Fixed-dose combination: statin plus intestinal cholesterol absorption inhibitor
ATC code: C10BA05 (Atorvastatin and ezetimibe)
Atorvastatin blocks HMG-CoA reductase in the liver – hepatocytes synthesize less cholesterol and take up more from the bloodstream. Ezetimibe blocks the intestinal NPC1L1 protein, reducing dietary and biliary cholesterol absorption. Additive effect: on top of the 30-50% LDL-C reduction from the statin, ezetimibe adds another 20-25%. IMPROVE-IT (NEJM 2015) showed a 6.4% reduction in cardiovascular events over 7 years.
Second line
Primary hypercholesterolemia and mixed dyslipidemia in patients not reaching -C goal on the maximum tolerated dose of atorvastatin. Per 2019 and SEA 2023, post-MI or post-stroke LDL-C goal is <55 mg/dL; very high ASCVD risk also <55 mg/dL; high risk <70 mg/dL. Dose: 10/10, 20/10, 40/10, 80/10 mg once daily in the evening (cholesterol synthesis peaks at night). Effect at 4-6 weeks; lipid check at 6-8 weeks and every 6-12 months thereafter.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Atorvastatin + ezetimibe is sometimes sold as a longevity drug and as cholesterol lowering for healthy young adults with -C <130 mg/dL and ASCVD risk <5%. Per 2019, 2018, and SEA 2023, statin therapy is not initiated for ASCVD risk <5% – benefits do not exceed harms (myopathy, transaminitis, hyperglycemia). Ezetimibe + statin has no indication in young patients without diagnosed dyslipidemia or familial hypercholesterolemia. If prescribed for anti-aging without calculation or a familial form, consider getting a second opinion and a formal ASCVD risk estimate.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Contraindicated. Statins are teratogenic (impair fetal cholesterol synthesis). Effective contraception in women of reproductive age; stop the statin 1-2 months before planned conception.
Contraindicated. Statins pass into milk in clinically relevant amounts; theoretical risk for infant neurodevelopment. Defer statin therapy during breastfeeding or use only colestyramine/colestipol (non-absorbed).
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Atorvastatin + Ezetimibe is evaluated for the following indications with varying evidence strength: Dyslipidemia (evidence tier A), Anti-aging and longevity (evidence tier D). See the full indication matrix with dosing and citations above on this page.
Common side effects of Atorvastatin + Ezetimibe (≥ 1 in 100): Myalgia, Arthralgia, GI upset, Transaminase elevation, Headache, Slightly higher risk of new-onset type 2 diabetes in predisposed. See the Safety section for uncommon and serious reactions.
FDA category X. Contraindicated. Statins are teratogenic (impair fetal cholesterol synthesis). Effective contraception in women of reproductive age; stop the statin 1-2 months before planned conception.
Contraindicated. Statins pass into milk in clinically relevant amounts; theoretical risk for infant neurodevelopment. Defer statin therapy during breastfeeding or use only colestyramine/colestipol (non-absorbed).
Atorvastatin + Ezetimibe is contraindicated in: Hypersensitivity; Active liver disease or persistent unexplained transaminase elevation; Pregnancy and breastfeeding; Concomitant strong CYP3A4 inhibitors at high doses (telaprevir, tipranavir/ritonavir). Full list in the Safety section.