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

Stem definitionDrug idCAS RN
antihistaminics 977 90729-43-4

Description:

MoleculeDescription

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:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Jan. 1, 1990 YEAR INTRODUCED

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 95.62 26.21 68 2608 129493 50472955
Allergy test positive 76.82 26.21 14 2662 391 50602057
Gallbladder polyp 68.76 26.21 14 2662 707 50601741
Drug reaction with eosinophilia and systemic symptoms 64.49 26.21 31 2645 28393 50574055
Angioedema 59.01 26.21 32 2644 37644 50564804
Mixed liver injury 30.24 26.21 10 2666 3441 50599007
Systemic infection 29.94 26.21 9 2667 2274 50600174
Rhinorrhoea 28.84 26.21 23 2653 51560 50550888
Oesophagitis 28.53 26.21 14 2662 13369 50589079
Mechanical urticaria 27.96 26.21 6 2670 391 50602057
Sprue-like enteropathy 26.31 26.21 6 2670 517 50601931

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
Dental caries 84.40 29.36 23 1529 4157 29568818
Vitamin D deficiency 60.86 29.36 19 1533 5510 29567465
Diabetes mellitus inadequate control 60.30 29.36 23 1529 12111 29560864
Blood pressure fluctuation 52.46 29.36 24 1528 19870 29553105
Hepatitis 39.39 29.36 20 1532 20763 29552212
Rheumatoid arthritis 38.92 29.36 23 1529 32129 29540846
Colitis 36.90 29.36 22 1530 31226 29541749
Musculoskeletal stiffness 35.68 29.36 23 1529 37435 29535540
Hypocoagulable state 33.14 29.36 8 1544 890 29572085
Haematochezia 31.07 29.36 21 1531 36962 29536013
Gastrointestinal disorder 30.77 29.36 19 1533 28687 29544288

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 106.61 21.32 84 4224 147233 64347191
Allergy test positive 78.72 21.32 15 4293 421 64494003
Drug reaction with eosinophilia and systemic symptoms 69.70 21.32 44 4264 54173 64440251
Angioedema 59.72 21.32 42 4266 61779 64432645
Gallbladder polyp 56.80 21.32 13 4295 899 64493525
Dental caries 53.96 21.32 22 4286 10778 64483646
Diabetes mellitus inadequate control 42.46 21.32 23 4285 21298 64473126
Eczema 40.38 21.32 25 4283 29695 64464729
Vitamin D deficiency 39.29 21.32 18 4290 11674 64482750
Mechanical urticaria 27.18 21.32 6 4302 352 64494072
Hypocoagulable state 25.48 21.32 8 4300 1845 64492579
Hepatitis 24.60 21.32 22 4286 45560 64448864
Blood pressure fluctuation 24.05 21.32 23 4285 51848 64442576
Musculoskeletal stiffness 22.54 21.32 34 4274 123172 64371252
Systemic infection 22.26 21.32 9 4299 4312 64490112
Colitis 21.66 21.32 23 4285 58651 64435773

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 8.87 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 Ki 8 WOMBAT-PK SCIENTIFIC LITERATURE
D(1A) dopamine receptor GPCR Ki 6.22 DRUG MATRIX
D(2) dopamine receptor GPCR IC50 7.21 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.51 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 6.55 WOMBAT-PK
Multidrug resistance protein 1 Transporter IC50 5.82 CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 6.34 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR IC50 7.33 CHEMBL
5-hydroxytryptamine receptor 2A GPCR Ki 7.59 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 6.70 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.91 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 5.99 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.47 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 7.38 DRUG MATRIX
Histamine H2 receptor GPCR Ki 5.54 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR IC50 5.96 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 6.55 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 6.86 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 6.19 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 6.62 DRUG MATRIX
Beta-3 adrenergic receptor GPCR Ki 5.72 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 7.40 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 7.11 DRUG MATRIX
Adenosine receptor A3 GPCR Ki 5.74 DRUG MATRIX
D(4) dopamine receptor GPCR Ki 6.34 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 6.06 DRUG MATRIX
Acetylcholinesterase Enzyme IC50 5.13 DRUG MATRIX
Epidermal growth factor receptor Kinase IC50 6.25 DRUG MATRIX
Tyrosine-protein kinase Fyn Kinase IC50 6.09 DRUG MATRIX
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 5.98 DRUG MATRIX
Substance-K receptor GPCR Ki 6.19 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 6.94 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 6.63 DRUG MATRIX
5-hydroxytryptamine receptor 1B GPCR Ki 5.85 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 5.87 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 5.58 CHEMBL
Histamine H1 receptor GPCR IC50 7.35 CHEMBL

External reference:

IDSource
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