desloratadine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
histamine-H1 receptor antagonists, tricyclic compounds 814 100643-71-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • SCH-34117
  • SCH 34117
  • desloratadine
  • azomyr
  • delopedil
  • descarboethoxyloratadine
  • descarboethoxyloratidine
  • neoclarityn
major metabolite of loratadine
  • Molecular weight: 310.83
  • Formula: C19H19ClN2
  • CLOGP: 3.83
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 24.92
  • ALOGS: -4.90
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
5 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.23 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 %
fu (Fraction unbound in plasma) 0.15 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.321 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.274 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 21.478 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.550 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 11.480 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 24.790 % High 1
herg hERG pIC50 5.691 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.762 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.758 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 20.040 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MAPK10,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 18
kinase-selectivity-class AXL,EIF2AK3 2
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 4.519 High 1
mh-clint Mouse hepatocyte intrinsic clearance 19.634 High 1
mppb Mouse plasma protein binding (% unbound) 8.790 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 11.588 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 23.110 % High 1
rh-clint Rat hepatocyte intrinsic clearance 27.290 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 31.770 % High 1
rppb Rat plasma protein binding (% unbound) 17.920 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 860.994 uM High 1

Approvals:

DateAgencyCompanyOrphan
Dec. 21, 2001 FDA MERCK SHARP DOHME

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
Angioedema 192.89 12.11 140 20028 64736 90543543
Intentional overdose 107.47 12.11 118 20050 93716 90514563
Endocrine ophthalmopathy 73.24 12.11 21 20147 1053 90607226
Nasal ulcer 72.89 12.11 26 20142 2640 90605639
Urticaria 68.77 12.11 188 19980 312546 90295733
Erythema 66.32 12.11 153 20015 229093 90379186
Toxic shock syndrome 64.92 12.11 19 20149 1025 90607254
Systemic lupus erythematosus 61.78 12.11 5 20163 361891 90246388
Glossodynia 59.21 12.11 3 20165 321776 90286503
Drug reaction with eosinophilia and systemic symptoms 56.41 12.11 58 20110 42700 90565579
Hyponatraemia 56.13 12.11 104 20064 133434 90474845
Wound 55.19 12.11 3 20165 302977 90305302
Acute kidney injury 54.61 12.11 176 19992 320211 90288068
Hand deformity 53.78 12.11 3 20165 296359 90311920
Allergy test positive 52.81 12.11 15 20153 727 90607552
Intentional self-injury 52.35 12.11 47 20121 29287 90578992
Toxic skin eruption 51.34 12.11 36 20132 15738 90592541
Eyelid disorder 50.99 12.11 19 20149 2184 90606095
Drug intolerance 49.29 12.11 19 20149 447572 90160707
Face oedema 48.97 12.11 41 20127 23277 90585002
Inflammatory bowel disease 47.05 12.11 23 20145 5148 90603131
Hallucination, auditory 44.11 12.11 33 20135 15942 90592337
Mean cell haemoglobin increased 43.60 12.11 20 20148 3885 90604394
Pruritus 43.46 12.11 236 19932 541289 90066990
Hyperkalaemia 42.78 12.11 62 20106 64902 90543377
Dermatitis bullous 41.86 12.11 27 20141 10289 90597990
Somnolence 41.31 12.11 121 20047 208963 90399316
Coma 40.29 12.11 64 20104 72568 90535711
Helicobacter infection 39.07 12.11 3 20165 226847 90381432
Rheumatoid arthritis 38.91 12.11 16 20152 362598 90245681
Paranoia 38.65 12.11 28 20140 12880 90595399
