Identification

Summary

Colesevelam is a bile acid sequestrant used to lower LDL-C in adults with hyperlipidemia and pediatric patients with heterozygous familial hypercholesterolemia, and to improve glycemic control in type 2 diabetes.

Brand Names
Cholestagel, Lodalis, Welchol
Generic Name
Colesevelam
DrugBank Accession Number
DB00930
Background

Colesevelam is a bile acid sequestrant. Colesevelam is used with exercise and diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in the blood. It works by binding bile acids in the intestine. Bile acids are made when cholesterol is broken down in the body. Removing these bile acids helps to lower blood cholesterol.

Type
Small Molecule
Groups
Approved
Synonyms
  • Colesevelam

Pharmacology

Indication

For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa).

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Colesevelam is a high capacity bile-acid binding molecule. Colesevelam binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associated with LDL-C) are associated with an increased risk of atherosclerosis in humans. Similarly, decreased levels of high-density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the levels of total-C and LDL-C, and inversely with the level of HDL-C. The combination of colesevelam and an HMG-CoA reductase inhibitor is effective in further lowering serum total-C and LDL-C levels beyond that achieved by either agent alone.

Mechanism of action

Colesevelam binds bile acids in the intestine and prevents their reabsorption. Colesevelam is not absorbed itself. The depletion of bile acid causes the upregulation of cholesterol 7-alpha-hydroxylase and conversion of cholesterol to bile acid. this increases the production and activity of hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase in the liver as well as an increase in the number of low density lipoprotein (LDL) receptors. This process clears LDL cholesterol from the blood.

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
Humans
Absorption

Not hydrolyzed by digestive enzymes and is not absorbed.

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

Excretion: In 16 healthy volunteers, an average of 0.05% of administered radioactivity from a single 14C-labeled colesevelam hydrochloride dose was excreted in the urine.

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colesevelam is not absorbed, the risk of systemic toxicity is low. Doses in excess of 4.5 g per day have not been tested.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

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.
DrugInteraction
AceclofenacColesevelam can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcemetacinColesevelam can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcenocoumarolColesevelam can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetazolamideColesevelam can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetyl sulfisoxazoleColesevelam can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetyldigitoxinColesevelam can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylsalicylic acidColesevelam can cause a decrease in the absorption of Acetylsalicylic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlclofenacColesevelam can cause a decrease in the absorption of Alclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlfacalcidolThe serum concentration of Alfacalcidol can be decreased when it is combined with Colesevelam.
AminophenazoneColesevelam can cause a decrease in the absorption of Aminophenazone resulting in a reduced serum concentration and potentially a decrease in efficacy.
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Food Interactions
  • Drink plenty of fluids.
  • Take with food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Colesevelam hydrochlorideP4SG24WI5Q182815-44-7VTAKZNRDSPNOAU-UHFFFAOYSA-M
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CholestagelTablet, film coated625 mgOralCheplapharm Arzneimittel Gmb H2016-09-08Not applicableEU flag
CholestagelTablet, film coated625 mgOralCheplapharm Arzneimittel Gmb H2016-09-08Not applicableEU flag
CholestagelTablet, film coated625 mgOralCheplapharm Arzneimittel Gmb H2016-09-08Not applicableEU flag
CholestagelTablet, film coated625 mgOralCheplapharm Arzneimittel Gmb H2016-09-08Not applicableEU flag
Colesevelam hydrochlorideTablet, film coated625 mg/1OralOhm Laboratories, Inc.2018-05-232023-11-30US flag
Colesevelam HydrochlorideFor suspension3.75 g/1OralCosette Pharmaceuticals, Inc.2022-08-01Not applicableUS flag
Colesevelam HydrochlorideTablet, film coated625 mg/1OralCosette Pharmaceuticals, Inc.2022-08-01Not applicableUS flag
Colesevelam hydrochloridePowder, for suspension3.75 g/1OralOhm Laboratories, Inc.2018-07-172023-11-30US flag
LodalisTablet625 mgOralBausch Health, Canada Inc.2012-02-06Not applicableCanada flag
LodalisPowder, for suspension3.75 g / sachetOralBausch Health, Canada Inc.2015-04-02Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-colesevelamTablet625 mgOralApotex Corporation2020-07-23Not applicableCanada flag
ColesevelamTablet, film coated625 mg/1OralZydus Pharmaceuticals (USA) Inc.2019-10-11Not applicableUS flag
ColesevelamTablet625 mg/1OralZydus Lifesciences Limited2019-10-11Not applicableUS flag
Colesevelam HCLTablet, film coated625 mg/1OralA-S Medication Solutions2018-10-06Not applicableUS flag
Colesevelam HCLTablet, film coated625 mg/1Oralbryant ranch prepack2018-10-06Not applicableUS flag
Colesevelam HCLTablet, film coated625 mg/1OralAscend Laboratories, LLC2018-10-06Not applicableUS flag
Colesevelam HydrochlorideTablet625 mg/1OralDr.Reddys Laboratories Inc2018-10-05Not applicableUS flag
Colesevelam HydrochlorideTablet, coated625 mg/1OralAmerican Health Packaging2018-07-19Not applicableUS flag
Colesevelam HydrochlorideTablet625 mg/1OralGolden State Medical Supply2018-10-05Not applicableUS flag
Colesevelam HydrochlorideTablet, film coated625 mg/1OralAmerican Health Packaging2021-11-01Not applicableUS flag

