Colestipol

Mechanism-of-action classes: Bile-acid Binding Activity; Binding Activity.

• & USAGE Since no drug is innocuous, strict attention should be paid to the indications and contraindications, particularly when selecting drugs for chronic long-term use. Colestipol hydrochloride tablets are indicated as adjunctive therapy to diet for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet.ICD-10: E78.00

• Colestipol hydrochloride tablets are contraindicated in those individuals who have shown hypersensitivity to any of their components.contraindicated

DOSAGE & ADMINISTRATION For adults, colestipol hydrochloride tablets are recommended in doses of 2 to 16 grams/day given once or in divided doses. The starting dose should be 2 grams once or twice daily. Dosage increases of 2 grams, once or twice daily should occur at 1-or 2-month intervals. Appropriate use of lipid profiles as per NCEP guidelines including LDL-C and triglycerides, is advised so that optimal but not excessive doses are used to obtain the desired therapeutic effect on LDL-C level. If the desired therapeutic effect is not obtained at a dose of 2 to 16 grams/day with good compliance and acceptable side effects, combined therapy or alternate treatment should be considered. Colestipol hydrochloride tablets must be taken one at a time and be promptly swallowed whole, using plenty of water or other appropriate liquid. Do not cut, crush, or chew the tablets. Patients should take other drugs at least one hour before or four hours after colestipol hydrochloride tablets to minimize possible interference with their absorption. (See Drug Interactions.) Before Administration of Colestipol Hydrochloride Tablets Define the type of hyperlipoproteinemia, as described in NCEP guidelines. Institute a trial of diet and weight reduction. Establish baseline serum total and LDL-C and triglyceride levels. During Administration of Colestipol Hydrochloride Tablets The patient should be carefully monitored clinically, including serum cholesterol and triglyceride levels.

Gastrointestinal The most common adverse reactions are confined to the gastrointestinal tract. To achieve minimal GI disturbance with an optimal LDL-C lowering effect, a gradual increase of dosage starting with 2 grams, once or twice daily is recommended. Constipation is the major single complaint and at times is severe. Most instances of constipation are mild, transient, and controlled with standard treatment. Increased fluid intake and inclusion of additional dietary fiber should be the first step; a stool softener may be added if needed. Some patients require decreased dosage or discontinuation of therapy. Hemorrhoids may be aggravated. Other, less frequent gastrointestinal complaints consist of abdominal discomfort (abdominal pain and cramping), intestinal gas (bloating and flatulence), indigestion and heartburn, diarrhea and loose stools, and nausea and vomiting. Bleeding hemorrhoids and blood in the stool have been infrequently reported. Peptic ulceration, cholecystitis, and cholelithiasis have been rarely reported in patients receiving colestipol hydrochloride granules, and are not necessarily drug related. Difficulty swallowing and transient esophageal obstruction have been rarely reported in patients taking colestipol hydrochloride tablets. Transient and modest elevations of aspartate aminotransferase (AST, SGOT), alanine aminotransferase (ALT, SGPT) and alkaline phosphatase were observed on one or more occasions in various patients treated with colestipol hydrochloride.

Use in Pregnancy Since colestipol hydrochloride is essentially not absorbed systemically (less than 0.17% of the dose), it is not expected to cause fetal harm when administered during pregnancy in recommended dosages. There are no adequate and well-controlled studies in pregnant women, and the known interference with absorption of fat-soluble vitamins may be detrimental even in the presence of supplementation. The use of colestipol hydrochloride tablets in pregnancy or by women of childbearing potential requires that the potential benefits of drug therapy be weighed against possible hazards to the mother or child. Nursing Mothers: Caution should be exercised when colestipol hydrochloride tablets are administered to a nursing mother. The possible lack of proper vitamin absorption described in the “Pregnancy” section may have an effect on nursing infants.

Overdosage of colestipol hydrochloride tablets has not been reported. Should overdosage occur, however, the chief potential harm would be obstruction of the gastrointestinal tract. The location of such potential obstruction, the degree of obstruction and the presence or absence of normal gut motility would determine treatment.

• Apr 4, 1977NDANDA017563Pfizer
• Jul 19, 1994NDANDA020222Pfizer
• May 2, 2006ANDAANDA077277Impax Labs
• Oct 24, 2006ANDAANDA077510Impax Labs
• Mar 10, 2022ANDAANDA215223Zydus Pharms
• Mar 10, 2023ANDAANDA216517Ani Pharms
• Aug 16, 2024ANDAANDA217667Edenbridge Pharms
• Dec 3, 2024ANDAANDA217462Riconpharma Llc

1. 1Diarrhoea36714%
2. 2Off Label Use27511%
3. 3Nausea2258.9%
4. 4Fatigue2158.5%
5. 5Drug Ineffective1736.8%
6. 6Headache1395.5%
7. 7Vomiting1265.0%
8. 8Pain1204.7%
9. 9Weight Decreased1144.5%
10. 10Asthenia1124.4%
11. 11Dizziness1104.3%
12. 12Arthralgia1074.2%
13. 13Dyspnoea1024.0%
14. 14Crohn^s Disease993.9%
15. 15Malaise973.8%

