From the Guidelines
Statins are the first-line medication for hyperlipidemia, with options including atorvastatin, rosuvastatin, simvastatin, and pravastatin. These medications work by inhibiting HMG-CoA reductase, an enzyme crucial for cholesterol production in the liver, thereby reducing LDL cholesterol levels by 20-60% 1. For patients who cannot tolerate statins or need additional lipid lowering, second-line options include ezetimibe (which blocks intestinal cholesterol absorption), PCSK9 inhibitors (evolocumab, alirocumab), bile acid sequestrants, fibrates (gemfibrozil, fenofibrate), and niacin.
Some key points to consider when treating hyperlipidemia include:
- The decision to start pharmacological therapy is dependent on the clinician’s judgment between triglyceride levels of 200 mg/dl and 400 mg/dl, with strong consideration given to pharmacological treatment of triglyceridemia above 400 mg/dl to minimize the risk of pancreatitis 1.
- Treatment is typically lifelong and should be accompanied by lifestyle modifications including a heart-healthy diet, regular exercise, weight management, and smoking cessation.
- Medication choice depends on the specific lipid abnormality, cardiovascular risk factors, potential drug interactions, and individual tolerance.
- Regular monitoring of lipid levels and liver function is important to assess treatment effectiveness and detect potential side effects.
The most recent and highest quality study, published in 2022, supports the use of PCSK9 inhibitors and ezetimibe for the reduction of cardiovascular events in high-risk patients with primary hypercholesterolaemia and mixed dyslipidaemia who are intolerant to statins or who fail to meet target LDL cholesterol levels despite statin therapy 1. However, the choice of medication should always be individualized based on the patient's specific needs and circumstances.
From the FDA Drug Label
What is ezetimibe tablets Ezetimibe tablets is a medicine used with a cholesterol lowering diet: and with other cholesterol medicines called a statin, or alone (when additional cholesterol lowering treatments are not possible), to lower elevated low-density lipoprotein cholesterol (LDL-C) or bad cholesterol in adults with primary hyperlipidemia (too many fats in your blood), including heterozygous familial hypercholesterolemia (HeFH).
The medication for hyperlipidemia is ezetimibe.
- It is used to lower elevated low-density lipoprotein cholesterol (LDL-C) or bad cholesterol in adults with primary hyperlipidemia.
- It can be used alone or with other cholesterol medicines, such as a statin.
- It is also used to treat heterozygous familial hypercholesterolemia (HeFH) and homozygous familial sitosterolemia. 2
From the Research
Medications for Hyperlipidemia
The following medications are used to treat hyperlipidemia:
- Statins, such as atorvastatin 3, 4 and rosuvastatin 3, 4, 5
- Ezetimibe, often used in combination with simvastatin 5
- Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors 6
- Fibrate, prescription-grade omega-3 fatty acid, and/or niacin 7
- Icosapent ethyl, added to a statin in patients with established ASCVD or diabetes with ≥2 ASCVD risk factors and triglycerides between 135 and 499 mg/dL 7
- Bempedoic acid 7
- Colesevelam 7
Dosages and Efficacy
- Atorvastatin: 80 mg/day, reduces LDL-C by approximately 50% 3
- Rosuvastatin: 40 mg/day, reduces LDL-C by 43% to 63% 4, and is superior to atorvastatin in decreasing LDL-C 3, 4
- Ezetimibe/simvastatin: results in significantly greater reductions in LDL compared to rosuvastatin or atorvastatin 5
Treatment Guidelines
- Patients at extreme ASCVD risk should be treated with high-intensity statin therapy to achieve a goal LDL-C of <55 mg/dL 7
- Patients at very high ASCVD risk should be treated to achieve LDL-C <70 mg/dL 7
- Treatment for moderate and high ASCVD risk patients may begin with a moderate-intensity statin to achieve an LDL-C <100 mg/dL 7