Colestipol 1g tablets
Prescription only
Requires a prescription from a doctor or prescriber
Tablet
1g
Oral
Active ingredients:
Colestipol
1 safety notice
Safety information for pregnancy and breastfeeding
Pregnancy
No clinical data are available on the use of colestipol in pregnant women and during lactation [FDA Label, L6115, F4555, F4567].
Due to its known interference with absorption of fat-soluble vitamins, the use of colestipol in pregnancy or lactation or by women of childbearing potential requires that the benefits of drug therapy be weighed against the possible hazards to the mother and the child [FDA Label, L6115, F4555, F4567].
Breastfeeding
No clinical data are available on the use of colestipol in pregnant women and during lactation [FDA Label, L6115, F4555, F4567].
Due to its known interference with absorption of fat-soluble vitamins, the use of colestipol in pregnancy or lactation or by women of childbearing potential requires that the benefits of drug therapy be weighed against the possible hazards to the mother and the child [FDA Label, L6115, F4555, F4567].
Always consult your doctor or midwife before taking any medicine during pregnancy or while breastfeeding. Source: DrugBank (CC BY-NC 4.0).
Official documents, adverse reaction reporting, and safety monitoring
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Safety monitoring data
Yellow Card reports
MHRA
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Colestipol
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Report a side effect
Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
EMA
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
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Suspected adverse reactions reported for Colestipol
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Learn about EU pharmacovigilance and safety monitoring
EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
2 branded products available
WHO defined daily dose (DDD)
20 gram
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
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Colestipol 5g granules for oral suspension sachets sugar free
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Same therapeutic group
Colestyramine 4g oral powder sachets
Powder
4g
Same therapeutic group
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(2)
Bile acid malabsorption: colesevelam (ESUOM22)
ESUOM22
Evidence summary
Updated Oct 2013SeHCAT (tauroselcholic [75 selenium] acid) for diagnosing bile acid diarrhoea (HTG598)
HTG598
Guidance
Updated Nov 2021Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & safety information
Official UK regulator monitoring and safety alerts
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. Shortage and safety information sourced from MHRA drug safety updates (gov.uk, Crown Copyright under OGL v3.0).
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Searching UK clinical trials...
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 1 · Randomised trials: 1 · 1970–2025
Showing the 50 most relevant studies, sorted by most relevant.
Randomized controlled trial of colestipol in antibiotic‐associated colitis (opens in a new tab)
G. Mogg, R. George, D. Youngs, et al.
British Journal of Surgery, 1982
Randomised trial
Cited by 67Beneficial effects of combined colestipol-niacin therapy on coronary atherosclerosis and coronary venous bypass grafts. (opens in a new tab)
D. Blankenhorn, S. Nessim, R. Johnson, et al.
JAMA, 1987
Cited by 1,707
Beneficial effects of colestipol-niacin on coronary atherosclerosis. A 4-year follow-up. (opens in a new tab)
L. Cashin-Hemphill, W. Mack, J. Pogoda, et al.
JAMA, 1990
Cited by 504
Beneficial Effects of Colestipol‐Niacin Therapy on the Common Carotid Artery. Two‐ and Four‐Year Reduction of Intima‐Media Thickness Measured by Ultrasound (opens in a new tab)
David H. Blankenhornt, R. Selzer, D. Crawfordt, et al.
Circulation, 1993
Cited by 400
Colestipol hydrochloride in hypercholesterolemic patients--effect on serum cholesterol and mortality. (opens in a new tab)
A. Dorr, K. Gundersen, J. Schneider, et al.
Journal of chronic diseases, 1978
Cited by 220
Mevinolin and colestipol stimulate receptor-mediated clearance of low density lipoprotein from plasma in familial hypercholesterolemia heterozygotes. (opens in a new tab)
D. Bilheimer, S. Grundy, M. Brown, et al.
Proceedings of the National Academy of Sciences of the United States of America, 2004
Cited by 215
Effects of colestipol-niacin therapy on human femoral atherosclerosis. (opens in a new tab)