Recent PubMed references pinned to Colestipol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Tolerability and efficacy of colestipol hydrochloride for accelerated elimination of teriflunomide.
  Expert review of clinical pharmacology · 2017 · Robertson D, Dixon C, Aungst A, et al.
  PMID 29064296DOI 10.1080/17512433.2017.1395280
• Treatment of Severe Hypercholesterolemia in a Woman With Advanced Primary Sclerosing Cholangitis.
  JAMA cardiology · 2017 · Xiao C, Hegele RA, Lewis GF, et al.
  PMID 28384790DOI 10.1001/jamacardio.2017.0263
• The Cholesterol Lowering Atherosclerosis Study (CLAS): what it tells us about niacin/colestipol therapy.
  Journal of clinical lipidology · 2015 · Hemphill LC
  PMID 25670355DOI 10.1016/j.jacl.2014.09.010
• Feasibility study of colestipol as an oral phosphate binder in hemodialysis patients.
  Nephrology (Carlton, Vic.) · 2015 · Hood CJ, Wolley MJ, Kam AL, et al.
  PMID 25557531DOI 10.1111/nep.12388
• Colestipol granules in the colon: macroscopic and microscopic findings.
  Histopathology · 2015 · Gonzalez RS, Schwartz DA, Shi C, et al.
  PMID 25406854DOI 10.1111/his.12618
• Colesevelam and colestipol: novel medication resins in the gastrointestinal tract.
  The American journal of surgical pathology · 2014 · Arnold MA, Swanson BJ, Crowder CD, et al.
  PMID 24921636DOI 10.1097/PAS.0000000000000260
• Treatment of erythropoietic protoporphyria with the oral sorbent colestipol: a proof-of-concept clinical trial.
  Journal of the American Academy of Dermatology · 2014 · Tishler PV, Rosner B
  PMID 24438965DOI 10.1016/j.jaad.2013.10.011
• Alteration of aluminium inhibition of synaptosomal (Na(+)/K(+))ATPase by colestipol administration.
  Journal of inorganic biochemistry · 2013 · Silva VS, Oliveira L, Gonçalves PP, et al.
  PMID 23829947DOI 10.1016/j.jinorgbio.2013.06.011

The 8 most recently updated of 8 ClinicalTrials.gov registrations naming Colestipol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• The Precision CAD Trial
  Active not recruiting · Interventional · 276 enrolled · Emory University
  NCT04755413updated 2025-11-21
• Effect of the Sequestrant Colesevelam in Bile Acid Diarrhoea
  Completed · Phase 4 · Interventional · 255 enrolled · Lars Kristian Munck
  NCT03876717updated 2022-08-23
• An Open-Label Study to Characterize the Incidence and Severity of Diarrhea in Patients With Early-Stage HER2+ Breast Cancer Treated With Neratinib and Loperamide
  Completed · Phase 2 · Interventional · 563 enrolled · Puma Biotechnology, Inc.
  NCT02400476updated 2022-05-06
• Rapid Elimination Procedure of Teriflunomide With Colestipol Hydrochloride
  Terminated · Phase 1 · Interventional · 14 enrolled · Derrick Scott Robertson
  NCT02263547updated 2020-04-03
• Sorbent Therapy of the Cutaneous Porphyrias
  Completed · Phase 2 · Phase 3 · Interventional · 4 enrolled · Brigham and Women's Hospital
  NCT01422915updated 2017-04-25
• Familial Atherosclerosis Treatment Study
  Completed · Phase 3 · Interventional · 146 enrolled · University of Washington
  NCT00000512updated 2015-12-03
• A Prospective, Open Label Comparison of Ezetimibe, Niacin, and Colestipol as Adjunct Therapy in Lipid Reduction
  Completed · Phase 4 · Interventional · 30 enrolled · Tuscaloosa Research & Education Advancement Corporation
  NCT00203476updated 2014-08-12
• Cholesterol-Lowering Atherosclerosis Study (CLAS)
  Completed · Phase 3 · Interventional · National Heart, Lung, and Blood Institute (NHLBI)
  NCT00000599updated 2013-12-13

Frequently asked questions

How does Colestipol work?

Mechanism-of-action classes: Bile-acid Binding Activity; Binding Activity.

What is Colestipol used for?

According to FDA labeling, Colestipol carries indications including: & USAGE Since no drug is innocuous, strict attention should be paid to the indications and contraindications, particularly when selecting drugs for chronic long-term use. Colestipol hydrochloride tablets are indicated as adjunctive therapy to diet for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Colestipol?

Colestipol is classified as Bile acid sequestrants, Bile Acid Sequestrant, Bile-acid Binding Activity, Binding Activity, Decreased Cholesterol Absorption.

What are the brand names for Colestipol?

Colestipol is marketed under brand names including Colestid.

What are the contraindications for Colestipol?

Colestipol labeling lists contraindications including: Colestipol hydrochloride tablets are contraindicated in those individuals who have shown hypersensitivity to any of their components.. Always consult the full prescribing information and a clinician.