Cholesterol Medications: What You Should Know about Side Effects, Dosage and More

A diabetes pharmacist tells you what you need to know about statin medications—their risks and benefits. Cholesterol and triglycerides also covered.

two butterflies on orange flowerwhen considering cholesterol medication to help prevent heart disease, it all comes down to benefits vs. risk. (Photo: Unsplash, Oshua Torres)

The correlation between diabetes and high cholesterol is well established. It is a known fact that diabetes affects heart health and a healthy heart is directly related to cholesterol; particularly HDL and LDL.1 The statins are the leaders of the pack for the effective lowering of cholesterol, and remain one the most prescribed medications in the pharmacy today.

They are capable of reducing cholesterol by as much as 50% and can potentially reduce deaths from coronary heart disease.2 With the introductions of generic versions of the statins, they are not only effective, but also affordable as cholesterol lowering agents.

Types of Statins

The statins currently available are atorvastatin (brand name Lipitor) probably the most popular statin), rosuvastatin (brand name Crestor), pravastatin, fluvastatin, lovastatin, simvastatin, and pitavistatin. Statins work by interfering with the ability of the liver to make cholesterol.

Side Effects of Statins

One of the main side effects from statins is muscle pain that is experienced by a small percent of the population taking statins. It is hard to interpret muscle pain in studies because the causes can come from a variety of other factors; such as exertion from exercise, etc.

People who start statins should report symptoms of unusual muscle aches, cramps, fever, or dark urine to their health care team as this could signal a rare but potentially dangerous condition that breaks down muscle tissue. This is why periodic blood work is done on patients taking statins to monitor potential side effects. 

If you experience side effects from one statin, you may be able to tolerate one of the others-some are more apt to potentially cause muscle pain than others. (Simvastatin is most likely and fluvastatin and pitavistatin are least likely according to some studies).

This does not mean that you should discontinue taking medications; with statins as you will see below the risk of problems is relatively low. In addition, some statins are prescribed for their ability to lower cholesterol (potency), which can substantially decrease your risk of a cardiac event.3

To reduce the chance of side effects with statins, avoid taking these medications with grapefruit juice as grapefruit juice can interfere with the breakdown of many of the statins, increasing their potency. Low vitamin D levels have also been found to increase the side effect profile of statins, so making sure your Vitamin D level is within a good (Normal) range and taking supplements if needed is also important.4

Lastly, statins have the ability to decrease a vitamin, co-enzyme Q10, in the body. Supplementation while taking a statin is often recommended to offset this potential deficiency.

Dosage of Statins

Statins are dosed once daily, preferably taken at bedtime. Many statins are best taken at bedtime because this is when the liver produces the most cholesterol; an example of a statin to be taken at bedtime is simvastatin. Lovastatin is best taken after a meal (dinner). Check with your pharmacist for the best advice on how/when to take your medications.

What the American Heart Association Says

To clear up some of the controversy related to statin use about published reports concerning diabetes risk and side effects the American Heart Association (AHA) has released the following statement, which may clear up misconceptions:

“For the overwhelming majority of patients, statins are very safe and should be recommended to at-risk patients most likely to benefit, especially those with established cardiovascular disease [and] diabetes, and select primary prevention patients with multiple major risk factors,” said Dave Dixon, PharmD, CLS, FNLA, FACC, associate professor and vice-chair for clinical services at Virginia Commonwealth University School of Pharmacy in Richmond.

The statement, which is more than 70 pages and was published in Arteriosclerosis, Thrombosis, and Vascular Biology in December 2018, draws on 30-plus years of clinical investigation showing that statins exhibit few serious adverse effects. For instance, researchers concluded that:

  • Myopathy, including rhabdomyolysis attributable to statin therapy, occurs in fewer than 0.1% of treated patients.
  • Non-serious muscle symptoms are commonly reported during statin treatment and interfere with treatment compliance, but overall, fewer than 1% of statin-treated patients have muscle symptoms of pharmacological origin.
  • Severe liver toxicity is very rare, reported in approximately 0.001% of patients.
  • Statins modestly increase the risk of newly diagnosed diabetes in clinical trials of up to 5 years’ duration.

Other Meds Used to Treat High Cholesterol

Other medications for cholesterol include ezetimbe, otherwise know as Zetia®. This drug inhibits the intestinal absorption of cholesterol, and is often given along with certain statins or a vibrate if necessary as a “booster” to help keep lower lipids when a statin alone may not be enough. It is given once a day and can be taken without regard to meals.

Triglycerides: The Other “Bad Fats”

Statins are used primarily for decreasing LDL cholesterol and have a small effect on triglycerides. If triglycerides are high, you may be put on medications specific to lowering these pesky fats. Up to 80% of patients with type 2 diabetes have high triglycerides, which can cause cardiac issues if not addressed by diet/medication.5

Common medications used for high triglyceride levels are a class of drugs known as fibrates, (which includes gemfibrozil, fenofibrate, and clofibrate) and fish oil supplements.

Some fish oil supplements are prescription strength which have higher levels of omega-3s and are more regulated than over the counter supplements. The prescription fish oils are Lovaza and Vascepa. Lovaza is now available in a generic formulation, which may help with cost. Fibrates have the additional benefit of raising HDL, which is a cardioprotective lipid.

Some potential side effects of fibrates are nausea, diarrhea, and occasionally gallstones. Certain fibrates can increase blood levels of certain statins when taken together, potentially increasing the risk of sustain side effects. Simvastatin and lovastatin seem to have the highest risk for this interaction. Both the vibrates and Omega 3s can interfere /interact with blood thinners-caution is advised in patients taking warfarin, for example.

There are now some recently introduced injectable agents for the treatment of high cholesterol.--Praluent((R) (alirocumab) and Repatha(R) (evolocumab). These drugs are utilized along with diet and statin therapy in patients with a genetic predisposition to high cholesterol or who have atherosclerotic heart disease and have been treated on maximum does of statins without the desired lipid lowering effect.  

Most of the time these are injected every two weeks subcutaneously. Adverse reactions can include hypersensitivity reaction, allergy, injection side reactions, neck pain, and respiratory tract infection-among some of the most common possibilities. 

As new drug entities, these are expensive and some insurance companies may not cover them without a note from the doctor stating why they are needed. The companies that make these drugs do offer robust patient assistance programs as well.

Keep in mind that a heart healthy diet and plenty of exercise are all part of keeping blood lipids low and making sure you stay well.  Drugs are not a substitute for healthy living!

Here are some guidelines for numbers that may help you:6

Your LDL cholesterol number is:

  • Optimal if it is less than 100.
  • Near optimal/above optimal if it is 100-129.
  • Borderline high if it is 130-159.
  • High if it is 160-189.
  • Very high if it is 190 or above.

Your triglyceride numbers are:

  • Normal if they are less than 150.
  • Borderline high if they are 150-199.
  • High if they are 200-499.
  • Very high if they are 500 or higher.
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