ezetimibe

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ezetimibe

Ezetrol (UK), Zetia

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.

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ezetimibe

(ĭ-zĕt′ə-mīb′)

A drug that inhibits the absorption of cholesterol from the intestine and is used to treat primary hypercholesterolemia.

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.

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References in periodicals archive ?

* If patient is unable to achieve 50% reduction in LDL-C and/or have an LDL-C level of 100 mg/dL, the addition of ezetimibe therapy is reasonable.

AHA/ACC updates blood cholesterol management advice

This drug looks safe and very effective at modifying LDL, about as much so as ezetimibe and maybe a little bit more," said Dr.

Novel agent cut LDL in statin-intolerant patients

That being said, the Dietary Approaches to Stop Hypertension (DASH) diet has been shown to lower LDL by as much as 11 mg/ dL--nearly as much as ezetimibe. The DASH diet emphasizes fruits, vegetables, low-fat dairy, lean meats and fish, whole grains, nuts, legumes and heart-healthy fats and is low in sodium, saturated fat and sugar.

When Statins Are Not the Answer: There are other medications and methods to help lower cholesterol

Phytosterolaemia responds well to dietary modification and ezetimibe. In view of the gravity of FH and phytosterolaemia, we recommend that plasma cholesterol and triglyceride measurements should be done before as well as after embarking on a high-fat diet, to ensure that high cardiovascular risk receives appropriate attention.

Severe hypercholesterolaemia with a high risk of atherosclerosis may be precipitated by a high-sterol diet

(30) to determine the mean percent change from baseline for lovastatin (10, 20, 40, and 80 mg), pravastatin (10, 20, and 40 mg), simvastatin (5, 10, 20, 40, and 80 mg), atorvastatin (10, 20, 40, and 80 mg), fluvastatin (20 and 40 mg), rosuvastatin (5, 10, 20, and 40 mg), and ezetimibe (10 mg; all daily doses).

Imputation of Baseline LDL Cholesterol Concentration in Patients with Familial Hypercholesterolemia on Statins or Ezetimibe

The liver samples of the ezetimibe group showed moderate chronic diffuse liver congestion with periportal fibrosis and there was moderate intrahepatic cholestasis (40x magnification) (Figure 1(c)).

The Hypocholesterolemic Effects of Eryngium carlinae F. Delaroche Are Mediated by the Involvement of the Intestinal Transporters ABCG5 and ABCG8

In case of ezetimibe treatment, the total chol absorption rate and thus the net daily amount of absorbed chol introduced to the liver via chylomicrons is strongly reduced and causes the hepatic chol pool to diminish strongly.

The Interpretation of Cholesterol Balance Derived Synthesis Data and Surrogate Noncholesterol Plasma Markers for Cholesterol Synthesis under Lipid Lowering Therapies

The results were taken from the baseline and third-month data of ezetimibe treatment.

The effect of ezetimibe monotheraphy on mean platelet volume in patients with hyperlipidaemia: a retrospective study of 45 patients

The two agents in the miscellaneous category are ezetimibe and lomitapide.

The safety of lipid-lowering drugs in pregnancy

In a phase 2 trial (multicenter, randomized, placebo-controlled), conducted in adults with HeFH,the subjects received REGN727 150, 200, or 300 mg every 4 weeks, or 150 mg every 2 weeks, or placebo every 2 weeks (in addition to statin, with or without ezetimibe).

Alirocumab--a novel drug for familial hypercholesterolemia

Usefulness of nutraceuticals (Armolipid Plus) vs Ezetimibe and combination in statin-intolerant patients with dyslipidaemia with coronary heart disease.

Nutraceutical combination compared with and added to ezetimibe in patients with dyslipidaemia and coronary heart disease

A drug called ezetimibe, marketed as Zetia, lowers LDL by inhibiting activity of the same protein.