Ezetrol Ezetimibe Tablets

1. Indications and Usage
Primary Hypercholesterolemia: As an adjunct to diet, ezetimibe may be used alone or in combination with HMG-CoA reductase inhibitors (statins) to reduce total cholesterol (TC), LDL-C, apolipoprotein B, and triglycerides.
Homozygous Familial Hypercholesterolemia (HoFH): Used as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or statins in patients with HoFH.
Homozygous Sitosterolemia: Used as an adjunct to diet to reduce elevated sitosterol and plant sterol levels.
2. Dosage and Administration
Recommended Dose: The recommended dose is 10 mg taken once daily.
Administration: Can be taken with or without food, at any time of day. Tablets can be taken alone or in combination with a statin.
Special Populations: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment (Child-Pugh score 5 or 6) or renal impairment.
3. Mechanism of Action
Inhibition of Absorption: Ezetimibe works by inhibiting cholesterol absorption from the small intestine.
Site of Action: It selectively inhibits the Niemann-Pick C1-Like 1 (NPC1L1) protein at the brush border of enterocytes, reducing the delivery of intestinal cholesterol to the liver, thereby lowering plasma cholesterol levels.
4. Safety and Warnings
Hepatic Effects: When used with a statin, serum transaminases (ALT and/or AST) should be monitored. Persistent elevations (≥3 times the upper limit of normal) have been reported and require clinical evaluation.
Myopathy and Rhabdomyolysis: When used with a statin, patients should be advised to report any unexplained muscle pain or weakness immediately.
5. Adverse Reactions and Clinical Research
Monotherapy: Common adverse reactions include headache, abdominal pain, and diarrhea.
Combination with Statins: Common adverse reactions include headache, fatigue, abdominal pain, constipation, diarrhea, bloating, nausea, and elevated transaminases.
Rare Adverse Reactions: Post-marketing reports include hypersensitivity reactions (e.g., angioedema, rash), arthralgia, myalgia, and very rarely rhabdomyolysis.
6. Drug Interactions
Fibrates: Concomitant use with fibrates (e.g., fenofibrate, gemfibrozil) increases ezetimibe exposure and may increase the risk of gallstones; safety and efficacy of this combination have not been established.
Cyclosporine: Cyclosporine can significantly increase ezetimibe exposure (up to 3.4-fold); caution is advised.
Bile Acid Sequestrants: Co-administration with resins (e.g., cholestyramine) decreases ezetimibe exposure; ezetimibe should be taken at least 2 hours before or 4 hours after the resin.
7. Pharmaceutical Information
Active Ingredient: Ezetimibe.
Excipients: Lactose monohydrate, microcrystalline cellulose, hydroxypropyl cellulose, colloidal silicon dioxide, and magnesium stearate.
Appearance: White or off-white tablets.
Storage: Store at controlled room temperature, protecting from moisture.