Zetia Generic Name & Formulations
Mechanism of Action
In combination with a statin, or alone when additional LDL-C lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients ≥10yrs with HeFH. In combination with fenofibrate as an adjunct to diet to reduce elevated LDL-C in adults with mixed hyperlipidemia. In combination with a statin, and other LDL-C lowering therapies, to reduce elevated LDL-C levels in adults and in pediatric patients aged ≥10yrs with homozygous familial hypercholesterolemia (HoFH). As an adjunct to diet for the reduction of elevated sitosterol and campesterol levels in adults and in pediatric patients ≥9yrs with homozygous familial sitosterolemia.
Zetia Dosage and Administration
≥10yrs (with hyperlipidemia, HeFH, or HoFH) or ≥9yrs (with homozygous familial sitosterolemia): 10mg once daily. Concomitant bile acid sequestrants: give ezetimibe at least 2hrs before or 4hrs after.
<10yrs (with HeFH or HoFH) or <9yrs (with homozygous familial sitosterolemia) or those with other hyperlipidemia types: not established.
The use of ezetimibe in combination with a statin, fenofibrate, or other LDL-C lowering therapy is contraindicated in patients for whom a statin, fenofibrate, or other LDL-C lowering therapy are contraindicated.
Zetia Boxed Warnings
Risks associated with combination therapy with a statin, fenofibrate, or other LDL-C lowering therapies: refer to the prescribing information of these products. Assess LDL-C when appropriate (as early as 4 weeks after initiation). Increases in serum transaminases (esp. in combination with a statin). Perform liver enzyme testing as clinically indicated; consider ezetimibe withdrawal if increases in ALT/AST ≥3×ULN persist. Risk for myopathy/rhabdomyolysis (esp. in combination with a statin, other agents, or fibrates). Discontinue ezetimibe, other concomitant agents if myopathy is suspected. Moderate to severe hepatic impairment: not recommended. Pregnancy. Nursing mothers: not recommended.
Mean peak plasma concentrations of 3.4–5.5 ng/mL were reached within 4–12 hours.
Plasma protein bound: >90%.
Fecal (78%), renal (11%). Half-life: ~22 hours.
Concomitant fibrates (except fenofibrate): not recommended. Concomitant fenofibrate; consider alternative lipid-lowering therapy if cholelithiasis is suspected. Potentiates and potentiated by cyclosporine; monitor levels. Antagonized by bile acid sequestrants (eg, cholestyramine). Separate ezetimibe dosing at least 2hrs before or 4hrs after cholestyramine.
Zetia Adverse Reactions
Upper respiratory tract infection, diarrhea, arthralgia, sinusitis, pain in extremity, fatigue, influenza; rare: myopathy/rhabdomyolysis; w. statin: nasopharyngitis, myalgia, back pain, increased serum transaminases.
Zetia Clinical Trials
Zetia Patient Counseling