Xelevia 100 mg film-coated tablets

 

What is it and how is it used?

Xelevia is a member of a class of medicines you take by mouth called DPP-4 inhibitors (dipeptidyl peptidase-4 inhibitors) that lowers blood sugar levels in patients with type 2 diabetes mellitus. Type 2 diabetes is also called non-insulin-dependent diabetes mellitus, or NIDDM.

Xelevia helps to improve the levels of insulin after a meal and decreases the amount of sugar made by the body. It is unlikely to cause low blood sugar because it does not work when your blood sugar is low. However, when Xelevia is used in combination with a sulphonylurea medicine or with insulin, low blood sugar (hypoglycaemia) can occur.

Your doctor has prescribed Xelevia to help lower your blood sugar, which is too high because of your type 2 diabetes. Xelevia can be used alone or in combination with certain other medicines (insulin, metformin, sulphonylureas, or glitazones) that lower blood sugar, which you may already be taking for your diabetes together with a food and exercise plan.

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 like heart disease, kidney disease, blindness, and amputation.

What do you have to consider before using it?

Do not take Xelevia

  • if you are allergic (hypersensitive) to sitagliptin or any of the other ingredients of Xelevia.

Take special care with Xelevia
Cases of inflammation of the pancreas (pancreatitis) have been reported in patients receiving Xelevia. Pancreatitis can be a serious, potentially life-threatening medical condition. Stop taking Xelevia and call your doctor if you experience severe and persistent stomach pain, with or without vomiting, because you could have pancreatitis.

Tell your doctor if you have or have had:

  • pancreatitis, gallstones, alcoholism or very high triglycerides. These medical conditions can increase your chance of getting pancreatitis, or getting it again.
  • type 1 diabetes
  • diabetic ketoacidosis (a complication of diabetes with high blood sugar, rapid weight loss, nausea or vomiting)
  • any kidney problems, or any past or present medical problems. If you have kidney problems, Xelevia may not be the right medicine for you.
  • an allergic reaction to Xelevia.

If you are taking a sulphonylurea or insulin with Xelevia you may experience low blood sugar. Your doctor may reduce the dose of your sulphonylurea or insulin medicine.

Taking other medicines
Xelevia may be taken with most medicines. Tell your doctor or pharmacist about all the medicines you take or have recently taken. This includes prescription and non-prescription medicines, and herbal supplements.

Taking Xelevia with food and drink
You can take Xelevia with or without food and drink.

Pregnancy and breast-feeding
Women who are pregnant or plan to become pregnant should consult their doctor before taking Xelevia. You should not use Xelevia during pregnancy.

It is not known if Xelevia passes into breast milk. You should not use Xelevia if you are breast-feeding or plan to breast-feed.

Driving and using machines
Xelevia has no known influence on the ability to drive and use machines. However, when driving or operating machinery, it should be taken into account that dizziness and drowsiness have been reported.

Taking Xelevia in combination with medicines called sulphonylureas or with insulin can cause hypoglycaemia, which may affect your ability to drive and use machines or work without safe foothold.

How is it used?

Always take Xelevia exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.

The usual dose is:

  • one 100 mg film-coated tablet
  • once a day
  • by mouth

Your doctor may prescribe Xelevia alone or with certain other medicines that lower blood sugar.

Continue to take Xelevia as long as your doctor prescribes it so you can continue to help control your blood sugar.

Diet and exercise can help your body use its blood sugar better. It is important to stay on the diet, exercise and weight loss program recommended by your doctor while taking Xelevia.

If you take more Xelevia than you should
If you take more than the prescribed dosage of Xelevia, contact your doctor immediately.

If you forget to take Xelevia
If you miss a dose, take it 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 a double dose of Xelevia.

What are possible side effects?

Like all medicines, Xelevia may cause side effects, although not everybody gets them.