Haemangioma congenital 38.49 12.11 11 20157 545 90607734
Terminal dribbling 38.22 12.11 6 20162 11 90608268
Swelling of eyelid 37.26 12.11 20 20148 5434 90602845
Cholestasis 35.35 12.11 42 20126 36257 90572022
Rash maculo-papular 34.44 12.11 44 20124 40889 90567390
Pericarditis 34.09 12.11 9 20159 270142 90338137
Impaired healing 33.20 12.11 6 20162 234193 90374086
Myalgia 32.36 12.11 99 20069 175026 90433253
Contraindicated product administered 31.42 12.11 16 20152 320123 90288156
Neonatal infection 31.25 12.11 8 20160 260 90608019
Hypotension 29.64 12.11 147 20021 325250 90283029
Folliculitis 29.48 12.11 5 20163 204348 90403931
Cerebral thrombosis 29.18 12.11 12 20156 1791 90606488
Hepatic enzyme increased 27.38 12.11 24 20144 360712 90247567
Victim of chemical submission 27.19 12.11 9 20159 730 90607549
Eczema 27.16 12.11 45 20123 52825 90555454
Blood immunoglobulin E increased 26.84 12.11 15 20153 4410 90603869
Psoriatic arthropathy 26.28 12.11 9 20159 228326 90379953
Aggression 26.20 12.11 31 20137 26637 90581642
Synovitis 26.18 12.11 21 20147 329731 90278548
Irritable bowel syndrome 26.00 12.11 7 20161 207441 90400838
Dyslipidaemia 25.96 12.11 20 20148 10087 90598192
Hepatocellular injury 25.74 12.11 32 20136 28926 90579353
Therapeutic product effect decreased 25.59 12.11 15 20153 277556 90330723
Skin dystrophy 25.36 12.11 5 20163 47 90608232
Type 2 diabetes mellitus 25.20 12.11 7 20161 203237 90405042
Vitamin D decreased 25.02 12.11 21 20147 11958 90596321
Oxalosis 24.48 12.11 5 20163 57 90608222
Tooth injury 24.46 12.11 10 20158 1471 90606808
Hepatic cytolysis 24.08 12.11 32 20136 30884 90577395
Eye infection 23.79 12.11 22 20146 14232 90594047
Onycholysis 23.58 12.11 11 20157 2219 90606060
Synovial cyst 23.31 12.11 20 20148 11732 90596547
Gestational hypertension 23.11 12.11 12 20156 3050 90605229
Type IV hypersensitivity reaction 22.98 12.11 13 20155 3913 90604366
Suicide attempt 22.51 12.11 51 20117 75348 90532931
Completed suicide 22.17 12.11 3 20165 145055 90463224
Swelling 22.13 12.11 37 20131 419021 90189258
Haemorrhagic erosive gastritis 22.12 12.11 7 20161 492 90607787
Wrong patient received product 21.67 12.11 12 20156 3465 90604814
Poisoning deliberate 21.08 12.11 22 20146 16464 90591815
Infection 21.00 12.11 30 20138 362064 90246215
Joint swelling 20.97 12.11 51 20117 503249 90105030
Death 20.86 12.11 44 20124 456507 90151772
Psychotic disorder 20.84 12.11 30 20138 31200 90577079
Fibromyalgia 20.70 12.11 10 20158 206259 90402020
Pelvic pain 20.55 12.11 21 20147 15336 90592943
Arthrodesis 20.45 12.11 11 20157 3001 90605278
Arrhythmia 20.37 12.11 35 20133 42297 90565982
Feeding disorder 19.98 12.11 22 20146 17490 90590789
Flatulence 19.64 12.11 34 20134 41333 90566946
Vertigo 19.49 12.11 46 20122 69765 90538514
Coombs negative haemolytic anaemia 19.46 12.11 6 20162 387 90607892
Tongue oedema 19.04 12.11 13 20155 5441 90602838
Abortion spontaneous 18.92 12.11 39 20129 54017 90554262
Hyperoxaluria 18.88 12.11 5 20163 186 90608093
Musculoskeletal stiffness 18.79 12.11 23 20145 296509 90311770
Dermatitis exfoliative generalised 18.75 12.11 13 20155 5580 90602699
Burn oral cavity 18.60 12.11 5 20163 197 90608082
Drug ineffective 18.22 12.11 209 19959 1384089 89224190
Metabolic acidosis 18.13 12.11 39 20129 55637 90552642
Joint range of motion decreased 18.12 12.11 4 20164 135639 90472640
Alopecia 17.75 12.11 54 20114 495017 90113262
Nightmare 17.72 12.11 23 20145 21702 90586577
Urine oxalate increased 17.71 12.11 5 20163 237 90608042
Urticaria thermal 17.66 12.11 6 20162 527 90607752
HLA-B*27 positive 17.47 12.11 5 20163 249 90608030
Guttate psoriasis 17.06 12.11 6 20162 585 90607694
Eosinophilia 17.01 12.11 26 20142 28507 90579772
Intentional product use issue 16.97 12.11 14 20154 216878 90391401
