The Status of Statins

FDA revises cholesterol drug safety information
Author: Sarah Aldridge

Statins’ star power has been phenomenal. The 2010 annual report of the US Centers for Disease Control and Prevention’s National Center for Health Statistics showed that statin use in adults 45 years and older jumped from 2% to 25% between 1988 and 2008. Although millions of Americans take the drug to stave off clogged arteries and heart disease, it can produce adverse effects. The US Food and Drug Administration (FDA) announced in February that it is changing the safety information packaged with statins to reflect new patient data.

Cholesterol’s Effects

Cholesterol is a fatty substance produced by the liver. It is needed for proper functioning of cell membranes and serves as a precursor molecule for bile acids, vitamin D and several hormones. It’s consumed in foods containing animal fats, such as eggs, beef, poultry and pork. It is also found in fried foods, some dairy products and in trans fats found in baked goods. While the body needs cholesterol to function, too much of it can be detrimental. Cholesterol when packaged with fat is sticky, so the excess gloms onto artery walls, where it can form hard substances called plaques. Atherosclerosis literally means “hardening of the arteries” and is characterized by narrowed blood vessels that have lost their elasticity. Stiff, blocked arteries reduce blood flow, which can lead to heart attacks and strokes.

Hypercholesterolemia, high cholesterol levels in the blood, can be due to a genetic predisposition, a high-fat diet or the presence of another disease, such as diabetes. If diet and exercise do not adequately lower the level of low-density lipoprotein, the so-called “bad” cholesterol in the body, and your doctor considers you at high risk, then a statin may be prescribed. Statins block the enzyme HMG-CoA from being converted into a form the liver can use to synthesize cholesterol. 

Revised Safety Warnings

According to the FDA, the package inserts for statins will now include several new or modified safety warnings. One will alert patients to the possibility of cognitive impairment. Some patients on statins have reported memory loss, forgetfulness and confusion. Another warning will mention the risk of type 2 diabetes due to an increase in blood sugar levels. A third alert will notify patients of the risk of drug-induced myopathy, muscle weakness and pain, especially from drug interactions with lovastatin. The final revision will notify patients that their liver enzymes will no longer need to be routinely monitored because the incidence of liver injury directly related to statin use is so rare. However, the FDA recommends that liver enzymes be measured before statin treatment begins and as needed if patients develop symptoms of liver damage, such as jaundice, fatigue and abdominal pain.

Cholesterol and Hemophilia

Although having hemophilia might seem to confer a protective effect against cardiovascular disease, that’s not the case. A 2010 study in the Journal of Thrombosis and Haemostasis found that people with hemophilia had equivalent degrees of atherosclerosis as their unaffected peers. Autopsies revealed no difference in the amount of hypertension, hypercholesterolemia, smoking and diabetes between the two groups. Further, the degree of stenosis, or abnormal artery narrowing, was comparable. 

“People with hemophilia can develop high cholesterol,” says Patrick Fogarty, MD, director of the Penn Comprehensive Hemophilia and Thrombosis Program at the University of Pennsylvania Medical Center in Philadelphia. “It’s not uncommon for individuals who have concurrent HIV infection to develop hyperlipidemia (elevated lipids, or fats, in the blood).” That’s because the highly active antiretroviral therapy (HAART) drugs prescribed for patients with HIV affect lipid, or fat, metabolism. HAART drugs can cause lipodystrophy, abnormal fat accumulation in different parts of the body.

Of all the FDA modifications to the new product inserts for statins, Fogarty is most concerned about the one for patients with pre-existing liver disease. “Everyone going on statins still will have to be monitored initially for changes in liver function tests,” he says. “You have to be even more cautious in a person who has underlying liver inflammation and high transaminases (elevated liver enzymes) to begin with.”

If you’re on HAART medications to treat HIV, or you have a family history of diabetes, heart disease or obesity, it’s important that your primary care physician evaluates your cholesterol values, says Fogarty. Routine screening is important for those without risk factors, too. “By the age of 40, every person should have his cholesterol levels measured,” Fogarty says.