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.

1. Drug name and main ingredients

Common name: Ezetimibe

Product Name: ZETIA ®

Dosage form: Oral tablets

Main ingredients: Each tablet contains 10mg of ezetimibe

Accessories: cross-linked carboxymethyl cellulose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyvinylpyrrolidone, sodium dodecyl sulfate

2. Indications

Primary hypercholesterolemia:

Monotherapy: As a dietary supplement, it reduces total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), and apolipoprotein B (ApoB).

Combination therapy: Used in combination 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 treatments.

Homozygous sitosterolemia: reduces plasma levels of sitosterols and brassinosteroids.

3. Specifications and characteristics

Specification: 10mg/tablet

Appearance: White to off white capsule shaped film coated with the word "414" printed on it.

4. Usage and dosage

Regular dose: 10mg once daily, can be taken before or after meals.

Combination statins: can be taken simultaneously with statins, please refer to the instructions for statins for specific timing.

Omission treatment: Take the medication immediately when remembered, skip if it is close to the next medication time, and prohibit double dosage.

Bile acid chelator combination: at least 2 hours (before) or 4 hours (after) interval is required.

5. Dose adjustment

Liver dysfunction:

Mild (Child Pugh 5-6): No adjustment required.

Moderate to severe (Child Pugh ≥ 7): contraindicated.

Renal insufficiency: No adjustment required.

Elderly patients: No adjustment required, but adverse reactions need to be monitored.

6. Medication precautions

Diet: It is necessary to maintain a low cholesterol diet.

Liver function monitoring: When combined with statins, regular checks of liver enzymes are necessary.

Muscle symptoms: If there is unexplained muscle pain or weakness, seek medical attention immediately.

Pregnancy/lactation: Do not use in combination with statins; Single medication requires weighing the pros and cons.

7. Medication for special populations

Children: Safe and effective for ages ≥ 10, data is insufficient for ages<10.

Elderly individuals: No need for adjustment, but may have higher exposure levels.

Pregnant women: avoid using statins in combination; Single drug should only be used when the benefits outweigh the risks.

Breastfeeding period: Do not use in combination with statins; Single drug suspension for breastfeeding.

8. Adverse reactions

Common (≥ 2%): Abdominal pain (3.0%), diarrhea (3.7%), fatigue (2.2%), joint pain (3.8%).

Serious but rare:

Elevated liver enzymes (monotherapy 0.5% vs statin combination 1.3%).

Myopathy/rhabdomyolysis (caution should be exercised when combined with statins).

9. Contraindications

Individuals who are allergic to ezetimibe or excipients.

Active liver disease or continuous elevation of liver enzymes for unknown reasons (when combined with statins).

Pregnancy (in combination with statins).

10. Drug interactions

Bile acid chelators (such as colexamide): reduce the AUC of ezetimibe by about 55% and require intermittent administration.

Fenofibrate: Increase the blood concentration of ezetimibe by 48-64%.

Cyclosporine: Increase exposure to ezetimibe by 12 times and require close monitoring.

Statins: No clinically significant interactions.

11. Storage method

Temperature: 15-30 ° C, keep away from moisture.

Packaging: 30/90/500 tablets in bottles or 100 tablets in unit dose packaging.

12. Manufacturer

Manufacturer: Merck/Schering Plough Pharmaceuticals (USA).

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