Pharyngeal oedema 16.94 12.11 18 20150 13753 90594526
Shock haemorrhagic 16.85 12.11 17 20151 12228 90596051
Memory impairment 16.36 12.11 12 20156 197232 90411047
Photosensitivity reaction 16.35 12.11 20 20148 17787 90590492
Patent ductus arteriosus 16.21 12.11 11 20157 4558 90603721
Pain 16.16 12.11 143 20025 996198 89612081
Liver injury 16.03 12.11 9 20159 170558 90437721
Keratopathy 16.00 12.11 6 20162 702 90607577
Skin disorder 15.92 12.11 29 20139 36677 90571602
Treatment failure 15.88 12.11 27 20141 303901 90304378
Therapeutic product effect incomplete 15.82 12.11 12 20156 193884 90414395
Abortion 15.67 12.11 9 20159 2786 90605493
Pulmonary embolism 15.56 12.11 64 20104 130756 90477523
Drug dose titration not performed 15.49 12.11 6 20162 766 90607513
Conjunctivitis allergic 15.43 12.11 7 20161 1325 90606954
Intraocular haematoma 15.33 12.11 3 20165 27 90608252
Food intolerance 15.31 12.11 10 20158 3892 90604387
Lower respiratory tract infection 15.30 12.11 20 20148 250639 90357640
Arteriospasm coronary 15.22 12.11 11 20157 5039 90603240
Tenosynovitis stenosans 15.19 12.11 10 20158 3943 90604336
Acarodermatitis 15.17 12.11 7 20161 1379 90606900
Injury 15.12 12.11 13 20155 197336 90410943
Faecal calprotectin increased 15.11 12.11 10 20158 3977 90604302
Amnestic disorder 15.04 12.11 5 20163 411 90607868
Vitamin D deficiency 14.97 12.11 19 20149 17537 90590742
Upper respiratory tract infection bacterial 14.92 12.11 4 20164 156 90608123
Skin laceration 14.51 12.11 23 20145 26012 90582267
Pancoast's syndrome 14.32 12.11 3 20165 39 90608240
Skin papilloma 14.15 12.11 11 20157 5619 90602660
Stomatitis 13.81 12.11 25 20143 274673 90333606
Abdominal discomfort 13.80 12.11 57 20111 477271 90131008
Discomfort 13.76 12.11 25 20143 274310 90333969
Lip oedema 13.74 12.11 10 20158 4629 90603650
Anaphylactic shock 13.74 12.11 25 20143 31592 90576687
Off label use 13.48 12.11 169 19999 1102083 89506196
Lip dry 13.44 12.11 3 20165 100952 90507327
Pericardial effusion 13.39 12.11 27 20141 36806 90571473
Chronic spontaneous urticaria 13.35 12.11 7 20161 1813 90606466
Systolic hypertension 13.27 12.11 5 20163 592 90607687
Subretinal haematoma 13.26 12.11 3 20165 57 90608222
Hypokalaemia 13.19 12.11 61 20107 131055 90477224
Rash erythematous 13.14 12.11 38 20130 65066 90543213
Agranulocytosis 13.14 12.11 26 20142 34976 90573303
Skin lesion 13.12 12.11 27 20141 37338 90570941
Asthmatic crisis 13.04 12.11 7 20161 1903 90606376
Chest discomfort 12.92 12.11 63 20105 138302 90469977
Hallucination 12.84 12.11 38 20130 65921 90542358
Hypersensitivity pneumonitis 12.82 12.11 9 20159 3939 90604340
Road traffic accident 12.80 12.11 4 20164 107622 90500657
Pulmonary fibrosis 12.78 12.11 4 20164 107499 90500780
Ligament sprain 12.76 12.11 16 20152 14583 90593696
Foetal exposure during pregnancy 12.74 12.11 29 20139 42946 90565333
Maternal exposure before pregnancy 12.64 12.11 14 20154 11199 90597080
Dyspnoea exertional 12.54 12.11 40 20128 72248 90536031
Retinal exudates 12.53 12.11 5 20163 691 90607588
Hypersensitivity vasculitis 12.40 12.11 9 20159 4150 90604129
Swelling face 12.32 12.11 43 20125 81309 90526970
Pharyngeal swelling 12.23 12.11 13 20155 9931 90598348
Bunion operation 12.23 12.11 6 20162 1352 90606927
Anaphylactic reaction 12.18 12.11 45 20123 87479 90520800
Nasal pruritus 12.17 12.11 5 20163 745 90607534
Gastrointestinal erosion 12.13 12.11 5 20163 750 90607529

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
Intentional overdose 70.71 14.22 74 10208 51382 42559671
Dermatitis bullous 63.75 14.22 34 10248 8422 42602631
Pemphigoid 59.20 14.22 36 10246 11431 42599622
Troponin T increased 52.02 14.22 21 10261 2759 42608294
Eosinophilia 46.40 14.22 48 10234 32851 42578202
Rash maculo-papular 46.33 14.22 51 10231 37452 42573601
Toxic skin eruption 46.22 14.22 33 10249 13697 42597356
