Ezetimibe

What is Ezetimibe?

• Ezetimibe (Zetia) is an inhibitor of intestinal cholesterol (and related phytosterol) absorption that is widely used in the therapy of hypercholesterolemia, usually in combination with other agents.

Ezetimibe

What are the uses of this medicine?

Ezetimibe (Zetia) is used as an adjunct to diet to:

• Reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary hyperlipidemia, alone or in combination with an HMG-CoA reductase inhibitor (statin).
• Reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia in combination with fenofibrate.
• Reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH), in combination with atorvastatin or simvastatin.
• Reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia (phytosterolemia).

Limitations of use:

• The effect of Ezetimibe Tablets on cardiovascular morbidity and mortality has not been determined.
• Ezetimibe Tablets has not been studied in Fredrickson Type I, III, IV, and V dyslipidemias.

Cholesterol:

• Cholesterol is a type of fat found in your blood. Your total cholesterol is made up of LDL and HDL cholesterol.
• LDL cholesterol is called “bad” cholesterol because it can build up in the wall of your arteries and form plaque. Over time, plaque build-up can cause a narrowing of the arteries. This narrowing can slow or block blood flow to your heart, brain, and other organs. High LDL cholesterol is a major cause of heart disease and one of the causes for stroke.
• HDL cholesterol is called “good” cholesterol because it keeps the bad cholesterol from building up in the arteries.
• Triglycerides also are fats found in your blood.

How does this medicine work?

• Ezetimibe (e zet' i mibe) is a synthetic azetidinone that inhibits cholesterol absorption from the intestine.
• Ezetimibe acts by binding to and inhibiting the Niemann-Pick C1-like 1 protein (NPC1), the major transporter of cholesterol in the intestinal brush border.
• Ezetimibe by itself lowers serum cholesterol, but the inhibition of cholesterol absorption is usually followed by a compensatory increase in hepatic cholesterol synthesis, a response that can be blocked by hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors [statins].
• For this reason, ezetimibe is commonly used in combination with a statin.
• Addition of ezetimibe to a maximized dose of statins generally lowers LDL-cholesterol levels by 22% to 24%.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to ezetimibe, the active ingredient in Ezetimibe Tablets, or to the inactive ingredients.
• have active liver disease.
• are pregnant or breast-feeding.
• are a woman of childbearing age, you should use an effective method of birth control to prevent pregnancy while using Ezetimibe Tablets.

What drug interactions can this medicine cause?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Be sure to mention any of the following:

• anticoagulants (blood thinners) such as warfarin (Coumadin)
• cyclosporine (Neoral, Sandimmune)
• fenofibrate (TriCor)
• gemfibrozil (Lopid)

• If you are taking cholestyramine (Questran), colesevelam (WellChol), or colestipol (Colestid), take it 4 hours before or 2 hours after ezetimibe.

Is this medicine FDA approved?

• Ezetimibe was approved for use in the United States in 2002 and is usually recommended as an adjunctive therapy to diet or in combination with a statin in management of patients with hypercholesterolemia at high risk for cardiovascular or cerebrovascular disease.
• It is also used alone in patients who are intolerant of statins and can be combined with other lipid-lowering agents (such as fibrates or anti-PCSK9 monoclonal antibodies).

How should this medicine be used?

Recommended dosage:

• The recommended dose of Ezetimibe Tablets is 10 mg once daily.
• Dosing of Ezetimibe Tablets should occur either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant.
• Ezetimibe Tablets may be administered with a statin (in patients with primary hyperlipidemia) or with fenofibrate (in patients with mixed hyperlipidemia) for incremental effect.
• For convenience, the daily dose of Ezetimibe Tablets may be taken at the same time as the statin or fenofibrate, according to the dosing recommendations for the respective medications.

