betahistine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

ADMET properties:

None

Approvals:

None

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
Hyponatraemia 96.04 17.06 103 9263 96036 50499722
Pituitary tumour benign 92.32 17.06 27 9339 1754 50594004
Parkinsonism 83.20 17.06 38 9328 8809 50586949
Enthesopathy 80.81 17.06 35 9331 7158 50588600
Dizziness 78.12 17.06 187 9179 346182 50249576
Dementia 69.79 17.06 41 9325 15956 50579802
Tenosynovitis 65.11 17.06 34 9332 10531 50585227
Palpitations 60.86 17.06 81 9285 94425 50501333
Hyperprolactinaemia 60.66 17.06 23 9343 3342 50592416
Fall 56.15 17.06 162 9204 334770 50260988
Secondary adrenocortical insufficiency 53.44 17.06 16 9350 1127 50594631
Multiple drug therapy 52.87 17.06 18 9348 1919 50593839
Oral pain 48.78 17.06 39 9327 24994 50570764
Syncope 46.96 17.06 75 9291 102927 50492831
Bursitis 46.39 17.06 36 9330 22099 50573659
Hypoglycaemia 45.85 17.06 53 9313 53528 50542230
Sinus bradycardia 45.26 17.06 29 9337 13154 50582604
Neuropathy, ataxia, retinitis pigmentosa syndrome 45.20 17.06 8 9358 48 50595710
Hypomagnesaemia 44.96 17.06 36 9330 23120 50572638
Therapy partial responder 42.87 17.06 22 9344 6569 50589189
Atrioventricular block first degree 41.21 17.06 21 9345 6180 50589578
Poor peripheral circulation 40.64 17.06 17 9349 3191 50592567
Vertigo 38.96 17.06 48 9318 51784 50543974
Hyperreflexia 38.94 17.06 19 9347 5099 50590659
Scleritis 37.22 17.06 16 9350 3211 50592547
Confabulation 36.97 17.06 9 9357 287 50595471
Drug dependence 36.83 17.06 30 9336 19729 50576029
Melaena 36.38 17.06 34 9332 26830 50568928
Vitamin B12 decreased 35.93 17.06 15 9351 2800 50592958
Cognitive disorder 35.01 17.06 42 9324 44081 50551677
Apraxia 33.14 17.06 12 9354 1533 50594225
Perseveration 32.87 17.06 8 9358 255 50595503
Blood cholesterol decreased 28.39 17.06 9 9357 767 50594991
Osteoporosis 28.14 17.06 38 9328 44841 50550917
Stomatitis 27.46 17.06 59 9307 101285 50494473
Cerebellar ataxia 27.30 17.06 9 9357 869 50594889
Metastases to fallopian tube 27.11 17.06 5 9361 39 50595719
Disorientation 26.88 17.06 33 9333 35451 50560307
Hyperkalaemia 26.10 17.06 38 9328 48051 50547707
Death 25.91 17.06 14 9352 325365 50270393
Therapeutic product effect incomplete 25.62 17.06 54 9312 91461 50504297
Pain 24.20 17.06 44 9322 578859 50016899
Loss of control of legs 23.83 17.06 9 9357 1292 50594466
Drug interaction 22.89 17.06 85 9281 199536 50396222
Pharyngeal mass 22.69 17.06 6 9360 268 50595490
Lethargy 22.50 17.06 36 9330 49396 50546362
Sputum discoloured 22.19 17.06 19 9347 13376 50582382
Initial insomnia 22.01 17.06 13 9353 5102 50590656
Vision blurred 21.54 17.06 46 9320 78601 50517157
Urinary retention 20.88 17.06 25 9341 26165 50569593
Serum serotonin increased 20.35 17.06 5 9361 166 50595592
Metastases to bladder 20.12 17.06 5 9361 174 50595584
Lactic acidosis 19.04 17.06 27 9339 33328 50562430
Endometrial cancer stage I 18.94 17.06 5 9361 222 50595536
Swelling 18.54 17.06 7 9359 200865 50394893
Crystal arthropathy 18.44 17.06 5 9361 246 50595512
Peripheral circulatory failure 18.44 17.06 6 9360 556 50595202
Sinus arrest 18.21 17.06 8 9358 1690 50594068
Infective exacerbation of chronic obstructive airways disease 17.92 17.06 7 9359 1101 50594657
Urine output decreased 17.71 17.06 15 9351 10406 50585352
Carcinoid tumour 17.43 17.06 5 9361 303 50595455
Sinusitis 17.39 17.06 5 9361 170553 50425205
Eye pruritus 17.23 17.06 16 9350 12518 50583240