Death 41.43 14.22 32 10250 471153 42139900
Hepatic haematoma 40.11 14.22 11 10271 431 42610622
Hyperleukocytosis 39.68 14.22 17 10265 2591 42608462
Urticaria 39.56 14.22 67 10215 73969 42537084
Hyperkaliuria 38.15 14.22 8 10274 96 42610957
Pruritus 35.46 14.22 113 10169 188658 42422395
Corneal abscess 35.42 14.22 6 10276 19 42611034
N-terminal prohormone brain natriuretic peptide increased 35.12 14.22 17 10265 3436 42607617
Electrocardiogram QT prolonged 34.84 14.22 50 10232 47895 42563158
Acute generalised exanthematous pustulosis 34.44 14.22 23 10259 8572 42602481
Prothrombin time abnormal 32.61 14.22 11 10271 872 42610181
Oral dysaesthesia 31.81 14.22 7 10275 107 42610946
Hypertrophic cardiomyopathy 30.66 14.22 12 10270 1453 42609600
Electrocardiogram T wave peaked 30.10 14.22 10 10272 756 42610297
Ischaemic cerebral infarction 29.33 14.22 12 10270 1631 42609422
Livedo reticularis 29.30 14.22 14 10268 2750 42608303
Arrhythmia 29.22 14.22 42 10240 40275 42570778
Pancreatitis acute 28.89 14.22 38 10244 33526 42577527
Xerosis 28.35 14.22 10 10272 906 42610147
Disease prodromal stage 26.79 14.22 5 10277 31 42611022
Hepatitis fulminant 26.70 14.22 16 10266 4943 42606110
Caput succedaneum 26.19 14.22 6 10276 111 42610942
Wrong patient received product 25.86 14.22 14 10268 3569 42607484
Rash pustular 25.79 14.22 17 10265 6198 42604855
Purpura 25.73 14.22 22 10260 11857 42599196
Keratitis 25.05 14.22 11 10271 1780 42609273
Blood immunoglobulin E decreased 24.00 14.22 5 10277 58 42610995
Prurigo 23.31 14.22 8 10274 668 42610385
Eczema 22.52 14.22 34 10248 34052 42577001
Angioedema 22.09 14.22 38 10244 42439 42568614
Eyelid ptosis congenital 21.85 14.22 5 10277 92 42610961
Dermatitis exfoliative 21.79 14.22 16 10266 6931 42604122
Miosis 21.48 14.22 21 10261 13425 42597628
Oedema genital 20.96 14.22 7 10275 538 42610515
Rhabdomyolysis 20.75 14.22 53 10229 77966 42533087
Bulbar palsy 20.66 14.22 6 10276 290 42610763
Suicide attempt 19.85 14.22 38 10244 46062 42564991
Alopecia areata 19.67 14.22 6 10276 344 42610709
Cholangiocarcinoma 19.49 14.22 9 10273 1637 42609416
Troponin I increased 19.18 14.22 11 10271 3135 42607918
Polyuria 18.60 14.22 17 10265 9994 42601059
Spermatic cord disorder 17.83 14.22 3 10279 9 42611044
Dermatitis psoriasiform 17.32 14.22 9 10273 2113 42608940
Rhinitis allergic 17.14 14.22 11 10271 3831 42607222
Retinopathy 16.71 14.22 9 10273 2272 42608781
Type III immune complex mediated reaction 16.67 14.22 6 10276 576 42610477
Hepatic cytolysis 16.64 14.22 26 10256 26818 42584235
Wrong product administered 16.57 14.22 13 10269 6213 42604840
Hyperlipasaemia 16.52 14.22 6 10276 591 42610462
Cardiac pacemaker evaluation 15.37 14.22 4 10278 128 42610925
Neonatal pneumonia 15.28 14.22 4 10278 131 42610922
Enuresis 15.14 14.22 9 10273 2739 42608314
Myoglobin blood increased 15.10 14.22 10 10272 3672 42607381
Hyperkalaemia 14.91 14.22 48 10234 80410 42530643
Acute haemorrhagic oedema of infancy 14.80 14.22 3 10279 30 42611023
Sinus bradycardia 14.65 14.22 18 10264 14835 42596218
Renal tubular necrosis 14.60 14.22 20 10262 18334 42592719
Intentional self-injury 14.31 14.22 18 10264 15184 42595869
Purulent pericarditis 14.30 14.22 3 10279 36 42611017

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
Angioedema 162.45 11.73 156 26362 98344 110464437
Intentional overdose 130.74 11.73 160 26358 132341 110430440
Urticaria 98.01 11.73 228 26290 318629 110244152
Dermatitis bullous 95.87 11.73 57 26461 17472 110545309
Toxic skin eruption 85.81 11.73 63 26455 27452 110535329
Rash maculo-papular 77.03 11.73 92 26426 74130 110488651
Pruritus 76.85 11.73 309 26209 581251 109981530
Nasal ulcer 71.76 11.73 26 26492 2561 110560220
Endocrine ophthalmopathy 66.60 11.73 21 26497 1352 110561429
Erythema 64.26 11.73 184 26334 291263 110271518
