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

Stem definitionDrug idCAS RN
histamine-H1 receptor antagonists, tricyclic compounds 2413 158876-82-5

Description:

MoleculeDescription

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:

DoseUnitRoute
10 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 27, 2017 PMDA Teikoku Seiyaku

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Urticaria 190.88 30.38 103 2412 129458 50473151
Asthma 131.15 30.38 71 2444 89266 50513343
Skin plaque 116.44 30.38 32 2483 6296 50596313
Wheezing 71.07 30.38 42 2473 62005 50540604
Angioedema 60.89 30.38 32 2483 37644 50564965
Pruritus 56.92 30.38 70 2445 283498 50319111
Therapeutic product effect incomplete 56.19 30.38 42 2473 91473 50511136
Vascular access site infection 49.84 30.38 7 2508 35 50602574
Vascular access site thrombosis 49.67 30.38 7 2508 36 50602573
Sleep disorder due to a general medical condition 48.66 30.38 17 2498 7354 50595255
Lipohypertrophy 47.99 30.38 10 2505 603 50602006
Obstructive airways disorder 39.39 30.38 18 2497 15634 50586975
Nasal polyps 38.23 30.38 11 2504 2543 50600066
Cutaneous T-cell lymphoma 35.76 30.38 9 2506 1255 50601354
Expiratory reserve volume decreased 34.03 30.38 5 2510 36 50602573
Paranasal sinus inflammation 33.79 30.38 7 2508 410 50602199
Sinonasal obstruction 32.59 30.38 6 2509 189 50602420
Osteoporotic fracture 31.76 30.38 10 2505 3135 50599474
Sneezing 31.75 30.38 15 2500 14029 50588580
Anaphylactic reaction 31.33 30.38 24 2491 54031 50548578

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Obstructive airways disorder 82.04 42.03 25 928 10991 29562583
Pleural thickening 80.28 42.03 13 940 298 29573276
Asthma 67.64 42.03 29 924 33820 29539754
Bronchial wall thickening 64.46 42.03 13 940 1039 29572535
Urticaria 57.24 42.03 30 923 54630 29518944
Nasal oedema 52.52 42.03 9 944 293 29573281
Upper-airway cough syndrome 50.89 42.03 13 940 2990 29570584
Pulmonary function test decreased 46.68 42.03 13 940 4150 29569424

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Urticaria 241.35 31.07 127 3175 147190 64348240
Asthma 175.46 31.07 89 3213 95136 64400294
Skin plaque 104.52 31.07 32 3270 8908 64486522
Obstructive airways disorder 81.42 31.07 34 3268 23151 64472279
Pruritus 75.41 31.07 86 3216 312314 64183116
Wheezing 74.21 31.07 48 3254 80531 64414899
Upper-airway cough syndrome 64.14 31.07 22 3280 8748 64486682
Therapeutic product effect incomplete 61.16 31.07 47 3255 103435 64391995
Angioedema 57.31 31.07 37 3265 61784 64433646
Bronchial wall thickening 50.71 31.07 13 3289 1894 64493536
Vascular access site thrombosis 49.46 31.07 7 3295 36 64495394
Nasal polyps 46.73 31.07 14 3288 3615 64491815
Pleural thickening 46.19 31.07 13 3289 2697 64492733
Lipohypertrophy 45.14 31.07 10 3292 782 64494648
Rhinorrhoea 43.87 31.07 31 3271 59938 64435492
Vascular access site infection 43.63 31.07 7 3295 92 64495338
Full blood count abnormal 41.03 31.07 23 3279 29734 64465696
Nasal oedema 37.52 31.07 9 3293 999 64494431
Pulmonary function test decreased 35.08 31.07 13 3289 6448 64488982
Cough 31.77 31.07 56 3246 302092 64193338

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AX28 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use

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

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Urticaria indication 126485001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST IC50 8.41 CHEMBL KEGG DRUG
Platelet-activating factor receptor GPCR IC50 5.43 CHEMBL

External reference:

IDSource
D07407 KEGG_DRUG
C0534301 UMLSCUI
CHEBI:135673 CHEBI
CHEMBL91397 ChEMBL_ID
DB11614 DRUGBANK_ID
C103639 MESH_SUPPLEMENTAL_RECORD_UI
133017 PUBCHEM_CID
10103 IUPHAR_LIGAND_ID
7443 INN_ID
2AE8M83G3E UNII
013131 NDDF
013132 NDDF
1162935008 SNOMEDCT_US
1162955009 SNOMEDCT_US
699252008 SNOMEDCT_US
182349-12-8 SECONDARY_CAS_RN

Pharmaceutical products:

None