Statins — prescription drugs that lower cholesterol to reduce the risk of heart attacks and strokes — can save lives but they also have side-effects that can be debilitating for some patients.

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Doctors say most patients tolerate statins well but in some cases patients experience muscle pain and weakness, which can range from mild to severe.

Researchers at UBC’s faculty of medicine and the University of Wisconsin-Madison have shed light on what causes this side-effect and suggested how to fix it, in a first-of-its-kind study that could one day provide enormous relief for patients who need to take statins.

The study, published recently in Nature Communications, focused on atorvastatin, one of the most widely prescribed statins.

What the researchers discovered is how the statin binds to a protein that’s essential for muscle function.

“Not only do they bind, they actually drastically alter the function of that protein to a way that can actually cause muscle damage,” said Filip Van Petegem, the senior author and a professor at the UBC faculty of medicine’s department of biochemistry and molecular biology.

“And the way we did that is by using a visualization method where we can literally see the statins bind to that muscle protein and see what it does.”

He said the findings will help scientists eventually create new statins that don’t interact with muscle tissue.

“We know exactly what parts of the statin are important for inhibiting cholesterol synthesis, and now that we have very detailed 3D image of how the statins bind this critical muscle protein, we actually noticed that the way the statins interact is actually different between the two proteins,” he said.

It’s the first time that scientists have discovered how statins affect this muscle protein.

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“There have been many theories before on why statins affect muscles. None was really proven. And I think there was always a lot of skepticism on what mechanism is really responsible, but I think now seeing it really bind, that’s definitely a first.”

Why this matters

Van Petegem says more than 200 million people worldwide, including more than 2.8 million in Canada, rely on statins to keep their cholesterol at safe levels.

While a healthy diet low in cholesterol is beneficial, he said many people have a genetic disposition that makes it difficult to keep their levels down, raising their risk for stroke and heart disease.

Van Petegem said absolutely they are life-saving drugs, especially for a large swath of the population born with an inability to process cholesterol.

“In those cases, it almost doesn’t matter how much cholesterol you take from the diet, your blood cholesterol will be high no matter what,” he said. “There’s no doubt statins save lives.”

What’s next?

It will take time before new statins are developed and tested to provide relief from muscle fatigue so patients should follow the advice of their doctor and take statins if they can’t reduce their cholesterol, he said.

“If you have to choose between dying from cardiovascular disease or having muscle side-effects, obviously you should take the statins,” said Van Petegem.

Those with severe muscle pain must be very careful because it can lead to muscle breakdown, kidney failure and death. Anyone in this situation should talk with their doctor about alternative therapies that may include a different type of statin.

“In all other cases, it’s just a matter of being very careful and following the guidelines.”

Van Petegem’s team will next compare this research with different types of statins and determine which drugs are best for fewer side-effects.

ticrawford@postmedia.com