Eosinophilia 62.07 11.73 73 26445 57863 110504918
Acute kidney injury 57.40 11.73 302 26216 635128 109927653
Pemphigoid 56.71 11.73 43 26475 19664 110543117
Toxic shock syndrome 56.49 11.73 19 26499 1501 110561280
Allergy test positive 52.72 11.73 16 26502 907 110561874
Face oedema 51.37 11.73 51 26467 33418 110529363
Eczema 50.80 11.73 74 26444 72219 110490562
Hyponatraemia 49.49 11.73 139 26379 217514 110345267
Drug intolerance 49.19 11.73 18 26500 406494 110156287
Somnolence 49.16 11.73 170 26348 297279 110265502
Hyperkalaemia 48.27 11.73 103 26415 135693 110427088
Wrong patient received product 48.10 11.73 26 26492 6648 110556133
Eyelid disorder 47.99 11.73 19 26499 2386 110560395
Drug reaction with eosinophilia and systemic symptoms 47.77 11.73 77 26441 82018 110480763
Coma 47.31 11.73 94 26424 117775 110445006
Arrhythmia 47.12 11.73 70 26448 69505 110493276
Electrocardiogram QT prolonged 45.06 11.73 88 26430 108872 110453909
Suicide attempt 44.59 11.73 85 26433 103309 110459472
Death 44.14 11.73 62 26456 698807 109863974
Troponin T increased 43.30 11.73 21 26497 4285 110558496
Hallucination, auditory 41.95 11.73 41 26477 26356 110536425
Hand deformity 40.86 11.73 3 26515 218503 110344278
Inflammatory bowel disease 40.80 11.73 24 26494 7210 110555571
Pancreatitis acute 39.90 11.73 60 26458 60214 110502567
Hepatic cytolysis 39.61 11.73 57 26461 54996 110507785
Wound 39.17 11.73 5 26513 234432 110328349
Glossodynia 38.93 11.73 4 26514 222000 110340781
Systemic lupus erythematosus 38.89 11.73 7 26511 254331 110308450
Hyperleukocytosis 38.33 11.73 18 26500 3421 110559360
Terminal dribbling 37.77 11.73 6 26512 11 110562770
Cholestasis 36.83 11.73 60 26458 64458 110498323
Rheumatoid arthritis 35.01 11.73 14 26504 299599 110263182
Swelling of eyelid 34.73 11.73 21 26497 6632 110556149
Aggression 33.71 11.73 55 26463 59155 110503626
Acute generalised exanthematous pustulosis 33.22 11.73 33 26485 21631 110541150
Hyperkaliuria 33.15 11.73 8 26510 188 110562593
Mean cell haemoglobin increased 32.64 11.73 19 26499 5598 110557183
Anti-cyclic citrullinated peptide antibody positive 32.64 11.73 3 26515 181981 110380800
Helicobacter infection 32.61 11.73 3 26515 181874 110380907
Rhabdomyolysis 32.52 11.73 82 26436 120319 110442462
Blood immunoglobulin E increased 32.46 11.73 21 26497 7461 110555320
Completed suicide 32.38 11.73 9 26509 242372 110320409
Hepatic haematoma 31.71 11.73 11 26507 954 110561827
Duodenal ulcer perforation 31.68 11.73 3 26515 177697 110385084
Oral dysaesthesia 30.60 11.73 8 26510 262 110562519
Pemphigus 30.53 11.73 7 26511 214563 110348218
Livedo reticularis 30.35 11.73 18 26500 5488 110557293
Hepatocellular injury 30.14 11.73 48 26470 50594 110512187
Vertigo 29.84 11.73 65 26453 86805 110475976
Corneal abscess 28.80 11.73 6 26512 70 110562711
Prothrombin time abnormal 28.66 11.73 11 26507 1271 110561510
Poisoning deliberate 27.90 11.73 33 26485 26298 110536483
Cerebral thrombosis 27.86 11.73 13 26505 2435 110560346
Rash erythematous 27.84 11.73 61 26457 81771 110481010
Impaired healing 26.85 11.73 7 26511 196710 110366071
Alopecia areata 26.09 11.73 12 26506 2175 110560606
Pericarditis 25.99 11.73 10 26508 219104 110343677
Gestational hypertension 25.85 11.73 12 26506 2222 110560559
Electrocardiogram T wave peaked 25.84 11.73 10 26508 1182 110561599
Therapeutic product effect incomplete 25.27 11.73 11 26507 223794 110338987
Victim of chemical submission 25 11.73 9 26509 870 110561911
Hypertrophic cardiomyopathy 24.70 11.73 13 26505 3150 110559631
Synovial cyst 24.51 11.73 21 26497 11409 110551372
Prurigo 24.28 11.73 10 26508 1390 110561391
Irritable bowel syndrome 24.08 11.73 5 26513 164210 110398571
Skin dystrophy 23.95 11.73 5 26513 59 110562722
Oedema genital 23.76 11.73 8 26510 634 110562147
