Welcome to Mayo Clinic's podcast. This month's topic is controlling cholesterol with statin medications. I'm your host, Rich Dietman.

We may not know exactly what it does, but most of us have heard of cholesterol, and most of us know that too much of one type of cholesterol — LDL, or low-density lipoprotein — can be bad for us. Indeed, too much LDL can lead to a buildup of deposits called plaques on the inner walls of our arteries, making them hard and narrow. That can lead to things like high blood pressure, and when plaques tear or rupture, blood clots can form and these clots can block blood flow to the heart muscle, leading to a heart attack.

In recent years, a class of drugs called statins has made it easier for doctors to control high cholesterol. Also called cholesterol-lowering drugs, statins block a substance your liver needs for the natural production of cholesterol. This, in turn, depletes cholesterol in your liver, which causes your liver to remove cholesterol that's circulating in your blood. Statins are effective in lowering cholesterol, but there can be side effects, including, in rare cases, serious muscle damage.

Here to talk about cholesterol-lowering drugs is Mayo Clinic cardiologist, Dr. Gerald Gau. Dr. Gau is a consultant in the division of cardiology and vascular medicine at Mayo Clinic. He's also a professor of medicine at Mayo Clinic College of Medicine. Dr. Gau has served on the National Cholesterol Education Program Committee, and he's a medical editor with MayoClinic.com. Dr. Gau, thanks for being with us today.

Dr. Gau: Thank you for asking me.

Rich Dietman: Before we get started talking about statins, give us a brief definition of what cholesterol or cholesterols are.

Dr. Gau: Cholesterol is a very important component of our body. We're made of cholesterol. All of our cells are cholesterol based. The membranes that surround every cell of our body are made from cholesterol. You need them. We have to have cholesterol. We take it in by what we eat. We also produce it in our body. And if everything is in good balance, we produce enough cholesterol that's needed — our cells all function normally. Our endocrine system, which is dependent on this, also functions normally, and we don't have disease. It's management of this that becomes a problem — because of lifestyles, by what we eat and what happens to this cholesterol, because too much of it can cause disease. And when it builds up in the tissues, that's what leads to heart disease, vascular disease and the problems that we're talking about, which is what led up to the evolution of drugs to help lower cholesterol. In actual fact, if we would all eat better, watch what we eat, eat less calories, keep our weight ideal and exercise, we probably wouldn't need all these drugs that we're using here today.

Rich Dietman: But for most of us, that just doesn't work out that way.

Dr. Gau: It doesn't work. In the American population, we run high cholesterols on average. The median cholesterol in our country right now is an LDL cholesterol of about 130. We do know that a cholesterol that's down below 60 is ideal. We're a long ways away from that. And since we eat this way, and we're heavier in this country, a lot of people want the quick fix. And the quick fix is we can lower your cholesterol with these drugs effectively. It's just that, until we change our lifestyle here, we're not really going to turn things around to a great degree.

Rich Dietman: And statins do something with what goes on in the liver as far as managing cholesterol.

Dr. Gau: Statins work directly in the liver. There is a system in our liver that produces cholesterol. Cholesterol is necessary in our body, and the statin mechanism, it creates bile — it's one of the mechanisms of bile creation — and bile is necessary in our digestion and absorption. So the liver makes cholesterol to make this happen. It can also remove cholesterol from the blood for this purpose. Statins work by attacking in the liver the enzyme system that produces cholesterol in the liver. And that forces the liver cells to pull it from the blood and thereby lowers your cholesterol. And so our cholesterol comes down because we stop the production in the liver.

Rich Dietman: Statins, as you said, very, very effective. If not a wonder drug, then certainly a class of drugs, that's been, it sounds like, has either prolonged lives or saved lives, but there are side effects, as you say. Talk a little bit more about those. What are some of the more prominent side effects in taking statins?

Dr. Gau: The side effect of statins, primarily in the office practice is myalgia.

Rich Dietman: Which is?

Dr. Gau: Which is an aching in our muscles, where the muscles just hurt when you walk. If the myalgia gets more severe, when you squeeze your muscles with your hands, it hurts. A lot of people find they can't climb stairs, they feel they've lost their energy, and they do a little exercise and their muscles keep on hurting after they finish. It's an effect on the muscle that is producing this by the statin. This is probably in the range, by the literature from the trials, of 1 to 5 percent. The clinic in my office, I would guess, it's closer to 10 percent to 15 percent of patients, maybe more. Other side effects are less common. It can cause nausea, stomach upset, some people get bowel disturbance, either constipation or diarrhea, you can get different drug reactions that occur. These are enhanced with increasing age. If you have a smaller body mass, a small frame, you tend to have more of these side effects as well.

Rich Dietman: What about memory loss? Is that an issue?

Dr. Gau: Memory loss is an interesting one. It's been looked at in several different ways. In case-control studies, when they followed these studies, they found that there appeared to be less progression of dementia, or cognitive loss of function, in people that were on statins vs. not on statins. However, when it was looked at in two big clinical trials — the heart protection study done in England, which is 20,000 patients, and the PROSPER study done in this country, in older patients — they found when they looked at the older patients in these two studies, that there was no difference between cognitive loss or dementia.

Rich Dietman: Well, I was also going to say, as I get older, my muscles naturally seem to be achier and I forget things more and all that sort of thing, so how do you sort that out?

Dr. Gau: It is hard. What I tell patients that come in that tell me that they are finding it difficult when they walk, that their muscles start hurting, and they sit down and it goes away after a while, and they get up and do it again and it's back, I say "Take a holiday from the statin drug." You stop this drug for 10 days, two weeks in time, and these symptoms all go away. You can then reintroduce the drug and produce it again and they know what they're looking for. It isn't that they're getting older, and it's usually a nice surprise for them when they find, "Oh my God, I feel normal again."

