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

Stem definition	Drug id	CAS RN
antihistaminics	4353	202189-78-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: bellozal F-96221-BM1 bilastine bilaxten	Molecular weight: 463.62 Formula: C28H37N3O3 CLOGP: 1.95 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 67.59 ALOGS: -5.36 ROTB: 10

Molecule

Description

Molfile Inchi Smiles

Synonyms:

bellozal
F-96221-BM1
bilastine
bilaxten

Molecular weight: 463.62
Formula: C28H37N3O3
CLOGP: 1.95
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 67.59
ALOGS: -5.36
ROTB: 10

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	0.61 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.87 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.13 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5.16 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
None	PMDA

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
Urticaria	233.62	22.81	143	4258	129418	50471305
Pruritus	92.39	22.81	118	4283	283450	50317273
Erythema	62.41	22.81	70	4331	146344	50454379
Angioedema	61.02	22.81	39	4362	37637	50563086
Urticaria chronic	55.29	22.81	12	4389	497	50600226
Skin plaque	48.88	22.81	19	4382	6309	50594414
Monocyte count abnormal	48.26	22.81	9	4392	170	50600553
Urticarial vasculitis	42.97	22.81	10	4391	569	50600154
Diverticulum oesophageal	37.25	22.81	7	4394	138	50600585
Lymphocyte count abnormal	36.98	22.81	9	4392	621	50600102
Mandibular mass	35.67	22.81	7	4394	175	50600548
Prescription form tampering	32.76	22.81	8	4393	560	50600163
Inflammatory bowel disease	32.58	22.81	12	4389	3438	50597285
Malaise	29.15	22.81	79	4322	335453	50265270
Lymphadenopathy mediastinal	28.47	22.81	10	4391	2501	50598222
Chronic spontaneous urticaria	28.29	22.81	7	4394	517	50600206
Dyshidrotic eczema	27.84	22.81	7	4394	552	50600171
Lichen planus	26.79	22.81	9	4392	1970	50598753
Inappropriate schedule of product administration	26.60	22.81	32	4369	71799	50528924
Allergic oedema	25.69	22.81	7	4394	755	50599968
Face oedema	25.28	22.81	17	4384	17822	50582901
Asthma	24.04	22.81	34	4367	89303	50511420

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
Urticaria	86.48	35.80	43	1184	54617	29518683
Angioimmunoblastic T-cell lymphoma	56.55	35.80	10	1217	302	29572998
Urticaria chronic	45.33	35.80	7	1220	89	29573211
Rash maculovesicular	45.10	35.80	6	1221	23	29573277
Lip erythema	42.88	35.80	6	1221	36	29573264
Nasal mucosal disorder	37.86	35.80	6	1221	91	29573209
Lichenoid keratosis	37.23	35.80	10	1217	2160	29571140

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
Urticaria	279.89	21.45	166	5241	147151	64346174
Pruritus	110.38	21.45	133	5274	312267	64181058
Angioedema	66.44	21.45	49	5358	61772	64431553
Erythema	66.43	21.45	80	5327	186990	64306335
Angioimmunoblastic T-cell lymphoma	46.46	21.45	10	5397	413	64492912
Urticaria chronic	45.83	21.45	10	5397	441	64492884
Skin plaque	43.21	21.45	19	5388	8921	64484404
Asthma	42.68	21.45	46	5361	95179	64398146
Rash maculovesicular	40.28	21.45	6	5401	26	64493299
Inappropriate schedule of product administration	36.90	21.45	42	5365	92244	64401081
Diverticulum oesophageal	36.73	21.45	7	5400	155	64493170
Mandibular mass	34.85	21.45	7	5400	205	64493120
Lip erythema	30.45	21.45	6	5401	159	64493166
Malaise	30.25	21.45	87	5320	396160	64097165
Inflammatory bowel disease	29.81	21.45	12	5395	4526	64488799
Urticarial vasculitis	29.59	21.45	7	5400	444	64492881
Lichen planus	29.57	21.45	10	5397	2318	64491007
Eye discharge	28.49	21.45	12	5395	5072	64488253
Dyshidrotic eczema	28.06	21.45	7	5400	555	64492770
Nasal mucosal disorder	26.13	21.45	6	5401	334	64492991
Allergic oedema	26.11	21.45	7	5400	737	64492588
Lichenoid keratosis	26.06	21.45	10	5397	3324	64490001
Face oedema	25.17	21.45	19	5388	24742	64468583
Lymphadenopathy mediastinal	24.60	21.45	10	5397	3866	64489459
Conjunctival hyperaemia	24.54	21.45	10	5397	3889	64489436
Chronic spontaneous urticaria	23.79	21.45	6	5401	497	64492828
Genital ulceration	22.33	21.45	6	5401	637	64492688
Functional residual capacity increased	21.52	21.45	4	5403	77	64493248
Enanthema	21.49	21.45	6	5401	735	64492590

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R06AX29	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
ATC	S01GX13	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics

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

Disease	Relation	SNOMED_ID	DOID
Allergic rhinitis	indication	61582004
Urticaria	indication	126485001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.42	acidic
pKa2	7.88	Basic
pKa3	5.11	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 H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.19		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

External reference:

ID	Source
D09570	KEGG_DRUG
C1101148	UMLSCUI
CHEBI:135954	CHEBI
CHEMBL1742423	ChEMBL_ID
DB11591	DRUGBANK_ID
C445659	MESH_SUPPLEMENTAL_RECORD_UI
11579	IUPHAR_LIGAND_ID
7905	INN_ID
PA1123N395	UNII
185460	PUBCHEM_CID
013709	NDDF
697973006	SNOMEDCT_US
714622001	SNOMEDCT_US

Pharmaceutical products:

None