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

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	2413	158876-82-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rupatadine fumarate rupatadine alergoliber pafinur rinialer rupafin rupax	Rupatadine is a second-generation antihistamine, long-acting histamine antagonist with selective peripheral H1-receptor and platelet activating factor (PAF) antagonistic activities. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug, maintaining activity for up to 24 hours. Molecular weight: 415.97 Formula: C26H26ClN3 CLOGP: 5.06 LIPINSKI: 1 HAC: 3 HDO: 0 TPSA: 29.02 ALOGS: -4.88 ROTB: 2

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rupatadine fumarate
rupatadine
alergoliber
pafinur
rinialer
rupafin
rupax

Rupatadine is a second-generation antihistamine, long-acting histamine antagonist with selective peripheral H1-receptor and platelet activating factor (PAF) antagonistic activities. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug, maintaining activity for up to 24 hours.

Molecular weight: 415.97
Formula: C26H26ClN3
CLOGP: 5.06
LIPINSKI: 1
HAC: 3
HDO: 0
TPSA: 29.02
ALOGS: -4.88
ROTB: 2

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 27, 2017	PMDA	Teikoku Seiyaku

FDA Adverse Event Reporting System (Female)

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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	409.38	31.44	231	5790	165571	63317430
Asthma	216.28	31.44	140	5881	127421	63355580
Ear pruritus	190.20	31.44	49	5972	3916	63479085
Pulmonary function test abnormal	188.86	31.44	42	5979	1788	63481213
Nasal polyps	183.24	31.44	52	5969	5987	63477014
Wheezing	171.97	31.44	109	5912	95486	63387515
Chest X-ray abnormal	169.39	31.44	46	5975	4503	63478498
Sneezing	158.43	31.44	61	5960	18157	63464844
Angioedema	151.52	31.44	79	5942	47886	63435115
Blood lactic acid increased	149.25	31.44	46	5975	7040	63475961

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FDA Adverse Event Reporting System (Male)

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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	85.92	37.89	44	1337	62333	34893217
Obstructive airways disorder	83.79	37.89	29	1352	15465	34940085
Pleural thickening	81.64	37.89	14	1367	371	34955179
Asthma	70.22	37.89	34	1347	42622	34912928
Bronchial wall thickening	63.92	37.89	14	1367	1354	34954196
Nasal oedema	55.33	37.89	10	1371	360	34955190
Upper-airway cough syndrome	55.27	37.89	15	1366	3543	34952007
Full blood count abnormal	46.88	37.89	20	1361	18648	34936902
Pulmonary function test decreased	45.99	37.89	14	1367	4961	34950589
Bronchial obstruction	40.64	37.89	10	1371	1606	34953944

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FDA Adverse Event Reporting System (Geriatric)

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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	473.20	27.53	259	6893	184942	79552294
Asthma	263.96	27.53	159	6993	134936	79602300
Upper-airway cough syndrome	196.34	27.53	63	7089	11630	79725606
Ear pruritus	191.08	27.53	49	7103	4066	79733170
Nasal polyps	184.94	27.53	54	7098	7273	79729963
Wheezing	169.49	27.53	114	7038	116550	79620686
Pulmonary function test abnormal	157.05	27.53	42	7110	4102	79733134
Chest X-ray abnormal	146.92	27.53	46	7106	7837	79729399
Sneezing	146.53	27.53	58	7094	19625	79717611
Full blood count abnormal	144.06	27.53	71	7081	40403	79696833

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AX28	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use

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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	8.22	Basic
pKa2	3.82	Basic
pKa3	3.17	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	IC50	8.41		CHEMBL	KEGG DRUG
Platelet-activating factor receptor	GPCR	P25105	PTAFR_HUMAN		IC50	5.43		CHEMBL

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External reference:

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ID	Source
013131	NDDF
013132	NDDF
10103	IUPHAR_LIGAND_ID
1162935008	SNOMEDCT_US
1162955009	SNOMEDCT_US
133017	PUBCHEM_CID
182349-12-8	SECONDARY_CAS_RN
2AE8M83G3E	UNII
699252008	SNOMEDCT_US
7443	INN_ID

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Pharmaceutical products:

None