Preventive Cardiology: Statins
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Preventive Cardiology: Statins

Medication (Name): Statins

Commonly Used Brand and Generic Names:

Generic Names—lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, cerivastatin, rosuvastatin

Common Brand NamesMevacor, Zocor, Pravachol, Lescol, Lipitor, Baycol, Crestor

General CategoriesHMG-CoA reductase inhibitor (systemic), antihyperlipidemic

Current Uses

Treatment for the Following Conditions

Prevention

Statins help reduce the risk of a heart attack in people who have:

  • High total cholesterol
  • High LDL cholesterol
  • High triglyceride levels
  • Low HDL cholesterol (slightly effective)
  • Coronary artery disease

What the Research Shows

Numerous studies suggest that statins can dramatically reduce LDL cholesterol ('bad cholesterol") levels and reduce the risk of death from heart disease. According to the US Food and Drug Administration (FDA), statins can lower LDL cholesterol levels by as much as 60%, depending on the drug and dosage. One study published in the March 1998 issue of Circulation found that, with every 10 percentage points cholesterol was reduced, the risk of death from coronary heart disease dropped by 15%. A 2002 study showed that lowering the LDL cholesterol level to <77 mg/dL (2.0 mmol/L) decreased the number of cardiovascular events such as heart attacks or stroke among patients in the study.

The National Cholesterol Eudcation Program Adult Treatment Panel III (NCEP ATP III) guidelines of 2004 set slightly different criteria for LDL cholesterol when compared to the 2001 criteria:

Risk2001 2004
High<100 mg/dL (<2.6 mmol/L)<70 mg/dL (<1.8 mmol/L)
Moderate<130 mg/dL (<3.4 mmol/L)<100 mg/dL (<2.6 mmol/L)
Low<160 mg/dL (<4.1 mmol/L)<160 mg/dL (<4.1 mmol/L)

Mechanism for How It Works

HMG-CoA reductase is an enzyme that helps your body make cholesterol. Statins help to block this enzyme, which in turn causes your body to make less cholesterol. When you make less cholesterol, your liver makes more LDL receptors, which attract LDL particles in the blood. This reduces the amount of LDL ("bad") cholesterol in your bloodstream. Lower LDL cholesterol levels also tend to lead to lower levels of triglycerides and higher HDL (“good”) cholesterol levels in the blood. Statins have anti-inflammatory effects on blood vessels which help reduce the formation of fatty plaque on blood vessel walls.

Side Effects

Drug Interactions

  • Cyclosporine (eg, Sandimmune)
  • Gemfibrozil (eg, Lopid)
  • Clofibrate (eg, Atromid-S)
  • Fenofibrate (eg, Tricor)
  • Niacin—statins may increase the risk of kidney failure and muscle problems
  • Digoxin (eg, Lanoxin)—may increase blood levels of digoxin and side effects if used with atorvastatin, fluvastatin, or simvastatin
  • Oral Contraceptives (birth control pills)—increased side effects and blood levels of birth control hormones possible if used with atorvastatin
  • HIV Protease Inhibitors—(amprenavir (eg, Agenerase), indinavir (eg, Crixivan), nelfinavir (eg, Viracept), ritonavir (eg, Norvir), saquinavir (eg, Fortovase, Invirase))
  • Nefazodone (eg, Serzone)—may increase the risk of kidney failure and muscle problems if used with simvastatin
  • Verapamil (eg, Calan, Isoptin)—may increase risk of muscle problems if used with simvastatin
  • Erythromycin—may increase risk of muscle problems with statins

Nutrient/Supplement Interactions

Do not take the following with statins except on medical advice:

  • Grapefruit Juice—increases the absorption of most statins, allowing potentially excessive levels to build up in the bloodstream
  • Chaparral, Comfrey, and Coltsfoot—may increase the risk of liver problems
  • St. John’s Wort—may decrease blood levels of some statins
  • Vitamin B3 (Niacin)—possibly increases the risk of developing a potentially fatal condition called rhabdomyolysis. Rhabdomyolysis occurs when skeletal muscles are damaged, thereby releasing myoglobin into the bloodstream. Myoglobin is an iron-containing pigment that can cause severe damage to the kidneys.)
  • Red Yeast Rice—contains a mixture of statins and should not be combined with statin drugs without medical supervision