Disease prodromal stage 23.72 11.73 5 26513 62 110562719
N-terminal prohormone brain natriuretic peptide increased 23.69 11.73 16 26502 6105 110556676
Paranoia 23.64 11.73 28 26490 22346 110540435
Ischaemic cerebral infarction 22.70 11.73 12 26506 2933 110559848
Abortion spontaneous 22.50 11.73 34 26484 34248 110528533
Therapeutic product effect decreased 21.85 11.73 16 26502 244300 110318481
Purpura 21.71 11.73 28 26490 24360 110538421
Psoriatic arthropathy 21.69 11.73 10 26508 196751 110366030
Intentional self-injury 21.62 11.73 35 26483 37394 110525387
Vitamin D decreased 21.36 11.73 20 26498 12195 110550586
Hepatitis fulminant 21.00 11.73 17 26501 8543 110554238
Folliculitis 20.99 11.73 7 26511 167646 110395135
Synovitis 20.80 11.73 21 26497 274071 110288710
Arthrodesis 20.74 11.73 11 26507 2707 110560074
Dermatitis exfoliative 20.65 11.73 19 26499 11328 110551453
Urinary retention 20.45 11.73 49 26469 69634 110493147
Onycholysis 20.44 11.73 11 26507 2788 110559993
Oxalosis 19.91 11.73 5 26513 139 110562642
Tooth injury 19.76 11.73 10 26508 2236 110560545
Xerosis 19.52 11.73 9 26509 1640 110561141
Abortion 19.50 11.73 9 26509 1645 110561136
Bulbar palsy 19.45 11.73 6 26512 359 110562422
Joint range of motion decreased 19.40 11.73 3 26515 121829 110440952
HLA-B*27 positive 19.36 11.73 5 26513 156 110562625
Type IV hypersensitivity reaction 19.23 11.73 14 26504 6019 110556762
Enuresis 19.02 11.73 12 26506 4084 110558697
Myalgia 18.85 11.73 104 26414 222277 110340504
Intentional product use issue 18.80 11.73 19 26499 247887 110314894
Burn oral cavity 18.70 11.73 5 26513 179 110562602
Pelvic pain 18.60 11.73 21 26497 15921 110546860
Haemorrhagic erosive gastritis 18.53 11.73 7 26511 775 110562006
Eye infection 18.45 11.73 20 26498 14498 110548283
Nightmare 18.06 11.73 33 26485 38830 110523951
Stomatitis 18.01 11.73 23 26495 270219 110292562
Miosis 17.66 11.73 24 26494 21959 110540822
Urine oxalate increased 17.63 11.73 5 26513 223 110562558
Hypersensitivity vasculitis 17.49 11.73 14 26504 6923 110555858
Altered state of consciousness 17.42 11.73 41 26477 57585 110505196
Tongue oedema 17.36 11.73 15 26503 8241 110554540
Dermatitis exfoliative generalised 17.36 11.73 17 26501 10955 110551826
Urticaria thermal 17.24 11.73 6 26512 525 110562256
Disease progression 17.07 11.73 20 26498 244014 110318767
Guttate psoriasis 17.03 11.73 6 26512 545 110562236
Maternal exposure before pregnancy 16.92 11.73 14 26504 7251 110555530
Dyslipidaemia 16.90 11.73 20 26498 15945 110546836
Fibromyalgia 16.90 11.73 10 26508 170899 110391882
Feeding disorder 16.67 11.73 23 26495 21339 110541442
Coombs negative haemolytic anaemia 16.59 11.73 6 26512 588 110562193
Keratitis 16.54 11.73 12 26506 5132 110557649
Type III immune complex mediated reaction 16.51 11.73 7 26511 1046 110561735
Musculoskeletal stiffness 16.48 11.73 26 26492 279796 110282985
Cerebral venous thrombosis 16.27 11.73 10 26508 3252 110559529
Sinus bradycardia 16.26 11.73 27 26491 29456 110533325
Fixed eruption 16.23 11.73 11 26507 4221 110558560
Sudden death 15.74 11.73 24 26494 24371 110538410
Type 2 diabetes mellitus 15.34 11.73 12 26506 177220 110385561
Dermatitis psoriasiform 15.25 11.73 10 26508 3634 110559147
Hyperoxaluria 15.21 11.73 5 26513 368 110562413
Rash pustular 15.14 11.73 17 26501 12812 110549969
Cardiac pacemaker evaluation 15.10 11.73 4 26514 138 110562643
Chronic spontaneous urticaria 15.02 11.73 8 26510 1985 110560796
Photosensitivity reaction 14.88 11.73 24 26494 25565 110537216
Anaphylactic shock 14.86 11.73 36 26482 51510 110511271
Pain 14.81 11.73 152 26366 954803 109607978
Cholangiocarcinoma 14.78 11.73 9 26509 2876 110559905
Hypotension 14.74 11.73 191 26327 523658 110039123
Chest discomfort 14.52 11.73 81 26437 173767 110389014
Arteriospasm coronary 14.21 11.73 14 26504 9086 110553695
