Colestyramine

Overview

Colestyramine (INN) or cholestyramine (USAN) (trade names Questran, Questran Light, Cholybar, Olestyr, Quantalan, Vasosan) is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. It is a strong ion exchange resin, which means it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer. WP

Colestyramine removes bile acids from the body by forming insoluble complexes with bile acids in the intestine, which are then excreted in the feces. As a result of this loss of bile acids, more plasma cholesterol is converted to bile acids in the liver to normalise levels. This conversion of cholesterol into bile acids lowers plasma cholesterol levels.[1] WP

Uses, dosage and effects

Medical uses

Bile acid sequestrants such as colestyramine were first used to treat high levels of cholesterol, but since the introduction of statins, now have only a minor role for this indication. They can also be used to treat the pruritus, or itching, that often occurs during liver failure and other types of cholestasis where the ability to eliminate bile acids is reduced. WP⚠ Wikipedia itself has flagged this text: citation needed.

Colestyramine is commonly used to treat diarrhea resulting from bile acid malabsorption. It was first used for this in Crohn's disease patients who had undergone ileal resection. The terminal portion of the small bowel (ileum) is where bile acids are reabsorbed. When this section is removed, the bile acids pass into the large bowel and cause diarrhea due to stimulation of chloride/fluid secretion by the colonocytes resulting in a secretory diarrhea. Colestyramine prevents this increase in water by making the bile acids insoluble and osmotically inactive.[2][3] WP

Colestyramine is also used in the control of other types of bile acid diarrhea. The primary, idiopathic form of bile acid diarrhea is a common cause of chronic functional diarrhea, often misdiagnosed as diarrhea-predominant irritable bowel syndrome (IBS-D), and most of these patients respond to colestyramine. It is beneficial in the treatment of postcholecystectomy syndrome chronic diarrhea. Colestyramine is also useful in treating post-vagotomy diarrhea.[4–8] WP

Colestyramine can be helpful in the treatment of Clostridioides difficile infections, to absorb toxins A and B, and reduce the diarrhea and the other symptoms these toxins cause. However, because it is not an anti-infective, it is used in concert with vancomycin.[9] WP

It is also used in the "wash out" procedure in patients taking leflunomide or teriflunomide to aid drug elimination in the case of drug discontinuation due to severe side effects caused by leflunomide or teriflunomide.[10] WP

A case report suggests that colestyramine may be useful for cyanobacterial (microcystin) poisoning in dogs.[11] WP

Ointments containing colestyramine compounded with Aquaphor have been used in topical treatment of diaper rash in infants and toddlers.[12] WP

Cholestyramine also binds with oxalate in the GI tract, ultimately reducing urine oxalate and calcium oxalate stone formation.[13] WP

Available forms

Colestyramine is available as powder form, in 4-g packets, or in larger canisters. In the United States, it can be purchased either as a generic medicine, or as Questran or Questran Light (Bristol-Myers Squibb). WP

Dosage

A typical dose is 4 to 8 g once or twice daily, with a maximum dose of 24 g/d. WP

Risks and side effects

Side effects

These side effects have been noted:[14] WP

• Most frequent: constipation[14] WP
• Increased plasma triglycerides[15] WP

Intestinal obstruction has been reported in patients with previous bowel surgery who should use colestyramine cautiously. Cholestyramine-induced hyperchloremic metabolic acidosis has also been reported rarely.[16][17][18] WP

Patients with hypothyroidism, diabetes, nephrotic syndrome, dysproteinemia, obstructive liver disease, kidney disease, or alcoholism should consult their doctor before taking this medication. Other drugs should be taken at least one hour before or four to six hours after colestyramine to reduce possible interference with absorption. Patients with phenylketonuria should consult with a physician before taking Questran Light because that product contains phenylalanine.[14] WP

Interactions

Drug interactions

Interactions with these drugs have been noted:[14] WP

• Digitalis[14] WP
• Estrogens and progestins[14] WP
• Oral diabetes drugs[14] WP
• Penicillin G[14] WP
• Phenobarbital[14] WP
• Spironolactone[14] WP
• Tetracycline[14] WP
• Thiazide-type diuretic pills[14] WP
• Thyroid medication[14] WP
• Warfarin[14] WP
• Leflunomide[14] WP

Most interactions are due to the risk of decreased absorption of these drugs. The duration of treatment is not limited, but the prescribing physician should reassess at regular intervals if continued treatment is still necessary. The principal overdose risk is blockage of intestine or stomach.[17] WP

Colestyramine may interfere in the absorption of fat-soluble vitamins such as vitamins A, D, E, and K. No special considerations regarding alcohol consumption are made.[14] WP

Research

Research

Studies in rodents have shown an association between alterations in the metabolism of bile acids with age-related cognitive decline. Experiments in rodents have shown that the use of cholestyramine alleviates cognitive decline in normalising conjugated primary bile acids and ammonia; findings that indicate a potential therapeutic role for cholestyramine in targeting intestinal bile acid absorption for age-related cognitive impairment. In humans, patients with Alzheimer's or mild cognitive impairment were given cholestyramine if they had a history of exposure to environmental toxins. Along with other specialized treatment, cholestyramine was administered to remove these toxins from the body. This treatment, part of a precision medicine protocol, produced significant improvement in various cognitive test scores and improved MRI volumetrics.[19][20] WP

