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Statin Drugs
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Statin Drugs

(HMG-CoA Reductase Inhibitors)

Type of Medication

3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, commonly referred to as "statins"

Medications and Their Commonly Used Brand Names

Generic nameBrand name
atorvastatinLipitor
fluvastatinLescol
lovastatinMevacor
pravastatinPravachol
simvastatinZocor
rosuvastatinCrestor

What They Are Prescribed For

Hypercholesterolemia or dyslipidemia—high levels of LDL-cholesterol in the blood. May be accompanied by low levels of HDL-cholesterol and/or high levels of triglyceride.

Before prescribing medication to lower your cholesterol, your doctor will probably suggest that you try to control the levels of cholesterol in your blood through diet and exercise. This typically involves reducing your intake of total fat, saturated fat, and, if you are overweight, total calories. Some, but not all, people are able to lower their cholesterol through such changes. Medicine is prescribed only when additional help is needed. It is most effective in combination with dietary changes and regular exercise.

How Statins Work

Statins block an enzyme in the liver (HMG-CoA reductase) that produces cholesterol. They are particularly effective at reducing LDL-cholesterol.

Precautions While Using These Medicines

See Your Doctor Regularly

It is important that your doctor check your progress. Regular visits will allow for dosage adjustments and to help monitor for any side effects.

Avoid Pregnancy

Statins should not be taken during pregnancy. Cholesterol production is essential for normal fetal development. Statins decrease cholesterol production and therefore may cause birth defects. Use birth control while taking a statin drug. Tell your doctor if you think you might be pregnant or you are considering becoming pregnant. Also tell your doctor if you are breast feeding, as statins may cause problems for a nursing baby.

Control Your Weight

If you are overweight or obese, losing weight may help decrease the need for or amount of medication. Check with your doctor about this.

Manage Your Medications

Tell your doctor about all the medications you take. Some medications should not be taken with statins, while others may require a different dosage level. These include:

  • Antifungals—fluconazole (eg Diflucan), itraconazole (eg Sporanox), ketoconazole (eg Nizoral)
  • Cyclosporine (eg Neoral, Sandimmune, SangCya)
  • Digoxin (eg Lanoxin)—Use with atorvastatin, fluvastatin, or simvastatin may increase blood levels of digoxin, increasing the risk of side effects.
  • Macrolide antibiotics—erythromycin (eg E-Base, E-Mycin, ERYC, Ery-Tab, EES, EryPed, Erythro, Erythrocin, Erythro cot, Ilotycin, Ilosone, My-E, PCE, Wintrocin) and clarithromycin (eg Biaxin)
  • Fibric acid derivatives—gemfibrozil (eg Lopid), fenofibrate (eg TriCor), clofibrate (eg Atromid)
  • Niacin or nicotinic acid ( eg Endur-Acin, Nia-Bid, Niacor, Nico-400, Nicobid Tempules, Nicolar, Nicotinex Elixir, Slo-Niacin)—Use of this type of medicine with a statin may increase the risk of developing muscle problems and kidney failure.
  • Oral contraceptives/birth control pills (estrogens and progestins)—Some statin drugs may increase the blood levels of the hormones in birth control pills, increasing the risk of side effects.
  • Danazol (eg Danocrine)
  • Nefazodone (eg Serzone)
  • Anti-retroviral protease inhibitors—saquinavir (eg Invirase), ritonavir (eg Norvir), indinavir (eg Crixivan), nelfinavir (eg Viracept), amprenavir (eg Agenerase)
  • Verapamil (eg Calan, Isoptin)—Use with simvastatin may increase the risk of muscle problems

Be Cautious with Certain Medical Conditions

The presence of other medical problems may affect the use of statins. Tell your doctor if you have any other medical problems, especially:

  • Alcohol abuse (or history of)
  • Convulsions (seizures) that are not well controlled
  • Electrolyte or metabolic enzyme deficiencies or disorders
  • Infection
  • Liver disease or persistently high levels of liver enzymes—statin drugs may make liver problems worse
  • Low blood pressure
  • Organ transplant with therapy to prevent transplant rejection
  • Kidney failure
  • Recent major surgery or trauma, which may increase the risk of problems that may lead to kidney failure
  • Impending surgery, including dental surgery or emergency treatment—be sure to tell the doctor or dentist treating you that you are taking a statin drug

Avoid Excessive Alcohol

Excessive amounts of alcohol combined with statin drugs can have bad affects on the liver. Moderation in alcohol consumption is generally defined as one drink per day for women and two drinks per day for men.

Avoid Grapefruit Juice

Grapefruit juice appears to interfere with the metabolism of most statin drugs. It is best to avoid it during treatment.

Don't Stop On Your Own

Do not stop taking your statin medication without first checking with your doctor. When you stop, your cholesterol levels may increase, and your doctor may want to implement other means to keep cholesterol levels within a more desirable range.

Mind Your Meals with Lovastatin

Lovastatin works better when it is taken with food. If you are taking lovastatin once a day, take it with the evening meal. If you are taking more than one dose a day, take each dose with a meal or snack.

Missed Dose

If you miss a dose of your statin drug, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Avoid double doses.

Possible Side Effects

Statin drugs are generally considered safe and few patients need to discontinue them due to adverse effects. The side effects listed here have been reported for at least one of the statins, not necessarily all of them. However, since many of the effects of statins are similar, it is possible that these side affects may occur with any one of these medicines, although they may be more common with some than with others.

Adverse Effects

The most significant adverse effects, though rare, involve the liver (elevated liver enzymes) and the muscles (different conditions called myopathy and rhabdomyolysis). Following up regularly with your doctor will allow him or her to detect these problems through your medical history and blood tests.

Common Side Effects

More common side effects include:

Check with your doctor as soon as possible if any of the following side effects occur.

  • Ankle, feet, or leg swelling
  • Chest pain
  • Fever
  • Muscle aches, cramps, stiffness, tenderness, or weakness, especially if accompanied by unusual tiredness and/or fever
  • Skin rash
  • Constant or worsening stomach pain
  • Unusual tiredness or weakness
  • Jaundice (yellowing of the eyes or skin)

Check with your doctor if any of the following side effects occur frequently and/or become bothersome:

  • Constipation
  • Diarrhea
  • Dizziness
  • Gas
  • Headache
  • Heartburn
  • Indigestion
  • Nausea
  • Skin rash
  • Stomach pain
  • Decreased sexual ability
  • Trouble sleeping

RESOURCES:

American Academy of Family Physicians
http://familydoctor.org/

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

CANADIAN RESOURCES:

Canadian Pharmacists Association
www.pharmacists.ca

Health Canada
http://www.hc-sc.gc.ca/index_e.html

References:

USP Drug Information database. Available at: http://library.dialog.com/bluesheets/html/bl0461.html.



Last reviewed March 2008 by Michael J. Fucci, DO

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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