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Ezetimibe (Zetia) is a selective cholesterol absorption inhibitor that reduces intestinal cholesterol absorption and lowers plasma low-density lipoprotein cholesterol (LDL-C) levels by inhibiting the activity of NPC1L1 protein in the small intestine.
Common name :Ezetimibe (Ezetimibe)
Trade name u200 c: ZETIA®
Dosage form : Oral tablets
Main ingredient : Each tablet contains 10mg ezetimibe
Excipients : Croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate
Primary hypercholesterolemia :
Monotherapy: as a dietary supplement to reduce total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C) and apolipoprotein B (ApoB).
Combination therapy: combined with statins to further reduce TC, LDL-C and ApoB.
Homozygous familial hypercholesterolemia (HoFH) : Used in combination with statins as an adjunct to other lipid-lowering therapies.
Homozygous sitosterolemia : Decreased plasma sitosterol and campesterol levels.
Specifications : 10mg/tablet
Characteristics : White to off-white capsule-shaped film-coated tablets, printed with "414".
Regular dosage of : 10 mg once a day, before or after a meal.
Combined statin : Can be taken at the same time as statins. For specific times, refer to the statin instructions.
Handling of missed doses : Take it immediately when you remember it. If it is close to the next dose time, skip it. Double dose is prohibited.
Combined use of bile acid sequestrants : The interval between administration should be at least 2 hours (before) or 4 hours (after).
Hepatic insufficiency :
Mild (Child-Pugh5-6): no adjustment required.
Medium to severe (Child-Pugh≥7): disabled.
Renal insufficiency : No adjustment required.
U200c for elderly patients: No adjustment is required, but adverse reactions need to be monitored.
Diet : A low-cholesterol diet is required.
Liver function monitoring : When combined with statins, liver enzymes need to be checked regularly.
Muscle symptoms : If you have unexplained myalgia or weakness, you should seek medical attention immediately.
Pregnancy/lactation : It is forbidden to use it in combination with statins; the pros and cons of a single drug need to be weighed.
Children : It is safe and effective for ≥10 years old, but there is insufficient data for <10 years old.
Older adults : No adjustment required, but exposure may be higher.
Pregnant women : Avoid combined use with statins; single drugs should only be used when the benefits outweigh the risks.
U200c during lactation: It is forbidden to use it in combination with statins; breastfeeding is suspended with single drug.
Common (≥2%) : Abdominal pain (3.0%), diarrhea (3.7%), fatigue (2.2%), joint pain (3.8%).
Severe but rare :
Elevated liver enzymes (0.5% for single drug vs. 1.3% for statin combination).
Myopathy/rhabdomyolysis (need to be wary when combined with statins).
Those who are allergic to ezetimibe or excipients.
Active liver disease or unexplained persistent elevation of liver enzymes (when combined with statins).
Pregnancy (combined with statins).
Bile acid sequestrant (such as cholestyramine) : Reduces the AUC of ezetimibe by about 55%, and requires interval administration.
Fenofibrate : Increases the plasma concentration of ezetimibe by 48-64%.
Cyclosporine : Increases ezetimibe exposure by 12-fold and requires close monitoring.
Statin : No clinically significant interaction.
Temperature :15-30°C, avoid moisture.
Packaging : 30/90/500 tablet bottles or 100 tablet unit dose packaging.
Manufacturer : Merck/Schering-PloughPharmaceuticals (USA).