betahistine ๐Ÿถ 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:

PropertyValueReference
S (Water solubility) 38 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

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 116.02 17.06 119 10963 111781 63366159
Parkinsonism 101.21 17.06 45 11037 10394 63467546
Pituitary tumour benign 95.22 17.06 28 11054 1967 63475973
Dizziness 87.24 17.06 215 10867 429710 63048230
Dementia 86.86 17.06 49 11033 18745 63459195
Enthesopathy 76.72 17.06 35 11047 8579 63469361
Hypoglycaemia 71.65 17.06 69 11013 59996 63417944
Multiple drug therapy 71.13 17.06 26 11056 3620 63474320
Fall 66.95 17.06 184 10898 392150 63085790
Syncope 66.89 17.06 92 10990 117293 63360647
Atrioventricular block first degree 66.18 17.06 30 11052 7243 63470697
Hyperprolactinaemia 62.21 17.06 24 11058 3876 63474064
Tenosynovitis 58.47 17.06 34 11048 13761 63464179
Peripheral circulatory failure 56.99 17.06 16 11066 952 63476988
Palpitations 56.31 17.06 83 10999 112687 63365253
Secondary adrenocortical insufficiency 55.04 17.06 17 11065 1411 63476529
Melaena 50.30 17.06 42 11040 30323 63447617
Vertigo 50.23 17.06 57 11025 59830 63418110
Therapy partial responder 47.12 17.06 27 11055 10631 63467309
Oral pain 46.46 17.06 39 11043 28355 63449585
Urinary retention 46.27 17.06 40 11042 30261 63447679
Neuropathy, ataxia, retinitis pigmentosa syndrome 45.67 17.06 8 11074 48 63477892
Sinus bradycardia 44.19 17.06 29 11053 14522 63463418
Drug dependence 42.92 17.06 35 11047 24448 63453492
Neuroglycopenia 42.79 17.06 11 11071 467 63477473
Hypomagnesaemia 42.00 17.06 37 11045 28700 63449240
Confabulation 41.94 17.06 10 11072 310 63477630
Cognitive disorder 41.59 17.06 50 11032 55765 63422175
Dopamine transporter scintigraphy abnormal 41.45 17.06 8 11074 87 63477853
Hyperkalaemia 39.48 17.06 48 11034 54155 63423785
Poor peripheral circulation 39.04 17.06 17 11065 3732 63474208
Metastases to fallopian tube 38.32 17.06 7 11075 55 63477885
Hyperreflexia 37.33 17.06 19 11063 5915 63472025
Osteoporosis 37.33 17.06 48 11034 57290 63420650
Gastric polyps 37.29 17.06 16 11066 3389 63474551
Blood cholesterol decreased 35.38 17.06 11 11071 933 63477007
Initial insomnia 33.82 17.06 18 11064 6139 63471801
Bradykinesia 33.77 17.06 17 11065 5171 63472769
Scleritis 33.27 17.06 16 11066 4412 63473528
Vitamin B12 decreased 33.15 17.06 15 11067 3605 63474335
Perseveration 32.98 17.06 8 11074 267 63477673
Bursitis 32.32 17.06 36 11046 37005 63440935
Apraxia 31.90 17.06 12 11070 1809 63476131
Cerebellar ataxia 31.68 17.06 10 11072 892 63477048
Pain 31.12 17.06 51 11031 740577 62737363
Serum serotonin increased 29.97 17.06 7 11075 198 63477742
Metastases to bladder 29.42 17.06 7 11075 215 63477725
Serotonin syndrome 28.75 17.06 30 11052 28652 63449288
Death 28.39 17.06 15 11067 374366 63103574
Endometrial cancer stage I 28.13 17.06 7 11075 260 63477680
Micturition disorder 28.04 17.06 12 11070 2526 63475414
Crystal arthropathy 26.54 17.06 7 11075 329 63477611
Drug interaction 26.45 17.06 94 10988 229037 63248903
Labelled drug-drug interaction issue 25.82 17.06 9 11073 1092 63476848
Swelling 25.80 17.06 8 11074 275370 63202570
Disorientation 25.63 17.06 33 11049 39419 63438521
Carcinoid tumour 25.48 17.06 7 11075 384 63477556
Stupor 24.90 17.06 13 11069 4262 63473678
Metastases to ovary 24.39 17.06 7 11075 451 63477489
Sinusitis 24.27 17.06 5 11077 226648 63251292
Loss of control of legs 23.73 17.06 9 11073 1387 63476553
Lethargy 23.40 17.06 38 11044 55969 63421971
Dysuria 23.15 17.06 29 11053 33709 63444231
Vision blurred 22.93 17.06 50 11032 91874 63386066
Hypomenorrhoea 22.85 17.06 7 11075 565 63477375
Synovitis 22.51 17.06 3 11079 186915 63291025
Pharyngeal mass 22.40 17.06 6 11076 299 63477641
Motor dysfunction 22.34 17.06 17 11065 10744 63467196
Subcutaneous haematoma 21.92 17.06 9 11073 1709 63476231
Sputum discoloured 21.81 17.06 20 11062 16327 63461613
Urine output decreased 21.51 17.06 17 11065 11353 63466587
Infusion related reaction 21.48 17.06 8 11074 245513 63232427
Rash 21.36 17.06 41 11041 560830 62917110
Peptic ulcer 21.29 17.06 12 11070 4575 63473365
Hypotension 21.24 17.06 99 10983 272505 63205435
Diabetes mellitus inadequate control 21.15 17.06 19 11063 15107 63462833
Adrenal insufficiency 20.25 17.06 20 11062 17895 63460045
Dropped head syndrome 20.14 17.06 5 11077 184 63477756
Arthropathy 19.96 17.06 8 11074 234784 63243156
Endometrial hyperplasia 19.89 17.06 7 11075 873 63477067
Maternal exposure during pregnancy 19.54 17.06 7 11075 220055 63257885
Stomatitis 18.72 17.06 60 11022 138665 63339275
Drug intolerance 18.52 17.06 16 11066 308645 63169295
Nystagmus 17.92 17.06 12 11070 6208 63471732
Overweight 17.92 17.06 10 11072 3741 63474199
Therapeutic product effect incomplete 17.71 17.06 55 11027 125001 63352939
Abdominal discomfort 17.64 17.06 18 11064 320867 63157073
Sinus arrest 17.60 17.06 8 11074 1941 63475999
Exposure during pregnancy 17.57 17.06 3 11079 155544 63322396
Infective exacerbation of chronic obstructive airways disease 17.46 17.06 7 11075 1250 63476690
Lactic acidosis 17.40 17.06 27 11055 38260 63439680

