What Are Statins?
Statins are a class of lipid-lowering medications that function by inhibiting the enzyme 3-hydroxy-3-methyl-glutaryl coenzyme A reductase, which is involved in the rate-limiting step in the production of cholesterol. 1 These medications are foundational therapy for reducing cardiovascular disease risk through their powerful LDL-cholesterol lowering effects.
Mechanism of Action
Statins work primarily by:
- Inhibiting HMG-CoA reductase, the key enzyme in cholesterol biosynthesis
- Reducing levels of total cholesterol and LDL-C (low-density lipoprotein cholesterol)
- Moderately reducing triglyceride levels
- Exerting anti-inflammatory and plaque stabilization effects 1
Types of Statins
Currently available statins include:
- Lovastatin
- Simvastatin
- Pravastatin
- Fluvastatin
- Atorvastatin
- Rosuvastatin
- Pitavastatin 1
Clinical Benefits
Statins provide significant cardiovascular benefits:
- Reduce major vascular events by approximately 22% for each 1.0 mmol/L (~40 mg/dL) reduction in LDL cholesterol 1
- Reduce all-cause mortality by approximately 10% 1
- Decrease myocardial infarctions, revascularization procedures, stroke, and peripheral vascular disease 1
- Halt progression or contribute to regression of coronary atherosclerosis 2
Indications for Statin Therapy
The U.S. Preventive Services Task Force (USPSTF) recommends statins for:
- Adults 40-75 years with one or more cardiovascular risk factors (dyslipidemia, diabetes, hypertension, or smoking) and a calculated 10-year cardiovascular disease risk of 10% or greater 1
- Adults 40-75 years with risk factors and a 10-year risk of 7.5-10% may also benefit, though the evidence is less strong 1
- All patients with established atherosclerotic disease 2
Statins are not recommended for adults with LDL-C levels greater than 190 mg/dL or known familial hypercholesterolemia, as these individuals are considered to have very high cholesterol levels and require specialized management 1.
Potential Side Effects
While statins are generally well-tolerated, potential adverse effects include:
- Myalgia (muscle ache or weakness without CK elevation) in approximately 5-10% of patients 1, 2
- Myositis (muscle symptoms with increased CK levels) - less common 1
- Rhabdomyolysis (severe muscle injury) - rare, occurring in <0.1% of patients 2
- Elevated hepatic transaminases in 0.5-2.0% of cases (dose-dependent) 1
- Possible small increased risk of new-onset diabetes, particularly with high-dose statins 1, 2
Dosing Considerations
Statin dosing should be tailored based on:
- Primary prevention: Low-to-moderate intensity statins are generally sufficient 2
- Secondary prevention: High-intensity statins (atorvastatin 40-80 mg or rosuvastatin 20-40 mg) are recommended 2
- Elderly patients (>75 years): Consider moderate-intensity statins 2
- Renal impairment: Monitor for myopathy development; reduced dosing may be required 3, 4
Monitoring
Appropriate monitoring includes:
- Checking lipid levels 4-6 weeks after starting therapy to assess response 2
- Monitoring liver enzymes when clinically indicated rather than routinely 2
- Assessing for muscle symptoms, particularly in high-risk groups (elderly, those with renal impairment) 3, 4
Important Considerations
- Statins are contraindicated during pregnancy and breastfeeding 3, 4
- Drug interactions should be carefully monitored, particularly with medications that may increase the risk of myopathy 1
- Benefits typically outweigh risks in appropriately selected patients 2
Statins remain the cornerstone of cardiovascular risk reduction therapy due to their well-established efficacy and generally favorable safety profile when used appropriately.