Ezetimibe
Brand Name: Zetia
Generic Available
Common Dosage Forms:
Tablets: 10 mg
FDA Indications/Dosages:
For the adjunct therapy to diet for the reduction of elevated total-C, LDL-C, and ApoB in patients with primary (familial and nonfamilial);
In combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and ApoB in patients with primary (familial and nonfamilial) hypercholesterolemia;
In combinations with atorvastatin or simvastatin, for the reduction of elevated total-C and LDL-C levels in patients with homozygous familial hypercholesterolemia (HoFH), as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis or if such treatments are unavailable);
As an adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia;
As an adjunctive therapy to diet, in combination with fenofibrate, for the reduction of elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia:
The recommended daily dose for all indications is 10 mg.
Monitor: Lipid panel
Pharmacology/Pharmacokinetics: Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. It appears to act at the brush border of the small intestine to inhibit cholesterol absorption thereby decreasing the delivery of cholesterol to the liver. After oral administration, ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide. Peak plasma levels of ezetimibe-glucuronide occurs in 1-2 hours. Elimination occurs primarily through the feces. The elimination half-life for both ezetimibe and ezetimibe-glucuronide is 22 hours. Both are highly (>90%) bound to plasma proteins.
Drug Interactions: Gemfibrozil and fenofibrate increased plasma concentrations of ezetimibe. Cholestyramine decreases plasma concentrations of ezetimibe.
Contraindications/Precautions: Contraindicated in patients hypersensitive to any component. Do not use in patients with moderate to severe hepatic insufficiency. Normal precautions for HMG-CoA reductase should be employed when ezetimibe is used concomitantly with these drugs. Pregnancy Category C.
Adverse Effects: Myalgia, increased CPK, elevations in liver transaminases, hepatitis, thrombocytopenia, urticaria, arthralgia, and myopathy/rhabdomyolysis have been reported during therapy.
Patient Consultation:
Do not take within 2 hours before or 4 hours after the administration of a bile acid sequestrant (cholestyramine).
Closely follow prescribed diet.
May be taken without regard to meals.
Contact physician if symptoms of myopathy occur (e,g,, muscle pain or tenderness, especially if accompanied by malaise or fever) when Zetia is used with an HMG-CoA reductase inhibitor.
Store in a cool, dry place away from sunlight and children.
If a dose is missing, take it as soon as possible. If more than 8 hours has lapsed between the time the dose was to be taken, skip it and return to normal dosing schedule.
