Cholesterol drug may also help ease chronic diarrhea
Cholestyramine is an oral drug known as a bile acid sequestrant that can be used to treat diarrhea caused by the malabsorption of bile acid (referred to as bile acid diarrhea). Bile acid malabsorption is one of the more common causes of chronic diarrhea associated with conditions like Crohn's disease and medical treatments like cholecystectomy (gallbladder removal). Hpmc Ph Manufacturer
Cholestyramine is used "off-label" for the treatment of bile acid diarrhea. The drug is officially approved for the treatment of high cholesterol and itching caused by cholestasis (the impaired flow of bile).
This article explains how and when cholestyramine is used to treat chronic diarrhea. It also describes how the drug is taken along with the possible risks and side effects.
TEK IMAGE / SCIENCE PHOTO LIBRARY / Getty Images
Cholestyramine is a bile acid sequestrant approved by the U.S. Food and Drug Administration (FDA) for the treatment of hypercholesterolemia (high cholesterol) and pruritus (itching) caused by cholestasis.
Cholestyramine works by binding to bile acids and removing them from the body in stools.
Bile is a fluid produced in the liver and stored in the gallbladder that aids with digestion. Bile breaks down fats into fatty acids, which are then absorbed in the digestive tract. Bile acids make up around 80% of the organic compounds in bile.
Cholesterol is another major component of bile. In people with hypercholesterolemia, the removal of bile from the body forces the liver to produce more bile by using cholesterol in the blood. This helps lower cholesterol levels.
The same mechanism of action can alleviate cholestasis-related itching. Cholestasis is caused by the impaired flow of bile from the liver to the intestines, leading to a buildup of bile acids in the blood. These acids irritate nerves and cause itching. By lowering bile acid levels, itching is relieved.
Cholestyramine is used off-label (meaning for purposes other than those approved by the FDA) to treat diarrhea caused by bile acid malabsorption (BAM).
Under normal circumstances, bile is reabsorbed and returned to the liver after it has broken down dietary fats. But with BAM, bile doesn't get reabsorbed and instead starts to build up in the intestines, causing watery diarrhea.
By removing excess bile, cholestyramine can help ease bile acid diarrhea. However, the drug is not a quick fix and can take several weeks to work depending on the severity of your symptoms.
Cholestyramine is not the same as Imodium (loperamide). Imodium is an opioid receptor agonist that relieves diarrhea by slowing the muscular contractions of the gastrointestinal tract (referred to as peristalsis ). This, in turn, helps increase the absorption of water in stools.
Cholestyramine may also be used off-label to treat Grave's disease. This is an autoimmune disorder that causes an overproduction of thyroid hormones (thyrotoxicosis ). Cholestyramine also binds with a compound in the thyroid hormones called iodothyronine and, by doing so, helps remove them from the body.
Some healthcare providers may test a stool sample for high bile acids. Others may prescribe cholestyramine without tests if they suspect BAM is the cause. This is because at least 30% of people diagnosed with functional diarrhea (chronic diarrhea with no known cause) have BAM.
BAM can also affect people who have undergone medical treatments like:
Cholestyramine should not be taken if you're allergic to the drug or your bile duct is completely blocked (meaning that no bile is being released into your intestines).
Phenylketonuria (PKU) is a genetic disorder characterized by the inability to break down a protein called phenylalanine. Because people with PKU need to avoid phenylalanine—and cholestyramine contains phenylalanine—the drug should not be used as it can be dangerous.
Cholestyramine is available as a generic drug and typically comes in a powder form that is mixed into beverages. It is also available as a chewable bar.
When used for diarrhea, cholestyramine is typically prescribed at 4 grams (g) per day. If needed, the dose can be increased to 4 g six times per day.
Children's doses are based on body weight but generally do not exceed 8 g per day, split into two or three equal doses.
Cholestyramine is most effective when used as follows:
Your healthcare provider may recommend a daily vitamin supplement while taking cholestyramine as the drug can make it harder to absorb vitamins from food.
If cholestyramine is left on the teeth for a long time, it can cause tooth discoloration, erosion of enamel, and tooth decay.
Drink the liquid quickly and brush your teeth regularly to avoid dental problems.
As with all drugs, cholestyramine can cause side effects. People over age 60 are at highest risk.
Common side effects of cholestyramine include:
Seek medical help if you experience the following uncommon side effects:
Tell your healthcare provider if you're pregnant, breastfeeding, or have a chronic health condition like diabetes, kidney disease, or heart disease. Cholestyramine needs to be used with caution in these groups.
Cholestyramine can affect the absorption of other drugs. Let your healthcare provider know if you take any of the following as the dose may need to be adjusted or a substitute found:
Take other medications or vitamins at least one hour before or four hours after taking cholestyramine as it can interfere with their absorption.
Cholestyramine is a bile acid sequestrant mainly used to treat high cholesterol but it can also be used off-label to treat bile acid diarrhea. The drug is taken by mouth and works by clearing excess bile acid from the body. Many cases of chronic diarrhea are caused by bile acid malabsorption.
Cholestyramine typically comes in powder form and is taken before meals or bedtime. Side effects include constipation, gas, and stomach upset. As cholestyramine can affect the absorption of other drugs, the doses should be separated by one or several hours.
Vijayvargiya P, Camilleri M. Current practice in the diagnosis of bile acid diarrhea. Gastroenterol. 2019;156(5):1233-1238. doi:10.1053/j.gastro.2018.11.069
Lee KJ. Pharmacologic agents for chronic diarrhea. Intest Res. 2015;13(4):306–12. doi:10.5217/ir.2015.13.4.306
National Institutes of Health. Cholestyramine - cholestyramine powder, for suspension.
Marasco G, Cremon C, Barbaro MR, et al.Pathophysiology and clinical management of bile acid diarrhea.J Clin Med.2022 Jun;11(11):3102.doi:10.3390/jcm11113102
Senderovich H, Khani EG. The role of bile acid sequestrant in diarrhea management: Too good to be true? J Clin Gastroenterol Hepatol. 2018;3:19.
DiBaise JK. Does your patient have bile acid malabsorption? Practical Gastroenterol. May 2020.
National Institute of Diabetes and Digestive and Kidney Diseases. Graves’ disease.
University of Michigan Health. Cholestyramine.
National Library of Medicine. Cholestyramine resin.
By Barbara Bolen, PhD Barbara Bolen, PhD, is a licensed clinical psychologist and health coach. She has written multiple books focused on living with irritable bowel syndrome.
Thank you, {{form.email}}, for signing up.
There was an error. Please try again.
Tylose Chemical Manufacturer By clicking “Accept All Cookies”, you agree to the storing of cookies on your device to enhance site navigation, analyze site usage, and assist in our marketing efforts.