- Accession Number
- DB00375 (APRD00884)
- Small Molecule
Bile acid sequestrants like colestipol have been in use since the 1970s.Label,4,6,3 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.Label,4,6,3
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.Label,4,6,3
Alternatively, colestipol predominantly elicits its activities within the gut environment because it undergoes little absorption and metabolism.Label,4,6,3 The resultant lack of systemic exposure consequently means the medication generally demonstrates very few adverse effects inside the body.Label,4,6,3
- Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
- Epichlorohydrin-tetraethylenepentamine polymer
- External IDs
- U 26597 A
- Product Ingredients
Ingredient UNII CAS InChI Key Colestipol hydrochloride X7D10K905G 37296-80-3 Not applicable
- Product Images
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Colestid Granule, for suspension 5 g/5g Oral Pharmacia and Upjohn Company LLC 1977-04-04 Not applicable Colestid Granule, for suspension 5 g/5g Oral Physicians Total Care, Inc. 1977-04-04 2010-06-30 Colestid Tablet 1 g/1 Oral Pharmacia and Upjohn Company LLC 1994-07-19 Not applicable Colestid Granules Granule Oral Pfizer Canada Ulc 1985-12-31 Not applicable Colestid Orange Granules Granule Oral Pfizer Canada Ulc 1995-12-31 Not applicable Colestid Tablets 1 G Tablet Oral Pfizer Canada Ulc 1995-12-31 Not applicable Flavored Colestid Granule, for suspension 5 g/7.5g Oral Physicians Total Care, Inc. 1977-04-04 2011-06-30 Flavored Colestid Granule, for suspension 5 g/7.5g Oral Pharmacia and Upjohn Company LLC 1977-04-04 Not applicable
- Generic Prescription Products
- International/Other Brands
- Cholestabyl / Lestid (Pfizer)
- Anion Exchange Resins
- Bile Acid Sequestrants
- Bile-acid Binding Activity
- Compounds used in a research, industrial, or household setting
- Hypolipidemic Agents
- Lipid Modifying Agents
- Lipid Modifying Agents, Plain
- Lipid Regulating Agents
- Macromolecular Substances
- Sequestering Agents
- CAS number
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 diet Label,1,4.
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 Label,1,4. Treatment should begin and continue with dietary therapy Label,1,4. 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 Label,4. Shorter periods may be considered in patients with severe elevations of LDL-C or with definite coronary heart disease Label,4.
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 1. 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 6.
- Associated Conditions
Cholesterol is the major, and probably the sole precursor of bile acids Label,4. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines Label,4. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption Label,4. 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 Label,4. Only very small amounts of bile acids are found in normal serum Label,4.
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces Label,4. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption Label,4. 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 Label,4.
- 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 Label,4,6. This non-systemic action results in a continuous, partial removal of bile acids from the enterohepatic circulation preventing their reabsorption Label,4,6. This increased fecal loss of bile acids due to colestipol hydrochloride administration leads to increased oxidation of cholesterol to bile acids Label,4,6. 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 Label,4,6. Although hydrochloride produces an increase in the hepatic synthesis of cholesterol in man, serum cholesterol levels fall Label,4,6.
Target Actions Organism ABile acidsbinder Humans
Colestipol is hydrophilic, but it is virtually water-insoluble (99.75%) Label,1,4,6. 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 Label,1,4,6. The action of colestipol is ultimately limited to the lumen of the gastrointestinal tract Label,1,4,6. It binds bile acids in the intestinal lumen and causes them to be excreted in the feces together with the polymer Label,1,4,6. When the enterohepatic circulation of bile acids is interrupted, cholesterol conversion to bile acids is enhanced and plasma cholesterol levels are thereby lowered Label,1,4,6.
- Volume of distribution
- Protein binding
- Route of elimination
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is then ultimately excreted in the feces Label,1,4,6. 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 Label,4. The increased fecal loss of bile acids due to colestipol hydrochloride administration leads to increased oxidation of cholesterol to bile acids Label,4.
- Half life
Colestipol is not absorbed into the systemic circulation nor is it hydrolyzed by any digestive enzymes Label,1,4,6. Its action is ultimately limited to the lumen of the gastrointestinal tract, where it is eventually passed into the feces Label,1,4,6.
