colesevelam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4405 182815-43-6

Description:

MoleculeDescription

Synonyms:

  • cholestagel
  • colesevelam
  • colesevelam hydrochloride
  • WELCHOL
  • colesevelam HCl
An allylamine derivative that binds BILE ACIDS in the intestine and is used as an ANTICHOLESTEREMIC AGENT in the treatment of HYPERCHOLESTEROLEMIA and HYPERLIPIDEMIAS.
  • Molecular weight:
  • Formula: C12H26Cl5N2O(C5H12N)a(C15H32N)c(C14H32ClN2)d
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
3.75 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 26, 2000 FDA DAIICHI SANKYO

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
No adverse event 598.43 18.06 213 6476 34018 46645355
Off label use 290.53 18.06 311 6378 379530 46299843
Product administration error 102.56 18.06 52 6637 19629 46659744
Incorrect dose administered 77.63 18.06 59 6630 45491 46633882
Myalgia 58.90 18.06 80 6609 123008 46556365
Blood cholesterol increased 51.51 18.06 44 6645 39969 46639404
Anembryonic gestation 33.12 18.06 9 6680 580 46678793
Low density lipoprotein increased 31.66 18.06 16 6673 5984 46673389
Constipation 31.60 18.06 74 6615 174023 46505350
Bile acid malabsorption 29.95 18.06 6 6683 99 46679274
Muscle spasms 26.44 18.06 56 6633 123057 46556316
Flatulence 24.14 18.06 25 6664 28853 46650520
Dysphagia 21.22 18.06 39 6650 77273 46602100
Diarrhoea 20.81 18.06 144 6545 559458 46119915
Lipids increased 20.31 18.06 7 6682 1001 46678372

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
No adverse event 259.73 21.56 86 2660 17333 29932399
Off label use 133.63 21.56 137 2609 249153 29700579
Cerebrovascular accident 51.83 21.56 50 2696 83427 29866305
Pancreatitis 41.50 21.56 31 2715 36459 29913273
Product administration error 41.32 21.56 22 2724 14355 29935377
Myalgia 35.05 21.56 39 2707 76628 29873104
Incorrect dose administered 25.51 21.56 22 2724 31664 29918068
Pulmonary renal syndrome 23.76 21.56 5 2741 169 29949563
Blood cholesterol increased 22.88 21.56 16 2730 16954 29932778

Pharmacologic Action:

SourceCodeDescription
ATC C10AC04 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
Bile acid sequestrants
FDA MoA N0000175365 Bile-acid Binding Activity
MeSH PA D000924 Anticholesteremic Agents
MeSH PA D000963 Antimetabolites
MeSH PA D000960 Hypolipidemic Agents
MeSH PA D057847 Lipid Regulating Agents
FDA EPC N0000180292 Bile Acid Sequestrant
CHEBI has role CHEBI:35821 hypocholesteremic agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypercholesterolemia indication 13644009
Type 2 Diabetes Mellitus Treatment Adjunct indication
Dysphasia contraindication 20301004
Vitamin D deficiency contraindication 34713006
Vitamin K deficiency contraindication 52675005 DOID:11249
Vitamin E deficiency contraindication 54137008
Vitamin A deficiency contraindication 72000004
Intestinal obstruction contraindication 81060008 DOID:8437
Chronic idiopathic constipation contraindication 82934008
Gastrointestinal obstruction contraindication 126765001
Gastroparesis contraindication 235675006
Esophageal dysmotility contraindication 266434009 DOID:9192
Hypertriglyceridemia contraindication 302870006
Operation on gastrointestinal tract contraindication 386621005
Gastrointestinal hypomotility contraindication 421807004
Predisposition To Hypertriglyceridemia contraindication
Esophageal Obstruction contraindication

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
bile acids Metabolite CHELATING AGENT DRUG LABEL DRUG LABEL

External reference:

IDSource
D03582 KEGG_DRUG
4021227 VUID
N0000148671 NUI
182815-44-7 SECONDARY_CAS_RN
4021227 VANDF
4029706 VANDF
C1160749 UMLSCUI
CHEBI:59594 CHEBI
CHEMBL1201473 ChEMBL_ID
CHEMBL1201677 ChEMBL_ID
DB00930 DRUGBANK_ID
D000069472 MESH_DESCRIPTOR_UI
160051 PUBCHEM_CID
7621 INN_ID
1XU104G55N UNII
141625 RXNORM
15635 MMSL
26906 MMSL
280036 MMSL
37702 MMSL
d04695 MMSL
008852 NDDF
008853 NDDF
127965004 SNOMEDCT_US
441851004 SNOMEDCT_US
442510005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Colesevelam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-1320 TABLET, COATED 625 mg ORAL ANDA 27 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 21695-779 FOR SUSPENSION 3.75 g ORAL NDA 28 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 21695-781 TABLET, FILM COATED 625 mg ORAL NDA 28 sections
Colesevelam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 27808-190 TABLET 625 mg ORAL ANDA 25 sections
Colesevelam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-147 TABLET, COATED 625 mg ORAL ANDA 28 sections
Colesevelam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 43598-230 TABLET 625 mg ORAL ANDA 27 sections
Colesevelam HCL Human Prescription Drug Label 1 50090-4371 TABLET, FILM COATED 625 mg ORAL ANDA 29 sections
Colesevelam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 51407-159 TABLET 625 mg ORAL ANDA 27 sections
Colesevelam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 51660-995 POWDER, FOR SUSPENSION 3.75 g ORAL NDA 32 sections
Colesevelam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 51660-996 TABLET, FILM COATED 625 mg ORAL NDA 32 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 54868-4474 TABLET, FILM COATED 625 mg ORAL NDA 29 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 54868-6136 FOR SUSPENSION 3.75 g ORAL NDA 29 sections
Colesevelam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60687-385 TABLET, COATED 625 mg ORAL ANDA 28 sections
COLESEVELAM HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 63629-2446 TABLET, FILM COATED 625 mg ORAL ANDA 28 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 65597-701 TABLET, FILM COATED 625 mg ORAL NDA 32 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 65597-902 FOR SUSPENSION 3.75 g ORAL NDA 32 sections
Colesevelam HCL Human Prescription Drug Label 1 67877-506 TABLET, FILM COATED 625 mg ORAL ANDA 28 sections
Colesevelam hydrochloride Human Prescription Drug Label 1 67877-523 POWDER, FOR SUSPENSION 3.75 g ORAL ANDA 28 sections
Welchol HUMAN PRESCRIPTION DRUG LABEL 1 68151-4362 TABLET, FILM COATED 625 mg ORAL NDA 27 sections
Colesevelam HUMAN PRESCRIPTION DRUG LABEL 1 68382-619 TABLET, FILM COATED 625 mg ORAL ANDA 26 sections
colesevelam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68462-433 TABLET, FILM COATED 625 mg ORAL ANDA 26 sections
Colesevelam Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68462-620 POWDER, FOR SUSPENSION 3.75 g ORAL ANDA 26 sections
COLESEVELAM HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 69452-158 TABLET, FILM COATED 625 mg ORAL ANDA 29 sections
COLESEVELAM HUMAN PRESCRIPTION DRUG LABEL 1 70771-1368 TABLET 625 mg ORAL ANDA 1 sections
colesevelam hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 75834-152 TABLET, COATED 625 mg ORAL ANDA 18 sections