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 144.32 24.53 32 3774 1167 34951958
Soft tissue mass 143.85 24.53 31 3775 988 34952137
Multimorbidity 140.58 24.53 30 3776 912 34952213
Superinfection 115.96 24.53 31 3775 2488 34950637
Transplant failure 109.81 24.53 32 3774 3521 34949604
Immunosuppressant drug level increased 104.84 24.53 35 3771 6020 34947105
Oesophageal carcinoma 97.31 24.53 37 3769 9267 34943858
Inflammatory marker increased 94.80 24.53 31 3775 4997 34948128
Lung consolidation 89.75 24.53 31 3775 5905 34947220
Rales 74.38 24.53 31 3775 9852 34943273
Myocardial ischaemia 69.10 24.53 35 3771 17373 34935752
Cardiomegaly 61.15 24.53 31 3775 15407 34937718
Lower respiratory tract infection 56.83 24.53 38 3768 31599 34921526
Labelled drug-drug interaction medication error 56.27 24.53 29 3777 14910 34938215
Anticoagulation drug level above therapeutic 52.11 24.53 16 3790 2100 34951025
Drug level increased 50.75 24.53 31 3775 22065 34931060
Hypoglycaemia 40.43 24.53 39 3767 54601 34898524
Haemoptysis 40.00 24.53 32 3774 34974 34918151
Productive cough 37.84 24.53 32 3774 37781 34915344
Hepatitis acute 35.24 24.53 17 3789 7584 34945541
Ascites 32.12 24.53 32 3774 46539 34906586
Product prescribing error 30.63 24.53 23 3783 22904 34930221
Dysphagia 29.28 24.53 35 3771 62346 34890779
Swelling 29.01 24.53 29 3777 42337 34910788
Loss of proprioception 28.61 24.53 7 3799 393 34952732
Acute kidney injury 28.46 24.53 85 3721 304903 34648222
Intercepted medication error 26.95 24.53 7 3799 501 34952624
Vascular dementia 26.64 24.53 7 3799 524 34952601
Renal impairment 26.09 24.53 41 3765 94472 34858653
Malaise 25.67 24.53 60 3746 185765 34767360
Pleural effusion 24.79 24.53 37 3769 81509 34871616

