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CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, COMBINATIONS › Combinations of various lipid modifying agents
atorvastatin and ezetimibe
C10BA05
Forms & Strengths
- Atorvastatin/Ezetimibe oral tablets: 10/10 mg
- Atorvastatin/Ezetimibe oral tablets: 20/10 mg
- Atorvastatin/Ezetimibe oral tablets: 40/10 mg
- Atorvastatin/Ezetimibe oral tablets: 80/10 mg
Adult Dosing
- Primary hyperlipidemia: 10/10 mg to 80/10 mg orally once daily
- Initial dose usually selected based on baseline LDL-C and individual risk
- Maximum recommended dose is atorvastatin 80 mg / ezetimibe 10 mg daily
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 10 years of age
- Heterozygous familial hypercholesterolemia (pediatric patients 10-17 years): 10/10 mg to 40/10 mg orally once daily
Indications
- Adjunct to diet for treatment of primary heterozygous familial or non-familial hyperlipidemia
- Reduction of elevated total-C, LDL-C, Apo B, and triglycerides
- Increase in HDL-C in patients with hyperlipidemia
- Reduction of cardiovascular events in patients with coronary heart disease
Mechanism of Action
- Atorvastatin inhibits HMG-CoA reductase, preventing hepatic cholesterol synthesis and upregulating LDL receptors
- Ezetimibe localizes at the brush border of the small intestine and inhibits absorption of cholesterol, decreasing delivery to the liver
- Dual inhibition reduces hepatic cholesterol stores and clears cholesterol from the blood
Contraindications
- Active liver disease or unexplained persistent elevations of serum transaminases
- Hypersensitivity to atorvastatin, ezetimibe, or any component of the product
- Pregnancy and lactation due to potential fetal harm from HMG-CoA reductase inhibitors
Adverse Reactions
- Nasopharyngitis
- Myalgia and arthralgia
- Elevated serum transaminases (ALT/AST)
- Diarrhea and upper respiratory tract infections
- Rare: rhabdomyolysis, immune-mediated necrotizing myopathy
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, HIV protease inhibitors) increase atorvastatin exposure and myopathy risk
- Cyclosporine significantly increases systemic exposure of both atorvastatin and ezetimibe
- Gemfibrozil increases risk of myopathy and rhabdomyolysis; avoid coadministration
- Bile acid sequestrants decrease ezetimibe absorption; administer at least 2 hours before or 4 hours after
Curated Content: Needs Vetting Before Put to Clinical Use