The Statin Drugs

The Statin Drugs

Statins are drugs that improve cholesterol levels primarily by inhibiting the liver enzyme called "HMG C-A reductase." Statins have proven to be very effective in reducing cholesterol and in reducing the risk of heart attack and death. For this reason, and because they are generally well tolerated, they have become some of the most commonly prescribed drugs in the United States. Even so, recent federal guidelines indicate that statins are significantly underused, and that millions more Americans would benefit from them.

Which drugs are the statin drugs?

There are currently 6 statins on the market:

• atorvastatin (Lipitor)
• fluvastatin (Lescol)
• lovastatin (Mevacor)
• pravastatin (Pravachol)
• simvastatin (Zocor)
• rosuvastatin (Crestor)

A seventh statin, cerivastatin (Baycol) was removed from the market during the summer of 2001 because of potentially serious side effects.

How do statins work?

Statins reduce the liver's production of cholesterol, and increase the ability of the liver to remove LDL cholesterol ("bad" cholesterol) from the blood. They significantly reduce the level of LDL cholesterol in the blood. They also have a moderate ability to reduce triglyceride levels, and increase levels of HDL cholesterol ("good" cholesterol.)

Which statin is "best?"

For the most part, doctors decide which statin to use based on three factors: effectiveness in reducing cholesterol, effectiveness in clinical trials, and cost. To a large extent, however, statins can be used interchangeably.

Distinguishing features among statins

• The newest statin, rosuvastatin (approved August, 2003) has been called a "superstatin" because it appears to reduce LDL cholesterol to a greater degree than the other approved statin drugs.


• While all statins significantly reduce cholesterol, atorvastatin and simvastatin seem to reduce cholesterol levels to a greater extent than other "non-superstatins."


• Evidence of effectiveness in clinical trials is particularly strong for lovastatin, pravastatin, and simvastatin.


• While the cost of statins varies wildly, in general fluvastatin is the cheapest, and atorvastatin and simvastatin (and probably just-released rosuvastatin) are the most expensive.


• Simvastatin appears to increase HDL cholesterol to a greater extent than other statins.


• Simvatatin was used in the Heart Protection Study - a study showing for the first time that statins significantly reduce heart attack and stroke in high risk patients regardless of cholesterol levels.


• Lovastatin soon will become a generic drug, and the price will drop significantly.

What are the common side effects of statins?

• The most common side effects of the statins are gastrointestinal - nausea, gas, upset stomach. Less common are headache, dizziness, rash, and sleep disturbances (sleep disturbances appear to be more common with atorvastatin and simvastatin.)


• Statins cause elevations in liver enzymes in 1 of 100 patients. Blood tests should be checked after a few weeks of treatment.
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• Statins cause a muscle disorder producing muscle weakness, and occasionally pain, in 1 of 1000 patients. If muscle destruction is widespread, kidney failure and death can result.


• An exaggerated and potentially fatal form of this muscle disorder is the reason cerivastatin (Baycol) was removed from the market.


• Rosuvastatin was also seen to cause the severe form of muscle disorder, but only with the 80 mg dose (doses up to only 40 mg are approved.)


• Rosuvastatin also was reported to cause a poorly-explained kidney disorder in some patients with the 80 mg (unapproved) dose.

Drugs that interact with statins

• Grapefruit juice can increase the absorption of most statins. If statin levels go up too much, muscle damage can occur.


• Certain antibiotics and cyclosporin can increase the effect of statins, and increase the risk of muscle damage.


• Taking statins with gemfibrozil (a different kind of lipid lowering agent) can increase the risk of muscle damage.


• Atorvastatin and simvastatin can increase the effect of Coumadin, and can increase blood levels of digoxin.

Tricks for reducing the cost of statin therapy

• Ask your doctor if he/she can prescribe one of the cheaper statins


• Some statin pills can be cut in half with a pill splitter. Taking half of a larger pill (for instance, half of a 40 mg pill) is cheaper than taking a whole smaller pill (e.g., a 20 mg pill.)


• Ask your doctor if lovastatin would be suitable. When lovastatin becomes available in generic form in 2002, the price will plummet.


• Grapefruit juice can increase the absorption of statins. Suggest to your doctor that if you agree to take your statin drug with grapefruit juice, you might be able to get by with a lower dose.