Hyperlipasaemia 14.19 11.73 7 26511 1482 110561299
Platelet count decreased 13.96 11.73 21 26497 230422 110332359
Bunion operation 13.90 11.73 6 26512 936 110561845
Myoglobin blood increased 13.90 11.73 10 26508 4222 110558559
White blood cell count decreased 13.81 11.73 21 26497 229369 110333412
Contraindicated product administered 13.75 11.73 24 26494 248243 110314538
Bursitis 13.71 11.73 7 26511 129911 110432870
Infection 13.66 11.73 43 26475 362157 110200624
Skin plaque 13.65 11.73 16 26502 12629 110550152
Hepatic enzyme increased 13.63 11.73 36 26482 320856 110241925
Rhinitis allergic 13.54 11.73 19 26499 17903 110544878
Upper respiratory tract infection bacterial 13.49 11.73 4 26514 209 110562572
Retinopathy 13.49 11.73 10 26508 4419 110558362
Skin disorder 13.49 11.73 31 26487 42882 110519899
Hallucination 13.41 11.73 54 26464 101378 110461403
Drug level increased 13.40 11.73 33 26485 47686 110515095
Acute haemorrhagic oedema of infancy 13.35 11.73 3 26515 51 110562730
Off label use 13.30 11.73 267 26251 1499918 109062863
Pharyngeal oedema 13.29 11.73 18 26500 16410 110546371
Drug dose titration not performed 13.20 11.73 6 26512 1059 110561722
Lip swelling 13.15 11.73 34 26484 50633 110512148
Febrile neutropenia 13.11 11.73 36 26482 316731 110246050
Swelling 13.01 11.73 42 26476 350999 110211782
Tenosynovitis stenosans 12.96 11.73 9 26509 3594 110559187
Memory impairment 12.87 11.73 17 26501 196927 110365854
Hypokalaemia 12.67 11.73 81 26437 182367 110380414
Treatment failure 12.63 11.73 30 26488 277204 110285577
Drug ineffective 12.48 11.73 274 26244 1520266 109042515
Lip oedema 12.44 11.73 12 26506 7588 110555193
Sepsis 12.24 11.73 39 26479 327307 110235474
Anaphylactic reaction 12.16 11.73 57 26461 114243 110448538
Lower respiratory tract infection 12.15 11.73 25 26493 243081 110319700
Liver injury 12.02 11.73 11 26507 150402 110412379
Suffocation feeling 11.96 11.73 7 26511 2084 110560697
Nutritional condition abnormal 11.94 11.73 6 26512 1321 110561460
Coronavirus infection 11.87 11.73 13 26505 9532 110553249
Amnestic disorder 11.81 11.73 5 26513 745 110562036
Keratopathy 11.75 11.73 6 26512 1367 110561414

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AX27 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
FDA MoA N0000000190 Histamine H1 Receptor Antagonists
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018494 Histamine Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:37955 H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role CHEBI:48873 cholinergic antagonist
CHEBI has role CHEBI:49103 drug metabolite
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:50857 anti-allergic agent
CHEBI has role CHEBI:66981 ophthalmology drug

Related Drugs by ATC class:

R06AX Other antihistamines for systemic use 26 drugs
acrivastineantazolineastemizoleazatadineazelastinebamipinebilastinecyproheptadinedeptropineebastineepinastinefexofenadine show all 26 →

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

DiseaseRelationSNOMED_IDDOID
Vasomotor rhinitis indication 8229003 DOID:4730
Allergic urticaria indication 40178009 DOID:10612
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Sneezing indication 76067001
Common cold indication 82272006 DOID:10459
Chronic idiopathic urticaria indication 302162004
Seasonal allergic rhinitis indication 367498001
Allergic conjunctivitis indication 473460002 DOID:11204
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Diabetes mellitus contraindication 73211009 DOID:9351
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Angle-closure glaucoma contraindication 392291006 DOID:13550
Hypertensive urgency contraindication 443482000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.92 Basic
pKa2 2.48 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 9.40 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 7.30 WOMBAT-PK
