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.

See 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.

f

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

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.

单词	ezetimibe
释义	ezetimibe e·zet·i·mibe E5323250 (ē′zĕt′ə-mĭb)n. A drug, C₂₄H₂₁F₂NO₃, that inhibits the absorption of cholesterol from the intestine and is used to treat high cholesterol. [ezet-, alteration of azet(idine), one of its constituents (az(o)- + -et(e), unsaturated heterocyclic compound suffix) + -imibe, cholesterol-lowering drug suffix (perhaps ultimately shortening and alteration of inhibitor).] Translations ezetimibe 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. See 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. f 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 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. ThesaurusSeeatorvastatin
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ezetimibe

e·zet·i·mibe

ezetimibe

ezetimibe

Action

Availability

Indications and dosages

Contraindications

Precautions

Administration

Adverse reactions

Interactions

Patient monitoring

Patient teaching

f

ezetimibe

ezetimibe