D. Blankenhorn, S. Azen, D. Crawford, et al.
Circulation, 1991
Cited by 175
One‐Year Reduction and Longitudinal Analysis of Carotid Intima‐Media Thickness Associated With Colestipol/Niacin Therapy (opens in a new tab)
W. Mack, R. Selzer, H. Hodis, et al.
Stroke, 1993
Cited by 141
Use of combined diet and colestipol in long-term (7--7 1/2 years) treatment of patients with type II hyperlipoproteinemia. (opens in a new tab)
P. Kuo, K. Hayase, J. Kostis, et al.
Circulation, 1979
Cited by 136
Mevinolin plus colestipol in therapy for severe heterozygous familial hypercholesterolemia. (opens in a new tab)
D. Illingworth
Annals of internal medicine, 1984
Cited by 121
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
Not available
Mechanism
Colestipol is a lipid-lowering polymer that binds with bile acids in the intesti…
Food interactions
2 warnings
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
99.75%
Colestipol is hydrophilic, but it is virtually water-insoluble (99.75%)…
Half-life
Colestipol is not absorbed into the systemic circulation nor is it hydrolyzed by any digestive enzymes [FDA Label, L6115, F4555, F4567].…
Protein binding
Colestipol is not absorbed into the systemic circulation [FDA Label, L6115, F4555, F4567].
Volume of distribution
Colestipol is not absorbed into the systemic circulation [FDA Label, L6115, F4555, F4567].
Metabolism
Colestipol is not absorbed into the systemic circulation nor is it hydrolyzed by any digestive enzymes [FDA Label, L6115, F4555, F4567].
Elimination
0.17%
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is then ultimately excreted in the feces [FDA Label, L6115, F4555, F4567].…
Clearance
Colestipol is not absorbed into the systemic circulation [FDA Label, L6115, F4555, F4567].
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Small molecule
About this compound
Bile acid sequestrants like colestipol have been in use since the 1970s.[FDA Label, F4555, F4567, L6262] And even though such an agent may very well be useful in reducing elevated cholesterol levels and decreasing the risk for atherosclerotic vascular disease due to hypercholesterolemia, colestipol is still generally only employed as an adjunct therapy and the relatively physical nature of its pharmacological activity sometimes limits its usefulness.[FDA Label, F4555, F4567, L6262]
In particular, as colestipol's general mechanism of action ultimately results in the decreased absorption and enhanced secretion of bile acids and lipids in the feces, patients who take complicated medication regimens, experience constipation or biliary obstruction, etc. may not be good candidates for using the agent owing to its physical effects on the gut.[FDA Label, F4555, F4567, L6262]
Alternatively, colestipol predominantly elicits its activities within the gut environment because it undergoes little absorption and metabolism.[FDA Label, F4555, F4567, L6262] The resultant lack of systemic exposure consequently means the medication generally demonstrates very few adverse effects inside the body.[FDA Label, F4555, F4567, L6262]
In particular, as colestipol's general mechanism of action ultimately results in the decreased absorption and enhanced secretion of bile acids and lipids in the feces, patients who take complicated medication regimens, experience constipation or biliary obstruction, etc. may not be good candidates for using the agent owing to its physical effects on the gut.[FDA Label, F4555, F4567, L6262]
Alternatively, colestipol predominantly elicits its activities within the gut environment because it undergoes little absorption and metabolism.[FDA Label, F4555, F4567, L6262] The resultant lack of systemic exposure consequently means the medication generally demonstrates very few adverse effects inside the body.[FDA Label, F4555, F4567, L6262]
Properties:
View FDA drug labelsolid
DrugBank indication
Colestipol is indicated as adjunctive therapy to diet for the reduction of elevated serum total and low-density lipoprotein cholesterol (LDL-C) in patients with primary hypercholesterolemia (a condition that features elevated LDL-C) who do not respond adequately to dietary changes .[FDA Label,L6115,F4555]
Therapy with lipid-altering agents like colestipol should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia [FDA Label, L6115, F4555]. Treatment should begin and continue with dietary therapy [FDA Label, L6115, F4555]. In general, a minimum of six months of intensive dietary therapy and counseling should be carried out prior to initiation of drug therapy such as that with colestipol [FDA Label, F4555].
