Ezetimibe reduces blood cholesterol by acting at the brush border of the small intestine to inhibit the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This reduces hepatic cholesterol stores and increases the clearance of cholesterol from the blood.
藥動學
Absorption:
Tmax, Oral: 4 to 12 hours [3]; 1.5 hours (pediatric 6 to 10 years of age).
Effects of food: No effect on extent of absorption; Cmax increased 38% with high-fat meal.
Distribution:
Protein binding: Greater than 90%; Vd: 105.3 L.
Metabolism:
Hepatic and intestinal wall: Extensive via glucuronide conjugation; 10% to 20% unchanged.
Excretion:
Fecal: 78%; primarily unchanged.
Renal: 11%, primarily as changed drug.
Elimination Half Life: 22 hours.
禁忌症
Active liver disease or unexplained persistent hepatic transaminases, when used with a statin.
Pregnant or nursing mothers, when used with a statin.
Hypersensitivity to ezetimibe or any component of the product.
懷孕分類
C (FDA)
哺乳分類
Infant risk cannot be ruled out.
副作用
Common:
Gastrointestinal: Diarrhea (2.5% to 4.1%).
Musculoskeletal: Arthralgia (2.6% to 3%), Myalgia (3.2%).
Respiratory: Nasopharyngitis (3.7%), Sinusitis (2.8%), Upper respiratory infection (2.9% to 4.3%).
Serious:
Hepatic: Hepatitis, Increased liver enzymes (0.5% to 3%).
Immunologic: Anaphylaxis.
Musculoskeletal: Disorder of muscle, Rhabdomyolysis.
劑量和給藥方法
Disorder of cardiovascular system, Post acute coronary syndrome; Prophylaxis: 10 mg orally once daily in combination with simvastatin 40 mg orally once daily (study dosage).
Familial hypercholesterolemia - homozygous: 10 mg orally once daily with atorvastatin or simvastatin.
Mixed hyperlipidemia: 10 mg orally once daily in combination with fenofibrate.
Primary hypercholesterolemia:
10 mg orally once daily alone or in combination with an HMG-CoA reductase inhibitor (FDA dosage).
Sitosterolemia, Homozygous familial:
10 mg orally once daily.
小兒調整劑量
腎功能調整劑量
Adjustment not necessary
肝功能調整劑量
Moderate to severe (Child-Pugh score 7 to 15): Use not recommended.