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How Statins Work - Lipitor Pills and Pillbox

How Statins Work to Lower Cholesterol

Lipitor is the brand name for a type of medication that is classified as statins. There are many varieties and brands, but here’s how statins work…

The purpose of statins are to lower cholesterol. As such, they are commonly prescribed for people with high cholesterol who cannot lower it with lifestyle changes. The good news is that statins are clinically proven to be effective in both men and women to lower cholesterol. They are also proven to lower the chances of cardiovascular disease for people who are otherwise prone to high cholesterol.

However, statins must be perpetually used in order to keep working. So if you go off a statin once you become dependent on it, your cholesterol can go back up. Even worse, the chance of cardiovascular disease will return.

Atorvastatin is the first statin, invented back in 1985. It is more commonly known by its brand name, Lipitor. It is the best selling drug of all time, with over $125 billion in sales.

Today, there are many statin formulas and brand names. These variations are easy to spot since their generic names always contain “statin,” such as:

  • Atorvastatin (brand names Lipitor, Ator)
  • Cerivastatin (brand names Lipobay, Baycol)
  • Fluvastatin (brand names Lescol)
  • Lovastatin (brand names Altocor, Mevaor)
  • Mevastatin (brand name Compactin)
  • Pitavastatin (brand names Livalo, Pitava)
  • Pravastatin (brand names Lipostat, Pravochol, Selektine)
  • Rosuvastatin (brand name Crestor)
  • Simvastatin (brand names Lipex, Zocor)

Regardless of the brand, they’re all based on the same principle.

To explain how how statins work, it first helps to understand how the body gets cholesterol in the first place.

Nutrition labels indicate how many milligrams of cholesterol are in food products. This is misleading and makes it seem like high cholesterol in your blood comes from the cholesterol in food.

But in fact, most of the body’s cholesterol is produced internally by the liver.

McDonald's Big Mac Nutrition Label with 85mg Cholesterol

McDonald’s Big Mac nutrition label. One Big Mac has 85 mg of cholesterol.

For example, even though a Big Mac has 85 mg of cholesterol, the Big Mac’s cholesterol is not going to raise your body’s cholesterol as much as your natural liver function. (But don’t get me wrong…Big Macs are not healthy and can lead to high cholesterol, just don’t directly equate their cholesterol value on the nutrition label to high cholesterol in your body).

Now that we know that most of the body’s cholesterol is made by the liver, it becomes a lot easier to know how statins work.

Also – without going into detail on “good cholesterol vs bad cholesterol” – suffice it to say that our bodies need cholesterol to survive. Making cholesterol is part of what the liver is designed to do.

How Cholesterol is Made

Cholesterol production starts when HMG-CoA enzymes enter the liver.

Think of these enzymes as little keys that fit into tiny keyholes in the liver, and only a limited number of these keyholes exist.

When one of the enzymes snaps into a keyhole, it unlocks a reaction that eventually produces cholesterol.

So as more keyholes are filled with enzymes, more locks are unlocked…and more cholesterol is made.

How Statins Work

Continuing with the key analogy, statins enter the liver and mimic the enzymes. So now, both the statins and the enzymes are competing against each other for the same limited number of keyholes.

When an enzyme makes it into a keyhole, cholesterol is produced just as usual.

But when a stain enters the keyhole, it does NOT unlock the reaction to produce cholesterol. Even more, it BLOCKS an enzyme from otherwise turning the same lock.

The statins lower the amount of cholesterol reactions that are initiated, which leads to less overall cholesterol production and – ta da – lower cholesterol levels.

Which is why going OFF statins will allow cholesterol levels to go back up. Without the statins blocking the keyholes, the enzymes that trigger cholesterol production go right back to work.

This article published at the Lancet goes into greater depth on the upside of statins, but it’s important to remember that statins are not a permanent cure for high cholesterol.

So this is good news for those with dangerously high cholesterol levels. If you truly cannot lower your cholesterol though lifestyle changes, and you’ve worked with your doctor to exhaust other alternatives, then statins are a viable option…and the research backs it up.