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
Oesophageal perforation 81.57 24.40 18 2794 737 29570978
Soft tissue mass 78.97 24.40 17 2795 619 29571096
Multimorbidity 75.53 24.40 16 2796 539 29571176
Oesophageal carcinoma 68.93 24.40 23 2789 4524 29567191
Immunosuppressant drug level increased 67.87 24.40 23 2789 4742 29566973
Transplant failure 62.05 24.40 19 2793 2837 29568878
Superinfection 59.62 24.40 17 2795 1984 29569731
Anticoagulation drug level above therapeutic 56.55 24.40 16 2796 1815 29569900
Inflammatory marker increased 49.48 24.40 17 2795 3650 29568065
Lung consolidation 44.19 24.40 17 2795 5026 29566689
Hepatitis acute 40.11 24.40 17 2795 6445 29565270
Rales 37.65 24.40 17 2795 7493 29564222
Myocardial ischaemia 35.68 24.40 21 2791 16007 29555708
Drug level increased 32.60 24.40 21 2791 18766 29552949
Lower respiratory tract infection 30.45 24.40 23 2789 26479 29545236
Loss of proprioception 30.02 24.40 7 2805 367 29571348
Intercepted medication error 28.40 24.40 7 2805 465 29571250
Vascular dementia 28.13 24.40 7 2805 484 29571231
Cardiomegaly 27.93 24.40 17 2795 13759 29557956
Acute kidney injury 27.04 24.40 70 2742 265197 29306518
Product prescribing error 26.14 24.40 18 2794 17958 29553757
Atrial thrombosis 25.95 24.40 9 2803 1984 29569731
Labelled drug-drug interaction medication error 24.64 24.40 15 2797 12144 29559571

FDA Adverse Event Reporting System (Geriatric)

