ebastine ๐Ÿถ 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 ยตM/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
COVID-19 164.59 20.69 109 5375 112994 63370544
Urticaria 117.25 20.69 104 5380 165698 63317840
Endocrine ophthalmopathy 85.38 20.69 18 5466 653 63482885
Angioedema 76.38 20.69 49 5435 47916 63435622
Toxic shock syndrome 70.39 20.69 16 5468 826 63482712
Allergy test positive 69.60 20.69 15 5469 605 63482933
Nasal ulcer 67.85 20.69 19 5465 2285 63481253
Gallbladder polyp 60.67 20.69 14 5470 773 63482765
Eyelid disorder 57.89 20.69 16 5468 1833 63481705
Drug reaction with eosinophilia and systemic symptoms 57.42 20.69 36 5448 33800 63449738
Mean cell haemoglobin increased 54.73 20.69 17 5467 2926 63480612
Swelling of eyelid 49.45 20.69 16 5468 3140 63480398
Systemic infection 43.35 20.69 16 5468 4644 63478894
Blood immunoglobulin E increased 38.71 20.69 14 5470 3835 63479703
Abdominal pain upper 37.11 20.69 65 5419 206379 63277159
Dyslipidaemia 36.20 20.69 16 5468 7377 63476161
Chronic spontaneous urticaria 36.17 20.69 10 5474 1147 63482391
Skin disorder 34.68 20.69 25 5459 29482 63454056
Vitamin D decreased 31.23 20.69 16 5468 10226 63473312
Synovial cyst 30.95 20.69 16 5468 10417 63473121
Feeding disorder 29.90 20.69 17 5467 13345 63470193
Eye infection 28.67 20.69 16 5468 12129 63471409
Lymphangiectasia 27.99 20.69 5 5479 74 63483464
Pruritus 27.67 20.69 81 5403 361372 63122166
Pelvic pain 27.07 20.69 16 5468 13503 63470035
Drug ineffective 26.44 20.69 31 5453 1044734 62438804
Neisseria infection 26.08 20.69 5 5479 111 63483427
Injection site oedema 25.49 20.69 8 5476 1424 63482114
Mechanical urticaria 23.94 20.69 6 5478 470 63483068
Acarodermatitis 23.30 20.69 7 5477 1076 63482462
Hypercholesterolaemia 22.64 20.69 17 5467 21317 63462221
Mixed liver injury 22.38 20.69 10 5474 4725 63478813
Death 22.28 20.69 3 5481 374378 63109160
Skin laceration 21.69 20.69 17 5467 22691 63460847
Temperature intolerance 21.67 20.69 12 5472 8952 63474586
Sprue-like enteropathy 21.29 20.69 6 5478 737 63482801
Ear swelling 21.06 20.69 7 5477 1494 63482044

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
COVID-19 82.58 23.75 58 2522 77492 34876859
Dental caries 78.96 23.75 24 2556 4515 34949836
Vitamin D deficiency 54.84 23.75 20 2560 6588 34947763
Diabetes mellitus inadequate control 53.52 23.75 24 2556 13440 34940911
Blood pressure fluctuation 47.17 23.75 27 2553 25222 34929129
Hepatitis 32.85 23.75 21 2559 23883 34930468
Rheumatoid arthritis 32.45 23.75 25 2555 38213 34916138
Blood pressure increased 30.57 23.75 35 2545 88067 34866284
Hypocoagulable state 30.01 23.75 8 2572 938 34953413
Toxic skin eruption 29.11 23.75 15 2565 11370 34942981
Colitis 28.42 23.75 23 2557 37727 34916624
Musculoskeletal stiffness 28.08 23.75 25 2555 46655 34907696
Discoloured vomit 24.27 23.75 6 2574 522 34953829
Gastrointestinal disorder 24.11 23.75 20 2560 33928 34920423

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
COVID-19 226.86 18.37 161 7996 157513 79578718
Urticaria 128.60 18.37 124 8033 185077 79551154
Endocrine ophthalmopathy 80.87 18.37 18 8139 710 79735521
Angioedema 72.59 18.37 61 8096 75974 79660257
Allergy test positive 70.01 18.37 16 8141 712 79735519
Nasal ulcer 66.05 18.37 19 8138 2121 79734110
Toxic shock syndrome 61.43 18.37 16 8141 1233 79734998
Drug reaction with eosinophilia and systemic symptoms 58.15 18.37 50 8107 64194 79672037
Eyelid disorder 54.15 18.37 16 8141 1962 79734269
Gallbladder polyp 50.23 18.37 13 8144 977 79735254
Dental caries 45.99 18.37 23 8134 11797 79724434
Mean cell haemoglobin increased 45.64 18.37 17 8140 4268 79731963
Swelling of eyelid 43.84 18.37 16 8141 3795 79732436
Pruritus 41.95 18.37 111 8046 394537 79341694
Eczema 37.39 18.37 32 8125 40786 79695445
Toxic skin eruption 37.18 18.37 25 8132 22268 79713963
Chronic spontaneous urticaria 33.94 18.37 10 8147 1214 79735017
Blood immunoglobulin E increased 33.86 18.37 15 8142 5867 79730364
Diabetes mellitus inadequate control 32.97 18.37 24 8133 24240 79711991
Death 32.34 18.37 9 8148 566505 79169726
Vitamin D deficiency 31.23 18.37 19 8138 14260 79721971
Haematochezia 30.36 18.37 41 8116 87604 79648627
Abdominal pain upper 30.15 18.37 69 8088 223750 79512481
Skin disorder 29.85 18.37 26 8131 33917 79702314
Vitamin D decreased 29.45 18.37 16 8141 9709 79726522
Systemic infection 29.41 18.37 16 8141 9736 79726495
Synovial cyst 28.94 18.37 16 8141 10049 79726182
Injection site oedema 28.60 18.37 9 8148 1362 79734869
SARS-CoV-2 antibody test negative 27.07 18.37 6 8151 232 79735999
Dyslipidaemia 26.78 18.37 16 8141 11617 79724614
Eye infection 26.42 18.37 16 8141 11904 79724327
Lymphangiectasia 25.32 18.37 5 8152 109 79736122
Pelvic pain 24.72 18.37 16 8141 13365 79722866
Feeding disorder 24.20 18.37 17 8140 16237 79719994
Gastrointestinal disorder 23.93 18.37 44 8113 122161 79614070
Mechanical urticaria 23.42 18.37 6 8151 433 79735798
Neisseria infection 23.21 18.37 5 8152 169 79736062
Product availability issue 22.51 18.37 10 8147 3937 79732294
Hypocoagulable state 20.94 18.37 8 8149 2151 79734080
Acarodermatitis 20.38 18.37 7 8150 1391 79734840
Blood pressure increased 19.96 18.37 57 8100 211303 79524928
Ear swelling 19.33 18.37 7 8150 1624 79734607
Anaphylactic shock 19.26 18.37 21 8136 35975 79700256
Hypercholesterolaemia 18.93 18.37 17 8140 23078 79713153
Temperature intolerance 18.91 18.37 12 8145 9693 79726538
Tendinous contracture 18.38 18.37 4 8153 142 79736089

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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ 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(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 serotonin transporter Transporter Ki 6.19 DRUG MATRIX
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
D(1A) dopamine receptor GPCR Ki 6.22 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