Shorter periods may be considered in patients with severe elevations of LDL-C or with definite coronary heart disease [FDA Label, F4555].
Although colestipol is effective in all types of hypercholesterolemia, some regional prescribing information note in particular that it is medically most appropriate in patients with Fredrickson's type II hyperlipoproteinemia .
[L6115]
Nevertheless, in patients with combined hypercholesterolemia and hypertriglyceridemia, although colestipol may be helpful in reducing elevated cholesterol, it is not formally indicated where hypertriglyceridemia is the abnormality of greatest concern [F4567].
Therapy with lipid-altering agents like colestipol should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia [FDA Label, L6115, F4555]. Treatment should begin and continue with dietary therapy [FDA Label, L6115, F4555]. In general, a minimum of six months of intensive dietary therapy and counseling should be carried out prior to initiation of drug therapy such as that with colestipol [FDA Label, F4555].
Shorter periods may be considered in patients with severe elevations of LDL-C or with definite coronary heart disease [FDA Label, F4555].
Although colestipol is effective in all types of hypercholesterolemia, some regional prescribing information note in particular that it is medically most appropriate in patients with Fredrickson's type II hyperlipoproteinemia .
[L6115]
Nevertheless, in patients with combined hypercholesterolemia and hypertriglyceridemia, although colestipol may be helpful in reducing elevated cholesterol, it is not formally indicated where hypertriglyceridemia is the abnormality of greatest concern [F4567].
Also known as(4)
Colestipol
Colestipolum
Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
Epichlorohydrin-tetraethylenepentamine polymer
Drug interactions(351)
Known interactions with other medicines. Always consult a healthcare professional.
Colestipol can cause a decrease in the absorption of Diltiazem resulting in a reduced serum concentration and potentially a decrease in efficacy.
Amiodarone
Moderate
The excretion of Amiodarone can be increased when combined with Colestipol.
Pravastatin
Moderate
Colestipol can cause a decrease in the absorption of Pravastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lovastatin
Moderate
Colestipol can cause a decrease in the absorption of Lovastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cerivastatin
Moderate
Colestipol can cause a decrease in the absorption of Cerivastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Simvastatin
Moderate
Colestipol can cause a decrease in the absorption of Simvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Atorvastatin
Moderate
Colestipol can cause a decrease in the absorption of Atorvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fluvastatin
Moderate
Colestipol can cause a decrease in the absorption of Fluvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rosuvastatin
Moderate
Colestipol can cause a decrease in the absorption of Rosuvastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mevastatin
Moderate
Colestipol can cause a decrease in the absorption of Mevastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pitavastatin
Moderate
Colestipol can cause a decrease in the absorption of Pitavastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ursodeoxycholic acid
Moderate
Colestipol can cause a decrease in the absorption of Ursodeoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Glycochenodeoxycholic Acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholic Acid
Moderate
Colestipol can cause a decrease in the absorption of Cholic Acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Glycocholic acid
Moderate
Colestipol can cause a decrease in the absorption of Glycocholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Deoxycholic acid
Moderate
Colestipol can cause a decrease in the absorption of Deoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Taurocholic acid
Moderate
Colestipol can cause a decrease in the absorption of Taurocholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Chenodeoxycholic acid
Moderate
Colestipol can cause a decrease in the absorption of Chenodeoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Taurochenodeoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tauroursodeoxycholic acid
Moderate
Colestipol can cause a decrease in the absorption of Tauroursodeoxycholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Bamet-UD2 resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dehydrocholic acid
Moderate
Colestipol can cause a decrease in the absorption of Dehydrocholic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hyodeoxycholic Acid
Moderate
Colestipol can cause a decrease in the absorption of Hyodeoxycholic Acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Deferasirox
Moderate
Colestipol can cause a decrease in the absorption of Deferasirox resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Ezetimibe resulting in a reduced serum concentration and potentially a decrease in efficacy.
Leflunomide
Moderate
Colestipol may increase the excretion rate of Leflunomide which could result in a lower serum level and potentially a reduction in efficacy.
Teriflunomide
Moderate
Colestipol may increase the excretion rate of Teriflunomide which could result in a lower serum level and potentially a reduction in efficacy.
