EZETIMIBE

EZETIMIBE
(e-ze-ti'mibe)
Zetia, Ezetrol

Classifications: antilipemic;
Therapeutic: cholesterol lowering agent
Pregnancy Category: C

Availability

10 mg tablets

Action

Works at the lining of the small intestine inhibiting the absorption of cholesterol, but does not inhibit cholesterol synthesis in the liver or increases bile acid excretion. Thus it decreases the amount of intestinal cholesterol available to the liver.

Therapeutic Effect

Lowers both total cholesterol and low-density lipid (LDL) cholesterol; its mechanism of action is complementary to statins.

Uses

Treatment of primary hypercholesterolemia alone or with an HMG-CoA reductase inhibitor (statin); treatment of homozygous sitosterolemia as an adjunct to diet.

Contraindications

Hypersensitivity to ezetimibe; concurrent use with HMG-CoA reductase inhibitor in patients with active liver disease or elevated serum transaminases; moderate to severe hepatic disease; concurrent administration with fibrates; lactation; pregnancy (category C); children <10 y.

Cautious Use

Mild hepatic insufficiency.

Route & Dosage

Hypercholesterolemia
Adult: PO 10 mg q.d.

Administration

Oral

Give no sooner than 2 h before or 4 h after administration of a bile acid sequestrant such as cholestyramine.
Store at 15°–30° C (59°–86° F). Protect from moisture.

Adverse Effects (≥1%)

Body as a Whole: Fatigue, arthralgia, back pain, myalgia, angioedema, myopathy. CNS: Dizziness, headache. GI: Abdominal pain, diarrhea. Respiratory: Pharyngitis, sinusitis, cough. Hematologic: Thrombocytopenia. Skin: Rash. Other: Hepatitis, pancreatitis, rhabdomyolysis.

Interactions

Drug: bile acid sequestrants (e.g., cholestyramine) may decrease absorption (give ezetimibe 2 h before or 4 h after these drugs); cyclosporine or fibric acid derivatives can significantly increase ezetimibe levels.

Pharmacokinetics

Absorption: Well absorbed from the small intestine. Peak: 4–12 h. Distribution: Ezetimibe-glucuronide is 99% protein bound. Metabolism: Extensively conjugated to an active glucuronide compound (ezetimibe-glucuronide). Metabolized in small intestine and liver. Elimination: Primarily in feces. Half-Life: 22 h.

Nursing Implications

Assessment & Drug Effects

Lab tests: Monitor baseline and periodic lipid profile; periodic Hgb & Hct and platelet count. Monitor baseline LFTs and when used with a statin, monitor periodic LFTs in accordance with the monitoring schedule for that statin.
Assess for and report unexplained muscle pain, especially when used in combination with a statin drug.
Monitor closely patients who take both ezetimibe and cyclosporine.

Patient & Family Education

Report unexplained muscle pain, tenderness, or weakness.
Females should use effective methods of contraception to prevent pregnancy while taking this drug.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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