Overdosage with colestipol has not been reported Label,1,4,6. Regardless, in the case of overdosage, the chief potential harm would be obstruction of the gastrointestinal tract Label,1,4,6. The location of such potential obstruction, the degree of obstruction and the presence or absence of normal gut motility would determine treatment Label,1,4,6.
No clinical data are available on the use of colestipol in pregnant women and during lactation Label,1,4,6. Colestipol does not appear to be absorbed systematically Label,1,4,6. 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 Label,1,4,6.
The use of colestipol in children is limited Label,1,4,6. Clinical trials conducted in children with colestipol ranules have usually employed doses of 5 to 20 g/day Label,1,4,6. 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 Label,1,4,6. In certain situations where a young child has extremely high serum cholesterol levels, drug treatment may even be initiated before 10 years of age Label,1,4,6. If the child is started on drug therapy, a carefully assessed diet therapy should also be continued in order to obtain optimal results Label,1,4,6. However, the safety of using colestipol tablets in patients under the age of 18 years has not been established Label,1,4,6. 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 Label,1,4,6.
Appropriate studies on the relationship of age to the effects of colestipol have not been performed in the geriatric population Label,1,4,6. However, patients over 60 years of age may be more likely to experience gastrointestinal side effects, as well as adverse nutritional effects Label,1,4,6.
Additionally, it has been determined that the oral LD50 in rats is > 1000 mg/kg MSDS.
- Affected organisms
- Humans and other mammals
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.Learn more
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- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction (6R)-Folinic acid The serum concentration of (6R)-Folinic acid can be decreased when it is combined with Colestipol. (6S)-5,6,7,8-tetrahydrofolic acid The serum concentration of (6S)-5,6,7,8-tetrahydrofolic acid can be decreased when it is combined with Colestipol. (R)-warfarin Colestipol can cause a decrease in the absorption of (R)-warfarin resulting in a reduced serum concentration and potentially a decrease in efficacy. (S)-Warfarin Colestipol can cause a decrease in the absorption of (S)-Warfarin resulting in a reduced serum concentration and potentially a decrease in efficacy. 1alpha-Hydroxyvitamin D5 The serum concentration of 1alpha-Hydroxyvitamin D5 can be decreased when it is combined with Colestipol. 1alpha,24S-Dihydroxyvitamin D2 The serum concentration of 1alpha,24S-Dihydroxyvitamin D2 can be decreased when it is combined with Colestipol. 4-hydroxycoumarin Colestipol can cause a decrease in the absorption of 4-hydroxycoumarin resulting in a reduced serum concentration and potentially a decrease in efficacy. 5-(2-methylpiperazine-1-sulfonyl)isoquinoline Colestipol can cause a decrease in the absorption of 5-(2-methylpiperazine-1-sulfonyl)isoquinoline resulting in a reduced serum concentration and potentially a decrease in efficacy. 5-methyltetrahydrofolic acid The serum concentration of 5-methyltetrahydrofolic acid can be decreased when it is combined with Colestipol. Aceclofenac Colestipol can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.Additional Data Available
- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.Learn more
A severity rating for each drug interaction, from minor to major.Learn more
- Evidence LevelEvidence Level
A rating for the strength of the evidence supporting each drug interaction.Learn more
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- Food Interactions
- Take with food.
- Synthesis Reference
Lednicer, D. and Peery,C.Y.; US. Patent 3,803,237; April 9, 1974; assigned to The Upjohn Co.
- General References
- Electronic Medicines Compendium: Colestid (colestipol hydrochloride) Orange 5g Monograph [Link]
- NCBI LactMed@NIH Drugs and Lactation Database (LactMed) [Internet]: Colestipol Profile [Link]
- Colestipol ScienceDirect Profile [Link]
- Colestid/Flavored Colestid (colestipol hydrochloride for oral suspension) [File]
- Pfizer MSDS for Colestipol Hydrochloride for Oral Suspension [File]
- Colestipol hydrochloride Canadian Product Monograph [File]
- External Links
- ATC Codes
- C10AC02 — Colestipol
- AHFS Codes
- 24:06.04 — Bile Acid Sequestrants
- FDA label
- Download (135 KB)
- Download (53.5 KB)
- Clinical Trials
Phase Status Purpose Conditions Count 1 Terminated Other Healthy Volunteers / Teriflunomide Elimination 1 2 Recruiting Treatment Early Stage HER2+ Breast Cancer 1 2, 3 Completed Treatment Protoporphyria, Erythropoietic 1 3 Completed Treatment Arterial Occlusive Diseases / Atherosclerosis / Cardiovascular Heart Disease / Carotid Artery Diseases / Cerebral Arteriosclerosis / Cerebrovascular Diseases / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia 1 3 Completed Treatment Cardiovascular Heart Disease / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia 1 4 Completed Treatment High Cholesterol / Hyperlipidemias 1
- Pharmacia and upjohn co
- Impax laboratories inc
- Catalent Pharma Solutions
- Global Pharmaceuticals
- Greenstone LLC
- Impax Laboratories Inc.