Very common side effects (more than 1 per 10 patients)
Common side effects (less than 1 per 10 but more than 1 per 100 patients)
Uncommon side effects (less than 1 per 100 but more than 1 per 1,000 patients)

Some patients have experienced the following side effects after adding sitagliptin to metformin: Common: nausea
Uncommon: weight loss, loss of appetite, abdominal pain, diarrhoea, low blood sugar, drowsiness.

Some patients have experienced the following side effects while taking Xelevia in combination with a sulphonylurea:
Common: low blood sugar

Some patients have experienced the following side effects while taking Xelevia in combination with a sulphonylurea:
Very common: low blood sugar

Some patients have experienced the following side effects while taking Xelevia in combination with a sulphonylurea and metformin:
Very common: low blood sugar
Common: constipation

Some patients have experienced the following side effects while taking Xelevia and pioglitazone: Common: low blood sugar and flatulence. In addition, some patients have reported foot swelling while taking Xelevia and pioglitazone. These side effects may be seen with sitagliptin and any glitazone (e.g., rosiglitazone).

Some patients have experienced the following side effects while taking Xelevia in combination with rosiglitazone and metformin:
Common: headache, cough, diarrhoea, vomiting, low blood sugar, fungal skin infection, upper respiratory infection, swelling of the hands or legs.

Some patients have experienced the following side effects while taking Xelevia in combination with insulin (with or without metformin):
Common: headache, low blood sugar and flu
Uncommon: dry mouth, constipation

Some patients have experienced the following side effects while taking Xelevia alone: Common: low blood sugar, headache
Uncommon: dizziness, constipation

In addition, some patients have reported the following side effects while taking Xelevia: Common: upper respiratory infection, stuffy or runny nose and sore throat, osteoarthritis, arm or leg pain.

During post-approval use of Xelevia by itself and/or with other diabetes medicines additional side effects have also been reported (frequency not known): allergic reactions, which may be serious, including rash, hives, and swelling of the face, lips, tongue, and throat that may cause difficulty in breathing or swallowing. If you have an allergic reaction, stop taking Xelevia and call your doctor right away. Your doctor may prescribe a medicine to treat your allergic reaction and a different medicine for your diabetes. Other side effects that have been reported include: inflammation of the pancreas; kidney problems (sometimes requiring dialysis); vomiting.

If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

How should it be stored?

Keep out of the reach and sight of children.

Do not use Xelevia after the expiry date which is stated on the blister and the carton. The expiry date refers to the last day of that month.

This medicine does not require any special storage conditions.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.

What is it?

Xelevia is a medicine that contains the active substance sitagliptin. It is available as round tablets (pink: 25 mg; beige: 50 and 100 mg).

What is it used for?

Xelevia is used in patients with type 2 diabetes to improve the control of blood glucose (sugar) levels. It is used in addition to diet and exercise in the following ways:

  • on its own, in patients who are not satisfactorily controlled on diet and exercise and in whom metformin (an antidiabetes medicine) is not suitable;
  • in combination with metformin or a PPAR-gamma agonist (a type of antidiabetes medicine) such as a thiazolidinedione, in patients who are not satisfactorily controlled on metformin or the PPAR-gamma agonist used on its own;
  • in combination with a sulphonylurea (another type of antidiabetes medicine) in patients who are not satisfactorily controlled with a sulphonylurea used on its own and in whom metformin is not suitable;
  • in combination with both metformin, and a sulphonylurea or a PPAR-gamma agonist, in patients who are not satisfactorily controlled on the two medicines;
  • in combination with insulin, with or without metformin, in patients who are not satisfactorily controlled on a stable dose of insulin. The medicine can only be obtained with a prescription.

How is it used?

Xelevia is taken at a dose of 100 mg once a day, with or without food. If Xelevia is taken with a sulphonylurea or insulin, the dose of the sulphonylurea or insulin may need to be lowered to reduce the risk of hypoglycaemia (low blood sugar levels).

How does it work?

