Did you know?
Although research supports its efficacy in binding bacterial toxins, there is limited clinical use and even fewer large-scale studies investigating cholestyramine’s potential use for other infectious diseases.
Cholestyramine
Researched by:
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Karen Pendergrass
ID
Karen Pendergrass
Karen Pendergrass is a microbiome researcher specializing in microbiome-targeted interventions (MBTIs). She systematically analyzes scientific literature to identify microbial patterns, develop hypotheses, and validate interventions. As the founder of the Microbiome Signatures Database, she bridges microbiome research with clinical practice. In 2012, based on her own investigative research, she became the first documented case of FMT for Celiac Disease—four years before the first published case study.
Cholestyramine, a polymer resin, binds bile acids, toxins, and heavy metals, reducing cholesterol and fat absorption, while altering gut microbiome and aiding detoxification.
Research feed -
Karen Pendergrass
Researched by:
-
Karen Pendergrass
ID
Karen Pendergrass
Microbiome Signatures identifies and validates condition-specific microbiome shifts and interventions to accelerate clinical translation. Our multidisciplinary team supports clinicians, researchers, and innovators in turning microbiome science into actionable medicine.
Karen Pendergrass
Overview 
Research Feed Overview
Cholestyramine is a bile acid sequestrant primarily used to lower cholesterol levels and treat certain types of diarrhea. It works by binding to bile acids in the intestine, preventing their reabsorption and promoting their excretion. This alteration in bile acid metabolism significantly affects the gut microbiome, as bile acids possess antimicrobial properties that influence the growth and composition of gut bacteria. Studies have shown that reducing bile acids with agents like cholestyramine can promote the growth of bacteria that are less bile-tolerant, potentially increasing microbial diversity. These microbiome changes can have various metabolic effects, such as influencing the production of short-chain fatty acids (SCFAs), which are crucial for gut health and systemic metabolic regulation. Understanding cholestyramine’s effects on the microbiome could open new therapeutic avenues for managing hypercholesterolemia and various metabolic and inflammatory diseases.
Mechanism of Action
Cholestyramine, a polystyrene-based polymer crosslinked with divinylbenzene and functionalized to quaternary ammonium units, serves as a robust anion exchange resin. Its primary mechanism involves binding bile acids, which not only increases the secretion of the pancreatic exocrine hormone cholecystokinin (CCK) but also impacts several other biological processes. By interrupting the enterohepatic circulation of bile acids, cholestyramine forces the liver to convert more cholesterol into bile acids, thereby lowering serum cholesterol levels. Additionally, it reduces fat absorption by binding to bile acids necessary for emulsifying dietary fats, modulates lipoprotein metabolism by increasing LDL clearance, and facilitates detoxification by binding to toxins and heavy metals in the gastrointestinal tract. [x] Furthermore, cholestyramine alters the gut microbiome by changing bile acid composition, which affects bacterial growth and diversity, and potentially influences immune modulation by impacting gut inflammatory processes. These mechanisms collectively contribute to its therapeutic effects in conditions such as hypercholesterolemia, bile acid malabsorption, and Clostridioides difficile infections.
Microbiome Impact
Cholestyramine, a bile acid sequestrant, is known for its primary use in lowering cholesterol levels and managing certain gastrointestinal conditions. However, its impact on the gut microbiome has garnered interest in recent years. Cholestyramine-induced microbiome alterations impact inflammatory responses in the gut, affecting conditions like inflammatory bowel disease (IBD). Clinical studies have explored cholestyramine’s use in managing Clostridioides difficile infection (CDI) by altering bile acid metabolism and gut microbiota composition.
| Impact on Gut Microbiome | Details |
| Bile Acid Metabolism | Cholestyramine binds bile acids in the intestine, preventing their reabsorption. This process alters the composition of bile acids in the gut, significantly affecting the gut microbiome. Bile acids have antimicrobial properties and can influence the growth and composition of gut bacteria. |
| Microbial Composition | Studies have shown that altering bile acid metabolism through agents like cholestyramine can lead to changes in the gut microbiome. Specifically, the reduction in bile acids may promote the growth of bacteria that are less bile-tolerant, potentially increasing microbial diversity. |
| Metabolic Effects | The changes in the gut microbiome induced by cholestyramine can have downstream metabolic effects. For example, it can influence the production of short-chain fatty acids (SCFAs), which play a crucial role in gut health and systemic metabolic regulation. |
| Inflammatory Responses | Some research suggests that the microbiome alterations caused by cholestyramine can impact inflammatory responses in the gut. By modulating the gut bacteria, cholestyramine might influence the levels of pro-inflammatory and anti-inflammatory compounds, potentially affecting conditions like inflammatory bowel disease (IBD). |
Research Feed
Role of Cholestyramine in Refractory Hyperthyroidism: A Case Report and Literature Review
July 24, 2015
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Autoimmune Diseases
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Autoimmune Diseases
Did you know?
Americans are over three times more likely to suffer from autoimmune diseases compared to the global average, with approximately 16.67% of the U.S. population affected versus 5% worldwide.
Metals
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Metals
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Microbes
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A 52-year-old woman with refractory iodine-induced hyperthyroidism showed significant improvement with cholestyramine, reducing FT4 by 30% in 5 days. Despite conventional treatments failing, cholestyramine proved effective, leading to euthyroidism. This highlights cholestyramine's potential as an adjunct therapy.
What was studied?
The study investigated the role of cholestyramine as an additional treatment for refractory iodine-induced hyperthyroidism in a patient who did not respond to conventional therapies.
Who was studied?
A 52-year-old female patient with a history of goiter who developed iodine-induced hyperthyroidism following a CT scan with contrast. The patient had obstructive symptoms and was unresponsive to standard treatments, including dexamethasone, carbimazole, and propranolol.
What were the most important findings?
After adding cholestyramine, the patient’s FT4 levels decreased by 30% within 5 days and normalized by 12 days.
What are the greatest implications of this study?
Cholestyramine can be an effective adjunct therapy for managing refractory iodine-induced hyperthyroidism, suggesting a potential new treatment avenue for similar cases, such as Grave's Disease (GD). This case highlights the need for alternative treatments when conventional therapies fail and emphasizes the utility of cholestyramine in rapid thyroid hormone reduction.
