Scroll

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

Stem definition	Drug id	CAS RN
antihistaminics	977	90729-43-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ebastine bastel ebastel ebastin erostin kestine	non-sedating second generation antihistamine which is used for allergic disorders Molecular weight: 469.67 Formula: C32H39NO2 CLOGP: 6.94 LIPINSKI: 1 HAC: 3 HDO: 0 TPSA: 29.54 ALOGS: -6.86 ROTB: 10

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ebastine
bastel
ebastel
ebastin
erostin
kestine

non-sedating second generation antihistamine which is used for allergic disorders

Molecular weight: 469.67
Formula: C32H39NO2
CLOGP: 6.94
LIPINSKI: 1
HAC: 3
HDO: 0
TPSA: 29.54
ALOGS: -6.86
ROTB: 10

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.61 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1990	YEAR INTRODUCED

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
COVID-19	164.59	20.69	109	5375	112994	63370544
Urticaria	117.25	20.69	104	5380	165698	63317840
Endocrine ophthalmopathy	85.38	20.69	18	5466	653	63482885
Angioedema	76.38	20.69	49	5435	47916	63435622
Toxic shock syndrome	70.39	20.69	16	5468	826	63482712
Allergy test positive	69.60	20.69	15	5469	605	63482933
Nasal ulcer	67.85	20.69	19	5465	2285	63481253
Gallbladder polyp	60.67	20.69	14	5470	773	63482765
Eyelid disorder	57.89	20.69	16	5468	1833	63481705
Drug reaction with eosinophilia and systemic symptoms	57.42	20.69	36	5448	33800	63449738
Mean cell haemoglobin increased	54.73	20.69	17	5467	2926	63480612
Swelling of eyelid	49.45	20.69	16	5468	3140	63480398
Systemic infection	43.35	20.69	16	5468	4644	63478894
Blood immunoglobulin E increased	38.71	20.69	14	5470	3835	63479703
Abdominal pain upper	37.11	20.69	65	5419	206379	63277159
Dyslipidaemia	36.20	20.69	16	5468	7377	63476161
Chronic spontaneous urticaria	36.17	20.69	10	5474	1147	63482391
Skin disorder	34.68	20.69	25	5459	29482	63454056
Vitamin D decreased	31.23	20.69	16	5468	10226	63473312
Synovial cyst	30.95	20.69	16	5468	10417	63473121
Feeding disorder	29.90	20.69	17	5467	13345	63470193
Eye infection	28.67	20.69	16	5468	12129	63471409
Lymphangiectasia	27.99	20.69	5	5479	74	63483464
Pruritus	27.67	20.69	81	5403	361372	63122166
Pelvic pain	27.07	20.69	16	5468	13503	63470035
Drug ineffective	26.44	20.69	31	5453	1044734	62438804
Neisseria infection	26.08	20.69	5	5479	111	63483427
Injection site oedema	25.49	20.69	8	5476	1424	63482114
Mechanical urticaria	23.94	20.69	6	5478	470	63483068
Acarodermatitis	23.30	20.69	7	5477	1076	63482462
Hypercholesterolaemia	22.64	20.69	17	5467	21317	63462221
Mixed liver injury	22.38	20.69	10	5474	4725	63478813
Death	22.28	20.69	3	5481	374378	63109160
Skin laceration	21.69	20.69	17	5467	22691	63460847
Temperature intolerance	21.67	20.69	12	5472	8952	63474586
Sprue-like enteropathy	21.29	20.69	6	5478	737	63482801
Ear swelling	21.06	20.69	7	5477	1494	63482044

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
COVID-19	82.58	23.75	58	2522	77492	34876859
Dental caries	78.96	23.75	24	2556	4515	34949836
Vitamin D deficiency	54.84	23.75	20	2560	6588	34947763
Diabetes mellitus inadequate control	53.52	23.75	24	2556	13440	34940911
Blood pressure fluctuation	47.17	23.75	27	2553	25222	34929129
Hepatitis	32.85	23.75	21	2559	23883	34930468
Rheumatoid arthritis	32.45	23.75	25	2555	38213	34916138
Blood pressure increased	30.57	23.75	35	2545	88067	34866284
Hypocoagulable state	30.01	23.75	8	2572	938	34953413
Toxic skin eruption	29.11	23.75	15	2565	11370	34942981
Colitis	28.42	23.75	23	2557	37727	34916624
Musculoskeletal stiffness	28.08	23.75	25	2555	46655	34907696
Discoloured vomit	24.27	23.75	6	2574	522	34953829
Gastrointestinal disorder	24.11	23.75	20	2560	33928	34920423