- Kaiser Foundation Hospital
- Murfreesboro Pharmaceutical Nursing Supply
- Patheon Inc.
- Pharmacia Inc.
- Physicians Total Care Inc.
- Southwood Pharmaceuticals
- Dosage forms
Form Route Strength Granule, for suspension Oral 5 g/5g Granule Oral Tablet Oral Suspension Oral 5 g/1 Tablet Oral 1 g/1 Tablet, film coated Oral 1 g/1 Granule, for suspension Oral 5 g/7.5g
Unit description Cost Unit Colestid 90 5 gm Packets Box 252.5USD box Colestid 30 5 gm Packets Box 81.11USD box Colestid Flavored 5 gm/7.5 gm Packets 3.29USD packet Colestid 5 g Powder Packet 1.04USD packet Colestid Orange 5 g Powder Packet 1.04USD packet Colestid 1 gm tablet 0.86USD tablet Colestipol hcl 1 gm tablet 0.66USD tablet Colestid 5 gm Granules 0.33USD gm Colestid Flavored 5 gm Granules 0.31USD gm Colestid flavored granules 0.3USD g Colestid 1 g Tablet 0.29USD tabletDrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent Number Pediatric Extension Approved Expires (estimated) US5490987 No 1996-02-13 2013-02-13Additional Data Available
- Filed OnFiled On
The date on which a patent was filed with the relevant government.Learn more
- Experimental Properties
Property Value Source water solubility Insoluble Not Available logP -2.206 Not Available
- Predicted Properties
- Not Available
- Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9221 Blood Brain Barrier + 0.8825 Caco-2 permeable - 0.5102 P-glycoprotein substrate Substrate 0.6506 P-glycoprotein inhibitor I Non-inhibitor 0.9435 P-glycoprotein inhibitor II Non-inhibitor 0.956 Renal organic cation transporter Non-inhibitor 0.6803 CYP450 2C9 substrate Non-substrate 0.8931 CYP450 2D6 substrate Non-substrate 0.7534 CYP450 3A4 substrate Non-substrate 0.7558 CYP450 1A2 substrate Non-inhibitor 0.7178 CYP450 2C9 inhibitor Non-inhibitor 0.8515 CYP450 2D6 inhibitor Non-inhibitor 0.8411 CYP450 2C19 inhibitor Non-inhibitor 0.7634 CYP450 3A4 inhibitor Non-inhibitor 0.8919 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9404 Ames test AMES toxic 0.9093 Carcinogenicity Non-carcinogens 0.6451 Biodegradation Not ready biodegradable 0.9346 Rat acute toxicity 2.5333 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.508 hERG inhibition (predictor II) Non-inhibitor 0.7601
- Mass Spec (NIST)
- Not Available
- Not Available
- Not classified
- LaRosa JC: The mechanism of action of lipid-lowering drugs. Angiology. 1982 Sep;33(9):562-76. [PubMed:7125296]
- Farmer JA, Gotto AM Jr: Currently available hypolipidaemic drugs and future therapeutic developments. Baillieres Clin Endocrinol Metab. 1995 Oct;9(4):825-47. [PubMed:8593127]
- Reiner Z: Combined therapy in the treatment of dyslipidemia. Fundam Clin Pharmacol. 2010 Feb;24(1):19-28. doi: 10.1111/j.1472-8206.2009.00764.x. Epub 2009 Aug 14. [PubMed:19682080]
Drug created on June 13, 2005 07:24 / Updated on January 18, 2020 13:23