Administration:

• Ezetimibe comes as a tablet to take by mouth.
• Take Ezetimibe Tablets once a day, with or without food.
• It may be easier to remember to take your dose if you do it at the same time every day, such as with breakfast, dinner, or at bedtime.
• If you also take another medicine to reduce your cholesterol, ask your doctor if you can take them at the same time.
• If you forget to take Ezetimibe Tablets, take it as soon as you remember.
• However, do not take more than one dose of Ezetimibe Tablets a day.
• Continue to follow a cholesterol-lowering diet while taking Ezetimibe Tablets.
• Ask your doctor if you need diet information.
• Keep taking Ezetimibe Tablets unless your doctor tells you to stop.
• It is important that you keep taking Ezetimibe Tablets even if you do not feel sick.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 10 mg

This medicine is available in fallowing brand namesː

• Zetia

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea, joint pains, and feeling tired

Ezetimibe Tablets co-administered with a statin:

• nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, and diarrhea

Ezetimibe Tablets administered alone:

• Upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremity

Additionally, the following side effects have been reported in general use:

• allergic reactions including swelling of the face, lips, tongue, and/or throat that may cause difficulty in breathing or swallowing, rash, and hives; raised red rash, sometimes with target-shaped lesions; joint pain; muscle aches; alterations in some laboratory blood tests; liver problems; stomach pain; inflammation of the pancreas; nausea; dizziness; tingling sensation; depression; headache; gallstones; inflammation of the gallbladder.

What special precautions should I follow?

• Concurrent administration of Ezetimibe Tablets with a specific statin or fenofibrate should be in accordance with the product labeling for that medication.
• Ezetimibe therapy is associated with a low rate of serum aminotransferase elevations and clinically apparent liver injury due to ezetimibe occurs, but is rare. Persistent elevations in hepatic transaminase can occur when Ezetimibe Tablet is added to a statin. Therefore, when Ezetimibe Tablet is added to statin therapy, monitor hepatic transaminase levels before and during treatment according to the recommendations for the individual statin used.
• Ezetimibe Tablet is not recommended in patients with moderate or severe hepatic impairment.
• Cases of myopathy and rhabdomyolysis have been reported in patients treated with Ezetimibe Tablets co-administered with a statin and with Ezetimibe Tablets administered alone. Risk for skeletal muscle toxicity increases with higher doses of statin, advanced age (>65), hypothyroidism, renal impairment, and depending on the statin used, concomitant use of other drugs.
• Women of childbearing age should be advised to use an effective method of birth control to prevent pregnancy while using Ezetimibe Tablets added to statin therapy. Patients should be advised that if they become pregnant they should stop taking combination Ezetimibe Tablets and statin therapy and call their healthcare professional.
• Women who are breastfeeding should be advised to not use Ezetimibe Tablets added to statin therapy. Patients who have a lipid disorder and are breastfeeding should be advised to discuss the options with their healthcare professionals.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• No reported clinical or laboratory adverse events.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• In the event of an overdose, symptomatic and supportive measures should be employed.

Can this medicine be used in pregnancy?

• Pregnancy Category C
• There are no adequate and well-controlled studies of ezetimibe in pregnant women.
• Ezetimibe should be used during pregnancy only if the potential benefit justifies the risk to the fetus.

Can this medicine be used in children?

• Ezetimibe Tablets has not been studied in children under age 10.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• Ezetimibe

Inactive ingredients:

• Lactose monohydrate, croscarmellose sodium, Hypromellose, sodium lauryl sulfate, crospovidone, microcrystaline cellulose, and magnesium stearate.

Who manufactures and distributes this medicine?

Manufactured by:

• Alkem Laboratories Ltd.
• Mumbai , INDIA

Distributed by:

• Ascend Laboratories, LLC
• Parsippany, NJ

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted between 15 to 30°C (59 to 86°F).
• Protect from moisture.

Lipid lowering medications

• Bile Acid Resins/Sequestrants

• • Cholestyramine
  • Colesevelam
  • Colestipol

• Fibrates
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

• Monoclonal Antibodies - Anti-PCSK9
  • Alirocumab
  • Evolocumab

• Niacin (Nicotinic Acid)

• • Omega-3 Fatty Acids,
  • Icosapent Ethyl
  • Omega-3 Acid Ethyl Esters
  • Omega-3 Carboxylic Acids

• Statins
  • Atorvastatin
  • Fluvastatin
  • Lovastatin
  • Pitavastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin

• Miscellaneous
  • Ezetimibe
  • Lomitapide
  • Mipomersen

• Dailymed label info on Ezetimibe
• FDA Ezetimibe

Ezetimibe Resources
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