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
COVID-19	226.86	18.37	161	7996	157513	79578718
Urticaria	128.60	18.37	124	8033	185077	79551154
Endocrine ophthalmopathy	80.87	18.37	18	8139	710	79735521
Angioedema	72.59	18.37	61	8096	75974	79660257
Allergy test positive	70.01	18.37	16	8141	712	79735519
Nasal ulcer	66.05	18.37	19	8138	2121	79734110
Toxic shock syndrome	61.43	18.37	16	8141	1233	79734998
Drug reaction with eosinophilia and systemic symptoms	58.15	18.37	50	8107	64194	79672037
Eyelid disorder	54.15	18.37	16	8141	1962	79734269
Gallbladder polyp	50.23	18.37	13	8144	977	79735254
Dental caries	45.99	18.37	23	8134	11797	79724434
Mean cell haemoglobin increased	45.64	18.37	17	8140	4268	79731963
Swelling of eyelid	43.84	18.37	16	8141	3795	79732436
Pruritus	41.95	18.37	111	8046	394537	79341694
Eczema	37.39	18.37	32	8125	40786	79695445
Toxic skin eruption	37.18	18.37	25	8132	22268	79713963
Chronic spontaneous urticaria	33.94	18.37	10	8147	1214	79735017
Blood immunoglobulin E increased	33.86	18.37	15	8142	5867	79730364
Diabetes mellitus inadequate control	32.97	18.37	24	8133	24240	79711991
Death	32.34	18.37	9	8148	566505	79169726
Vitamin D deficiency	31.23	18.37	19	8138	14260	79721971
Haematochezia	30.36	18.37	41	8116	87604	79648627
Abdominal pain upper	30.15	18.37	69	8088	223750	79512481
Skin disorder	29.85	18.37	26	8131	33917	79702314
Vitamin D decreased	29.45	18.37	16	8141	9709	79726522
Systemic infection	29.41	18.37	16	8141	9736	79726495
Synovial cyst	28.94	18.37	16	8141	10049	79726182
Injection site oedema	28.60	18.37	9	8148	1362	79734869
SARS-CoV-2 antibody test negative	27.07	18.37	6	8151	232	79735999
Dyslipidaemia	26.78	18.37	16	8141	11617	79724614
Eye infection	26.42	18.37	16	8141	11904	79724327
Lymphangiectasia	25.32	18.37	5	8152	109	79736122
Pelvic pain	24.72	18.37	16	8141	13365	79722866
Feeding disorder	24.20	18.37	17	8140	16237	79719994
Gastrointestinal disorder	23.93	18.37	44	8113	122161	79614070
Mechanical urticaria	23.42	18.37	6	8151	433	79735798
Neisseria infection	23.21	18.37	5	8152	169	79736062
Product availability issue	22.51	18.37	10	8147	3937	79732294
Hypocoagulable state	20.94	18.37	8	8149	2151	79734080
Acarodermatitis	20.38	18.37	7	8150	1391	79734840
Blood pressure increased	19.96	18.37	57	8100	211303	79524928
Ear swelling	19.33	18.37	7	8150	1624	79734607
Anaphylactic shock	19.26	18.37	21	8136	35975	79700256
Hypercholesterolaemia	18.93	18.37	17	8140	23078	79713153
Temperature intolerance	18.91	18.37	12	8145	9693	79726538
Tendinous contracture	18.38	18.37	4	8153	142	79736089

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R06AX22	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents

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

Disease	Relation	SNOMED_ID	DOID
Allergic rhinitis	indication	61582004
Chronic idiopathic urticaria	indication	302162004

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.87	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])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8	WOMBAT-PK	SCIENTIFIC LITERATURE
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		IC50	7.21	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.51	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.55	WOMBAT-PK
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.82	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.19	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	6.34	DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		IC50	7.33	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7.59	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.70	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.91	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.99	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.47	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	7.38	DRUG MATRIX
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.54	DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		IC50	5.96	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.55	DRUG MATRIX
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.86	DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.22	DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.62	DRUG MATRIX
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Ki	5.72	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.40	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	7.11	DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.74	DRUG MATRIX
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	6.34	DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.06	DRUG MATRIX
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN		IC50	5.13	DRUG MATRIX
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	6.25	DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		IC50	6.09	DRUG MATRIX
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN		IC50	5.98	DRUG MATRIX
Substance-K receptor	GPCR	P21452	NK2R_HUMAN		Ki	6.19	DRUG MATRIX
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	6.94	DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	6.63	DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	5.85	DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	5.87	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	5.58	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		IC50	7.35	CHEMBL

External reference:

ID	Source
D01478	KEGG_DRUG
C0058895	UMLSCUI
CHEBI:31528	CHEBI
CHEMBL305660	ChEMBL_ID
DB11742	DRUGBANK_ID
C058249	MESH_SUPPLEMENTAL_RECORD_UI
5633	INN_ID
TQD7Q784P1	UNII
3191	PUBCHEM_CID
23796	RXNORM
007136	NDDF

Pharmaceutical products:

None