Rich Dietman: So what do you do then for them?

Dr. Gau: You can try other agents. Some statins will do it where another statin might not, although there generally is a lot of crossover. If one does it, the next one will do it too.

Rich Dietman: How about alcohol use? Can I have a beer or two and not worry about its effect if I'm taking statins?

Dr. Gau: The answer is generally yes. Alcohol is related to liver disease. If you consume a lot of alcohol — generous amounts of alcohol — on a daily basis, your underlying liver disease changes, your liver function changes. And when you get an abnormal liver and then you give it an agent that is denatured in the liver, like statins, because that's how it is eliminated from the body, and you have already abnormal liver function going on, all of a sudden your liver says "No, we can't do this." You can also get myalgia because your statin dose is going to be higher because it's not being denatured in the liver. But more likely your liver is going to cause problems for you, and we get acute onset of liver problems. Generally, what we say if somebody's drinking alcohol in a little bit more than moderation, or they have a history of prior liver disease, we start statins with great caution. We do it slowly, we follow their liver function. Statins themselves, just using them in somebody who's not a drinker, really don't seem to cause any liver problems, although we check a liver enzyme, we rarely, if ever, seen any changes.

Rich Dietman: If I'm taking statins, you talked about liver enzyme tests, would I expect to have a routine set of blood tests?

Dr. Gau: It is recommended that before you start, we do get a baseline liver test. An AST is usually the one that is used, and this test is a simple liver test and a blood test that tells you whether your liver's having a problem or not. After you start a statin, we usually check that again at the first blood draw, six weeks to three months out. And if that remains normal, there's really not an indication you have to keep on measuring this. If I go up on the dose, I will recheck it again just to make sure that the new dose is not doing this.

Rich Dietman: If you're treating me with statins, and I know you've told me that there could be side effects, what are the side effects that you'd want me to get in touch with you right away on and others that could wait?

Dr. Gau: Every patient that we see, we tell them about the myalgia. I tell them that if they notice in doing routine, everyday activities, if their muscles start aching or they're aware that they're losing function in terms of being unable to climb stairs or be physically active or with their exercise, because I want everybody I'm treating here to be exercising. If they're aware that their muscles hurt longer after they exercise, then they should call me and let me know. I tell them, actually, to stop the statin and then call me. When you stop the statin, it takes about a week to 10 days for these symptoms to dissipate and usually the patient by that time will tell me, "I couldn't believe how much better I feel." And then we talk about what else we can do here, whether we're going to try another statin. If they're at a high dose, sometimes they'll tolerate a lower dose in combination with another agent, and there are several other agents that can be used.

Rich Dietman: Can I get rid of my side effects, if I have them, by taking coenzyme Q10?

Dr. Gau: That is a very popular belief. Remember I said in the liver where it attacks this enzyme, HMG-CoA reductase, the enzyme that leads to production of cholesterol, with our desired effect at lowering cholesterol. One of the other things that is dropped is coenzyme Q10, called ubiquinol. So they have a name for it, it's down there with the cholesterol, on another pathway that is also blocked by statins. When you start a statin, your coenzyme Q10 level in your blood drops by 50 percent. We've tried, in terms of replacing coenzyme Q10, limited studies are done on this, not a lot, no big trials, but we find that even though we give it back, this ratio sometimes does not change. It doesn't seem to have any effect on the myalgia. It is being recommended across the country over-the-counter, because coenzyme Q10 is not a prescription drug. Because of that, people take it over-the-counter and they use it, and it's being heavily marketed that if you're on a statin you should be on this, but there's no good trials, and there's no evidence that coenzyme Q10 changes the myalgia effect. So, in answer to your question, should you take it, I don't have any problem with a patient taking it, but they need to understand that coenzyme Q10 is not regulated by anybody.

Rich Dietman: Anything else that you can think of that we didn't cover that's important that we should talk about?

Dr. Gau: Well, one of the things that I get asked by my patients all the time is this thing about grapefruit juice. Statins are denatured in the liver by a system called the cytochrome P450 system. It's an enzyme system that breaks the statin down and eliminates it. In our liver, that same enzyme system is used for denaturing a whole lot of other things, and one of them is grapefruit. And so when you have a pathway that you take a lot of grapefruit juice and that pathway's busy breaking it down, you take a statin, the statin doesn't get broken down, your dose stays high in the blood. You get a bigger effect for the dose you're taking, maybe even twice, and therefore you can have more likely problems with myalgia and other symptoms because the dose is up. In the study that was done, you had to take a whole quart of grapefruit juice to get this effect.

Rich Dietman: A day?

Dr. Gau: Yeah, at once. And the statin was taken at the same time that you took the grapefruit. If you have a half a grapefruit in the morning and take your statin at night, it's not going to cause any problem for you; our liver's able to handle that without any trouble. I tell people that, yes this was done, it's in the literature, it's actually in the drug information when you read it, says avoid grapefruit juice, and then studies showed 1 quart of grapefruit juice. I have never met anybody that drinks a quart of grapefruit juice. But I tell people if they want to use grapefruit, they should know that they shouldn't take it at the same time as their statin because it will increase the dose effect. So I tell people, don't get concerned about the grapefruit, just don't drink a quart of it. And don't take it when you take your statin. Take your grapefruit in the morning and statin at night. If you do that, it's not a problem. But that's a common question asked by patients.

Rich Dietman: Well, thanks very much, Dr. Gau.

We've been talking with Dr. Gerald Gau, cardiologist and an expert in cholesterol management at Mayo Clinic. Dr. Gau is also medical editor at Mayo Clinic.com. I'm your host, Rich Dietman.