Identification

Name
Colestipol
Accession Number
DB00375  (APRD00884)
Type
Small Molecule
Groups
Approved
Description

Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels.

Synonyms
  • Colestipolum
  • Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
  • Epichlorohydrin-tetraethylenepentamine polymer
External IDs
U 26597 A
Product Ingredients
IngredientUNIICASInChI Key
Colestipol hydrochlorideX7D10K905G37296-80-3Not applicable
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ColestidGranule, for suspension5 g/5gOralPharmacia & Upjohn Inc1977-04-04Not applicableUs
ColestidTablet1 g/1OralPharmacia & Upjohn Inc1994-07-19Not applicableUs
ColestidGranule, for suspension5 g/5gOralPhysicians Total Care, Inc.1977-04-042010-06-30Us
Colestid GranulesGranule5 gOralPfizer1985-12-31Not applicableCanada
Colestid Orange GranulesGranule5 gOralPfizer1995-12-31Not applicableCanada
Colestid Tablets 1 GTablet1 gOralPfizer1995-12-31Not applicableCanada
Flavored ColestidGranule, for suspension5 g/7.5gOralPhysicians Total Care, Inc.1977-04-042011-06-30Us
Flavored ColestidGranule, for suspension5 g/7.5gOralPharmacia & Upjohn Inc1977-04-04Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Colestipol HydrochlorideTablet1 g/1OralCarilion Materials Management1994-07-19Not applicableUs68151 436120180907 15195 a7sxr3
Colestipol HydrochlorideTablet1 g/1OralPhysicians Total Care, Inc.2007-02-28Not applicableUs54868 061020180906 25352 dqp43k
Colestipol HydrochlorideTablet1 g/1OralAvera McKennan Hospital2015-03-202018-06-27Us
Colestipol HydrochlorideSuspension5 g/1OralImpax Generics2006-05-02Not applicableUs
Colestipol HydrochlorideTablet1 g/1OralGreenstone, Llc1994-07-19Not applicableUs59762 0450 01 nlmimage10 863a4302
Colestipol HydrochlorideGranule, for suspension5 g/5gOralGreenstone, Llc1977-04-04Not applicableUs
Colestipol HydrochlorideSuspension5 g/1OralImpax Generics2006-05-02Not applicableUs
Colestipol HydrochlorideTablet, film coated1 g/1OralImpax Generics2006-10-24Not applicableUs
International/Other Brands
Cholestabyl / Lestid (Pfizer)
Categories
UNII
K50N755924
CAS number
26658-42-4
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

For use, 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.

Associated Conditions
Pharmacodynamics

Cholesterol is the major, and probably the sole precursor of bile acids. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption. 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. Only very small amounts of bile acids are found in normal serum. Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption. 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.

Mechanism of action

Colestipol is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, and increasing the number of hepatic low-density lipoprotein (LDL) receptors. These compensatory effects result in increased clearance of LDL cholesterol (LDL-C) from the blood, resulting in decreased serum LDL-C levels. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol.

TargetActionsOrganism
ABile acids
binder
Human
Absorption

Not absorbed from the gastrointestinal tract.

Volume of distribution
Not Available
Protein binding

Not applicable (not hydrolyzed by digestive enzymes and not absorbed).

Metabolism

Not applicable (not hydrolyzed by digestive enzymes and not absorbed).

Route of elimination

Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. 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. The increased fecal loss of bile acids due to colestipol hydrochloride administration leads to an increased oxidation of cholesterol to bile acids.

Half life
Not Available
Clearance
Not Available
Toxicity

Oral LD50 in rats is > 1000 mg/kg. Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colestipol is not absorbed, the risk of systemic toxicity is low.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinColestipol can cause a decrease in the absorption of (R)-warfarin resulting in a reduced serum concentration and potentially a decrease in efficacy.
(S)-WarfarinColestipol can cause a decrease in the absorption of (S)-Warfarin resulting in a reduced serum concentration and potentially a decrease in efficacy.
1alpha-Hydroxyvitamin D5The serum concentration of 1alpha-Hydroxyvitamin D5 can be decreased when it is combined with Colestipol.
3,5-diiodothyropropionic acidColestipol can cause a decrease in the absorption of 3,5-diiodothyropropionic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
4-hydroxycoumarinColestipol can cause a decrease in the absorption of 4-hydroxycoumarin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AbaloparatideColestipol can cause a decrease in the absorption of Abaloparatide resulting in a reduced serum concentration and potentially a decrease in efficacy.
AceclofenacColestipol can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcemetacinColestipol can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcenocoumarolColestipol can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetyldigitoxinColestipol can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food Interactions
  • Take with food.

