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
BA (Bioavailability)	0.61 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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	358.49	22.41	230	7292	165572	63315928
Pruritus	154.30	22.41	201	7321	361252	63120248
Angioedema	104.24	22.41	67	7455	47898	63433602
Chronic spontaneous urticaria	89.89	22.41	22	7500	1135	63480365
Skin plaque	87.44	22.41	34	7488	8286	63473214
Inappropriate schedule of product administration	65.92	22.41	71	7451	103894	63377606
Erythema	59.96	22.41	88	7434	175663	63305837
Urticaria thermal	58.84	22.41	13	7509	426	63481074
Urticaria chronic	58.61	22.41	14	7508	651	63480849
Scratch	52.34	22.41	22	7500	6543	63474957
Mast cell activation syndrome	50.68	22.41	13	7509	812	63480688
Illness	46.96	22.41	42	7480	49017	63432483
Monocyte count abnormal	44.35	22.41	9	7513	194	63481306
Anaphylactic reaction	43.37	22.41	46	7476	66054	63415446
Asthma	39.37	22.41	61	7461	127500	63354000
Urticarial vasculitis	38.32	22.41	10	7512	669	63480831
Dizziness postural	37.35	22.41	18	7504	7358	63474142
Administration site erythema	37.13	22.41	10	7512	755	63480745
Diverticulum oesophageal	34.81	22.41	7	7515	144	63481356
Mandibular mass	33.50	22.41	7	7515	175	63481325
Lymphocyte count abnormal	33.08	22.41	9	7513	706	63480794
Stress	32.62	22.41	40	7482	67127	63414373
Malaise	32.02	22.41	115	7407	415839	63065661
Pigmentation disorder	31.89	22.41	14	7508	4625	63476875
Heart rate increased	31.81	22.41	47	7475	94191	63387309
Prescription form tampering	30.16	22.41	8	7514	570	63480930
Exposure to allergen	29.36	22.41	7	7515	323	63481177
Middle insomnia	28.27	22.41	18	7504	12625	63468875
Incorrect dose administered	27.97	22.41	35	7487	59933	63421567
Perfume sensitivity	27.54	22.41	8	7514	797	63480703
Inflammatory bowel disease	27.34	22.41	12	7510	3961	63477539
Nasal congestion	25.47	22.41	35	7487	65625	63415875
Functional residual capacity increased	25.39	22.41	5	7517	92	63481408
Throat tightness	25.19	22.41	22	7500	24865	63456635
Oropharyngeal spasm	25.05	22.41	6	7516	282	63481218
Face oedema	24.87	22.41	20	7502	20192	63461308
Eosinophilia	24.83	22.41	21	7501	22735	63458765
Dyshidrotic eczema	24.82	22.41	7	7515	627	63480873
Migraine	24.59	22.41	44	7478	103302	63378198
Lymphadenopathy mediastinal	24.37	22.41	10	7512	2798	63478702
Cough	24.26	22.41	83	7439	292660	63188840
Nasal disorder	24.18	22.41	10	7512	2854	63478646
Rhinorrhoea	24.01	22.41	34	7488	65543	63415957
Lactic acidosis	23.96	22.41	26	7496	38261	63443239
Oropharyngeal oedema	23.91	22.41	6	7516	343	63481157
Joint swelling	23.65	22.41	5	7517	327661	63153839
Papule	23.23	22.41	12	7510	5679	63475821
Skin lesion	23.07	22.41	23	7499	30698	63450802
Allergic oedema	22.98	22.41	7	7515	821	63480679
Lichen planus	22.61	22.41	9	7513	2329	63479171
Loose tooth	22.54	22.41	10	7512	3384	63478116

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	130.16	27.21	66	1964	62311	34892590
Angioimmunoblastic T-cell lymphoma	58.63	27.21	11	2019	328	34954573
Angioedema	56.50	27.21	32	1998	37342	34917559
Rash maculovesicular	50.03	27.21	7	2023	28	34954873
Pruritus	48.80	27.21	50	1980	141931	34812970
Lip erythema	45.59	27.21	7	2023	59	34954842
Urticaria chronic	42.97	27.21	7	2023	89	34954812
Nasal mucosal disorder	40.74	27.21	7	2023	125	34954776
Enanthema	32.52	27.21	7	2023	421	34954480
Lichenoid keratosis	32.46	27.21	10	2020	2498	34952403
Genital ulceration	32.22	27.21	7	2023	440	34954461
Mydriasis	32.07	27.21	13	2017	7224	34947677
Laryngeal discomfort	31.18	27.21	6	2024	205	34954696
Asthma	30.84	27.21	23	2007	42633	34912268
Lupus-like syndrome	27.45	27.21	9	2021	2747	34952154
Chronic spontaneous urticaria	27.34	27.21	5	2025	129	34954772

