Zituvimet

Pronunciation: zye-too-vi-met
Generic name: sitagliptin and metformin
Dosage form: Oral tablet

Medically reviewed by Carmen Pope, BPharm. Last updated on Nov 7, 2023.

What is Zituvimet?

Zituvimet is an oral combination treatment containing sitagliptin and metformin that may be used to lower blood glucose (sugar) in adults with type 2 diabetes alongside diet and exercise.

Sitagliptin is thought to work by increasing insulin release and decreasing glucagon levels by slowing the inactivation of incretin hormones. Incretin hormones are released by the intestine throughout the day and in response to food. These hormones are rapidly inactivated by an enzyme called dipeptidyl peptidase 4 (DPP-4). Sitagliptin inhibits DDP-4 and belongs to the class of medicines known as DPP-4 inhibitors.

Metformin works by increasing the ability of cells to uptake glucose by improving their insulin sensitivity. It also works by decreasing the amount of glucose made by the liver and decreasing the absorption of glucose from the intestine. Metformin belongs to the class of medicines known as biguanides.

Together, the combination lowers blood glucose levels by several mechanisms: increasing insulin release, decreasing glucagon levels, increasing the ability of cells to uptake glucose, decreasing the production of glucose by the liver, and decreasing the absorption of glucose from the intestine.

Zituvimet was FDA-approved on November 6, 2023.

Warnings

People with a history of hypersensitivity reactions to Zituvimet, sitagliptin, metformin, or any of the inactive ingredients in the tablets should not take this medicine. Symptoms of a serious allergic reaction may include rash, raised red patches on your skin (hives), or swelling of the face, lips, tongue, and throat that may cause difficulty in breathing or swallowing.

Also contraindicated in those with severe kidney disease (eGFR below 30 mL/min/1.73 m2), metabolic acidosis, or diabetic ketoacidosis. Not recommended for those with an eGFR between 30 and less than 45 mL/min/1.73 m2

Has been associated with lactic acidosis which may be fatal. Symptoms included muscle aches, a general feeling of unwellness, breathing problems, tiredness, and abdominal pain. The risk is higher in those with kidney or liver disease; use of certain drugs; age ≥65 years old; people undergoing radiological studies with contrast media (Zituvimet may need to be temporarily discontinued during these studies), surgery or other procedures; hypoxic (low oxygen) states; dehydration, or who have an excessive alcohol intake. Discontinue Zituvimet and seek urgent medical attention if these symptoms happen.

Fatal and nonfatal acute pancreatitis has been reported associated with Zituvimet. It is not known if you have a higher chance of getting pancreatitis with Zituvimet if you have had it in the past. The hallmark symptom of acute pancreatitis is persistent severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting. Stop taking Zituvimet and contact your healthcare provider immediately if these symptoms happen.

May also increase the risk for heart failure, acute kidney failure, severe joint pain, and bullous pemphigoid.

Long-term use has been associated with vitamin B12 deficiency – your healthcare provider should measure your B12 levels at 2 to 3-year intervals and treat if low.

It is not known if Zituvimet is safe and effective in children.

Zituvimet is not for people with type 1 diabetes.

Before taking

Before you take Zituvimet, tell your healthcare provider about all of your medical conditions, including if you have:

• kidney or liver problems
• heart failure
• stones in your gallbladder (gallstones)
• high blood triglyceride levels
• to get an injection of dye or contrast agents for an X-ray procedure
• or have had inflammation of your pancreas (pancreatitis)
• have low levels of vitamin B12 in your blood, or
• drink alcohol very often or drink a lot of alcohol in short-term “binge” drinking
• irregular periods or your periods do not come at all and are of childbearing potential
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

Ovulation, Pregnancy, and Breastfeeding

Zituvimet can cause the release of an egg from an ovary in a woman (ovulation). This can increase your chance of getting pregnant.

It is not known if Zituvimet will harm your unborn baby. If you are pregnant, talk with your healthcare provider about the best way to control your blood sugar while you are pregnant.

Tell your healthcare provider right away if you become pregnant while taking Zituvimet.

It is not known if Zituvimet will pass into your breast milk. Talk with your healthcare provider about the best way to feed your baby if you are taking Zituvimet.

How should I take Zituvimet?

Take 2 times a day by mouth. Your healthcare provider will tell you exactly how many Zituvimet tablets to take and when you should take them.

• Take it with meals to help to lower your chance of having an upset stomach.
• Do not break or cut the Zituvimet tablets before swallowing. If you cannot swallow the tablets whole, tell your healthcare provider.
• Low blood sugar levels may happen more frequently when you take Zituvimet alongside other diabetes medicines. The amount of diabetes medicine that you need may change when your body is under some type of stress, such as fever, trauma (such as a car accident), infection, or surgery. Tell your healthcare provider right away if you have any of these problems and follow your healthcare provider’s instructions.
• Your healthcare provider will do blood tests to check how well your kidneys are working before and during your treatment.

