Janumet XR

What is Janumet XR?

Janumet XR is a prescription medicine that contains 2 prescription diabetes medicines, sitagliptin (Januvia) and extended-release metformin hydrochloride. Janumet XR can be used along with diet and exercise to lower blood sugar in adults with type 2 diabetes.

Janumet XR is not for people with type 1 diabetes.

Janumet XR is not for people with diabetic ketoacidosis (increased ketones in your blood or urine).

If you have had pancreatitis (inflammation of the pancreas) in the past, it is not known if you have a higher chance of getting pancreatitis while you take Janumet XR.

It is not known if Janumet XR is safe and effective when used in children under 18 years of age.

What is type 2 diabetes?
Type 2 diabetes is a condition in which your body does not make enough insulin, and the insulin that your body produces does not work as well as it should. Your body can also make too much sugar. When this happens, sugar (glucose) builds up in the blood. This can lead to serious medical problems.
High blood sugar can be lowered by diet and exercise, and by certain medicines when necessary

Description

JANUMET XR tablets for oral use contain two antihyperglycemic medications: sitagliptin and metformin extended-release.

 

Sitagliptin

Sitagliptin is an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. Sitagliptin phosphate monohydrate drug substance is used to manufacture JANUMET XR. Sitagliptin phosphate monohydrate is described chemically as 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-α]pyrazine phosphate (1:1) monohydrate with an empirical formula of C16H15F6N5O•H3PO4•H2O and a molecular weight of 523.32. The structural formula is:

Sitagliptin phosphate monohydrate is a white to off-white, crystalline, non-hygroscopic powder. It is soluble in water and N,N-dimethyl formamide; slightly soluble in methanol; very slightly soluble in ethanol, acetone, and acetonitrile; and insoluble in isopropanol and isopropyl acetate.

 

Metformin

Metformin HCl (N,N-dimethylimidodicarbonimidic diamide HCl) is a white to off-white crystalline compound with a molecular formula of C4H11N5•HCl and a molecular weight of 165.63. Metformin HCl is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin HCl is 12.4. The pH of a 1% aqueous solution of metformin HCl is 6.68. The structural formula is as shown:

What is the most important information I should know about Janumet XR?

Serious side effects can happen in people taking Janumet XR, including:

• 1. Lactic Acidosis. Metformin, one of the medicines in Janumet XR, can cause a rare but serious condition called 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.

Call your doctor right away if you have any of the following symptoms, which could be signs of lactic acidosis:

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

Most people who have had lactic acidosis with metformin have other things that, combined with the metformin, led to the lactic acidosis. Tell your doctor if you have any of the following, because you have a higher chance for getting lactic acidosis with Janumet XR if you:

• have severe kidney problems or your kidneys are affected by certain x-ray tests that use injectable dye
• have liver problems
• drink alcohol very often, or drink a lot of alcohol in short-term “binge” drinking
• get dehydrated (lose a large amount of body fluids). This can happen if you are sick with a fever, vomiting, or diarrhea. Dehydration can also happen when you sweat a lot with activity or exercise and do not drink enough fluids
• have surgery
• have a heart attack, severe infection, or stroke

The best way to keep from having a problem with lactic acidosis from metformin is to tell your doctor if you have any of the problems in the list above. Your doctor may decide to stop your Janumet XR for a while if you have any of these things.

Janumet XR can have other serious side effects. See “What are the possible side effects of Janumet XR?”

• 2. Pancreatitis (inflammation of the pancreas) which may be severe and lead to death.
  Certain medical problems make you more likely to get pancreatitis.

Before you start taking Janumet XR:
Tell your doctor if you have ever had

• pancreatitis
• stones in your gallbladder (gallstones)
• a history of alcoholism
• high blood triglyceride levels

Stop taking Janumet XR and call your doctor 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.

• 3. Heart failure. Heart failure means that your heart does not pump blood well enough.

Before you start taking Janumet XR, tell your doctor if you have ever had heart failure or have problems with your kidneys. Contact your doctor 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

These may be symptoms of heart failure.

Who should not take Janumet XR?

Do not take Janumet XR if:

• you have severe kidney problems.
• you are allergic to any of the ingredients in Janumet XR. See the end of this Medication Guide for a complete list of ingredients in Janumet XR.

