betahistine indications/contra

Stem definitionDrug idCAS RN
346 5638-76-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • betahistine dihydrochloride
  • betahistine hydrochloride
  • betahistine methanesulfonate
  • betahistine dihydrobromide
  • betahistine
  • beta-histine
  • betahistine mesilate
  • merislon
  • betahistine mesylate
A histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
  • Molecular weight: 136.20
  • Formula: C8H12N2
  • CLOGP: 0.08
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 24.92
  • ALOGS: -0.44
  • ROTB: 3

Drug dosage:

DoseUnitRoute
24 mg O

Approvals:

None

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
Sputum discoloured 78.30 63.82 12 110 1257 3384480
Thrombocytosis 77.72 63.82 12 110 1320 3384417

Pharmacologic Action:

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SourceCodeDescription
ATC N07CA01 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
ANTIVERTIGO PREPARATIONS
Antivertigo preparations
CHEBI has role CHEBI:71173 H1-receptor agonist
CHEBI has role CHEBI:35620 vasodilator agent
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018494 Histamine Agents
MeSH PA D017442 Histamine Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Ménière's disease indication 13445001 DOID:9849

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.53 Basic
pKa2 3.77 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
Histamine H3 receptor GPCR INVERSE AGONIST EC50 9.52 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Histamine H3 receptor GPCR Ki 5.69 CHEMBL

External reference:

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IDSource
CHEBI:35677 CHEBI
4027336 VUID
N0000179397 NUI
C0282071 UMLSCUI
D01592 KEGG_DRUG
49K58SMZ7U UNII
5579-84-0 SECONDARY_CAS_RN
CHEMBL24441 ChEMBL_ID
418067008 SNOMEDCT_US
N0000167237 NDFRT
004531 NDDF
1511 RXNORM
350631001 SNOMEDCT_US
4033254 VANDF
N0000190653 NDFRT
006923 NDDF
CHEMBL1446813 ChEMBL_ID
DB06698 DRUGBANK_ID
1502 INN_ID
D001621 MESH_DESCRIPTOR_UI
2366 PUBCHEM_CID

Pharmaceutical products:

None