Lomitapide
Moderate
Colestipol can cause a decrease in the absorption of Lomitapide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methotrexate
Moderate
Colestipol may increase the excretion rate of Methotrexate which could result in a lower serum level and potentially a reduction in efficacy.
Colestipol can cause a decrease in the absorption of Niacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Propranolol
Moderate
Colestipol can cause a decrease in the absorption of Propranolol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Raloxifene
Moderate
Colestipol can cause a decrease in the absorption of Raloxifene resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vancomycin
Moderate
The therapeutic efficacy of Vancomycin can be decreased when used in combination with Colestipol.
Mycophenolate mofetil
Moderate
Colestipol can cause a decrease in the absorption of Mycophenolate mofetil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mycophenolic acid
Moderate
Colestipol can cause a decrease in the absorption of Mycophenolic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetyldigitoxin
Moderate
Colestipol can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Deslanoside
Moderate
Colestipol can cause a decrease in the absorption of Deslanoside resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Ouabain resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Digitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Oleandrin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Cymarin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Proscillaridin
Moderate
Colestipol can cause a decrease in the absorption of Proscillaridin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanatoside C
Moderate
Colestipol can cause a decrease in the absorption of Lanatoside C resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gitoformate
Moderate
Colestipol can cause a decrease in the absorption of Gitoformate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Peruvoside
Moderate
Colestipol can cause a decrease in the absorption of Peruvoside resulting in a reduced serum concentration and potentially a decrease in efficacy.
Desogestrel
Moderate
Colestipol can cause a decrease in the absorption of Desogestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Megestrol acetate
Moderate
Colestipol can cause a decrease in the absorption of Megestrol acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Levonorgestrel
Moderate
Colestipol can cause a decrease in the absorption of Levonorgestrel resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colestipol can cause a decrease in the absorption of Medroxyprogesterone acetate resulting in a reduced serum concentration and potentially a decrease in efficacy.
Norethisterone
Moderate
Colestipol can cause a decrease in the absorption of Norethisterone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Showing 50 of 351 interactions
Food & lifestyle interactions
Advice
Drink plenty of fluids. The tablet and granule formulations must be taken with plenty of water or other fluids.
Take With Food
Take with food.
Toxicity & overdose
Overdosage with colestipol has not been reported [FDA Label, L6115, F4555, F4567]. Regardless, in the case of overdosage, the chief potential harm would be obstruction of the gastrointestinal tract [FDA Label, L6115, F4555, F4567]. The location of such potential obstruction, the degree of obstruction and the presence or absence of normal gut motility would determine treatment [FDA Label, L6115, F4555, F4567].
No clinical data are available on the use of colestipol in pregnant women and during lactation [FDA Label, L6115, F4555, F4567]. Colestipol does not appear to be absorbed systematically [FDA Label, L6115, F4555, F4567].
Due to its known interference with absorption of fat-soluble vitamins, the use of colestipol in pregnancy or lactation or by women of childbearing potential requires that the benefits of drug therapy be weighed against the possible hazards to the mother and the child [FDA Label, L6115, F4555, F4567].
There are no data on the effect of colestipol on fertility in humans [FDA Label, L6115, F4555, F4567].
The use of colestipol in children is limited [FDA Label, L6115, F4555, F4567]. Clinical trials conducted in children with colestipol ranules have usually employed doses of 5 to 20 g/day [FDA Label, L6115, F4555, F4567]. The National Cholesterol Education Program (NCEP) Expert Panel recommends drug therapy be considered in children 10 years or older, who have previously undergone an adequate trial of diet therapy but still have unacceptably high serum cholesterol levels [FDA Label, L6115, F4555, F4567].
In certain situations where a young child has extremely high serum cholesterol levels, drug treatment may even be initiated before 10 years of age [FDA Label, L6115, F4555, F4567]. If the child is started on drug therapy, a carefully assessed diet therapy should also be continued in order to obtain optimal results [FDA Label, L6115, F4555, F4567]. However, the safety of using colestipol tablets in patients under the age of 18 years has not been established [FDA Label, L6115, F4555, F4567].
