Chronically high levels of cholesterol in your bloodstream can have devastating long-term consequences. As it builds up in the walls of your arteries, your chances of heart attack, stroke, and other serious ailments increases. Fortunately, we live in a time when we have several effective medications for lowering cholesterol.

The importance of lifestyle

Although medications can play a crucial role in getting your cholesterol down to a safer level, they should not be looked at as a magic bullet, a shortcut, or a substitute for a healthy diet and exercise routine. That’s not an anti-medication statement, and in fact represents the prevailing view of the manufacturers of cholesterol medications, who know their products work best when coupled with lifestyle changes. There are a few reasons for this.

First of all, a cholesterol drug is considered highly successful if it can consistently help patients lower their cholesterol by 50%. But lifestyle changes alone can result in a 15-20% reduction in LDL (“bad”) cholesterol and a 13% boost in HDL (“good”) cholesterol.  Cholesterol medication side effects are always a possibility (There are risks with every drug), so rushing to take a medication before trying to bring down cholesterol naturally is both inviting unnecessary risk and denying yourself a perfectly safe and effective method of treatment. Your doctor can guide you on how to lower cholesterol without medication.

Second, cholesterol is just one aspect of your health, albeit an important one. And while statin medications for cholesterol may help in some non-cholesterol-related areas of health (see below), the lifestyle modifications necessary to lower cholesterol—diet and exercise—are overwhelmingly good for every system in your body. Why not view diet and exercise as super-drugs, packed with all benefit and no risk, improving your overall health and not just your cholesterol?

And finally, to restate the case, cholesterol medications work best when accompanied by lifestyle changes. Unless you’re that rare person who is so at-risk that exercise is unsafe for you, when your doctor prescribes a cholesterol medication, he or she will almost certainly encourage you to start eating better and exercising so that you get the full benefit of the drug. There’s no reason not to start doing those things today.

Statins

By far the most commonly prescribed cholesterol medications, the class of drugs known as statins is considered one of the great success stories of modern medicine. The different statins vary in terms of their potency, and they may be given in different dosages to affect their intensity. The least potent of these oral therapies can lower LDL (“bad”) cholesterol by less than 30% on average, while the most potent can achieve reductions of 50% or more.

Even if you’re not taking a statin, you’ve probably heard of a few of them. Here’s a partial list:

  • Atorvastatin (Lipitor) 40-80 mg. High-intensity.
  • Rosuvastatin (Crestor) 20-40 mg. High-intensity.
  • Fluvastatin (Lescol) 80 mg. Medium-intensity
  • Lovastatin (Altoprev) 40-80 mg. Medium-intensity.
  • Simvastatin 10 mg. Low-intensity.
  • Pravastatin 10-20 mg. Low-intensity.

The technical name for these medications is “3-hydroxy-3 methylglutaryl coenzyme A reductase inhibitors,” which is enough of a mouthful to elicit gratitude toward whomever decided on the much simpler “statins.” The drugs get their hyper-syllabic name from the fact that they work by acting against an enzyme called 3-hydroxy-3 methylglutaryl coenzyme A (HMG-CoA). HMG-CoA’s role is to stimulate the liver to produce cholesterol. Blocking HMG-CoA causes LDL levels to fall while it increases levels of HDL (“good”) cholesterol.

Statins are generally well tolerated, but as with every drug, they carry some risk. A few people experience side effects such as muscle soreness and cramps, brain fog and forgetfulness, elevated blood sugar, and liver problems. Fortunately, other medications are available if the side effects make statins too unpleasant or dangerous.

Statins may carry extra benefits

Because statins are so widely prescribed and have been in use for decades now, researchers have been able to observe associations between them and certain non-cholesterol-lowering outcomes.

Injectable non-statins

Not only does the liver produce cholesterol, but it also traps and disposes of excess LDL moving through the bloodstream. Certain receptors on the liver allow it to do that, but their function can be disrupted by the presence of a protein called PCSK9 (proprotein convertase subtilisin kexin type 9). A relatively new class of drug called PCSK9 inhibitors stops that protein from blocking those liver receptors, thus allowing the liver to clear more harmful LDL out of the bloodstream.

Currently, only two PCSK9 inhibitors are on the market, although others are in development. The two we have to date are alirocumab (Praluent) and evolocumab (Repatha).

PCSK9 inhibitors are more powerful than statins but currently must be taken as injections semimonthly or monthly (Future drugs may be administered orally).  So far, PCSK9 drugs appear very well tolerated, without the occasional muscle pain associated with statin use. They are currently only prescribed to high-risk patients.

Another new drug affects PCSK9 in a different way. Rather than keeping the protein from blocking liver receptors, Inclisiran (Leqvio) stops the liver from producing PCSK9 to begin with. It, too, is injected, but only once every six months after an initial two doses spaced three months apart. It appears highly effective, reducing LDL by more than 50%, and is currently prescribed to high-risk patients including those who are already on the maximum statin dosage they can tolerate.

Other drugs

Numerous additional drugs are sometimes prescribed to supplement statin use or to substitute for it in patients who can’t tolerate statins:

  • Fenofibrate (Antara, TriCor) and gemfibrozil (Lopid), which tell the liver to produce less fat.
    • Omega-3 supplements (prescription-strength), which lower triglycerides.
    • Bempedoic Acid (Nexletol), which blocks the enzyme ATP citrate lyase to reduce the amount of cholesterol produced by the liver.
    • Ezetimibe (Zetia), which reduces the amount of cholesterol your small intestine absorbs.
    • Cholestyramine (Prevalite), colestipol (Colestid), and colesevelam (Welchol), which convert circulating cholesterol into bile acids.

Each of these drugs comes with its own set of tradeoffs in terms of side effects and benefits.

Related Articles