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	425.53	19.49	265	8985	184936	79550202
Pruritus	190.56	19.49	231	9019	394417	79340721
Angioedema	121.29	19.49	87	9163	75948	79659190
Chronic spontaneous urticaria	104.45	19.49	25	9225	1199	79733939
Skin plaque	89.77	19.49	37	9213	10708	79724430
Inappropriate schedule of product administration	80.60	19.49	88	9162	133540	79601598
Erythema	69.62	19.49	106	9144	223184	79511954
Asthma	66.32	19.49	80	9170	135015	79600123
Urticaria thermal	64.50	19.49	14	9236	431	79734707
Illness	58.07	19.49	46	9204	46465	79688673
Anaphylactic reaction	55.48	19.49	58	9192	83685	79651453
Mast cell activation syndrome	47.70	19.49	12	9238	708	79734430
Scratch	47.67	19.49	22	9228	8341	79726797
Angioimmunoblastic T-cell lymphoma	47.58	19.49	11	9239	453	79734685
Death	45.55	19.49	6	9244	566508	79168630
Urticaria chronic	44.66	19.49	11	9239	595	79734543
Rash maculovesicular	44.60	19.49	7	9243	31	79735107
Administration site erythema	44.53	19.49	10	9240	361	79734777
Malaise	38.11	19.49	134	9116	489735	79245403
Dizziness postural	35.43	19.49	20	9230	11529	79723609
Eosinophilia	34.76	19.49	34	9216	45311	79689827
Diverticulum oesophageal	34.34	19.49	7	9243	158	79734980
Middle insomnia	34.19	19.49	22	9228	16047	79719091
Pigmentation disorder	32.71	19.49	15	9235	5603	79729535
Mandibular mass	32.27	19.49	7	9243	215	79734923
Migraine	32.23	19.49	45	9205	87448	79647690
Psychological trauma	31.33	19.49	10	9240	1396	79733742
Stress	30.91	19.49	42	9208	79570	79655568
Lip erythema	30.70	19.49	7	9243	271	79734867
Heart rate increased	30.30	19.49	52	9198	120672	79614466
Lip swelling	30.10	19.49	30	9220	40881	79694257
Nasal mucosal disorder	28.52	19.49	7	9243	373	79734765
Throat tightness	27.34	19.49	24	9226	27883	79707255
Incorrect dose administered	26.14	19.49	38	9212	76592	79658546
Papule	25.94	19.49	14	9236	7393	79727745
Eye discharge	25.69	19.49	13	9237	6021	79729117
Cough	25.65	19.49	97	9153	366692	79368446
Urticarial vasculitis	25.54	19.49	7	9243	577	79734561
Dyshidrotic eczema	25.31	19.49	7	9243	596	79734542
Allergy to chemicals	25.31	19.49	10	9240	2592	79732546
Functional residual capacity increased	25.29	19.49	5	9245	96	79735042
Face oedema	25.20	19.49	23	9227	28113	79707025
Lichen planus	24.63	19.49	10	9240	2781	79732357
Skin lesion	24.22	19.49	27	9223	41817	79693321
Exposure to allergen	24.17	19.49	6	9244	335	79734803
Loose tooth	23.57	19.49	10	9240	3107	79732031
Inflammatory bowel disease	23.55	19.49	12	9238	5639	79729499
Allergic oedema	23.44	19.49	7	9243	784	79734354
Nasal congestion	23.31	19.49	36	9214	76516	79658622
Conjunctival hyperaemia	23.26	19.49	11	9239	4402	79730736
Eczema	23.04	19.49	26	9224	40792	79694346
Frustration tolerance decreased	23.03	19.49	13	9237	7489	79727649
Enanthema	22.95	19.49	7	9243	842	79734296
Perfume sensitivity	22.71	19.49	7	9243	872	79734266
Genital ulceration	21.16	19.49	7	9243	1093	79734045
Bruxism	21.11	19.49	10	9240	4016	79731122
Lichenoid keratosis	21.04	19.49	10	9240	4047	79731091
Laryngeal discomfort	20.81	19.49	6	9244	594	79734544
Lymphadenopathy mediastinal	20.28	19.49	10	9240	4386	79730752
Nervousness	20.09	19.49	22	9228	33393	79701745
Pharyngeal swelling	20.05	19.49	12	9238	7707	79727431
Swelling face	19.63	19.49	32	9218	71180	79663958
Lip oedema	19.54	19.49	11	9239	6305	79728833

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