ezetimibe


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ezetimibe

Pharmacologic class: Cholesterol absorption inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category C

Action

Inhibits cholesterol absorption in the intestine, decreasing intestinal delivery of cholesterol to the liver and increasing systemic cholesterol clearance. Net effect is decreased serum cholesterol level.

Availability

Tablets: 10 mg

Indications and dosages

Adjunct to diet to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), nonhigh-density lipoprotein cholesterol (non-HDL-C), and apolipoprotein B (Apo B) in patients with primary hyperlipidemia, alone or in combination with HMG-CoA reductase inhibitor; to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia, in combination with fenofibrate; to reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia, in combination with atorvastatin or simvastatin; to reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia

Adults: 10 mg/day P.O.

Contraindications

• Hypersensitivity to drug or its components
• Active hepatic disease or unexplained, persistent transaminase elevations (when given with a statin)
• Women who are pregnant or may become pregnant (when given with a statin)
• Breastfeeding patients (when given with a statin)

Precautions

Use cautiously in:
• moderate or severe hepatic impairment (use not recommended)
• skeletal muscle toxicity
• concurrent use of cyclosporine or fibrates other than fenofibrate (use not recommended)
• elderly patients
• pregnant or breastfeeding patients not receiving HMG-CoA reductase inhibitors
• children younger than age 10.

Administration

• Give with or without food.
• Be aware that drug may be given concurrently with HMG-CoA reductase inhibitor (such as atorvastatin or simvastatin).
• Give at least 2 hours before or 4 hours after bile acid sequestrant (if prescribed).

Adverse reactions

CNS: headache, dizziness, fatigue

EENT: nasopharyngitis, sinusitis

GI: diarrhea

Musculoskeletal: back pain, myalgia, joint pain, extremity pain, rhabdomyolysis

Respiratory: upper respiratory tract infection

Interactions

Drug-drug.Cholestyramine: decreased ezetimibe blood level

Cyclosporine, fenofibrate, gemfibrozil: increased ezetimibe blood level

Fibrates: increased risk of cholesterol excretion into gallbladder leading to cholelithiasis

Drug-diagnostic tests.Liver function tests: increased values

Patient monitoring

• Monitor hepatic and lipid profiles.
• Monitor cyclosporine concentration in patients receiving drug concurrently with cyclosporine.
• Monitor International Normalized Ratio if patient also receiving warfarin.
• Assess for and report unexplained muscle pain.
• If cholelithiasis is suspected in patient also receiving fenofibrate, obtain gallbladder studies and consider alternative lipid-lowering therapy.

Patient teaching

• Teach patient about the role of diet, exercise, and weight loss in lowering cholesterol levels.

Instruct patient to immediately report unexplained muscle pain, tenderness, or weakness while taking this drug.
• Advise breastfeeding patient not to take this drug while taking a statin.
• Advise female patient of childbearing age to use effective contraception while taking this drug concurrently with a statin and if she becomes pregnant to stop taking ezetimibe and statin and call her prescriber.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

ezetimibe

(ĭ-zĕt′ə-mīb′)
n.
A drug that inhibits the absorption of cholesterol from the intestine and is used to treat primary hypercholesterolemia.

ezetimibe

an antilipemic agent used to treat hypercholesterolemia, homozygous low-density lipoprotein receptor disorder, and homozygous sitosterolemia.

ezetimibe

A cholesterol absorption inhibitor drug that can be used alone or, more effectively, in conjunction with a statin drug (see STATINS) to reduce blood cholesterol levels in people with hypercholesterolaemia. Such people are at risk of developing ATHEROSCLEROSIS. The drug acts specifically to inhibit cholesterol absorption and does not affect the absorption of other lipids. A brand name is Ezetrol.
References in periodicals archive ?
Cytochrome P450: Ezetimibe had no significant effect on a series of probe drugs (caffeine, dextromethorphan, tolbutamide, and IV midazolam) known to be metabolized by cytochrome P450 (1A2, 2D6, 2C8/9 and 3A4) in a "cocktail" study of twelve healthy adult males.
Since IMPROVE-IT has now shown that the lower a patient's LDL the better the clinical outcomes, it makes sense to consider starting high-risk patients on maximal statin therapy--atorvastatin 80 mg/day or its equivalent along with ezetimibe, he said.
Two of the trials are evaluating efficacy of the ezetimibe/atorvastatin (10 mg/20 mg and 10 mg/40 mg) combination tablet compared to coadministration of ezetimibe and ator-vastatin in the same dosage amounts.
Merck had filed for approval of the claim that 10 mg of ezetimibe plus 20 mg of simvastatin (in the fixed-dose combination pill or taken separately) reduces the risk of major cardiovascular events in patients withchronic kidney disease on the basis of the SHARP results.
According to data from April 2017's IMS MAT report, ezetimibe tablets have predicted sales of USD2.
The researchers assumed that statins, ezetimibe, and the two approved PCSK9 inhibitors (evolocumab and alirocumab) each would reduce the risk of cardiovascular events by an identical amount per mg/dL of LDL cholesterol reduction.
16] The other two studies, referred to as ODYSSEY OPTIONS studies (OPTIONS I & II studies), were designed along similar lines and the key difference being OPTIONS I included patients specifically on atorvastatin at baseline with/without the addition of ezetimibe, and OPTIONS II included patients on rosuvastatin at baseline, again with/without the addition of ezetimibe.
Usefulness of nutraceuticals (Armolipid Plus) vs Ezetimibe and combination in statin-intolerant patients with dyslipidaemia with coronary heart disease.
Oftentimes, cholesterol-lowering statin medications are enough to achieve these goals, but some patients need extra help from a non-statin drug, like ezetimibe (Zetia[R]).
And while such low levels cannot be achieved without the help of a cholesterol-lowering medication, ezetimibe (Zetia) will do the job just as well as a statin.
A drug called ezetimibe, marketed as Zetia, lowers LDL by inhibiting activity of the same protein.