(ez ET i mibe)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Zetia: 10 mg
Generic: 10 mg
Brand Names: U.S.
- Antilipemic Agent, 2-Azetidinone
Inhibits absorption of cholesterol at the brush border of the small intestine via the sterol transporter, Niemann-Pick C1-Like1 (NPC1L1). This leads to a decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores and an increased clearance of cholesterol from the blood; decreases total C, LDL-cholesterol (LDL-C), ApoB, and triglycerides (TG) while increasing HDL-cholesterol (HDL-C).
Undergoes glucuronide conjugation in the small intestine and liver; forms metabolite (active); may undergo enterohepatic recycling
Feces (78%, 69% as ezetimibe); urine (11%, 9% as metabolite)
Onset of Action
Within 1 week; Maximum effect: 2-4 weeks
Time to Peak
Plasma: 4-12 hours (ezetimibe); 1-2 hours (active metabolite); Effects: ~2 weeks
22 hours (ezetimibe and metabolite)
>90% to plasma proteins
Special Populations: Elderly
Plasma concentrations are approximately 2-fold higher.
Special Populations: Gender
Plasma concentrations for total ezetimibe were slightly higher (less than 20%) in women than in men.
Use: Labeled Indications
Homozygous familial hypercholesterolemia: In combination with atorvastatin or simvastatin for the reduction of elevated total cholesterol (total-C) and low-density lipoprotein cholesterol (LDL-C) levels in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments (eg, LDL apheresis) or if such treatments are unavailable.
Homozygous sitosterolemia: As adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.
Combination therapy with HMG-CoA reductase inhibitors: In combination with a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor (statin) as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, apolipoprotein B (apo B), and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with primary (heterozygous familial and nonfamilial) hyperlipidemia.
Combination therapy with fenofibrate: In combination with fenofibrate as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, apo B, and non-HDL-C in adult patients with mixed hyperlipidemia.
Monotherapy: As adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, apo B, and non-HDL-C in patients with primary (heterozygous familial and nonfamilial) hyperlipidemia.
Guideline recommendations: The National Lipid Association (NLA) recommends ezetimibe in combination with a statin to reduce the risk of atherosclerotic cardiovascular disease (ASCVD) events for at-risk patients not at non-HDL-C and/or LDL-C goals despite receiving maximally tolerated statin therapy or for those who cannot tolerate higher statin doses (eg, the elderly) (NLA [Jacobson 2015]).
Hypersensitivity to ezetimibe or any component of the formulation; concomitant use with an HMG-CoA reductase inhibitor (statin) in patients with active hepatic disease or unexplained persistent elevations in serum transaminases; pregnancy and breast-feeding (when used concomitantly with a statin)
Homozygous familial hypercholesterolemia, primary hyperlipidemia, homozygous sitosterolemia: Oral: 10 mg once daily
Refer to adult dosing.
Children ≥10 years and Adolescents: Refer to adult dosing.
Dosing: Renal Impairment
No dosage adjustment necessary.
Dosing: Hepatic Impairment
Mild impairment (Child-Pugh class A): No dosage adjustment necessary.
Moderate to severe impairment (Child-Pugh class B or C): Use of ezetimibe not recommended.
May be administered without regard to meals. May be taken at the same time as a statin or fenofibrate. Administer ≥2 hours before or ≥4 hours after bile acid sequestrants.
Before initiation of therapy, patients should be placed on a standard cholesterol-lowering diet for 6 weeks and the diet should be continued during drug therapy.
Store at 25°C (77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F). Protect from moisture.
Bezafibrate: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Avoid combination
Bile Acid Sequestrants: May decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Consider therapy modification
CycloSPORINE (Systemic): Ezetimibe may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Ezetimibe. Monitor therapy
Eltrombopag: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. Monitor therapy
Fenofibrate and Derivatives: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Monitor therapy
Gemfibrozil: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Gemfibrozil may increase the serum concentration of Ezetimibe. Avoid combination
Teriflunomide: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. Monitor therapy
1% to 10%:
Central nervous system: Fatigue (2%)
Gastrointestinal: Diarrhea (4%)
Hepatic: Increased serum transaminases (with HMG-CoA reductase inhibitors; ≥3 x ULN: 1%)
Infection: Influenza (2%)
Neuromuscular & skeletal: Arthralgia (3%), limb pain (3%)
Respiratory: Upper respiratory tract infection (4%), sinusitis (3%)
<1%, postmarketing, and/or case reports: Abdominal pain, anaphylaxis, angioedema, autoimmune hepatitis (Stolk 2006), cholecystitis, cholelithiasis, cholestatic hepatitis (Stolk 2006), depression, dizziness, erythema multiforme, headache, hepatitis, hypersensitivity reaction, increased creatine phosphokinase, myalgia, myopathy, nausea, pancreatitis, paresthesia, rhabdomyolysis, skin rash, thrombocytopenia, urticaria
Concerns related to adverse effects:
• Elevated hepatic transaminases: A higher incidence of elevated transaminases (≥3 x ULN) has been observed with concomitant use of ezetimibe and statins compared to statin monotherapy; transaminase changes were generally not associated with symptoms or cholestasis and returned to baseline with or without discontinuation of therapy. Consider discontinuation of ezetimibe and/or the statin for persistently elevated transaminases (ALT or AST ≥3 x ULN).
• Myopathy: Myopathy, including rhabdomyolysis, has been reported (rarely) with ezetimibe monotherapy; risk may be increased with concomitant use of a statin or fibrate. Discontinue ezetimibe and statin or fibrate immediately if myopathy is suspected or confirmed (symptomatic patient with CPK >10 x ULN).
• Hepatic impairment: Systemic exposure is increased in hepatic impairment. Use with caution in patients with mild hepatic impairment (Child-Pugh class A); use is not recommended in patients with moderate or severe hepatic impairment (Child-Pugh classes B and C).
• Renal impairment: Use with caution in patients with severe renal impairment (CrCl ≤30 mL/minute/1.73 m2); systemic exposure is increased ~1.5-fold. If using concurrent simvastatin in patients with moderate to severe renal impairment (CrCl <60 mL/minute/1.73m2), the manufacturer of ezetimibe recommends that simvastatin doses exceeding 20 mg be used with caution and close monitoring for adverse events (eg, myopathy).
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant drug interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Hyperlipidemia: Secondary causes of hyperlipidemia should be ruled out prior to therapy.
Total cholesterol profile prior to therapy, and when clinically indicated and/or periodically thereafter. When used in combination with fenofibrate, monitor LFTs and signs and symptoms of cholelithiasis.
2013 ACC/AHA Blood Cholesterol Guideline recommendations (Stone, 2013): Baseline LFTs (reasonable); when used in combination with statin therapy, monitor LFTs when clinically indicated; discontinue use of ezetimibe if ALT elevations >3 times upper limit of normal persist.
Pregnancy Risk Factor
Adverse events were observed in some animal reproduction studies. Use is contraindicated in pregnant women who require combination therapy with an HMG-CoA reductase inhibitor. If treatment for familial hypercholesterolemia is needed during pregnancy, other agents are preferred (Wiegman 2015).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience joint pain, diarrhea, or loss of strength and energy. Have patient report immediately to prescriber muscle pain or muscle weakness (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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- Drug class: cholesterol absorption inhibitors
Other brands: Zetia