Atozet Ezetimibe and Atorvastatin Calcium Tablets (II)

1. Indications and Usage
Primary Hypercholesterolemia and Mixed Dyslipidemia: Treatment of primary hypercholesterolemia and mixed dyslipidemia in adults and pediatric patients (≥10 years of age) as an adjunct to diet when the response to statin therapy and dietary measures is insufficient.
Heterozygous Familial Hypercholesterolemia: Used as an adjunct to diet in patients with heterozygous familial hypercholesterolemia.
Homozygous Familial Hypercholesterolemia: Used as an adjunct to diet and other lipid-lowering treatments (e.g., lipid apheresis) in patients with homozygous familial hypercholesterolemia.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage:
Patients switching from monotherapy: The recommended starting dose is one tablet daily, matching the currently prescribed statin (e.g., 10 mg/10 mg, 20 mg/10 mg, 40 mg/10 mg, or 80 mg/10 mg).
Patients naïve to both agents: The recommended starting dose is 10 mg/10 mg (ezetimibe/atorvastatin). The dose may be titrated to 10 mg/20 mg, 10 mg/40 mg, or 10 mg/80 mg based on therapeutic goals.
Critical Administration Instructions:
Timing: Adminuted at any time of day, with or without food.
Bile Acid Sequestrants: If co-administered with bile acid-binding resins (e.g., cholestyramine), atorvastatin should be administered at least 2 hours before or 4 hours after the resin.
Missed Dose: Take it as soon as remembered on the same day. Do not double the dose to make up for a missed one.
3. Mechanism of Action
Ezetimibe: Selectively inhibits the absorption of cholesterol at the brush border of the small intestine, reducing the delivery of intestinal cholesterol to the liver.
Atorvastatin: A selective and competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in hepatic cholesterol synthesis.
Synergy: The combination blocks cholesterol synthesis and absorption at two distinct sites, providing additive LDL-C lowering effects.
4. Safety and Warnings
Hepatotoxicity: Elevations in serum transaminases (ALT/AST) have been observed. Liver function tests should be monitored before initiation and as clinically indicated.
Myopathy and Rhabdomyolysis: Statins may cause myopathy or rhabdomyolysis. Patients should be advised to report unexplained muscle pain, tenderness, or weakness immediately.
Hypersensitivity: Contraindicated in patients with known hypersensitivity to the active substances or any excipients, including active liver disease or unexplained persistent elevations of serum transaminases.
Pregnancy and Lactation: Contraindicated during pregnancy and breastfeeding due to potential adverse effects on fetal development.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: The most common adverse reactions include nasopharyngitis, pain in extremity, arthralgia, diarrhea, and dyspepsia. Elevations in liver enzymes and creatine phosphokinase (CPK) are also reported.
Clinical Research Highlights: Clinical trials demonstrate that the fixed-dose combination significantly improves treatment adherence and achieves greater LDL-C reduction compared to monotherapy.
6. Drug Interactions
CYP3A4 Inhibitors: Strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, erythromycin, clarithromycin, ritonavir) may increase plasma concentrations of atorvastatin, raising the risk of myopathy.
Fibrates: Concomitant use with fibrates (e.g., fenofibrate, gemfibrozil) increases the risk of myopathy and rhabdomyolysis.
Cyclosporine: Concomitant use is contraindicated due to the significantly increased risk of myopathy.
Digoxin: Atorvastatin may increase the plasma concentration of digoxin.
7. Pharmaceutical Information
Chemical Composition: Active Ingredients: Ezetimibe and Atorvastatin Calcium. Excipients: Lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, etc.
Appearance: Film-coated tablets (colors vary by strength).
Packaging: Blister packaging (e.g., 10 tablets per strip, 5 strips per box).
Storage: Store below 30°C, protected from moisture.