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Understanding Cholesterol-Lowering Medications (cont.)

Statins

What are some examples of statins prescribed?

Examples of statins approved in the U.S. include:

atorvastatin (Lipitor),
fluvastatin (Lescol),
lovastatin (Mevacor, Altocor),
pravastatin (Pravachol),
simvastatin (Zocor), and
rosuvastatin (Crestor).

How do statins work?

Statins inhibit the enzyme HMG-CoA reductase, which controls the rate of cholesterol production in the body. These drugs lower cholesterol levels from 20%-60% by slowing the production of cholesterol and by increasing the liver's ability to remove the "bad" cholesterol (low-density lipoprotein or LDL) already in the blood. Statins lower LDL cholesterol levels more effectively than other types of drugs. They also modestly increase "good" cholesterol (high-density lipoprotein or HDL) and decrease total cholesterol and triglycerides.

Results are usually seen after four to six weeks of taking statins. Statins have been studied extensively and overall have been proven to decrease the risk of heart attack, stroke, death, and other coronary artery diseases that are related to high cholesterol levels.

Who should not use these statins?

You should not use statins if you fit any of the following situations:

You are allergic to statins or their ingredients.
You are pregnant or are planning a pregnancy.
You are breastfeeding.
You have active liver disease.
You excessively consume alcohol.
You have a history of myopathy (a type of muscle disease).
You have renal failure due to rhabdomyolysis.

Use: Statins come in tablet or capsule forms and are usually taken with the evening meal or at bedtime because the body makes more cholesterol at night than during the day.

Children: Some statins are also indicated for children aged 10-17 years of age with heterozygous familial hypercholesterolemia (girls in this age range must have already begun menstruating). When used in combination with diet, statins reduce total cholesterol, LDL, and apo B levels in children with heterozygous familial hypercholesterolemia. After an adequate trial of diet therapy, statins may be considered for treatment in children if the following findings are present:

LDL-C remains greater than or equal to 190 mg/dL.
LDL-C remains greater than or equal to 160 mg/dL and one of the following exists:

A positive family history of premature cardiovascular disease
Two or more other cardiovascular disease risk factors in the pediatric patient

Drug or food interactions: Consuming large quantities of grapefruit juice, more than 1 quart per day, decreases the ability of the liver to metabolize some statins, such as atorvastatin, simvastatin, or lovastatin. Also, and possibly more importantly, statins and certain other medications can interact, causing serious side effects. Tell the doctor about any prescription and nonprescription medications the patient is taking, including the following:

Vitamins
Herbal supplements
Medication for your immune system, such as cyclosporine, a drug prescribed following organ transplantation
Other cholesterol medications, such as fibrates or nicotinic acid
Medication for infections, such as erythromycin, telithromycin, clarithromycin (Biaxin), itraconazole (Sporanox), or ketoconazole (Nizoral, Extina, Xolegel, Kuric)
Verapamil (Calan, Verelan, Verelan PM, Isoptin, Isoptin SR, Covera-HS), diltiazem (Cardizem, Dilacor, Tiazac and several others), amiodarone (Cordarone), or dioxin
Birth control pills
Medication for HIV or AIDS, such as indinavir (Crixivan) or ritonavir (Norvir)
Warfarin (Coumadin) (warfarin may have an increased effect when administered with some statins, such as rosuvastatin, lovastatin, or simvastatin. The international normalized ratio [INR] must be closely monitored when warfarin is administered with statins.)

Side Effects: Statins are well tolerated, and serious side effects are rare.

If you experience diffuse muscle soreness, pain, and weakness; vomiting; or stomach pain or if your urine is brown (a possible sign of muscle breakdown), contact your doctor immediately and stop taking the statin medication. You may need blood tests for possible muscle problems. Rarely, widespread muscle breakdown, known as rhabdomyolysis, can occur, usually in people who are taking other drugs that interfere with the breakdown of the statin and in people with advanced kidney problems. This is a medical emergency.
Some people experience an upset stomach, gas, constipation, and abdominal pain or cramps. These symptoms are usually mild to moderate and generally disappear as the body adjusts to the medication. Liver function is usually monitored in patients taking statins. Rare reports of neuropathy (numbness and tingling) affecting the hands, arms, feet, and legs have been described.