Symptoms of a serious allergic reaction to Janumet XR 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.

• you have diabetic ketoacidosis. See “What is Janumet XR?”.

What should I tell my healthcare provider before taking Janumet XR?

Before you take Janumet XR, tell your doctor if you:

• have or have had inflammation of your pancreas (pancreatitis).
• have severe kidney problems.
• have liver problems.
• have heart problems, including congestive heart failure.
• drink alcohol very often, or drink a lot of alcohol in short-term “binge” drinking.
• are going to get an injection of dye or contrast agents for an x-ray procedure; Janumet XR may need to be stopped for a short time. Talk to your doctor about when you should stop Janumet XR and when you should start Janumet XR again. See “What is the most important information I should know about Janumet XR?”.
• have any other medical conditions.
• are pregnant or plan to become pregnant. It is not known if Janumet XR will harm your unborn baby. If you are pregnant, talk with your doctor about the best way to control your blood sugar while you are pregnant.
  Pregnancy Registry: If you take Janumet XR at any time during your pregnancy, talk with your doctor about how you can join the Janumet XR pregnancy registry. The purpose of this registry is to collect information about the health of you and your baby. You can enroll in this registry by calling 1-800-986-8999.
• are breast-feeding or plan to breast-feed. It is not known if Janumet XR will pass into your breast milk. Talk with your doctor about the best way to feed your baby if you are taking Janumet XR.

Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Janumet XR may affect how well other drugs work and some drugs can affect how well Janumet XR works.
Know the medicines you take. Keep a list of your medicines and show it to your doctor and pharmacist when you get a new medicine.

How should I take Janumet XR?

• Take Janumet XR exactly as your doctor tells you. Your doctor will tell you how many Janumet XR tablets to take and when you should take them.
• Your doctor may change your dose of Janumet XR if needed.
• Your doctor may tell you to take Janumet XR along with certain other diabetes medicines. Low blood sugar (hypoglycemia) can happen more often when Janumet XR is taken with certain other diabetes medicines. See “What are the possible side effects of Janumet XR?”.
• Take Janumet XR 1 time each day with a meal to help to lower your chance of having an upset stomach. It is better to take Janumet XR with your evening meal.
• Take Janumet XR tablets whole. Do not break, cut, crush, dissolve, or chew Janumet XR tablets before swallowing. If you cannot swallow Janumet XR tablets whole, tell your doctor.
• You may see something that looks like the Janumet XR tablet in your stool (bowel movement). If you see tablets in your stool several times, talk to your doctor. Do not stop taking Janumet XR without talking to your doctor.
• Continue to take Janumet XR as long as your doctor tells you.
• If you take too much Janumet XR, call your doctor or local Poison Control Center right away.
• If you miss a dose, take it with food as soon as you remember. If you do not remember until it is time for your next dose, skip the missed dose and go back to your regular schedule. Do not take 2 doses of Janumet XR at the same time.
• You may need to stop taking Janumet XR for a short time. Call your doctor for instructions if you:
  • are dehydrated (have lost too much body fluid). Dehydration can occur if you are sick with severe vomiting, diarrhea or fever, or if you drink a lot less fluid than normal.
  • plan to have surgery.
  • are going to get an injection of dye or contrast agent for an x-ray procedure. See “What is the most important information I should know about Janumet XR?” and “What should I tell my healthcare provider before taking Janumet XR?”.
• When your body is under some types of stress, such as fever, trauma (such as a car accident), infection or surgery, the amount of diabetes medicine that you need may change. Tell your doctor right away if you have any of these problems and follow your doctor’s instructions.
• Check your blood sugar as your doctor tells you to.
• Stay on your prescribed diet and exercise program while taking Janumet XR.
• Talk to your doctor about how to prevent, recognize and manage low blood sugar (hypoglycemia), high blood sugar (hyperglycemia), and problems you have because of your diabetes.
• Your doctor will check your diabetes with regular blood tests, including your blood sugar levels and your hemoglobin A1C.
• Your doctor will do blood tests to check how well your kidneys are working before and during your treatment with Janumet XR.

What are the possible side effects of Janumet XR?

Serious side effects have happened in people taking Janumet XR or the individual medicines in Janumet XR.