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
Soft tissue mass 115.49 16.91 30 14648 1258 79728452
Oesophageal perforation 114.24 16.91 31 14647 1540 79728170
Multimorbidity 107.47 16.91 29 14649 1410 79728300
Hyponatraemia 93.67 16.91 138 14540 177710 79552000
Hypoglycaemia 91.68 16.91 103 14575 101491 79628219
Pituitary tumour benign 90.79 16.91 29 14649 2547 79727163
Dizziness 90.48 16.91 256 14422 526185 79203525
Transplant failure 81.22 16.91 31 14647 4610 79725100
Superinfection 76.05 16.91 30 14648 4872 79724838
Parkinsonism 71.22 16.91 42 14636 16542 79713168
Immunosuppressant drug level increased 70.33 16.91 34 14644 8993 79720717
Oesophageal carcinoma 69.42 16.91 36 14642 11048 79718662
Fall 69.40 16.91 222 14456 487407 79242303
Multiple drug therapy 66.94 16.91 26 14652 4052 79725658
Vertigo 63.94 16.91 71 14607 69011 79660699
Dementia 62.83 16.91 45 14633 24614 79705096
Enthesopathy 59.50 16.91 33 14645 11575 79718135
Inflammatory marker increased 59.10 16.91 32 14646 10708 79719002
Lung consolidation 58.75 16.91 30 14648 8917 79720793
Palpitations 57.80 16.91 92 14586 126518 79603192
Syncope 56.78 16.91 111 14567 179338 79550372
Hyperprolactinaemia 56.75 16.91 24 14654 4652 79725058
Peripheral circulatory failure 53.48 16.91 16 14662 1130 79728580
Atrioventricular block first degree 49.39 16.91 30 14648 12461 79717249
Tenosynovitis 48.14 16.91 32 14646 15522 79714188
Neuropathy, ataxia, retinitis pigmentosa syndrome 45.25 16.91 8 14670 48 79729662
Death 43.79 16.91 25 14653 566489 79163221
Cardiomegaly 43.06 16.91 37 14641 26315 79703395
Neuroglycopenia 42.07 16.91 11 14667 473 79729237
Secondary adrenocortical insufficiency 41.75 16.91 17 14661 2997 79726713
Rales 38.76 16.91 31 14647 19970 79709740
Sinus bradycardia 38.34 16.91 34 14644 25213 79704497
Myocardial ischaemia 38.03 16.91 34 14644 25485 79704225
Metastases to fallopian tube 37.95 16.91 7 14671 55 79729655
Urinary retention 37.31 16.91 49 14629 56581 79673129
Oral pain 37.11 16.91 37 14641 31761 79697949
Confabulation 37.02 16.91 10 14668 488 79729222
Gastric polyps 35.00 16.91 16 14662 3731 79725979
Osteoporosis 32.87 16.91 45 14633 54067 79675643
Hyperkalaemia 32.85 16.91 68 14610 114330 79615380
Anticoagulation drug level above therapeutic 32.38 16.91 15 14663 3605 79726105
Drug interaction 31.96 16.91 156 14522 415027 79314683
Labelled drug-drug interaction medication error 31.95 16.91 32 14646 27618 79702092
Hypomagnesaemia 31.54 16.91 41 14637 46870 79682840
Initial insomnia 30.91 16.91 18 14660 6920 79722790
Cognitive disorder 30.77 16.91 50 14628 69876 79659834
Hyperreflexia 30.25 16.91 19 14659 8366 79721344
Bursitis 30.03 16.91 35 14643 35809 79693901