Chemistry

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. September 2017. PMID 31643750
2. Journal / agency Wilcox C, Turner J, Green J. Systematic review: the management of chronic diarrhoea due to bile acid malabsorption. Alimentary Pharmacology & Therapeutics. May 2014. doi:10.1111/apt.12684 · PMID 24602022
3. Journal / agency Hofmann AF, Poley JR. Cholestyramine treatment of diarrhea associated with ileal resection. The New England Journal of Medicine. August 1969. doi:10.1056/NEJM196908212810801 · PMID 4894463
4. Journal / agency Wedlake L, A'Hern R, Russell D, Thomas K, Walters JR, Andreyev HJ. Systematic review: the prevalence of idiopathic bile acid malabsorption as diagnosed by SeHCAT scanning in patients with diarrhoea-predominant irritable bowel syndrome. Alimentary Pharmacology & Therapeutics. October 2009. doi:10.1111/j.1365-2036.2009.04081.x · PMID 19570102
5. Journal / agency Sciarretta G, Furno A, Mazzoni M, Malaguti P. Post-cholecystectomy diarrhea: evidence of bile acid malabsorption assessed by SeHCAT test. The American Journal of Gastroenterology. December 1992. PMID 1449156
6. Journal / agency Danley T, St Anna L. Clinical inquiry. Postcholecystectomy diarrhea: what relieves it?. The Journal of Family Practice. October 2011. PMID 21977493
7. Journal / agency George JD, Magowan J. Diarrhea after total and selective vagotomy. The American Journal of Digestive Diseases. July 1971. doi:10.1007/BF02239223 · PMID 5563217
8. Journal / agency Gorbashko AI. The pathogenesis, diagnosis and treatment of postvagotomy diarrhea. Vestnik Khirurgii imeni I. I. Grekova. March 1992. PMID 8594740
9. Journal / agency Stroehlein JR. Treatment of Clostridium difficile Infection. Current Treatment Options in Gastroenterology. June 2004. doi:10.1007/s11938-004-0044-y · PMID 15149585
10. Journal / agency Wong SP, Chu CM, Kan CH, Tsui HS, Ng WL. Successful treatment of leflunomide-induced acute pneumonitis with cholestyramine wash-out therapy. Journal of Clinical Rheumatology. December 2009. doi:10.1097/RHU.0b013e3181c3f87e · PMID 19955995
11. Journal / agency Rankin KA, Alroy KA, Kudela RM, Oates SC, Murray MJ, Miller MA. Treatment of cyanobacterial (microcystin) toxicosis using oral cholestyramine: case report of a dog from Montana. Toxins. June 2013. doi:10.3390/toxins5061051 · PMID 23888515 · PMC3717769
12. Journal / agency White CM, Gailey RA, Lippe S. Cholestyramine ointment to treat buttocks rash and anal excoriation in an infant. The Annals of Pharmacotherapy. September 1996. doi:10.1177/106002809603000907 · PMID 8876854
13. Other Kidney Stones – Medications
14. Other Questran
15. Other MedlinePlusEncyclopedia 003493 Triglyceride level
16. Journal / agency Merten DF, Grossman H. Intestinal obstruction associated with cholestyramine therapy. AJR. American Journal of Roentgenology. April 1980. doi:10.2214/ajr.134.4.827 · PMID 6767374
17. Journal / agency Jacobson TA, Armani A, McKenney JM, Guyton JR. Safety considerations with gastrointestinally active lipid-lowering drugs. The American Journal of Cardiology. March 2007. doi:10.1016/j.amjcard.2006.11.022 · PMID 17368279
18. Journal / agency Kamar FB, McQuillan RF. Hyperchloremic Metabolic Acidosis due to Cholestyramine: A Case Report and Literature Review. Case Reports in Nephrology. 2015. doi:10.1155/2015/309791 · PMID 26425378 · PMC4573617
19. Journal / agency Ren Z, Zhao L, Zhao M, Bao T, Chen T, Zhao A, Zheng X, Gu X, Sun T, Guo Y, Tang Y, Xie G, Jia W. Increased intestinal bile acid absorption contributes to age-related cognitive impairment. Cell Reports. Medicine. May 2024. doi:10.1016/j.xcrm.2024.101543 · PMID 38697101 · PMC11148718
20. Journal / agency Toups K, Hathaway A, Gordon D, Chung H, Raji C, Boyd A, Hill BD, Hausman-Cohen S, Attarha M, Chwa WJ, Jarrett M, Bredesen DE. Precision Medicine Approach to Alzheimer's Disease: Successful Pilot Project. Journal of Alzheimer's Disease. July 4, 2022. doi:10.3233/JAD-215707 · PMID 35811518 · PMC9484109

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