• See “What is the most important information I should know about Janumet XR?”.
• Low blood sugar (hypoglycemia). If you take Janumet XR with another medicine that can cause low blood sugar, such as a sulfonylurea or insulin, your risk of getting low blood sugar is higher. The dose of your sulfonylurea medicine or insulin may need to be lowered while you use Janumet XR. Signs and symptoms of low blood sugar may include:
  • headache
  • drowsiness
  • irritability
  • hunger
  • dizziness
  • confusion
  • sweating
  • feeling jittery
  • weakness
  • fast heart beat
• Serious allergic reactions. If you have any symptoms of a serious allergic reaction, stop taking Janumet XR and call your doctor right away. See “Who should not take Janumet XR?”. Your doctor may give you a medicine for your allergic reaction and prescribe a different medicine for your diabetes.
• Kidney problems, sometimes requiring dialysis.
• Joint pain. Some people who take medicines called DPP-4 inhibitors, one of the medicines in Janumet XR, may develop joint pain that can be severe. Call your doctor if you have severe joint pain.
• Skin reaction. Some people who take medicines called DPP-4 inhibitors, one of the medicines in Janumet XR, may develop a skin reaction called bullous pemphigoid that can require treatment in a hospital. Tell your doctor right away if you develop blisters or the breakdown of the outer layer of your skin (erosion). Your doctor may tell you to stop taking Janumet XR.

The most common side effects of Janumet XR include:

• stuffy or runny nose and sore throat
• gas, upset stomach, indigestion
• headache
• upper respiratory infection
• weakness
• diarrhea
• low blood sugar (hypoglycemia) when used in combination with certain medications, such as a sulfonylurea or insulin.
• nausea and vomiting

Taking Janumet XR with meals can help lessen the common stomach side effects of metformin that usually happen at the beginning of treatment. If you have unusual or sudden stomach problems, talk with your doctor. Stomach problems that start later during treatment may be a sign of something more serious.
Janumet XR may have other side effects, including swelling of the hands or legs. Swelling of the hands and legs can happen if you take Janumet XR in combination with rosiglitazone (Avandia). Rosiglitazone is another type of diabetes medicine.

These are not all the possible side effects of Janumet XR. For more information, ask your doctor or pharmacist.
Tell your doctor if you have any side effect that bothers you, is unusual, or does not go away.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

General information about the safe and effective use of Janumet XR

Medicines are sometimes prescribed for purposes other than those listed in Medication Guides. Do not use Janumet XR for a condition for which it was not prescribed. Do not give Janumet XR to other people, even if they have the same symptoms you have. It may harm them.
This Medication Guide summarizes the most important information about Janumet XR. If you would like to know more information, talk with your doctor. You can ask your doctor or pharmacist for additional information about Janumet XR that is written for health care professionals. For more information go to www.janumetxr.com or call 1-800-622-4477.

How should I store Janumet XR?

Store Janumet XR at 68°F to 77°F (20°C to 25°C). Store in a dry place and keep cap tightly closed.
Keep Janumet XR and all medicines out of the reach of children.

What are the ingredients in Janumet XR?

Active ingredients: sitagliptin and metformin hydrochloride extended-release
Inactive ingredients:

• All doses of Janumet XR Tablets contain: povidone, hypromellose, colloidal silicon dioxide, sodium stearyl fumarate, propyl gallate, polyethylene glycol, and kaolin. Film coating contains hypromellose, hydroxypropyl cellulose, titanium dioxide, FD&C #2/Indigo Carmine Aluminum Lake and carnauba wax.
• In addition the Janumet XR 50 mg/500 mg Tablets also contain: microcrystalline cellulose.
• In addition the Janumet XR 50 mg/1000 mg Tablets also contain: yellow iron oxide.

Label

PRINCIPAL DISPLAY PANEL – 50 MG/500 MG TABLET BOTTLE LABEL

• NDC 0006-0078-61
• Janumet® XR
  (sitagliptin and metformin HCl
  extended-release) tablets
• 50 mg/500 mg
• Dispense the accompanying Medication Guide
  to each patient.
• Each tablet contains 64.25 mg sitagliptin phosphate
  (equivalent to 50 mg sitagliptin) and 500 mg
  metformin hydrochloride extended-release.
• Rx only
• 60 Tablets

SRC: NLM .