Fibrates: Uses, common brands, and safety info

Fibrates, sometimes referred to as fibric acid derivatives, are a class of drugs used to treat cholesterol disorders. Dyslipidemia, or elevated cholesterol levels, can have a significant effect on your long-term health. Despite great advancements in the treatment of cholesterol disorders, the number of patients with uncontrolled lipid levels continues to be a concern. 

There are many other classes of drugs indicated to treat cholesterol disorders including statins (such as simvastatin), PCSK9 inhibitors, niacin, and omega-3 fatty acids. For the purposes of this article, we will focus on fibrates and the way they work, their safety, and their adverse event profiles.

Other fibrates:

• Triglide (fenofibrate)

• Lofibra (fenofibrate)

What are fibrates?

Fibrates are drugs used to treat hyperlipidemia. Specifically, fibric acid derivatives work mainly to lower triglycerides but also lower LDL-C while raising the levels of HDL-C. The decision to use fibrates in your treatment plan will be based on your serum cholesterol levels (collected in bloodwork) and also on the presence of other risk factors. The risk factors include family history of cholesterol disorders or premature coronary artery disease, hypertension (high blood pressure), diabetes mellitus, history of smoking, and age.

There are three types of cholesterol. Low density lipoprotein cholesterol (LDL-C) makes up most of the cholesterol in our body. Too much LDL cholesterol will build up on the surface of the blood vessels and cause atherosclerosis. This is a condition where blood vessels are hardened and blocked by a buildup of plaque. This will eventually impede blood flow through the body and increase your risk of a major cardiovascular event such as myocardial infarction or stroke. It is estimated that about one-third of adults in the United States have elevated LDL according to the Centers for Disease Control and Prevention (CDC). High density lipoprotein cholesterol (HDL-C) is actually a good cholesterol because it carries other cholesterol back to the liver to be removed from the body. Higher levels of HDL cholesterol are desirable, and low HDL levels can have a negative impact on your health. Triglycerides are a type of lipid or fat your body uses for energy. If your triglyceride levels are high,  you have an increased risk for heart attack and stroke. Lipoprotein disorders lead to serious health concerns such as atherosclerotic cardiovascular disease (ASCVD) and pancreatitis.

As a bonus, fenofibrate has been shown to decrease insulin resistance and lead to better glycemic control in Type 2 diabetes mellitus patients and patients with metabolic syndrome. This effect of fenofibrate leads to decreased incidence of coronary heart disease and coronary events.

How do fibrates work?

Fibrates work in multiple ways to lower triglycerides. First, they bind to receptors known as PPARs (peroxisome proliferator-activated receptor alpha). This action increases the activity of lipoprotein lipase (LPL), an enzyme responsible for lipid metabolism which ultimately breaks apart and clears triglyceride particles. Their second mechanism of action decreases the synthesis of new triglyceride particles by inhibiting acetyl-coenzyme A carboxylase and fatty acid synthetase. These actions combine to ultimately cause an increase in HDL-C and a decrease in triglycerides and LDL-C. Data suggests fibrates have a modest effect on primary prevention of cardiovascular events.

What are fibrates used for?

• Hypertriglyceridemia (high triglycerides)

• Hypercholesterolemia (high cholesterol)

Who can take fibrates?

Can men and women take fibrates?

Men and women can take fibrates safely as long as there is no history of kidney, liver, or gallbladder disease.

Can you take fibrates while pregnant or breastfeeding?

Fibrates are classified by the Food and Drug administration as pregnancy category C. This means fibrates have shown some harm to the fetus in animal studies, and there are no well-controlled human studies to show safety data. Fibrates should not be used in pregnant women unless there are clear benefits that justify the potential risk to the unborn child. Fibrates are contraindicated in women who are breastfeeding and should never be used.

Can children take fibrates?

Fibrates are not approved for use in children.

Can seniors take fibrates?

Some fibrates are indicated for use in the senior population. Seniors are more likely to have renal or hepatic impairment, necessitating dose adjustments and monitoring by their physician. 

Are fibrates safe?

Recalls

There are currently no FDA recalls for fibrate products.

Restrictions

Do not take fibrates if you have ever had an allergic reaction to a fibric acid derivative. In rare cases, fibrates have been linked to Stevens-Johnson syndrome and toxic epidermal necrolysis.

Fibrates should not be used in patients with a history of gallbladder disease as they increase the biliary excretion of cholesterol and decrease bile acid secretion. This can lead to gallstones, cholelithiasis, and cholecystitis.

Fibric acid derivatives, especially gemfibrozil, are associated with an increased risk of myopathy and rhabdomyolysis, pain-related disorders leading to tingling and discomfort. This risk is increased when combined with a statin therapy. 

The use of fibrates may increase your hepatic enzymes. Liver function tests should be done to establish a baseline prior to initiating therapy and repeated periodically. If the enzymes become too elevated, therapy may have to be discontinued. 

Fibrates may cause mild to moderate cases of anemia. Rarely, more severe cases of blood disorders such as eosinophilia, thrombocytopenia, and agranulocytosis have been reported. Periodic blood work to monitor for these conditions is important.

Fibrates have also been linked to higher rates of dangerous clotting conditions such as deep vein thrombosis and pulmonary embolism as compared to patients taking placebo drugs. Caution should be used in patients with a history of these disorders. 

It is important to note that an older fibrate drug known as Atromid-S (clofibrate) was removed from the market in 2002 due to its adverse event profile.

Are fibrates controlled substances?

No, fibrates are not controlled substances.

Common fibrates side effects

• Abdominal pain

• Arthralgia

• Cholelithiasis

• Constipation

• Diarrhea

• Dizziness

• Dyspepsia

• Elevated hepatic enzymes

• Headache

• Infection

• Myalgia

• Nausea

• Vomiting

• Back pain

• Hypertension

• Insomnia

• Muscle cramps

• Pharyngitis

• Sinusitis

• Fatigue

How much do fibrates cost?

There are many similar, but unique, fibrate drugs on the market. It is important to note that they are not all substitutable for each other. In other words, a fenofibrate product that is generic for TriCor is not the same as a fenofibrate product that is generic for Fenoglide. Your pharmacist can help you determine which products are interchangeable. Most fibrate drugs are now available generically which helps with cost and insurance coverage. Your insurance plan may prefer one product over another, and you should check your formulary when making treatment decisions with your physician. 

Luckily, with or without insurance coverage, SingleCare coupons can help lower the price of prescription medications. For instance, the average retail price for brand name TriCor is over $150 for a one-month supply. With a TriCor coupon from SingleCare, you can pay less than $6 for the generic at participating pharmacies. The retail cost for a one-month supply of Lopid can cost more than $50, but again, a generic Lopid coupon from SingleCare can lower the price to less than $10 a month. Overall, generic fibrate therapy is very cost-effective, especially with a SingleCare discount.