Bile acid sequestrants: Uses, common brands, and safety info

Cholesterol is a substance our bodies need to remain balanced and healthy, but only in the right amounts. Cholesterol is transported in our blood by two lipoproteins, low-density lipoprotein (LDL) and high-density lipoprotein (HDL). LDL is also known as “bad” cholesterol because it leads to a buildup of fatty deposits known as plaques. The presence of these plaques can lead to heart attack, stroke, or other health problems. HDL is known as “good” cholesterol. This is because it carries cholesterol back to the liver which then removes the cholesterol from your body. Healthy people with higher levels of HDL have a lower risk of heart disease. Risk factors for high cholesterol (hypercholesterolemia) include people 40 years and older, family history of high cholesterol, and race—with non-Hispanic white Americans having the highest likelihood of having high cholesterol.

There are many drug types aimed at reducing cholesterol levels. Dietary changes and exercise are also recommended in a plan to lower cholesterol levels. Examples of lipid-lowering drugs include HMG-CoA-reductase inhibitors (otherwise known as statins) and PCSK9 inhibitors.  Bile acid sequestrants are a class of dyslipidemia medications that reduce LDL cholesterol levels specifically, and we will discuss their various properties, common brand names, and safety. 

What are bile acid sequestrants?

Bile acid sequestrants are a type of cholesterol-lowering medication aimed specifically at lowering LDL cholesterol. They do have a slight effect on raising the good HDL cholesterol levels, but that is not the primary effect of bile acid sequestrants. While statins remain the most common class of drugs used to treat high blood cholesterol, sometimes statins may not be enough to lower the LDL. In some cases, patients are intolerant of the side effects of statins. Statins like Lipitor (atorvastatin) and Crestor (rosuvastatin) may cause peripheral nerve pain and lead to many drug interactions with other medications and supplements.  These patients need another option to treat high cholesterol and lower their cardiovascular disease risk, and bile acid sequestrants are a good option for lowering LDL.

How do bile acid sequestrants work?

Bile acid sequestrants are actually not absorbed into the bloodstream. When administered orally, their mechanism of action involves binding to bile acids in the small intestine. Cholesterol is contained within the bile acid. This binding forms a complex which is insoluble and prevents reabsorption of the LDL,  which is then excreted in the stool. As more bile acid is removed from the intestinal system, hepatic bile acid synthesis is stimulated, LDL receptor activity increases, and more LDL is removed by excretion. 

What are bile acid sequestrants used for?

• High choleserol

• Diarrhea

• Adjunct to diet and exercise in patients with with Type 2 Diabetes Mellitus (Welchol)

Who can take bile acid sequestrants?

Can men take bile acid sequestrants?

Healthy adult males can safely take bile acid sequestrants with two exceptions: Men with a gastrointestinal obstruction should not take it; neither should men with triglyceride levels above 500 mg/dl as bile sequestrant therapy and drugs can increase triglycerides even more over time. 

Can women take bile acid sequestrants?

Women with no other factors such as GI obstruction or high triglycerides can take bile acid sequestrants.

Can you take bile acid sequestrants while pregnant or breastfeeding?

Fetal exposure is not expected with bile acid sequestrants because they are not absorbed, however, there is not an adequate amount of well-controlled studies to define their safety in pregnancy. The primary concern in pregnancy is that bile acid sequestrants may interfere with the absorption of fat-soluble vitamins like vitamins A, D, E, and K. A vitamin K deficiency can be very serious and lead to clotting disorders which can be fatal during pregnancy. The lack of absorption also means it is not likely that bile acid sequestrants are excreted in breast milk. Bile acid sequestrants are considered a safe choice for a breastfeeding mother with high LDL levels.

Can children take bile acid sequestrants?

Children can take bile acid sequestrants for a limited number of indications. Welchol and Colestid are made in solid oral formulations which are large in size and hard to swallow. Welchol, Questran, Questran Light, and Prevalite are available in powder form to form oral suspensions that are easier for young people to swallow.

Can seniors take bile acid sequestrants?

Older adults can take bile acid sequestrants, however, caution should be used as bile acid sequestrants can cause extreme constipation. Elderly patients are predisposed to constipation and it can become difficult to treat if compounded by bile acid sequestrant use.

Are bile acid sequestrants safe?

Recalls

No active recalls at this time.

Restrictions

Bile acid sequestrants are contraindicated in someone with a GI obstruction and should never be used because they can cause constipation and worsen the blockage. They should be used with caution in patients with cholelithiasis (the formation of gallstones), liver disease, or complete biliary obstruction (blockage of hepatic bile ducts).  

Bile acid sequestrants can decrease the absorption of fat-soluble vitamins A, D, E, and K because they are removing fatty substances from the intestinal tract without absorption. Vitamin K deficiencies can be especially dangerous as lower vitamin K levels leave you at an increased risk for hemorrhaging. 

Bile acid sequestrants raise triglyceride levels. Triglycerides are the main component of natural lipids (fats) and higher levels carry an increased risk of stroke. Patients should have their triglyceride levels checked by their healthcare provider prior to initiating bile acid sequestrant therapy. Bile acid sequestrants should not be used in patients with a triglyceride level greater than 500 mg/dL.

Are bile acid sequestrants controlled substances?

No, bile acid sequestrants are not controlled substances.

Common bile acid sequestrants side effects

Serious adverse reactions:

• Hypersensitivity

• Esophageal obstruction

• Intestinal obstruction

• Fecal impaction

• Dysphagia

• Pancreatitis

Common side effects:

• Constipation

• Dyspepsia

• Nausea

• HEadache

• Fatigue

• Asthenia

• Flu-like symptoms

• Hypoglycemia (low blood sugar)

• Hypertension (high blood pressure)

• Vomiting

• Hypertriglyceridemia

• Back pain

How much do bile acid sequestrants cost?

Out-of-pocket costs for a one-month supply of bile acid sequestrants are similar across the generic equivalents. Brand name formulations can be very costly, however. Brand-name Colestid can cost over $300 per month without insurance, and brand name Welchol is over $800. SingleCare provides free drug coupons which can drastically reduce the cost for both brand and generic formulations. One month of generic Colestid can be less than $35 with a SingleCare coupon, and generic Welchol as low as $23 at participating pharmacies.

Your insurance may have formulary restrictions that will determine which bile acid sequestrant is preferred. Before filling your medication, always check with SingleCare to make sure you are paying the best price.