Dosage

Zituvimet is usually taken orally (by mouth) twice daily with food.

Your doctor will recommend a dosage for you based on your current treatment regimen and how well you tolerate Zituvimet.

People not currently treated with metformin

• The usual starting dose is sitagliptin 50mg/metformin 500mg twice daily.
• The dose should be increased gradually to limit the risk of gastrointestinal side effects.
• The maximum recommended dosage is sitagliptin 100mg/metformin 1000mg.

People currently treated with metformin

• Stop the metformin. Base the dosage on the amount of metformin usually taken.
• For people taking 500mg metformin twice daily: The usual starting dose is sitagliptin 50mg/metformin 500mg twice daily.
• For people taking 850mg metformin twice daily: The usual starting dose is sitagliptin 50mg/metformin 1000mg twice daily.
• The maximum recommended dosage is sitagliptin 100mg/metformin 1000mg twice daily.

What happens if I miss a dose?

If it is almost time for your next dose, do not take the missed dose. Just go back to your regular dosing schedule.

What happens if I overdose?

If you take too much Zituvemt call your healthcare provider or Poison Help Line at 1-800-222-1222 or go to the nearest hospital emergency room right away.

What are the side effects of Zituvimet?

If symptoms of an allergic reaction occur, such as a rash, hives, and swelling of the face, lips, tongue, and throat that may cause difficulty in breathing or swallowing, stop taking Zituvimet and seek medical advice promptly. 

Zituvimet can cause serious side effects, including lactic acidosis (a buildup of an acid in the blood) that can cause death. Lactic acidosis is a medical emergency and must be treated in the hospital. Stop taking Zituvimet and call your healthcare provider right away if you have any of the following symptoms, which could be signs of lactic acidosis:

• feel cold in your hands or feet
• feel dizzy or lightheaded
• have a slow or irregular heartbeat
• feel very weak or tired
• have unusual (not normal) muscle pain
• have trouble breathing
• feel sleepy or drowsy
• have stomach pains, nausea, or vomiting.

The best way to keep from having a problem with lactic acidosis from metformin contained in Zituvimet is to tell your healthcare provider if you become dehydrated, have a contrast X-ray, have kidney problems, drink alcohol excessively, have surgery, have a heart attack, severe infection, or stroke, are 65 years of age or older.

Inflammation of the pancreas (pancreatitis) is another, potentially fatal, serious side effect that may occur. Certain medical problems make you more likely to get pancreatitis. Stop taking Zituvimet and call your healthcare provider right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may be felt going from your abdomen through to your back. The pain may happen with or without vomiting. These may be symptoms of pancreatitis.

Zituvimet may also increase your risk of developing heart failure. Heart failure means that your heart does not pump blood well enough. Before you start taking Zituvimet tell your healthcare provider if you have ever had heart failure or have problems with your kidneys. Contact your healthcare provider right away if you have any of the following symptoms:

• increasing shortness of breath or trouble breathing, especially when you lie down
• swelling or fluid retention, especially in the feet, ankles, or legs
• an unusually fast increase in weight
• unusual tiredness.

The most common side effects of Zituvimet affecting 5% or more people include

• diarrhea
• upper respiratory
• tract infections
• and headache.

To report suspected adverse reactions, contact Zydus Pharmaceuticals (USA) Inc. at 1-877-993-8779 or FDA at 1-800-FDA1088 or www.fda.gov/medwatch.

What other drugs will affect Zituvimet?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Tell your doctor if you take:

• Carbonic anhydrase inhibitors - these may increase the risk of lactic acidosis
• Drugs that reduce metformin clearance (such as ranolazine, vandetanib, dolutegravir, and cimetidine)
• Other diabetes medications, including insulin. There may be an increased risk of low blood sugar levels when Zituvimet is used in combination with insulin and/or an insulin secretagogue. A lower dose of insulin or insulin secretagogue may be required
• Alcohol. Do not drink excessively.

Know the medicines you take. Keep a list of your medicines and show it to your healthcare provider and pharmacist when you get a new medicine. See the prescribing information for a full list of interactions.

Ingredients

Active: sitagliptin and metformin hydrochloride

Inactive: colloidal silicon dioxide, croscarmellose sodium, low substituted hydroxypropylcellulose, magnesium stearate, malic acid, microcrystalline cellulose, povidone, and sodium stearyl fumarate.

Film coating: (inactive): polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

The film coating of the 50 mg/1,000 mg tablet also contains FD&C yellow #6 aluminum lake, iron oxide red, and iron oxide yellow.

Available as:

• sitagliptin 50 mg and metformin HCl 500 mg tablets
• sitagliptin 50 mg and metformin HCl 1,000 mg tablets.

Storage

Store in the original container at room temperature, between 68°F to 77°F (20°C to 25°C).

Use within 3 months of opening the bottle.

Keep all medicines out of the reach of children.

Manufacturer

Zydus Lifesciences Ltd.

Further information

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

Medical Disclaimer