Furthermore, because bile acid sequestrants like colestipol may interfere with the absorption of fat-soluble vitamins, appropriate monitoring of growth and development is essential if colestipol is used in children [FDA Label, L6115, F4555, F4567].
Appropriate studies on the relationship of age to the effects of colestipol have not been performed in the geriatric population [FDA Label, L6115, F4555, F4567]. However, patients over 60 years of age may be more likely to experience gastrointestinal side effects, as well as adverse nutritional effects [FDA Label, L6115, F4555, F4567].
Additionally, it has been determined that the oral LD50 in rats is > 1000 mg/kg MSDS.
No clinical data are available on the use of colestipol in pregnant women and during lactation [FDA Label, L6115, F4555, F4567]. Colestipol does not appear to be absorbed systematically [FDA Label, L6115, F4555, F4567].
Due to its known interference with absorption of fat-soluble vitamins, the use of colestipol in pregnancy or lactation or by women of childbearing potential requires that the benefits of drug therapy be weighed against the possible hazards to the mother and the child [FDA Label, L6115, F4555, F4567].
There are no data on the effect of colestipol on fertility in humans [FDA Label, L6115, F4555, F4567].
The use of colestipol in children is limited [FDA Label, L6115, F4555, F4567]. Clinical trials conducted in children with colestipol ranules have usually employed doses of 5 to 20 g/day [FDA Label, L6115, F4555, F4567]. The National Cholesterol Education Program (NCEP) Expert Panel recommends drug therapy be considered in children 10 years or older, who have previously undergone an adequate trial of diet therapy but still have unacceptably high serum cholesterol levels [FDA Label, L6115, F4555, F4567].
In certain situations where a young child has extremely high serum cholesterol levels, drug treatment may even be initiated before 10 years of age [FDA Label, L6115, F4555, F4567]. If the child is started on drug therapy, a carefully assessed diet therapy should also be continued in order to obtain optimal results [FDA Label, L6115, F4555, F4567]. However, the safety of using colestipol tablets in patients under the age of 18 years has not been established [FDA Label, L6115, F4555, F4567].
Furthermore, because bile acid sequestrants like colestipol may interfere with the absorption of fat-soluble vitamins, appropriate monitoring of growth and development is essential if colestipol is used in children [FDA Label, L6115, F4555, F4567].
Appropriate studies on the relationship of age to the effects of colestipol have not been performed in the geriatric population [FDA Label, L6115, F4555, F4567]. However, patients over 60 years of age may be more likely to experience gastrointestinal side effects, as well as adverse nutritional effects [FDA Label, L6115, F4555, F4567].
Additionally, it has been determined that the oral LD50 in rats is > 1000 mg/kg MSDS.
How it works
Mechanism of action
Colestipol is a lipid-lowering polymer that binds with bile acids in the intestine forming a complex that is excreted in the feces [FDA Label, F4555, F4567]. This non-systemic action results in a continuous, partial removal of bile acids from the enterohepatic circulation preventing their reabsorption [FDA Label, F4555, F4567]. This increased fecal loss of bile acids due to colestipol hydrochloride administration leads to increased oxidation of cholesterol to bile acids [FDA Label, F4555, F4567]. This results in an increase in the number of hepatic low-density lipoprotein (LDL) receptors, and consequently an increased uptake of LDL and a decrease in serum/plasma beta lipoprotein or total and LDL cholesterol levels [FDA Label, F4555, F4567]. Although hydrochloride produces an increase in the hepatic synthesis of cholesterol in man, serum cholesterol levels fall [FDA Label, F4555, F4567].
Pharmacodynamics
Cholesterol is the major, and probably the sole precursor of bile acids [FDA Label, F4555]. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines [FDA Label, F4555]. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption [FDA Label, F4555]. A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle [FDA Label, F4555]. Only very small amounts of bile acids are found in normal serum [FDA Label, F4555].
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces [FDA Label, F4555]. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption [FDA Label, F4555]. Since colestipol hydrochloride is an anion exchange resin, the chloride anions of the resin can be replaced by other anions, usually those with a greater affinity for the resin than the chloride ion [FDA Label, F4555].
