Ezetrol


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ezetimibe

(e-zet-i-mibe) ,

Ezetrol

(trade name),

Zetia

(trade name)

Classification

Therapeutic: lipid lowering agents
Pharmacologic: cholesterol absorption inhibitors
Pregnancy Category: C

Indications

Alone or with other agents (HMG-CoA reductase inhibitors) in the management of dyslipidemias including primary hypercholesterolemia, homozygous familial hypercholesterolemia, and homozygous sitosterolemia.

Action

Inhibits absorption of cholesterol in the small intestine.

Therapeutic effects

Lowering of cholesterol, a known risk factor for atherosclerosis.

Pharmacokinetics

Absorption: Following absorption, rapidly converted to ezetimibe-glucaronide, which is active. Bioavailability is variable.
Distribution: Unknown.
Metabolism and Excretion: Undergoes enterhepatic recycling, mostly eliminated in feces, minimal renal excretion.
Half-life: 22 hr.

Time/action profile

ROUTEONSETPEAKDURATION
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Contraindications/Precautions

Contraindicated in: Hypersensitivity;Acute liver disease or unexplained laboratory evidence of liver disease (when used with HMG-CoA reductase inhibitor);Moderate or severe hepatic impairment;Concurrent use of fibrates; Obstetric: May cause fetal harm by interfering with cholesterol synthesis and, possibly, biologically active substances derived from cholesterol; Lactation: Potential for adverse effects in nursing infant.
Use Cautiously in: Pediatric: Children <10 yr (safety not established).

Adverse Reactions/Side Effects

Gastrointestinal

  • cholecystitis
  • cholelithiasis
  • ↑ liver enzymes (with HMG-CoA reductase inhibitors)
  • nausea
  • pancreatitis

Dermatologic

  • rash

Miscellaneous

  • angioedema (life-threatening)

Interactions

Drug-Drug interaction

Effects may be ↓ by cholestyramine or other bile acid sequestrants.Concurrent use of fibrates may ↑ levels and the risk of cholelithiasis.Cyclosporine may ↑ levels.May ↑ risk of rhabdomyolysis when used with HMG CoA-reductase inhibitors.

Route/Dosage

Oral (Adults) 10 mg once daily.

Renal Impairment

Oral (Adults) CCr <60 mL/min and concurrent use with simvastatin—Do not exceed simvastatin dose of 20 mg/day

Availability

Tablets: 10 mg Cost: $517.89 / 90
In combination with: simvastatin (Vytorin); atorvastatin (Liptruzet); see combination drugs.

Nursing implications

Nursing assessment

  • Obtain a diet history, especially with regard to fat consumption.
  • Lab Test Considerations: Evaluate serum cholesterol and triglyceride levels before initiating, after 2–4 wk of therapy, and periodically thereafter.
    • May cause ↑ liver transaminases when administered with HMG-CoA reductase inhibitors. Monitor liver enzymes prior to initiation and during therapy according to recommendations of HMG-CoA reductase inhibitor. Elevations are usually asymptomatic and return to baseline with continued therapy.

Potential Nursing Diagnoses

Noncompliance, related to diet and medication regimen (Patient/Family Teaching)

Implementation

  • Do not confuse Zetia with Zebeta (bisoprolol) or Zestril (lisinopril).
  • Oral: Administer without regard to meals. May be taken at the same time as HMG-CoA reductase inhibitors.

Patient/Family Teaching

  • Instruct patient to take medication as directed, at the same time each day, even if feeling well. Take missed doses as soon as remembered, but do not take more than 1 dose/day. Medication helps control but does not cure elevated serum cholesterol levels.
  • Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking. Ezetimibe does not assist with weight loss.
  • Instruct patient to notify health care professional if unexplained muscle pain, tenderness, or weakness occur. Risk may increase when used with HMG-CoA reductase inhibitors.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any other Rx, OTC, or herbal products.
  • Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
  • Instruct female patients to notify health care professional promptly if pregnancy is planned or suspected or if breast feeding. If regimen includes HMG-CoA reductase inhibitors, they are contraindicated in pregnancy.
  • Emphasize the importance of follow-up exams to determine effectiveness and to monitor for side effects.

Evaluation/Desired Outcomes

  • Decrease in serum LDL and total cholesterol levels.

Ezetrol

A brand name for EZETIMIBE.
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References in periodicals archive ?
Ezetrol is the first drug to work against cholesterol in the intestine in a different way, selectively targeting absorption.
Worldwide sales of ZETIA, marketed as EZETROL outside the United States, were $534 million in the third quarter of 2008, a decrease of 12 percent compared with the previous year's third quarter.
VYTORIN (also marketed as INEGY and ZINTREPID) has now been approved in 25 countries, including the United States, and ZETIA (also marketed as EZETROL and ZIENT) in 72 countries.
Worldwide sales of ZETIA, marketed as EZETROL outside the United States, were $560 million in the second quarter of 2008, a decrease of 3 percent compared with the previous year's second quarter.
Worldwide sales of ZETIA, marketed as EZETROL outside the United States, were $582 million in the first quarter of 2008, an increase of 7 percent compared with the previous year's first quarter.
Use of a controversial new cholesterol-lowering drug, ezetimibe (trade names: Zetia, Ezetrol, Vytorin), has increased in the United States, far beyond that seen in Canada, where direct-to-consumer advertising (DTCA) is prohibited and there is more government regulation of drug reimbursement in publicly-funded drug formularies.
Global sales of ZETIA, marketed as EZETROL outside the United States, reached $679 million in the fourth quarter, an increase of 27 percent compared with the fourth quarter of 2006.
Global sales of ZETIA, marketed as EZETROL outside the United States, reached $607 million in the third quarter, an increase of 21 percent compared with the third quarter of 2006.
Global sales of ZETIA, marketed as EZETROL outside the United States, reached $578 million in the second quarter, an increase of 21% compared with the second quarter of 2006.
Global sales of ZETIA, marketed as EZETROL outside the United States, reached $544 million in the first quarter, an increase of 31% compared with the first quarter of 2006.
and these medicines are marketed as EZETROL and INEGY, respectively, in many countries outside the U.
Global sales of ZETIA, the cholesterol-absorption inhibitor also marketed as EZETROL outside the United States, reached $536 million in the fourth quarter, an increase of 37% compared with the fourth quarter of 2005.