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

Stem definition	Drug id	CAS RN
	346	5638-76-6

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
24	mg	O

ADMET properties:

Property	Value	Reference
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
Ménière's disease	indication	13445001	DOID:9849

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN	INVERSE AGONIST	EC50	9.52		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Histamine H3 receptor	GPCR		HRH3_RAT		Ki	5.69		CHEMBL

External reference:

ID	Source
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