Multidrug resistance protein 1 Transporter IC50 4.37 WOMBAT-PK
Sodium-dependent serotonin transporter Transporter Ki 6.91 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.96 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 8.03 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 7.55 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 7.80 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 6.00 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.01 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.19 DRUG MATRIX
Histamine H2 receptor GPCR Ki 5.97 DRUG MATRIX
Histamine H4 receptor GPCR IC50 4.80 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 7.74 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 7.60 WOMBAT-PK
Muscarinic acetylcholine receptor M3 GPCR Ki 7.49 WOMBAT-PK
Sodium-dependent dopamine transporter Transporter Ki 5.51 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 7.70 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR Ki 5.70 DRUG MATRIX

External reference:

IDSource
4021292 VUID
N0000148729 NUI
D03693 KEGG_DRUG
275635 RXNORM
4021292 VANDF
C0908935 UMLSCUI
CHEBI:291342 CHEBI
Y5R PDB_CHEM_ID
CHEMBL1172 ChEMBL_ID
DB00967 DRUGBANK_ID
C121345 MESH_SUPPLEMENTAL_RECORD_UI
124087 PUBCHEM_CID
7157 IUPHAR_LIGAND_ID
7817 INN_ID
FVF865388R UNII
16243 MMSL
83662 MMSL
d04785 MMSL
009081 NDDF
134506008 SNOMEDCT_US
396015008 SNOMEDCT_US
FVF865388R INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Clarinex HUMAN PRESCRIPTION DRUG LABEL 1 21695-815 TABLET, FILM COATED 5 mg ORAL NDA 23 sections
Clarinex HUMAN PRESCRIPTION DRUG LABEL 1 50090-0765 TABLET, FILM COATED 5 mg ORAL NDA 29 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 50090-3975 TABLET 5 mg ORAL ANDA 29 sections
DESLORATADINE HUMAN PRESCRIPTION DRUG LABEL 1 50090-4794 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
DESLORATADINE HUMAN PRESCRIPTION DRUG LABEL 1 50090-6724 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Clarinex HUMAN PRESCRIPTION DRUG LABEL 1 54868-4624 TABLET, FILM COATED 5 mg ORAL NDA 12 sections
Clarinex-D 12 Hour HUMAN PRESCRIPTION DRUG LABEL 2 54868-5708 TABLET, EXTENDED RELEASE 2.50 mg ORAL NDA 29 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 55111-360 TABLET, ORALLY DISINTEGRATING 5 mg ORAL ANDA 26 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 55111-551 TABLET, ORALLY DISINTEGRATING 2.50 mg ORAL ANDA 26 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 62250-619 TABLET 5 mg ORAL ANDA 25 sections
Desloratadine Human Prescription Drug Label 1 62756-523 TABLET, FILM COATED 5 mg ORAL ANDA 28 sections
DESLORATADINE HUMAN PRESCRIPTION DRUG LABEL 1 68180-153 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Desloratadine Human Prescription Drug Label 1 69339-194 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 69452-363 TABLET, FILM COATED 5 mg ORAL ANDA 21 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 69543-107 TABLET 5 mg ORAL ANDA 29 sections
DESLORATADINE HUMAN PRESCRIPTION DRUG LABEL 1 71335-1000 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 72162-2308 TABLET 5 mg ORAL ANDA 28 sections
Desloratadine HUMAN PRESCRIPTION DRUG LABEL 1 72162-2308 TABLET 5 mg ORAL ANDA 28 sections
Desloratadine Oral Solution HUMAN PRESCRIPTION DRUG LABEL 1 74157-011 SOLUTION 0.50 mg ORAL ANDA 30 sections
Clarinex HUMAN PRESCRIPTION DRUG LABEL 1 78206-119 TABLET, FILM COATED 5 mg ORAL NDA 29 sections
CLARINEX-D 12 HOUR HUMAN PRESCRIPTION DRUG LABEL 2 78206-120 TABLET, EXTENDED RELEASE 2.50 mg ORAL NDA 29 sections
CLARINEX-D 12 HOUR HUMAN PRESCRIPTION DRUG LABEL 2 78206-120 TABLET, EXTENDED RELEASE 2.50 mg ORAL NDA 29 sections
Clarinex HUMAN PRESCRIPTION DRUG LABEL 1 78206-188 TABLET, FILM COATED 5 mg ORAL NDA 29 sections