Other Potential Concerns

The following should be considered if you are taking statins:

  • These conditions can affect the use of statins:
    • Allergy or intolerance to statins, allergies to other substances, including foods
    • Significant obesity—can make statins less effective
    • The effects of more healthful eating and exercise habits–may determine whether or not you need to take statins as well as the dose
  • Be sure to tell your doctor if you have any other medical problems such as:
    • Alcohol abuse
    • Liver disease
    • Seizures that are not well-controlled
    • Organ transplant with therapy to prevent transplant rejection
    • Recent major surgery

    Breastfeeding—statins may cause unwanted effects in nursing babies and therefore are not recommended for use during breastfeeding.

    Children—some statins have been used effectively in a small number of children but their long-term safety in children has not been established

    Pregnancy—statins may cause birth defects or other problems in the baby and therefore should not be taken during pregnancy

What to Watch For (Physical/Biochemical/Physiological)

Common Side Effects:

  • Nausea
  • Gas
  • Upset stomach
  • Heartburn
  • Abdominal pain
  • Headache
  • Dizziness
  • Skin rash

Less Common Side Effects:

  • Sleep disturbances
  • Decreased sexual ability
  • Blurry eyesight
  • Muscle pain (myopathy) or joint pain
  • Rhabdomyolysis with renal dysfunction
  • Elevated liver enzymes in the blood
  • Protein in urine

Recommendations

Take only the amount of statin ordered by your doctor .

  • Do not stop taking this medicine for any reason without first checking with the doctor who directed you to take it.
  • Tell your doctor or dentist about taking this medicine before having any kind of surgery, dental procedure, or emergency treatment.

RESOURCES:

American Heart Association
http://www.americanheart.org

US Food and Drug Administration
http://www.fda.gov

References:

Amarenco P, Bogousslavsky J, Callahan A III, et al. High-dose atorvastatin after stroke or transient ischemic attack. N Engl J Med . 2006;355:549-59.

Complementary Therapies

Grundy SM, Cleeman JL, Merz CN et al. National Heart, Lung, and Blood Institute, American College of Cardiology Foundation; American Heart Association. Implications of recent clinical trials for the National Cholesterol Eudcation Program Adult Treatment Panel III (NCEP ATP III) guidelines. Circulation . 2004;110:227-239.

HMG-CoA reductase inhibitors (systemic). US Pharmacopeia (USP-DI). Available at: http://www.usp.org. Accessed on January 28, 2003.

Keeping cholesterol under control. US Food and Drug Administration website. Available at: http://www.fda.gov/fdac/features/1999/199_chol.html. Accessed on January 28, 2003.

Lemaitre RN, Psaty B, Heckbert SR, et al. Therapy with hydroxymethylglutaryl coenzyme A reductase inhibitors (statins) and associated risk of incident cardiovascular events in older adults. Arch Intern Med . 2002;162:1395-1400.

Middleton A, Binbrek AS, Fonseca FA, et al. Achieving 2003 European lipid goals with rosuvastatin and comparator statins in 6743 patients in real-life clinical practice: DISCOVERY meta-analysis. Curr Med Res Opin . 2006;22: 1181-91.

Stender S, Schuster H, Barter P, et al. Comparison of rosuvastatin with atorvastatin, simvastatin, and pravastatin in achieving cholesterol goals and improving plasma lipids in hypercholesterolaemic patients with or without the metabolic syndrome in the MERCURY I trial. Diabetes Obes Metab. 2005;7:430-8.

Tahara N, Kai H, Ishibashi M, et al. Simvastatin attenuates plaque inflammation: evaluation by fuorodeoxyglucose positron emission tomography. J Am Coll Cardiol . 2006;48:1825-31.

Texas Heart Institute. Available at: http://www.tmc.edu/thi/. Accessed on January 28, 2003.



Last reviewed February 2007 by David Juan, MD

Please be aware that this information is provided to supplement the care provided by your physician. It is neither intended nor implied to be a substitute for professional medical advice. CALL YOUR HEALTHCARE PROVIDER IMMEDIATELY IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY. Always seek the advice of your physician or other qualified health provider prior to starting any new treatment or with any questions you may have regarding a medical condition.

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