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces [FDA Label, F4555]. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption [FDA Label, F4555]. Since colestipol hydrochloride is an anion exchange resin, the chloride anions of the resin can be replaced by other anions, usually those with a greater affinity for the resin than the chloride ion [FDA Label, F4555].
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Colestipol is hydrophilic, but it is virtually water-insoluble (99.75%) [FDA Label, L6115, F4555, F4567]. This water insolubility, combined with the high molecular weight polymer in colestipol basically means the agent and the complexes it forms when it binds with bile acids are not absorbed [FDA Label, L6115, F4555, F4567]. The action of colestipol is ultimately limited to the lumen of the gastrointestinal tract [FDA Label, L6115, F4555, F4567].
It binds bile acids in the intestinal lumen and causes them to be excreted in the feces together with the polymer [FDA Label, L6115, F4555, F4567]. When the enterohepatic circulation of bile acids is interrupted, cholesterol conversion to bile acids is enhanced and plasma cholesterol levels are thereby lowered [FDA Label, L6115, F4555, F4567].
It binds bile acids in the intestinal lumen and causes them to be excreted in the feces together with the polymer [FDA Label, L6115, F4555, F4567]. When the enterohepatic circulation of bile acids is interrupted, cholesterol conversion to bile acids is enhanced and plasma cholesterol levels are thereby lowered [FDA Label, L6115, F4555, F4567].
Half-life
Colestipol is not absorbed into the systemic circulation nor is it hydrolyzed by any digestive enzymes [FDA Label, L6115, F4555, F4567]. Its action is ultimately limited to the lumen of the gastrointestinal tract, where it is eventually passed into the feces [FDA Label, L6115, F4555, F4567].
Protein binding
Colestipol is not absorbed into the systemic circulation [FDA Label, L6115, F4555, F4567].
Volume of distribution
Colestipol is not absorbed into the systemic circulation [FDA Label, L6115, F4555, F4567].
Metabolism
Colestipol is not absorbed into the systemic circulation nor is it hydrolyzed by any digestive enzymes [FDA Label, L6115, F4555, F4567].
Route of elimination
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is then ultimately excreted in the feces [FDA Label, L6115, F4555, F4567]. In humans, less than 0.17% of a single 14C-labeled colestipol hydrochloride dose is excreted in the urine when given following 60 days of chronic dosing of 20 grams of colestipol hydrochloride per day [FDA Label, F4555]. The increased fecal loss of bile acids due to colestipol hydrochloride administration leads to increased oxidation of cholesterol to bile acids [FDA Label, F4555].
Clearance
Colestipol is not absorbed into the systemic circulation [FDA Label, L6115, F4555, F4567].
Drug targets(1)
ATC classification(1 code)
ATC C10AC02
Affected organisms(1)
Humans and other mammals
Salt forms(1)
Colestipol hydrochloride(DBSALT001058)
Experimental properties(2)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Colestipol
DrugBank citations
If you use DrugBank data in your research, please cite:
- DrugBank 6.02024Recommended citationKnox C., Wilson M., Klinger C.M., et alDrugBank 6.0: the DrugBank Knowledgebase for 2024Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
- DrugBank 5.02018Wishart D.S., Feunang Y.D., Guo A.C., et alDrugBank 5.0: a major update to the DrugBank database for 2018Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
- DrugBank 4.02014Law V., Knox C., Djoumbou Y., et alDrugBank 4.0: shedding new light on drug metabolismNucleic Acids Res. 2014 Jan 142(1):D1091-7
- DrugBank 3.02011Knox C., Law V., Jewison T., et alDrugBank 3.0: a comprehensive resource for 'omics' research on drugsNucleic Acids Res. 2011 Jan39(Database issue):D1035-41
- DrugBank 2.02008Wishart D.S., Knox C., Guo A.C., et alDrugBank: a knowledgebase for drugs, drug actions and drug targets.Nucleic Acids Research2008 Jan36(Database issue):D901-6
- DrugBank 1.02006Wishart D.S., Knox C., Guo A.C., et alDrugBank: a comprehensive resource for in silico drug discovery and exploration.Nucleic Acids Research2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 4 Mar 2026