Zenon Rosuvastatin Calcium and Ezetimibe Tablets (I)

1. Indications and Usage
Primary Hypercholesterolemia: Indicated as an adjunct to diet for adult patients with primary hyperlipidemia (including heterozygous familial hypercholesterolemia) who require reduction of LDL-C and cannot achieve this with rosuvastatin monotherapy.
Mixed Dyslipidemia: Indicated for adult patients with mixed dyslipidemia who require reduction of total cholesterol, LDL-C, and triglycerides.
Homozygous FH: Indicated as an adjunct to diet and other lipid-lowering treatments (e.g., LDL apheresis) for patients with homozygous familial hypercholesterolemia (HoFH) when other treatments are not sufficient.
2. Dosage and Administration
Route of Administration: Oral administration.
Recommended Dosage: One tablet once daily.
Administration Details: May be taken with or without food at any time of the day.
Concomitant Bile Acid Sequestrants: Administer this combination at least 2 hours before or 4 hours after taking bile acid sequestrants.
3. Mechanism of Action
Rosuvastatin: Inhibits HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis, thereby reducing endogenous cholesterol production.
Ezetimibe: Inhibits the absorption of cholesterol at the brush border of the small intestine.
Synergistic Effect: The combination provides an additive effect on lowering LDL-C by targeting both synthesis and absorption pathways.
4. Safety and Warnings
Hepatotoxicity: Elevations in ALT/AST may occur. Liver function tests should be monitored before initiation and as clinically indicated.
Myopathy and Rhabdomyolysis: Monitor for muscle pain or weakness, especially when combined with fibrates or other interacting drugs.
Renal Impairment: The combination is contraindicated in patients with severe renal impairment (CrCl <30 mL/min) not on dialysis.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Myalgia, abdominal pain, constipation, nasopharyngitis, and asthenia.
Clinical Research Highlights: Clinical trials have demonstrated significant reductions in LDL-C, total cholesterol, and triglycerides compared to monotherapy or placebo.
6. Drug Interactions
Cyclosporine: Concomitant use significantly increases rosuvastatin exposure; caution is advised.
Fibrates: Combined use may increase the risk of myopathy and rhabdomyolysis.
P-gp/BCRP Inhibitors: Drugs like digoxin or certain antifungals may increase plasma concentrations of rosuvastatin.
7. Pharmaceutical Information
Chemical Composition: Active ingredients: Rosuvastatin calcium and ezetimibe.
Appearance: White to off-white, round, biconvex, film-coated tablets.
Packaging: Available in blister packs (e.g., 10mg/10mg, 5mg/10mg).
Storage: Store at controlled room temperature; protect from moisture.