Categories

ATC Codes
C10AC04 — Colesevelam
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
1XU104G55N
CAS number
182815-43-6
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
Not Available
PubChem Substance
46505437
RxNav
141626
PharmGKB
PA449095
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Colesevelam
FDA label
Download (130 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceBileacid Malabsorption2
4CompletedBasic ScienceType 2 Diabetes Mellitus2
4CompletedOtherAtherosclerosis / Carotid Artery Diseases / Coronary Artery Disease (CAD)1
4CompletedPreventionDyslipidemia / Hyperglycemia / Hyperlipidemias1
4CompletedTreatmentBileacid Malabsorption / Chronic Functional Diarrhea1
4CompletedTreatmentDiarrhoea Predominant Irritable Bowel Syndrome1
4CompletedTreatmentDyslipidemia / Hyperlipidemias1
4CompletedTreatmentHealthy Subjects (HS)1
4CompletedTreatmentHigh Cholesterol5
4CompletedTreatmentHigh Cholesterol / Hyperlipidemia, Familial Combined1

Pharmacoeconomics

Manufacturers
  • Daiichi sankyo inc
Packagers
  • Daiichi Sankyo
  • Patheon Inc.
  • Physicians Total Care Inc.
  • Quality Care
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
Dosage Forms
FormRouteStrength
Tablet, film coatedOral625 mg
Powder, for suspensionOral1.875 g/1
Powder, for suspensionOral3.75 g/1
TabletOral625 mg/1
Tablet, coatedOral625 mg/1
PowderOral
Tablet, film coatedOral
Powder, for suspensionOral3.75 g / sachet
TabletOral625 mg
Bar, chewableOral3.75 g/1
For suspensionOral1.875 g/1
For suspensionOral3.75 g/1
Tablet, film coatedOral625 mg/1
Prices
Unit descriptionCostUnit
Welchol 625 mg tablet1.96USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5679717No1997-10-212014-04-29US flag
US7229613Yes2007-06-122022-10-17US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

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1. Bile acids
Kind
Group
Organism
Humans
Pharmacological action
Yes
Actions
Binder
References
  1. Levy P, Jellinger PS: The potential role of colesevelam in the management of prediabetes and type 2 diabetes mellitus. Postgrad Med. 2010 May;122(3Suppl):1-8. doi: 10.3810/pgm.2010.05.2168. [Article]
  2. Staels B: A review of bile acid sequestrants: potential mechanism(s) for glucose-lowering effects in type 2 diabetes mellitus. Postgrad Med. 2009 May;121(3 Suppl 1):25-30. doi: 10.3810/pgm.2009.05.suppl53.290. [Article]
  3. Corsini A, Windler E, Farnier M: Colesevelam hydrochloride: usefulness of a specifically engineered bile acid sequestrant for lowering LDL-cholesterol. Eur J Cardiovasc Prev Rehabil. 2009 Feb;16(1):1-9. doi: 10.1097/HJR.0b013e32831215db. [Article]
  4. Steinmetz KL, Schonder KS: Colesevelam: potential uses for the newest bile resin. Cardiovasc Drug Rev. 2005 Spring;23(1):15-30. [Article]
  5. Melian EB, Plosker GL: Colesevelam. Am J Cardiovasc Drugs. 2001;1(2):141-6; discussion 147-8. [Article]

Drug created at June 13, 2005 13:24 / Updated at September 27, 2022 08:31