Statins: The New Wonder Drugs

his class of drug, which also goes by the tongue-twisting name HMG-CoA reductase inhibitors, has revolutionized the treatment of high cholesterol more than any other medication. In use for more than a decade, the drugs are sold under the brand names Lescol (fluvastatin), Lipitor (atorvastatin), Mevacor (lovastatin), Pravachol (pravastatin), and Zocor (simvastatin), Additionally, an extended-release form of lovastatin, called Altocor, was approved in 2002. It needs to be taken only once a day; most statins must be taken more often. To prevent confusion, we’re going to stick to the brand names throughout this chapter.

Statins work by partially blocking an enzyme called HMG-CoA, which controls how quickly your body produces cholesterol. (Remember that your body makes about three or four times more cholesterol than you eat.) By blocking this enzyme, statins put the brakes on cholesterol production. They also increase your body’s ability to remove LDL frorn your bloodstream: and bring it to the liver, where it’s broken down and eventually excreted. While statins aren’t as good as some other drugs at raising HDL levels or lowering triglycerides, they do have some positive effects in those areas.

Statins aren’t perfect, however. They don’t work very well at transforming small, dense LDL particles (which are more likely to burrow into artery walls) into larger, fluffier particles, or lowering lipoprotein (a)—Lp(a)—another particle that may contribute: to blood clots and plaque formation. So even if you’re taking a statin, your doctor may prescribe additional medications, depending on your other coronary risk factors.

How Well Do They Work?

Overall, studies find that statins can lower LDL levels from 10 to 60 percent, depending on the drug and dosage used. One landmark study completed in 1994, the Scandinavian Simvastatin Survival Study, found deaths from heart disease plummeted 42 percent, and deaths from all causes 30 percent, over five years in patients with heart disease who took Zocor. Several other studies found that Pravachol reduced heart attacks, surgical bypass, and angioplasties in patients without heart disease by lowering LDL levels. And one study found the drug reduced overall deaths in patients who had had a previous heart attack but who had cholesterol levels that were more or less average for the general population. New statins currently under development can lower LDL levels even more—up to 80 percent in some cases— garnering them the moniker “super statins.”

Given their tremendous success, it’s no wonder that statins are among the most frequently prescribed drugs in the United States (Lipitor is prescribed more than any other drug in America). Approximately 12 million Americans take statins. That’s a small fraction of the estimated 36 million that doctors believe are eligible for the drugs based on guidelines set by the National Institutes of Health. In fact, some experts suspect that within a few years, half of all American adults will be taking statins, which some call the “drug of the century.”

Such faith in the drugs is fueled in part by a British study, published in the medical journal Lancet, which concluded that just about anyone, of any age and at any risk for heart disease, could benefit from statins. risk for heart disease, could benefit to statins that extend far beyond your cholesterol are the new aspirin


Some experts suspect that within a few years, alf of all Americans will be taking statins, which some call the “drug of the century.

Statins generally take between four which some call the to six weeks to reach their maximum | effectiveness. Dosages for statins vary | “drug of the century. : depending on the drug, but at least one dose will be taken at dinner or bedtime because the body manufactures more cholesterol at night than during the day.

Stick with It

Just because your cholesterol readings drop doesn’t mean you can stop taking a prescribed statin without your doctor’s say-so. Yet 25 percent of people 65 and older stop taking statins within the first six months, against their doctor’s orders. This is a bad idea for several reasons, not least of which is that statins can’t keep your cholesterol under control if you don’t take them. Moreover, some studies suggest that abruptly stopping the drugs could result in problems, including an increased risk of heart attack, unstable angina, and stroke. Studies in rats found that stopping the drug suddenly dried up production of nitric oxide, the compound responsible for keeping artery walls smooth and flexible and helping to make blood platelets less sticky.

Following the Plan may enable you to take fewer prescription drugs, or even stop taking them altogether eventually. But don’t taper off or forgo your medication without first talking to your doctor.

