alosetron indications/contra

Stem definitionDrug idCAS RN
serotonin receptor antagonists (5-HT3) 129 122852-42-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • alosetron
  • alosetron hydrochloride
  • alosetron HCl
  • alosetron monohydrochloride
  • GR68755
  • Molecular weight: 294.36
  • Formula: C17H18N4O
  • CLOGP: 1.74
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 53.92
  • ALOGS: -2.83
  • ROTB: 2

Drug dosage:

DoseUnitRoute
1 mg O

Approvals:

DateAgencyCompanyOrphan
Feb. 9, 2000 FDA PROMETHEUS LABS

FDA Adverse Event Reporting System

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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
Colitis ischaemic 226.31 78.55 31 65 2157 3383606
Constipation 88.34 78.55 21 75 30791 3354972

Pharmacologic Action:

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SourceCodeDescription
ATC A03AE01 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
Serotonin receptor antagonists
FDA MoA N0000175817 Serotonin 3 Receptor Antagonists
FDA EPC N0000175818 Serotonin-3 Receptor Antagonist
CHEBI has role CHEBI:55324 gastrointestinal drug
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:50919 antiemetic
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D012702 Serotonin Antagonists

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Irritable bowel syndrome with diarrhea indication 197125005
Rectal hemorrhage contraindication 12063002
Constipation contraindication 14760008 DOID:2089
Acute gastric ulcer with perforation contraindication 19850005
Toxic megacolon contraindication 28536002 DOID:1770
Crohn's disease contraindication 34000006
Hepatic failure contraindication 59927004
Thrombophlebitis contraindication 64156001 DOID:3875
Colitis contraindication 64226004 DOID:0060180
Ulcerative colitis contraindication 64766004 DOID:8577
Vascular insufficiency of intestine contraindication 82196007
Gastrointestinal obstruction contraindication 126765001
Thrombophilia contraindication 234467004 DOID:2452
Disease of liver contraindication 235856003 DOID:409
Diverticulitis of gastrointestinal tract contraindication 271366000
Adhesion of Gastrointestinal Tract contraindication

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.33 acidic
pKa2 6.11 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 3A Ion channel ANTAGONIST Ki 9.30 CHEMBL CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 7.19 DRUG MATRIX
Cytochrome P450 1A2 Enzyme IC50 6.22 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.64 CHEMBL

External reference:

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IDSource
2296 IUPHAR_LIGAND_ID
4021194 VUID
N0000148640 NUI
C0291772 UMLSCUI
D02829 KEGG_DRUG
13Z9HTH115 UNII
6906 INN_ID
122852-69-1 SECONDARY_CAS_RN
DB00969 DRUGBANK_ID
2099 PUBCHEM_CID
4021194 VANDF
N0000148640 NDFRT
N0000005874 NDFRT
008063 NDDF
d04516 MMSL
85248 RXNORM
116509006 SNOMEDCT_US
409148009 SNOMEDCT_US
CHEMBL1110 ChEMBL_ID
CHEBI:253342 CHEBI
CHEMBL1200885 ChEMBL_ID
C090840 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0295 TABLET 0.50 mg ORAL ANDA 20 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0296 TABLET 1 mg ORAL ANDA 20 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-123 TABLET, FILM COATED 0.50 mg ORAL ANDA 19 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42291-124 TABLET, FILM COATED 1 mg ORAL ANDA 19 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 45963-479 TABLET 0.50 mg ORAL NDA 20 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 45963-480 TABLET 1 mg ORAL NDA 20 sections
ALOSETRON HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 49884-819 TABLET 0.50 mg ORAL ANDA 20 sections
ALOSETRON HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 49884-820 TABLET 1 mg ORAL ANDA 20 sections
LOTRONEX HUMAN PRESCRIPTION DRUG LABEL 1 54766-894 TABLET 0.50 mg ORAL NDA 20 sections
LOTRONEX HUMAN PRESCRIPTION DRUG LABEL 1 54766-895 TABLET 1 mg ORAL NDA 20 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 65162-248 TABLET, FILM COATED 0.50 mg ORAL ANDA 18 sections
Alosetron Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 65162-249 TABLET, FILM COATED 1 mg ORAL ANDA 18 sections
LOTRONEX HUMAN PRESCRIPTION DRUG LABEL 1 65483-894 TABLET 0.50 mg ORAL NDA 20 sections
LOTRONEX HUMAN PRESCRIPTION DRUG LABEL 1 65483-895 TABLET 1 mg ORAL NDA 20 sections