Classifications: antilipemic; Therapeutic: cholesterol lowering agent
Pregnancy Category: C
10 mg tablets
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.
Lowers both total cholesterol and low-density lipid (LDL) cholesterol; its mechanism of action is complementary to statins.
Treatment of primary hypercholesterolemia alone or with an HMG-CoA reductase inhibitor (statin); treatment of homozygous sitosterolemia
as an adjunct to diet.
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.
Mild hepatic insufficiency.
Route & Dosage
Adult: PO 10 mg q.d.
- 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:
, cough. Hematologic:
Hepatitis, pancreatitis, rhabdomyolysis.
InteractionsDrug: bile acid sequestrants
) may decrease absorption (give ezetimibe 2 h before or 4 h after these drugs); cyclosporine
or fibric acid derivatives
can significantly increase ezetimibe levels.
Well absorbed from the small intestine. Peak:
412 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:
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.