Paying for Statins

The cost of statins varies widely—from about $55 a month to more than $200 a month (without insurance)—depending on the drug and the dosage. If your insurance plan doesn’t cover prescription drugs, the cost can be quite onerous. But there are ways to spend less. For instance, because drugs are sold by the pill, not by the strength, you can ask your doctor to prescribe double the strength you need (80 milligrams rather than 40 milligrams, for example), then buy a pill-splitter and cut the pills in half. Grapefruit juice increases absorption of statins. If you take your medication with grapefruit juice, let your doctor know; you may be able to get by with a lower dose.

Expect prices to begin dropping since the first generic statin—lovastatin—was approved in 2001. At about $1 a pill, it. costs about half as much as its branded version, Mevacor. In coming years more generic statins will become available and may significantly reduce overall prices in this class of drug.

Let your doctor know if you’re having trouble paying for your drugs, Most pharmaceutical companies have special programs in which they provide prescription drugs for free or reduced rates to people who can’t afford them. Your doctor can tell you more.

The Downside to Statins

Like all drugs, statins have their drawbacks. While they’re deemed extremely safe, given the large number of people who take them and the fact that they’ve been in use for more than 14 years, in rare cases they can cause problems. Among the potential side effects:

Muscle and kidney damage. In 2001 Bayer AG voluntarily recalled its statin drug, Baycol (cerivastatin), from the U.S. market because of reports of at least 31 deaths in the United States linked to the drug. The deaths were the result of a condition called rhabdomyolysis, in which muscle cells break down, releasing proteins that become trapped in the kidneys. This interferes with the kidneys’ ability to filter out toxins from the blood, leading to kidney failure and, potentially, death. Symptoms include muscle pain, weakness, tenderness, malaise, fever, dark urine, nausea, and vomiting. 

While all statins have been associated with very rare reports of rhabdomyolysis, according to the FDA the risk was 16 to 80 percent higher with Baycol, particularly when used at higher doses, in elderly patients, and in combination with Lopid (gemfibrozil), another lipid. lowering drug, The rhabdomyolysis risk associated with the statins that remain on the market, especially when the drugs are used alone by people without rhabdomyolysis risk factors such as renal impairment, is extremely small.

Much less serious is the muscle weakness or pain experienced by some people taking statins. You’re more susceptible if you’re older than 80, have a small body frame or are frail, have a multisystem disease (such as chronic renal insufficiency), or take multiple medications. Generally about 5 percent of people taking statins will experience these side effects. They usually go away once the drug is stopped and can often be prevented by taking coenzyme Q10), which you read about in this Chapter .

Liver damage. Like most drugs, statins are broken down in the liver, thus putting additional stress on the organ. That’s why your doctor will monitor your levels of liver enzymes—an indication of the health of your liver—for the first few months that you are taking the drugs. You should also limit your use of alcohol, which puts additional stress on your liver and increases the risk of liver failure if you’re taking statins (or other medications). Elevated liver enzymes occur in 0.5 to 2 percent of people taking statins—generally those taking the highest doses. Full liver failure is extremely rare, and reducing the drug dose usually reverses elevated enzymes.

Depletion of coenzyme Q10. As we discussed in Chapter, statins also seem to decrease the body’s production of the important substance coenzyme Q1LO0. Cells need CoQ10 to help them use energy, That’s why we recommend you supplement with 100 milligrams daily of CoQ10 if you take statins.

Cataracts. Statins alone don’t cause cataracts. But according to a study published in the Archives of Internal Medicine in September 2001, taking Zocor along with the antibiotic erythromycin might increase the risk. Just a single course of antibiotic, typically taken for 10 days, appeared to double the risk of cataracts, while two or more courses tripled it. If you take statins and need antibiotics, talk with your doctor.

Nerve damage. Researchers studying 500,000 Danish residents found that people who took statins were more likely to develop a form of nerve damage called polyneuropathy than those who never took the drugs. The condition, also known as peripheral neuropathy, results in weakness, tingling, pain in the hands and feet, and difficulty walking. Taking statins for one year those prescribed to humans. However, two later studies examining large populations of people taking statins found no connection between this class of drug and cancer. increased the risk of nerve damage about 15 percent, or one case for every 2,200 patients; for those taking the drug two or more years, the risk increased 26 percent.

