PCSK9 Management for Hypercholesterolemia

The main stay of treatment for all patients with high cholesterol or at high risk of heart disease is lifestyle modification, including weight loss in overweight patients, aerobic exercise, and eating a prudent diet. Ways to lower cholesterol with diet include lowering intake of saturated fat and cholesterol. Some foods that can be avoided include red meat, butter, fried foods, and cheese. Eating foods high in soluble fiber such as fruits, oats, barley, beans, and peas can also be helpful. Overall, no single diet is right for everyone, but in general a healthy diet should often include lots of fruits, vegetables, and whole grains while limiting sugar, sweets, and refined grains.

Many patients may not be able to reduce cardiovascular risk enough with lifestyle modifications alone and may require additional treatment with medication. It is important to note that any medication taken will be most effective when combined with lifestyle changes. Medication classes available to help lower cholesterol and reduce risk of cardiovascular disease are listed below. It is important to understand that treating high cholesterol is a lifelong process and will require committed adherence to therapy and lifestyle modifications. Stopping treatment usually allows lipid levels and risk to rise again.

Statins
First-line treatment for the vast majority of patients at risk for cardiovascular disease who are unable to be controlled with lifestyle changes alone, should be statin therapy. Statins are among the most powerful drugs for lowering LDL and have been shown to be effective in preventing heart attacks, strokes, or death. This class of medications works by blocking a substance your body needs to make cholesterol. Statins may also help your body reabsorb cholesterol that has built up in plaques on your artery walls, preventing further blockage in your blood vessels. Statin therapy should be maximally optimized in most patients before adding on other medications. Although usually safe and effective common side effects may include: muscle and joint aches (most common) and headache and nausea. Other, more serious risks include liver damage, increased blood glucose levels, higher risk for type 2 diabetes, cognitive (mental) problems. Severe muscle pain, especially if accompanied by dark-colored urine should be brought to the attention of a health care professional immediately.

  • Available statins include atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin.

Cholesterol absorption inhibitors
This class of medications lower the amount of “bad” cholesterol (LDL) your body absorbs. Common Side effects include: stomach ache, diarrhea, tiredness, and headache.

  • Available cholesterol absorption inhibitors include ezetimibe.

Bile-acid sequestrants
This class of medications are chemical substances that bind to cholesterol in the intestines and are then eliminated in the stool. Bile acid resins are sometimes prescribed in combination with a statin for patients with heart disease to increase cholesterol reduction. Other medications should be taken at least 1 hour before or 4 to 6 hours after the resin as bile-acid resins may interfere with absorption of other medications. Talk to your doctor about the best time to take this medicine, especially if you take other medications. Common side effects are gastrointestinal; constipation, diarrhea, bloating, vomiting.

  • Available bile-acid sequestrants include cholestyramine, colestipol, and colesevelam.

Niacin’s
This class of medications are prescribed as a treatment to increase your HDL cholesterol or correct a vitamin deficiency. High-dose niacin can cause stomach upset and make your skin flush or itch. More importantly, niacin can increase your risk of: bleeding, diabetes, infection, liver damage and or stroke. Taking niacin with food and taking aspirin 30 minutes before can decrease side effects.
Niacin is available in multiple immediate and extended-release formulations.
Fibric acid derivatives – This class of medications lowers blood triglyceride levels by reducing the livers production of a triglyceride that circulates in the blood. This speeds up the removal of triglycerides from the blood. Fibrinates are often prescribed in combination with a statin medication. The common side effects of fibrates include nausea, stomach upset, and sometimes diarrhea.

  • Available fibric acid derivatives include gemfibrozil and fenofibrate

PCSK9 inhibitors (Proprotein convertase subtilisin/kexin type 9)
This class of biological medications that are self-injected every two or four weeks targets and inactivates a specific protein (PCSK9) in the liver. By knocking out the protein, this dramatically reduces “bad” LDL cholesterol in the blood stream. They are specifically indicated for patients with more severe disease such as heterozygous or homozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease who have been unable to reach therapy goals with maximally tolerated statin therapy. Unless your provider has diagnosed you as statin intolerant, it is recommended that you should continue to take a maximally tolerated statin in combination with a PCSK9 inhibitor as prescribed by your physician. Continued adherence to statin therapy is critical as they have demonstrated the most ability of any medication to lower your chances heart attacks or strokes down the road. Common expected side effects of PCSK9 inhibitor therapy include injection-site swelling, itching or rash, limb pain, fatigue, muscle pain and eye-related events. Some patients also reported memory problems, runny nose and sneezing, upper respiratory tract infection, flu symptoms and back pain.

  • Available PCSK9 inhibitors include alirocumab and evolocumab.

Overcoming Medication Challenges

It is important for you to know the benefits of your medications. Here at Magellan Rx, we understand your concerns and want to help you with any difficulties you may encounter. For additional information on how to overcome medication challenges, please click here: Overcoming Medication Challenges