vomiting
  • Loss of appetite
  • Ketones in the urine
  • Increased urination (frequency and amount)
  • Fruit-like breath odor
  • Flushed, dry skin
  • Dry mouth
  • Drowsiness
  • Blurred vision

If you think that your blood sugar is too high, check your levels and then contact your GP for assistance.

It is a good idea to wear a medical alert bracelet or neck chain, just in case of emergencies related to your diabetes. You may also wish to carry a medical ID card in your purse or wallet, which gives details of your condition and has a list of all the medication you are taking.

This medication can cause pancreatitis. If you begin to notice any of the following symptoms, check with your GP right away:

  • Vomiting
  • Sudden and severe stomach pains
  • Nausea
  • Loss of appetite
  • Lightheadedness
  • Fever
  • Constipation
  • Chills

Sitagliptin and metformin combination can sometimes cause excruciating joint pain in some patients. If you begin to experience severe pain in your joints while using this medication, contact your GP right away.

If you think you may be pregnant, you should tell your doctor before commencing a course of sitagliptin and metformin combination. It is not known whether this medication presents a risk to the fetus, but you may want to discuss the risks and benefits of the drug before you begin using it.

It is not known if sitagliptin and metformin combination passes into breast milk. However, but you might want to consider asking your doctor or midwife for advice on alternatives for feeding your infant while you are using this medication.

Storage

You should always keep your supply of sitagliptin and metformin combination in a sealed container at room temperature. Do not refrigerate or freeze the medicine. Do not get the medication wet or place it near to sources of extreme heat or where it could be exposed to direct sunlight.

Always keep sitagliptin and metformin combination where it cannot be accessed by pets or children. If a pet does consume this medication, you should consult your vet immediately.

Do not keep any unused medication or consume any sitagliptin and metformin combination that has passed the use-by date that is shown on the package.

Do not throw unwanted tablets down the toilet or drain. Do not discard unused medication with your trash; it could be found and eaten by children and animals.

If you are not sure what to do with any left-over drugs, ask the advice of your GP or pharmacist on safe disposal procedures.

Summary

Metformin and sitagliptin combination is a drug that is used in the treatment of type 2 diabetes sufferers who have high blood sugar levels. This medication is not effective in treating people who have insulin-dependent type 1 diabetes. Your treatment package will most likely take the form of a lifestyle change program with a different diet and exercise regime, as well as a course of metformin and sitagliptin combination.

Although this is a very effective drug, it does pose a risk of side effects and there is a wide range of commonly prescribed medications that it cannot be used in conjunction with as interactions could occur. There is also a wide range of medical conditions that make this drug unsuitable for use in patients who have a history of them. For these reasons, it is extremely important that you discuss your medical history fully with your GP before commencing treatment with metformin and sitagliptin combination.

 

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Last Reviewed:
February 01, 2018
Last Updated:
February 10, 2018
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