Six Side Benefits of Statins

The more researchers study statins, the more potential uses they’re finding for this class of drug, prompting: some doctors to jokingly suggest that it be added to the water supply. Among its potential uses:

Lowering CRP. Numerous studies have found that statins can lower levels of C-reactive protein (CRP), a sign of inflammation that researchers now suspect may be a better predictor of heart disease than even high cholesterol. A study in the journal Circulation in August 2002 showed that Zocor lowered CRP levels in just two weeks.

Reducing stroke risk. In several large studies of statins in patients with existing heart disease. the drugs reduced the risk of a first-time stroke between 11 and 30 percent, An analysis of several published trials suggests statins’ effect on stroke risk’ may be due to more than just its ability to reduce cholesterol. For instance, statins. improve the function of endothelial cells (the cells that make up the artery walls), probably by boosting their production of nitric oxide. This helps keep artery walls smooth and flexible and reduces the likelihood of plaque formation. Statins also. reduce inflammation, make blood platelets less sticky, exert some antioxidant effects, help stabilize plaque so it doesn’t burst, and help prevent blood clots.

Treating autoimmune diseases and preventing transplant rejection. In autoimmune diseases such as psoriasis and rheumatoid arthritis, am overactive immune system 

gets confused, thinks the body’s own cells In the largest study so are foreign invaders, and begins attacking f h f a them. But researchers found that statins ar, TEsearcners LOUN block the action of certain immune cells that taking statins that play a role in these diseases. These ; immune cells are also involved in the reduced the risk of rejection of transplanted organs, leading developing Alzheimer’s researchers to suspect that a statin-like drug could one day be used in place of near. ly 80 percent. other transplant-rejection medications,

In the largest study so far researches found that taking statins reduced the risk of developing Alzheimer’s near 80 percent.

of statins on the immune system lies in the treatment of multiple sclerosis (MS), an autonmmune disease. In one study in the journal Neurology, statins prevented the growth of immune cells that contribute to this disease. When mice with MS were treated for a week with doses of Lipitor equal to the highest human dose, the drug reversed or prevented relapses and curbed brain inflammation, a hallmark of the disease, As of this writing. clinical trials in humans with MS were to begin in 2003,

Bettering bone health. Several animal and retrospective studies (in which researchers looked back at people who had been taking statins) found that statins may help bones grow, suggesting a possible use in osteoporosis, which causes brittle bones, Today most treatments for osteoporosis simply slow bone loss. A drug that could actually get bones to grow would be a major breakthrough.

The jury is still out on whether, and by how much, statins can increase bone density, Even if they can, don’t look for your doctor to prescribe them for osteoporosis anytime soon. Instead, they may pave the way for the development of drugs that have a similar molecular structure but are designed specifically for bone health.

Fighting dementia and Alzheimer’s disease. As we cliscussed in Chapter , there is increasing evidence that cholesterol may play a role in the development of certain dementias, including Alzheimer’s disease. This begs the question, of course, about whether cholesterol-lowering drugs could reduce the risk of Alzheimer’s disease and other dementias. The answer is “maybe.” In the largest study so far, researchers examined risk factors for Alzheimer’s and medication history in 912 people who either definitely or probably had Alzheimer’s, and 1,669 of their family members. They found that taking statins reduced the risk of developing Alzheimer’s nearly 80 percent. Statins appear to work by blocking the actions of a protein called A-beta, which makes blood vessels constrict, restricting the flow of blood to the brain.

Diabetes. When researchers evaluated data from one of the largest clinical trials on statins, they found that Pravachol reduced the risk of developing diabetes by 30 percent. They theorize the effect may be due to Pravachol’s ability to lower triglyceride levels. (Other statins may lower triglycerides as well.) High triglycerides lead to high circulating levels of free fatty acids, which in turn impair the ability of insulin to interact with its receptor. Lowering triglycerides is a way of preserving insulin sensitivity and preventing insulin resistance.

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