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CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, COMBINATIONS › Combinations of various lipid modifying agents
pravastatin and ezetimibe
C10BA11
Forms & Strengths
- Pravastatin/Ezetimibe 10/10 mg oral tablet
- Pravastatin/Ezetimibe 20/10 mg oral tablet
- Pravastatin/Ezetimibe 40/10 mg oral tablet
- Pravastatin/Ezetimibe 80/10 mg oral tablet
Adult Dosing
- Primary hyperlipidemia: 1 tablet (pravastatin/ezetimibe 10/10 mg to 80/10 mg) orally once daily
- Initial dose typically based on individual statin requirement and renal function
- Administer at bedtime for optimal efficacy
Pediatric Dosing
- Safety and efficacy not established in pediatric patients; use not generally recommended
Indications
- Adjunct to diet for reduction of elevated total cholesterol, LDL-C, ApoB, and non-HDL-C in patients with primary hyperlipidemia
- Reduction of elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH)
Mechanism of Action
- Pravastatin: Competitive inhibitor of HMG-CoA reductase, halting hepatic cholesterol biosynthesis
- Ezetimibe: Inhibits intestinal absorption of cholesterol and phytosterols by targeting the Niemann-Pick C1-Like 1 (NPC1L1) transporter
- Combined dual inhibition targets both endogenous synthesis and exogenous absorption of cholesterol
Contraindications
- Hypersensitivity to pravastatin, ezetimibe, or any component
- Active liver disease or unexplained persistent elevations of serum transaminases
- Pregnancy and lactation
Adverse Reactions
- Myalgia and arthralgia
- Elevated serum transaminases (ALT/AST)
- Nasopharyngitis and upper respiratory tract infections
- Headache and dizziness
- Rare: Myopathy, rhabdomyolysis, immune-mediated necrotizing myopathy
Drug Interactions
- Cyclosporine: Significantly increases exposure of both pravastatin and ezetimibe; monitor closely
- Bile acid sequestrants (e.g., cholestyramine): Decrease absorption of ezetimibe; administer at least 2 hours before or 4 hours after sequestrants
- Fibrates: Increase risk of myotoxicity; gemfibrozil should generally be avoided
- Strong CYP inhibitors have minimal impact on pravastatin compared to other statins, but monitor for myopathy symptoms
Curated Content: Needs Vetting Before Put to Clinical Use