References

Synthesis Reference

Lednicer, D. and Peery,C.Y.; US. Patent 3,803,237; April 9, 1974; assigned to The Upjohn Co.

General References
Not Available
External Links
Human Metabolome Database
HMDB0014519
KEGG Compound
C06925
PubChem Compound
62816
PubChem Substance
46505777
ChemSpider
56550
ChEMBL
CHEMBL1909303
PharmGKB
PA449096
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Colestipol
ATC Codes
C10AC02 — Colestipol
AHFS Codes
  • 24:06.04 — Bile Acid Sequestrants
MSDS
Download (53.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1TerminatedNot AvailableHealthy Volunteers / Teriflunomide Elimination1
2RecruitingTreatmentEarly Stage HER2+ Breast Cancer1
2, 3CompletedTreatmentProtoporphyria, Erythropoietic1
3CompletedTreatmentArterial Occlusive Diseases / Atherosclerosis / Cardiovascular Disease (CVD) / Carotid Artery Diseases / Cerebral Arteriosclerosis / Cerebrovascular Disorders / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia1
3CompletedTreatmentCardiovascular Disease (CVD) / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia1
4CompletedTreatmentHigh Cholesterol / Hyperlipidemias1

Pharmacoeconomics

Manufacturers
  • Pharmacia and upjohn co
  • Impax laboratories inc
Packagers
  • 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
FormRouteStrength
Granule, for suspensionOral5 g/5g
GranuleOral5 g
TabletOral1 g
SuspensionOral5 g/1
TabletOral1 g/1
Tablet, film coatedOral1 g/1
Granule, for suspensionOral5 g/7.5g
Prices
Unit descriptionCostUnit
Colestid 90 5 gm Packets Box252.5USD box
Colestid 30 5 gm Packets Box81.11USD box
Colestid Flavored 5 gm/7.5 gm Packets3.29USD packet
Colestid 5 g Powder Packet1.04USD packet
Colestid Orange 5 g Powder Packet1.04USD packet
Colestid 1 gm tablet0.86USD tablet
Colestipol hcl 1 gm tablet0.66USD tablet
Colestid 5 gm Granules0.33USD gm
Colestid Flavored 5 gm Granules0.31USD gm
Colestid flavored granules0.3USD g
Colestid 1 g Tablet0.29USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5490987No1993-02-132013-02-13Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
logP-2.206Not Available
Predicted Properties
Not Available
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9221
Blood Brain Barrier+0.8825
Caco-2 permeable-0.5102
P-glycoprotein substrateSubstrate0.6506
P-glycoprotein inhibitor INon-inhibitor0.9435
P-glycoprotein inhibitor IINon-inhibitor0.956
Renal organic cation transporterNon-inhibitor0.6803
CYP450 2C9 substrateNon-substrate0.8931
CYP450 2D6 substrateNon-substrate0.7534
CYP450 3A4 substrateNon-substrate0.7558
CYP450 1A2 substrateNon-inhibitor0.7178
CYP450 2C9 inhibitorNon-inhibitor0.8515
CYP450 2D6 inhibitorNon-inhibitor0.8411
CYP450 2C19 inhibitorNon-inhibitor0.7634
CYP450 3A4 inhibitorNon-inhibitor0.8919
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9404
Ames testAMES toxic0.9093
CarcinogenicityNon-carcinogens0.6451
BiodegradationNot ready biodegradable0.9346
Rat acute toxicity2.5333 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.508
hERG inhibition (predictor II)Non-inhibitor0.7601
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

1. Bile acids
Kind
Group
Organism
Human
Pharmacological action
Yes
Actions
Binder
References
  1. LaRosa JC: The mechanism of action of lipid-lowering drugs. Angiology. 1982 Sep;33(9):562-76. [PubMed:7125296]
  2. 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]
  3. 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 November 14, 2018 12:41