Endometrial cancer stage I 29.81 16.91 7 14671 192 79729518
Vitamin B12 decreased 29.73 16.91 14 14664 3491 79726219
Perseveration 29.64 16.91 8 14670 389 79729321
Malaise 29.48 16.91 172 14506 489697 79240013
Crystal arthropathy 29.27 16.91 7 14671 208 79729502
Melaena 28.80 16.91 45 14633 60845 79668865
Blood cholesterol decreased 28.32 16.91 11 14667 1714 79727996
Vascular dementia 27.33 16.91 9 14669 870 79728840
Metastases to bladder 27.26 16.91 7 14671 280 79729430
Drug dependence 26.43 16.91 35 14643 40734 79688976
Serum serotonin increased 26.29 16.91 7 14671 323 79729387
Apraxia 26.02 16.91 12 14666 2855 79726855
Bradykinesia 25.98 16.91 17 14661 8026 79721684
Metastases to ovary 25.75 16.91 7 14671 350 79729360
Hypomenorrhoea 24.56 16.91 7 14671 417 79729293
Drug level increased 24.11 16.91 33 14645 39618 79690092
Cerebellar ataxia 23.78 16.91 10 14668 1911 79727799
Loss of control of legs 23.56 16.91 10 14668 1955 79727755
Labelled drug-drug interaction issue 23.16 16.91 9 14669 1404 79728306
Lethargy 22.95 16.91 48 14630 81244 79648466
Off label use 22.83 16.91 88 14590 907127 78822583
Carcinoid tumour 22.67 16.91 7 14671 550 79729160
Micturition disorder 22.16 16.91 12 14666 4016 79725694
Endometrial hyperplasia 21.76 16.91 7 14671 629 79729081
Vision blurred 21.59 16.91 55 14623 105843 79623867
Renal impairment 21.57 16.91 71 14607 157712 79571998
Pharyngeal mass 21.48 16.91 6 14672 332 79729378
Disease progression 21.41 16.91 4 14674 184358 79545352
Stupor 20.93 16.91 14 14664 6858 79722852
Adrenal insufficiency 20.89 16.91 26 14652 28461 79701249
Confusional state 20.63 16.91 114 14564 317883 79411827
Loss of proprioception 20.30 16.91 7 14671 779 79728931
Completed suicide 20.19 16.91 10 14668 245757 79483953
Product prescribing error 19.65 16.91 32 14646 44781 79684929
Sputum discoloured 19.51 16.91 22 14656 21721 79707989
Sinusitis 19.27 16.91 6 14672 195495 79534215
Lentigo maligna 18.47 16.91 6 14672 556 79729154
Constipation 18.04 16.91 101 14577 282949 79446761
Drug abuse 17.92 16.91 4 14674 162687 79567023
Peptic ulcer 17.34 16.91 12 14666 6211 79723499
Subcutaneous haematoma 17.33 16.91 9 14669 2768 79726942
Dropped head syndrome 16.94 16.91 5 14673 337 79729373
Motor dysfunction 16.92 16.91 17 14661 14716 79714994

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 | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Mรฉniรจre's disease indication 13445001 DOID:9849




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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
322052003 SNOMEDCT_US
350631001 SNOMEDCT_US
418067008 SNOMEDCT_US
708177006 SNOMEDCT_US
4027336 VANDF
4033254 VANDF
000702 NDDF
004531 NDDF
005313 NDDF
006923 NDDF

Pharmaceutical products:

None