Zituvimet

Pronunciation: zye-too-vi-met
Generic name: sitagliptin and metformin
Dosage form: oral tablet
Drug class: Antidiabetic combinations

Medically reviewed by Carmen Pope, BPharm. Last updated on Jul 26, 2024.

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.

Zituvimet works in two different ways. The sitagliptin component 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. The metformin component works by increasing the ability of cells to uptake glucose by improving their insulin sensitivity. It also decreases the amount of glucose made by the liver and decreases 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.

Zituvimet side effects

The most common side effects of Zituvimet are:

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

Serious side effects and warnings

Zituvimet carries a Boxed Warning for lactic acidosis.

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 risk of developing lactic acidosis is increased in those who are dehydrated, have a contrast X-ray, have kidney problems, drink alcohol excessively, have surgery, have a heart attack, severe infection, or stroke, or 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.

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. If symptoms of an allergic reaction occur, stop taking Zituvimet and seek urgent medical advice.

May also increase the risk for 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.

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

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

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

Pregnancy

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.

Breastfeeding

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 Zituvimet tablets 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.

Zituvimet XR tablets are

Dosage

• Zituvimet tablets (normal release) are usually taken orally 2 times a day with food.
• Zituvimet XR tablets are usually taken orally 1 time a day with food.
  • If you take more than 1 tablet, take them as a single dose (both together).

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

People not currently treated with metformin

The usual starting dose of Zituvimet (normal release) (sitagliptin 50mg/metformin 500mg) 2 times a day.

• The dose should be increased gradually to limit the risk of gastrointestinal side effects.
• The maximum recommended dosage of Zituvimet is sitagliptin 100mg/metformin 1000mg.

The usual starting dose of Zituvimet XR (sitagliptin 100mg/metformin 1000mg)1 time a day.

• The dose should be increased gradually to limit the risk of gastrointestinal side effects.
• The maximum recommended dosage of Zituvimet XR is sitagliptin 100mg/metformin 2000mg.

People currently treated with metformin

Stop the metformin. Base the dosage of Zituvimet or Zituvimet XR on the amount of metformin usually taken.

For people taking 500mg of metformin twice daily

• The usual starting dose is Zituvimet (normal release) (sitagliptin 50mg/metformin 500mg) 2 times a day.
• The usual starting dose of Zituvimet XR (sitagliptin 50mg/metformin 1000mg) is 1 tablet 1 time a day.

For people taking 850mg of metformin twice daily

• The usual starting dose of Zituvimet (normal release) is sitagliptin 50mg/metformin 1000mg 2 times a day.
• The usual starting dose of Zituvimet XR (sitagliptin 50mg/metformin 1000mg) is 2 tablets 1 time a day.

Related/similar drugs

Mounjaro, Ozempic, metformin, Trulicity, Lantus, Tresiba, Basaglar, Victoza

What happens if I miss a dose?

Do not take the missed dose if it is almost time for your next 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 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

Zituvimet (normal release)

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 1000 mg tablets.

Zituvimet XR

Active ingredients: sitagliptin and metformin hydrochloride
Inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, dibasic calcium phosphate anhydrous, ferric oxide yellow, hypromellose, magnesium stearate, malic acid, microcrystalline cellulose, povidone, pregelatinized starch (maize) and sodium stearyl fumarate.

Film-coating: polyethylene glycol, polyvinyl alcohol-partially hydrolyzed, iron oxide yellow, talc, and titanium dioxide.

Additionally, Zituvimet XR 50 mg/500 mg and 100 mg/1,000 mg tablets film-coating contain the inactive
ingredient red iron oxide, and 50 mg/1,000 mg and 100 mg/1,000 mg tablets film-coating contain the FD&C yellow#6 Aluminum Lake.

Zituvimet XR is available as 50mg/500mg, 50mg/1000mg, and 100mg/1000mg 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.

Who makes Zituvimet?

Zydus Lifesciences Ltd. makes Zituvimet and Zituvimet XR.

Further information

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

Medical Disclaimer