Ezetrol


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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.

f

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
POunknownunknownunknown

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.
Mentioned in ?
References in periodicals archive ?
Ezetrol is the first drug to work against cholesterol in the intestine in a different way, selectively targeting absorption.
"Around one in four people with high cholesterol do not reach their target and Ezetrol should change all that."
La lucha contra las enfermedades cardiovasculares sigue en pie con lanzamiento del nuevo farmaco de Merck Sharp & Dohme Ezetrol (Ezetimiba), cuyo objetivo es impedir la absorcion de colesterol por via digestiva, a fin de reducir sus niveles en la sangre y, con ello, prevenir el desarrollo de padecimientos serios como la ateroscleroris.
Ezetrol ofrece varias ventajas, pues al trabajar solo a nivel digestivo para evitar la absorcion del colesterol, no genera efectos secundarios (solo nauseas, vomito y diarrea en el 2 por ciento de los pacientes), los primeros resultados se notan a las 2 semanas de iniciar el tratamiento, puede utilizarse en monoterapia o en terapia combinada con una estatina, y favorece el incremento del colesterol de alta densidad o bueno.