Cholesterol-Lowering Drugs

AHA Recommendation

Drug therapy can be considered for patients who — in spite of adequate dietary therapy, regular physical activity and weight loss — need further treatment for elevated blood cholesterol levels. The guidelines for those
who qualify are...

LDL Cholesterol

- Level for Drug Consideration (after therapeutic life changes)
- Goal of Therapy

Without coronary heart disease and with fewer than two risk factors+

- 190 mg/dL or higher*
- less than 160 mg/dL

Without coronary heart disease and with two or more risk factors 160 mg/dL or higher

- less than 130 mg/dL

With coronary heart disease

- 130 mg/dL or higher**
- 100 mg/dL or less

* Drug therapy is optional for LDL-C 160–189 mg/dL (after dietary therapy). For persons with severe elevations of LDL-C (e.g., >/= 220 mg/dL), drug therapy can be started together with dietary therapy.

** In coronary heart disease patients (or those with 2+ risk factors) with LDL cholesterol levels of 100 to 129 mg/dL, the physician should exercise clinical judgment in deciding whether to begin drug treatment.

In some cases, a physician may decide that using cholesterol-lowering drugs at lower LDL cholesterol levels is justified. On the other hand, drug therapy may not be appropriate for some patients who meet the above criteria. This may be true for elderly patients.

What drugs are most commonly used to treat high cholesterol?

The drugs of first choice for elevated LDL cholesterol are the HMG CoA reductase inhibitors, e.g., atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin and simvastatin. Statin drugs are very effective for lowering LDL cholesterol levels and have few immediate short-term side effects.

-They are easy to administer, have high patient acceptance and have few drug-drug interactions.

-Patients who are pregnant, have active or chronic liver disease, or who are allergic to statins shouldn't use statin drugs.

-The most common side effects are gastrointestinal, including constipation and abdominal pain and cramps. These symptoms are usually mild to severe and generally subside as therapy continues.

Another class of drugs for lowering LDL is the bile acid sequestrants — colesevelam, cholestyramine and colestipol — and nicotinic acid (niacin). These have been shown to reduce the risk for coronary heart disease in controlled clinical trials. Both classes of drugs appear to be free of serious side effects. But both can have troublesome side effects and require considerable patient education to achieve adherence. Nicotinic acid is preferred in patients with triglyceride levels that exceed 250 mg/dL because bile acid sequestrants tend to raise triglyceride levels.

Niacin (nicotinic acid) comes in prescription form and as “dietary supplements.” Dietary supplement niacin is not regulated by the U.S. Food and Drug Administration (FDA) the same way that prescription niacin is. It may contain widely variable amounts of niacin — from none to much more than the label states. The amount of niacin may even vary from lot to lot of the same brand.

-Dietary supplement niacin must not be used as a substitute for prescription niacin. It should not be used for cholesterol lowering because of potentially very serious side effects.