Atorvastatin

Atorvastatin, commonly known by the brand name Lipitor, belongs to a class of drugs called statins. It is prescribed to lower abnormal cholesterol and fat levels in the blood and to prevent cardiovascular disease in people at high risk. The medication is taken orally and works by blocking HMG-CoA reductase, a liver enzyme involved in cholesterol production. It is included on the World Health Organization's List of Essential Medicines and is widely available as a generic.

The drug is primarily used for two purposes: treating dyslipidemia (abnormal blood lipid levels) and preventing cardiovascular events. For dyslipidemia, it addresses conditions such as heterozygous familial and nonfamilial hypercholesterolemia, mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia, and combined hyperlipidemia. It can also be used in children with heterozygous familial hypercholesterolemia and in cases of homozygous familial hypercholesterolemia. In cardiovascular prevention, atorvastatin is used for primary prevention—reducing the risk of heart attack, stroke, and the need for revascularization in people with risk factors like age, smoking, high blood pressure, low HDL cholesterol, or a family history of early heart disease—even if they have no evidence of coronary artery disease. For secondary prevention, it lowers all-cause mortality, myocardial infarction, stroke, major coronary events, ischemic heart disease, and revascularization in those with established coronary artery disease. The effect is dose-dependent, with higher doses providing greater benefit, though close monitoring of liver function is needed at high doses. It is also used alongside lifestyle changes to prevent angina and to reduce heart attack and stroke risk in people with type 2 diabetes. A 2014 meta-analysis found high-dose statin therapy significantly superior to moderate or low doses for reducing plaque volume in acute coronary syndrome, a finding confirmed by the SATURN trial comparing high-dose atorvastatin and rosuvastatin.

Regarding kidney disease, atorvastatin may modestly reduce protein in the urine, but current evidence does not show it prevents progression to kidney failure. Before contrast medium administration, pretreatment with atorvastatin can lower the risk of contrast-induced acute kidney injury (CI-AKI) in people with pre-existing chronic kidney disease (eGFR below 60 mL/min/1.73 m²) undergoing procedures like cardiac catheterization, coronary angiography, or percutaneous coronary intervention. A meta-analysis of 21 randomized controlled trials found that short-term high-dose statin therapy, including atorvastatin, reduced CI-AKI incidence compared to low- or moderate-dose therapy or placebo in these patients. Atorvastatin can also help prevent in-hospital dialysis after contrast administration, though there is no evidence it reduces all-cause mortality from CI-AKI. Overall, statin therapy at any dose is more effective than no treatment for reducing CI-AKI risk.

For administration, statins with long half-lives like atorvastatin do not have a clear difference in cholesterol-lowering efficacy based on morning versus evening dosing, unlike short-half-life statins. A recent meta-analysis suggested that long-half-life statins might be more effective at lowering LDL cholesterol if taken in the evening, but the only atorvastatin study included did not specifically compare morning and evening dosing for LDL reduction. That trial confirmed that, regardless of timing, atorvastatin effectively reduces total cholesterol, LDL cholesterol, and triglycerides while increasing HDL cholesterol. Therefore, patients should take it at the same time each day, choosing a convenient time to ensure compliance.

In geriatric patients, plasma concentrations may be affected, but specific dosing adjustments are not detailed. Common side effects include diarrhea, heartburn, nausea, and muscle pain, which is typically mild and dose-dependent. Joint pain occurs less frequently. Muscle symptoms often appear in the first year and are commonly influenced by pre-existing health conditions and the nocebo effect. Most patients can continue therapy with dose adjustment or by switching to another statin. Rare but serious side effects (occurring in less than 0.1% of users) include rhabdomyolysis (a severe muscle disorder), liver problems, and diabetes. Use during pregnancy may harm the fetus. Atorvastatin was patented in 1986 and approved for medical use in the United States in 1996. In 2024, it was the most prescribed medication in the U.S., with over 115 million prescriptions for more than 29 million people. In Australia in 2023, it was the second most prescribed medication after rosuvastatin.