Ezetimibe

DEA Class; Rx

Common Brand Names; Zetia

Indicated for use as adjunctive therapy to diet and exercise for the reduction of elevated total cholesterol, LDL-cholesterol, Apo-B, and non-HDL-cholesterol in patients with primary (heterozygous familial and non-familial) hyperlipidemia; reduction of elevated sitosterol and campesterol in patients with homozygous familial sitosterolemia; in combination with atorvastatin or simvastatin for reduction of elevated total cholesterol and LDL-cholesterol in patients with homozygous familial hypercholesterolemia:.

Hypersensitivity

Coadministration with a statin in the presence of active liver disease or persistent, unexplained elevations of hepatic transaminase levels

• Diarrhea (4%)
• Upper respiratory tract symptoms (2-4%)
• Cough (2-4%)
• Pain in extremity (3%)
• Sinusitis (3%)
• Arthralgia (2-3%)
• Fatigue (2%)
• Influenza (2%)
• Increased liver transaminases (with HMG-CoA reductase inhibitors; ≥3 x ULN; 1%)
• Hepatitis/liver function test abnormalities (LFTs elevated slightly higher in combination with statin than with statin alone)
• Hypersensitivity reactions (including anaphylaxis, angioedema, rash, urticaria)
• Erythema multiforme
• Elevated creatine phosphokinase
• Myopathy/rhabdomyolysis
• Thrombocytopenia
• Back pain
• Abdominal pain
• Pancreatitis
• Nausea
• Dizziness
• Paresthesia
• Depression
• Headache
• Cholelithiasis and cholecystitis

Elevated hepatic transaminases (≥3 X ULN) reported with concomitant use of statins compared to statin monotherapy; consider discontinuation of therapy (ezetimibe and/or statin) for persistently elevated transaminases (ALT or AST (≥3 X ULN)

Myopathy, including rhabdomyolysis reported with monotherapy (rare); risk increased with concomitant use of statin or fibrate immediately if myopathy suspected or confirmed (symptomatic patient with CPK >10 X ULN)

Hepatic impairment may increase systemic exposure; use with caution in patient swith mild hepatic impairment (Child-Pugh class A); use not recommended in patients with moderate to severe hepatic impairment (Child-Pugh classes B and C)

Use with caution in patients with severe renal impairment (CrCl ≤30 mL/min/1.73 m²); if using concurrent simvastatin in patients with moderate to severe renal impairment (CrCl<60 mL/min/1.73 m²) use caution with simvastatin doses exceeding 20 mg; monitor for adverse events

Cholelithiasis reported (when coadministered with fibric acid derivatives)

Rule out secondary causes of hyperlipidemia prior to therapy

Pregnancy category: C

Lactation: Excretion in milk unknown; use with caution