The influence of cholestyramine on thyroxine absorption
Abstract
Cholestyramine resin, an anionic exchange resin, currently being investigated as an agent for lowering serum cholesterol levels, has been shown to interfere with the absorption of ingested thyroid hormone. A small quantity of the resin is capable of binding thyroxine under the conditions encountered in the gastrointestinal tract. Interference with thyroid hormone absorption by cholestyramine can be minimized by allowing a time interval of at least four hours between the ingestion of the two agents. Hypothyroid patients receiving cholestyramine should be examined periodically for evidence of hypothyroidism, and adjustments in dose and time interval between the two agents should be made if malabsorption of thyroid hormone is significant.
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The list of medications that can alter the absorption of LT4 is extensive and includes calcium carbonate, PPIs, bile acid sequestrants (cholestyramine and colesevelam), phosphate binders, ferrous sulfate, aluminum-containing antacids, and sucralfate.
“The list of medications that can alter the absorption of LT4 is extensive and includes calcium carbonate (132-134), PPIs (135), bile acid sequestrants (cholestyramine and colesevelam) (136,137), phosphate binders (138,139), ferrous sulfate (140,141), aluminum-containing antacids (142,143), and sucralfate (144,145).”
From Guidelines for the Treatment of Hypothyroidism: Prepared by the American Thyroid Association Task Force on Thyroid Hormone Replacement (2014) · cites this paper as [136]
Co-administration of bile acid sequestrants and LT4 reduces LT4 absorption in healthy volunteers.
“Both of these reports incorporated pharmacokinetic studies in healthy volunteers showing reduced absorption with co-administration of the agent and LT4.”
From Guidelines for the Treatment of Hypothyroidism: Prepared by the American Thyroid Association Task Force on Thyroid Hormone Replacement (2014) · cites this paper as [136]
Bile acid sequestrants bind LT4 within the intestine.
“Two studies have implicated bile acid sequestrants as being responsible for binding LT4 within the intestine (136,137).”
From Guidelines for the Treatment of Hypothyroidism: Prepared by the American Thyroid Association Task Force on Thyroid Hormone Replacement (2014) · cites this paper as [136]
Direct complexation and chelation play important roles in the malabsorption of LT4 induced by the intake of many drugs, including calcium and iron supplements, aluminum-containing antacids, bile acid sequestrants, and some foods (eg, fiber-rich foods, coffee, and milk).
“It is widely acknowledged that direct complexation and chelation play important roles in the malabsorption of LT4 induced by the intake of many drugs, including calcium and iron supplements (72, 73), aluminum-containing antacids (74), bile acid sequestrants (75, 76), and some foods (eg, fiber-rich foods, coffee, and milk) (22, 77, 78).”
From Levothyroxine: conventional and novel drug delivery formulations. (2023) · cites this paper as [75]
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- Authors
- Northcutt, R. C.
- Corresponding author
- Northcutt, Robert C.
- Venue
- JAMA: The Journal of the American Medical Association
- Publisher
- American Medical Association (AMA)
- Published
- 1969-06-09
- Volume
- 208
- Issue
- 10
- Pages
- 1857
- ISSN
- 0002-9955 (ISSN-L)
- 0098-7484
- OpenAlex
- W1998922937
- Cited by
- 144
- References
- 9
- Citations by year
- 2026: 1 · 2025: 3 · 2024: 2 · 2023: 2 · 2022: 3 · 2021: 1 · 2020: 1 · 2019: 2 · 2018: 5 · 2017: 2 · 2016: 4 · 2015: 2 · 2014: 3 · 2013: 3 · 2012: 1
- FWCI
- 10.22
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- JAMA (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Thyroid Disorders and Treatments
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Health Sciences › Medicine › Surgery › Thyroid and Parathyroid Surgery
- Keywords
- cholestyramine, anion exchange resin, hypothyroidism, drug interactions, serum cholesterol lowering, timing of drug administration
- MeSH terms
- Animals, Anticholesteremic Agents, Cholestyramine Resin, Female, Humans, Intestinal Absorption, Iodine, Iodine Isotopes, Ion Exchange Resins, Thyroid Hormones, Thyroxine, Time Factors, In Vitro Techniques
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