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
Dizziness 89.47 16.45 227 11864 429936 64056705
Pituitary tumour benign 89.40 16.45 28 12063 2265 64484376
Hyponatraemia 82.16 16.45 119 11972 148220 64338421
Palpitations 67.04 16.45 90 12001 104398 64382243
Enthesopathy 64.71 16.45 33 12058 9605 64477036
Oesophageal perforation 63.65 16.45 18 12073 1023 64485618
Soft tissue mass 61.43 16.45 17 12074 892 64485749
Fall 57.48 16.45 190 11901 416636 64070005
Parkinsonism 57.48 16.45 35 12056 14338 64472303
Hyperprolactinaemia 56.15 16.45 23 12068 4042 64482599
Tenosynovitis 55.66 16.45 32 12059 11801 64474840
Multimorbidity 55.16 16.45 16 12075 996 64485645
Oesophageal carcinoma 52.73 16.45 23 12068 4720 64481921
Vertigo 52.61 16.45 60 12031 58951 64427690
Dementia 50.25 16.45 37 12054 20729 64465912
Multiple drug therapy 49.97 16.45 18 12073 2236 64484405
Neuropathy, ataxia, retinitis pigmentosa syndrome 45.10 16.45 8 12083 48 64486593
Bursitis 44.74 16.45 35 12056 21450 64465191
Transplant failure 44.14 16.45 19 12072 3775 64482866
Hypoglycaemia 43.83 16.45 68 12023 89824 64396817
Immunosuppressant drug level increased 43.41 16.45 23 12068 7236 64479405
Secondary adrenocortical insufficiency 41.96 16.45 16 12075 2329 64484312
Oral pain 41.13 16.45 37 12054 27456 64459185
Syncope 41.06 16.45 91 12000 157544 64329097
Death 37.57 16.45 22 12069 482683 64003958
Superinfection 37.29 16.45 17 12074 3869 64482772
Hypomagnesaemia 36.73 16.45 40 12051 37336 64449305
Sinus bradycardia 34.62 16.45 31 12060 22862 64463779
Anticoagulation drug level above therapeutic 34.61 16.45 15 12076 3030 64483611
Confabulation 32.94 16.45 9 12082 450 64486191
Vitamin B12 decreased 32.92 16.45 14 12077 2701 64483940
Hyperreflexia 32.74 16.45 19 12072 7129 64479512
Atrioventricular block first degree 30.28 16.45 21 12070 10713 64475928
Perseveration 29.80 16.45 8 12083 374 64486267
Inflammatory marker increased 29.80 16.45 19 12072 8432 64478209
Vascular dementia 27.72 16.45 9 12082 817 64485824
Apraxia 27.41 16.45 12 12079 2483 64484158
Cognitive disorder 27.29 16.45 42 12049 55045 64431596
Metastases to fallopian tube 27.05 16.45 5 12086 39 64486602
Malaise 26.48 16.45 145 11946 396102 64090539
Lung consolidation 26.26 16.45 17 12074 7741 64478900
Drug interaction 25.20 16.45 134 11957 361949 64124692
Osteoporosis 25.07 16.45 35 12056 42045 64444596
Lethargy 24.91 16.45 47 12044 72547 64414094
Loss of control of legs 24.79 16.45 10 12081 1689 64484952
Hyperkalaemia 23.67 16.45 56 12035 101073 64385568
Drug dependence 23.35 16.45 30 12061 33282 64453359
Pharyngeal mass 22.51 16.45 6 12085 273 64486368
Blood cholesterol decreased 22.47 16.45 9 12082 1493 64485148
Vision blurred 22.22 16.45 51 12040 90265 64396376
Stomatitis 21.76 16.45 57 12034 109548 64377093
Melaena 21.34 16.45 37 12054 53511 64433130
Loss of proprioception 21.15 16.45 7 12084 675 64485966
Cerebellar ataxia 20.98 16.45 9 12082 1774 64484867
Cardiomegaly 20.95 16.45 24 12067 23660 64462981
Sputum discoloured 20.92 16.45 21 12070 17835 64468806
Endometrial cancer stage I 20.61 16.45 5 12086 155 64486486
Initial insomnia 20.34 16.45 13 12078 5791 64480850
Pain 19.67 16.45 47 12044 553464 63933177
Crystal arthropathy 19.66 16.45 5 12086 189 64486452
Urinary retention 19.61 16.45 34 12057 49167 64437474
Metastases to bladder 18.79 16.45 5 12086 226 64486415
Metastases to ovary 18.17 16.45 5 12086 257 64486384
Rales 18.01 16.45 18 12073 15211 64471430
Serum serotonin increased 17.87 16.45 5 12086 273 64486368
Antibiotic level above therapeutic 17.85 16.45 6 12085 607 64486034
Completed suicide 17.74 16.45 10 12081 224404 64262237
Peripheral circulatory failure 17.14 16.45 6 12085 685 64485956
Hypomenorrhoea 16.65 16.45 5 12086 351 64486290
Disorientation 16.55 16.45 34 12057 55794 64430847

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07CA01 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
ANTIVERTIGO PREPARATIONS
Antivertigo preparations
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
CHEBI has role CHEBI:35620 vasodilator agents
CHEBI has role CHEBI:71173 H1-receptor agonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ménière's disease indication 13445001 DOID:9849




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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:

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:

IDSource
4027336 VUID
N0000179397 NUI
D01592 KEGG_DRUG
5579-84-0 SECONDARY_CAS_RN
1511 RXNORM
C0005301 UMLSCUI
CHEBI:35677 CHEBI
CHEMBL4298035 ChEMBL_ID
CHEMBL24441 ChEMBL_ID
2366 PUBCHEM_CID
DB06698 DRUGBANK_ID
CHEMBL1446813 ChEMBL_ID
D001621 MESH_DESCRIPTOR_UI
1502 INN_ID
11937 IUPHAR_LIGAND_ID
54856-23-4 SECONDARY_CAS_RN
X32KK4201D UNII
NOCODE MMSL
000702 NDDF
004531 NDDF
005313 NDDF
006923 NDDF
4027336 VANDF
4033254 VANDF
322052003 SNOMEDCT_US
350631001 SNOMEDCT_US
418067008 SNOMEDCT_US
708177006 SNOMEDCT_US

Pharmaceutical products:

None