Zetia


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Related to Zetia: ezetimibe, Ezetrol

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.

Zetia

(zĕt′ē-ə)
A trademark for the drug ezetimibe.

Zetia®

Ezetimibe, see there.
References in periodicals archive ?
The two drug makers once heavily advertised Vytorin and Zetia, which brought their joint venture $5.1 billion in 2007 sales.
We anticipate that it will also strengthen our presence in Japan through the comarketing of Zetia [currently under review in that nation as a cholesterol absorption inhibitor] with Bayer for this key cardiovascular product."
Merck shares have fallen more sharply than rival drugmakers this year as it has seen demand falter for its Singulair asthma drug, Gardasil cervical cancer vaccine and its cholesterol fighters, Vytorin and Zetia. The drugmaker last week forecast 2009 earnings below Wall Street's targets, citing sluggish sales for key medicines and negative foreign currency trends.
intend to divide profits from the expected Food and Drug Administration clearance of Vytorin, a medicine combining Zetia, a drug that the two codeveloped its a therapy to block the intestines from absorbing artery-clogging fat, and Zocor, the Merck statin that limits the liver's production of cholesterol.
"For short-term investors, that's definitely an issue and something to monitor across all of the pharmaceutical companies." Merck Chief Financial Officer Peter Kellogg also told analysts that he expects combined global sales of its Vytorin and Zetia cholesterol fighters, which it sells in partnership with Schering-Plow Corp.
Notable products introduced in late 2002 or last year included two cholesterol treatments--AstraZeneca PLC's Crestor and Zetia from Schering-Plough Corp.
Vytorin and Zetia prescriptions have slumped since the release of two studies questioning their effectiveness.
The product will combine Merck's Zocor and Zetia, a complementary drug that Merck markets with Schering-Plough Corp.
The vaccine "has become increasingly more important from a profit standpoint because of the concerns over Singulair, Vytorin and Zetia." Merck is counting on Gardasil to help offset declining sales of cholesterol pills Vytorin and Zetia after a January study found they may work no better at unclogging arteries than a cheaper medicine.
Also known as ezetimibe/simvastatin, Vytorin combines Schering's Zetia (ezetimibe), a cholesterol-absorption inhibitor, and Merck's Zocor (simvastatin) statin product in a single tablet.
(Kenilworth NJ) already were facing a Thursday deadline to produce extensive data on a clinical study called SEAS that indicated a possible cancer risk from Vytorin, which combines Merck's Zocor, a statin, and Schering-Plough's Zetia, a different type of cholesterol fighter that is the component under suspicion.
The company's joint venture with Schering-Plough Corp., marketing Zetia for use with statins, is expected to turn a profit this year.