Type 2 diabetes is a disease in which the pancreas does not make enough insulin to control the level of glucose in the blood or when the body is unable to use insulin effectively. The active substance in Xelevia, sitagliptin, is a dipeptidyl-peptidase-4 (DPP-4) inhibitor. It works by blocking the breakdown of ‘incretin’ hormones in the body. These hormones are released after a meal and stimulate the pancreas to produce insulin. By increasing levels of incretin hormones in the blood, sitagliptin stimulates the pancreas to produce more insulin when blood glucose levels are high. Sitagliptin does not work when the blood glucose is low. Sitagliptin also reduces the amount of glucose made by the liver, by increasing insulin levels and decreasing the levels of the hormone glucagon. Together, these processes reduce blood glucose levels and help to control type 2 diabetes.

How has it been studied?

Xelevia was studied in nine studies, involving almost 6,000 patients with type 2 diabetes whose blood glucose levels were not adequately controlled:

  • four of the studies compared Xelevia with placebo (a dummy treatment): Xelevia or placebo were used on their own in two studies involving 1,262 patients, as an add-on to metformin in one study involving 701 patients, and as an add-on to pioglitazone (a PPAR-gamma agonist) in one study involving 353 patients;
  • two studies compared Xelevia with other antidiabetes medicines. One study compared Xelevia with glipizide (a sulphonylurea), when they were used as an add-on to metformin in 1,172 patients. The other study compared Xelevia with metformin, used on their own, in 1,058 patients;
  • three additional studies compared Xelevia with placebo when they were added to other antidiabetes medicines: glimepiride (another sulphonylurea), with or without metformin, in 441 patients; the combination of metformin and rosiglitazone (a PPAR gamma agonist) in 278 patients; and a stable dose of insulin, with or without metformin, in 641 patients. In all of the studies, the main measure of effectiveness was the change in the level of a substance in the blood called glycosylated haemoglobin (HbA1c), which gives an indication of how well the blood glucose is controlled.

What benefits has it shown during the studies?

Xelevia was more effective than placebo when it was taken alone or in combination with other antidiabetes medicines. In patients taking Xelevia on its own, HbA1c levels fell from around 8.0% at the start of the studies by 0.48% after 18 weeks and 0.61% after 24 weeks. In contrast, they rose by 0.12% and 0.18%, respectively, in the patients taking placebo. Adding Xelevia to metformin reduced HbA1c levels by 0.67% after 24 weeks, compared with a fall of 0.02% in the patients adding placebo. When added to pioglitazone, Xelevia reduced HbA1c levels by 0.85% after 24 weeks, compared with a fall of 0.15% in the patients adding placebo.
In the studies comparing Xelevia with other medicines, the effectiveness of adding Xelevia to metformin was similar to that of adding glipizide. When taken on their own, Xelevia and metformin produced similar reductions in HbA1c levels, but the effectiveness of Xelevia seemed to be slightly lower than that of metformin.
In the additional studies, adding Xelevia to glimepiride (with or without metformin) led to a reduction in HbA1c levels of 0.45% after 24 weeks, compared with an increase of 0.28% in those adding placebo. HbA1c levels were reduced by 1.03% after 18 weeks in patients adding Xelevia to metformin and rosiglitazone, compared with a fall of 0.31% in those adding placebo. Finally, they were reduced by 0.59% in patients adding Xelevia to insulin (with or without metformin), compared with a fall of 0.03% in those adding placebo.

What is the risk associated?

The most common side effects with Xelevia (generally seen in more than 5% of patients) include upper respiratory tract infections (colds) and nasopharyngitis (inflammation of the nose and throat). For the full list of all side effects reported with Xelevia, see the Package Leaflet.
Xelevia should not be used in people who may be hypersensitive (allergic) to sitagliptin or any of the other ingredients.

Why has it been approved?

The Committee for Medicinal Products for Human Use (CHMP) decided that Xelevia’s benefits are greater than its risks and recommended that it be given marketing authorisation.

Further information

The European Commission granted a marketing authorisation valid throughout the European Union for Xelevia to Merck Sharp & Dohme Ltd. on 21 March 2007. The marketing authorisation is valid for five years, after which it can be renewed.