CHOLESTEROL LOWERING THERAPIES
Diet and exercise not enough to lower cholesterol? Now what?
You have many options when it comes to lowering your cholesterol. Compare statins and other cholesterol lowering drugs below.
CHOLESTERAL OVERVIEW
What is cholesterol?
Cholesterol is an important building block that our body uses to build cells, and to make hormones, vitamin D, and bile salts which our bodies require everyday. Cholesterol is found in our blood and comes from 2 primary sources.
- Produced by our livers
Cholesterol synthesis occurs by enzymes in our liver and accounts for around 80% of our total cholesterol in our blood. - From our Diet
Cholesterol is absorbed by the intestines, from the food you eat.
There are two main types of cholesterol;
- Good cholesterol: high-density lipoprotein, or HDL-C—helps to get rid of LDL by picking it up and taking it to your liver so your body can remove it from your body
- Bad cholesterol: low-density lipoprotein, or LDL-C—too much of this can be a problem as it can build up in your arteries.
If untreated high cholesterol can lead to the accumulation of plaque in our arteries increasing ones risk of having a heart attack or stroke.
Statins are the first line of defense to lower your cholesterol
When diet and exercise are not enough, statins are the first line of defense when it comes to lowering cholesterol. Statins work by blocking an enzyme in our livers which produce cholesterol reducing our bodies overall cholesterol levels.
40–75% Will Stop Taking Their Statin In The First Year
Muscle pain is one of the more common side-effects from statin therapy. 62% of former statin users indicated that side-effects was the reason they stopped taking their medication.
Newer statins, like pitavastatin, are now available in the U.S and may be good options for those who have stopped taking their statin. In clinical studies, rate of muscle pain are only 3.1% with pitavastatin.
Don't Give Up On Your Statin. Not all Statins are the Same
There are 7 different statins. While they all lower cholesterol, there are some key differences to consider.
The current statins available in the U.S. include atorvastatin (Lipitor), fluvastatin (Lescol XL), lovastatin (Altoprev), pravastatin (Pravachol), rosuvastatin (Crestor), simvastatin (Zocor), and most recently approved pitavastatin (Zypitamag, Livalo).
Key Factors to Consider When Choosing a Statin
Are you taking other medications?
Most statins are metabolized by an enzyme called cytochrome P450 (CYP450). Unfortunately, 70-80% of medications are also processed by the same family of enzymes. When these enzyme pathways become too busy it can lead to drug interactions.
There are only two statins which have very limited interactions with this pathway, pitavastatin, and pravastatin. Because of this key difference, they both have a reduced potential for interactions many commonly prescribed medications.
Are you diabetic, or prediabetic?
Increases in blood sugar levels have been seen with statin medications. While all statins do have a warning and precaution that they can raise HbA1c and fasting serum glucose levels, there is data to suggest that this may not be the same across all statins.
For example, a clinical study compared pitavastatin (4 mg) with atorvastatin (20 mg) in those living with Type 2 Diabetes. They found that while cholesterol lowering effects of the medications were similar, only the atorvastatin group saw a significant increase in blood glucose levels.
If you have Type 2 Diabetes, or are worried about your glucose levels, ask your healthcare provider about pitavastatin.
Are you currently experience statin side effects?
While statins are generally well-tolerated, they are not without their risk of side effects. The most common side effect is muscle pain, and this goes up with dose of statin.
If you are currently having issues with your statin be sure to talk to your healthcare provider.
Newer statins like pitavastatin have rate of muscle pain of 3.1% and may be a good statin option for you.
Do you drink grapefruit juice?
Some statins interact with grapefruit juice and this can lead to statin side effects.
In fact, grapefruit juice is well-known to have an effect on several medications. Grapefruit juice interacts with the same enzyme our bodies use to break down atorvastatin (Lipitor), simvastatin (Zocor), and lovastatin (Altoprev).
If you enjoy grapefruit juice, you should consider statins like rosuvastatin (Crestor), pravastatin (Pravachol) and pitavastatin (Zypitamag).
Are you of Asian descent?
Certain statins, like rosuvastatin (Crestor) have dose restrictions for people of Asian descent.
Newer statins, like pitavastatin (Zypitamag), do not have this same dose limitation.
Are you taking any antiretroviral therapy?
Most statins including atorvastatin (Lipitor), rosuvastatin (Crestor), simvastatin (Zocor), fluvastatin (Lescol XL), and lovastatin (Altoprev) can interact with certain antiretroviral medications.
Statins like pravastatin (Pravachol) and pitavastatin (Zypitamag) do not appear to have this same limitation.
If you're taking antiretroviral therapy be sure to tell your healthcare provider.
Have you reached your cholesterol lowering goals?
If you haven't reached your cholesterol lowering goals you may need to make some additional changes. You have many options. You can increase the dose of your statin which should add an additional ~6% decrease in your bad cholesterol. You can also add on additional therapies such as ezetimibe to your statin regimen.
Another important thing to consider is your lifestyle. If you're not at your target yet, you may want to consider making additional changes to the foods you eat and the amount of exercise you are doing.
Most importantly, talk with your healthcare provider to come up with a plan to achieve your cholesterol goals.
What happens when statin therapy alone isn't enough?

If you are unable to achieve the desired level of LDL-C reduction with a statin, your healthcare provider may increase the dose of your statin, or suggest additional therapies, also known as combination therapy.
The most common add-on combination therapy is ezetimibe (generic Zetia®). Until recently when ezetimibe's patent life ended it was extremely expensive. But now, with increased competition of generic manufacturers we have been able to add ezetimibe to Marley Drug's Wholesale List.