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

Stem definitionDrug idCAS RN
antihistaminics/cerebral (or peripheral) vasodilators 1566 130018-77-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • levocetirizine hydrochloride
  • xyzal
  • levocetirizine
  • levocetirizine dihydrochloride
  • (R)-cetirizine
  • levocetirizine HCl
  • Molecular weight: 388.89
  • Formula: C21H25ClN2O3
  • CLOGP: 2.08
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 53.01
  • ALOGS: -3.77
  • ROTB: 8
  • 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) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 23 mg/mL Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine) 71 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.18 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.303 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.600 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 11.995 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.404 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 12.250 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 15.160 % High 1
herg hERG pIC50 4.701 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 2.529 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.281 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 13.650 % High 1
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K7,MAPK14,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK,TGFBR1,ZAP70 29
kinase-selectivity-class AXL,GRK2 2
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 8.670 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 3.296 High 1
mh-clint Mouse hepatocyte intrinsic clearance 11.885 High 1
mppb Mouse plasma protein binding (% unbound) 17.950 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 5.888 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 Moderate 0.76
pppb Pig plasma protein binding (% unbound) 17.710 % High 1
rat-kpuu-brain Rat brain Kpuu 0.062 % High 1
rh-clint Rat hepatocyte intrinsic clearance 3.899 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 87.090 % High 1
rppb Rat plasma protein binding (% unbound) 17.850 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 912.011 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 25, 2007 FDA UCB INC

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
Dermatitis atopic 221.74 10.38 134 39174 23338 90565801
Joint destruction 188.40 10.38 99 39209 13188 90575951
Drug tolerance 173.67 10.38 104 39204 17812 90571327
Polyarthritis 168.80 10.38 103 39205 18247 90570892
Adrenal insufficiency 129.71 10.38 106 39202 29815 90559324
Immunodeficiency 99.94 10.38 108 39200 43126 90546013
Product use in unapproved indication 96.69 10.38 343 38965 335893 90253246
Psoriasis 89.67 10.38 198 39110 147556 90441583
Asthma 85.61 10.38 265 39043 241895 90347244
Dry skin 71.24 10.38 133 39175 87940 90501199
Pruritus 68.48 10.38 435 38873 541090 90048049
Foot deformity 66.64 10.38 104 39204 59547 90529592
Gastroenteritis viral 63.54 10.38 72 39236 30283 90558856
Skin fissures 58.96 10.38 58 39250 20751 90568388
Eczema 57.42 10.38 91 39217 52779 90536360
Toxicity to various agents 55.11 10.38 28 39280 287818 90301321
Urticaria 53.84 10.38 273 39035 312461 90276678
Loss of consciousness 53.77 10.38 158 39150 140080 90449059
Lower respiratory tract infection 53.29 10.38 21 39287 250638 90338501
Injection site pain 52.25 10.38 180 39128 173519 90415620
Limb discomfort 52.07 10.38 73 39235 37987 90551152
Nodule 51.99 10.38 61 39247 26625 90562514
Red blood cell sedimentation rate abnormal 51.66 10.38 58 39250 24146 90564993
Death 51.38 10.38 74 39234 456477 90132662
COVID-19 50.82 10.38 175 39133 168668 90420471
Confusional state 48.15 10.38 58 39250 386147 90202992
Skin exfoliation 45.75 10.38 95 39213 67818 90521321
Anaphylactic reaction 45.06 10.38 110 39198 87414 90501725
Exposure via skin contact 42.39 10.38 36 39272 10669 90578470
Impaired quality of life 41.96 10.38 51 39257 23093 90566046
Angioedema 41.67 10.38 89 39219 64787 90524352
Joint swelling 41.20 10.38 99 39209 503201 90085938
Infusion related reaction 39.93 10.38 75 39233 416705 90172434
Product dose omission issue 39.71 10.38 239 39069 291448 90297691
Bronchitis 39.64 10.38 151 39157 152776 90436363
Completed suicide 38.46 10.38 8 39300 145050 90444089
Hypocalcaemia 38.08 10.38 67 39241 42301 90546838
Dry eye 37.81 10.38 80 39228 57851 90531288
Impaired healing 35.06 10.38 30 39278 234169 90354970
Ankle arthroplasty 34.28 10.38 19 39289 2812 90586327
Muscle injury 34.07 10.38 17 39291 176637 90412502
Arthritis 33.03 10.38 152 39156 167163 90421976
Folliculitis 32.04 10.38 25 39283 204328 90384811
Hypokalaemia 31.97 10.38 127 39181 130989 90458150
Cough 30.37 10.38 268 39040 368694 90220445
Upper respiratory tract infection 30.25 10.38 123 39185 128195 90460944
Nasal congestion 29.15 10.38 91 39217 83323 90505816
Illness 28.26 10.38 89 39219 81880 90507259
Eye pruritus 27.52 10.38 47 39261 28980 90560159
Nail growth abnormal 26.72 10.38 10 39298 592 90588547
Face oedema 26.51 10.38 41 39267 23277 90565862
Cerebral disorder 26.42 10.38 21 39287 5673 90583466
Product dose omission in error 26.09 10.38 38 39270 20465 90568674
No adverse event 25.47 10.38 76 39232 67906 90521233
Foot operation 25.33 10.38 25 39283 8976 90580163
Pulmonary fibrosis 25.30 10.38 103 39205 107400 90481739
Irritable bowel syndrome 24.94 10.38 32 39276 207416 90381723
Dermatitis contact 24.71 10.38 30 39278 13565 90575574
Injection site rash 24.06 10.38 40 39268 24133 90565006
Sleep disorder due to a general medical condition 23.84 10.38 57 39251 44681 90544458
Hepatitis chronic active 23.62 10.38 6 39302 94 90589045
Ear infection 23.36 10.38 75 39233 69700 90519439
Hepatic enzyme increased 22.87 10.38 80 39228 360656 90228483
Therapeutic product effect decreased 22.50 10.38 201 39107 277370 90311769
Sleep disorder due to general medical condition, insomnia type 22.48 10.38 14 39294 128680 90460459
Therapy non-responder 21.86 10.38 117 39191 136587 90452552
Lymphorrhoea 21.15 10.38 5 39303 57 90589082
Underdose 20.82 10.38 61 39247 53956 90535183
Eye oedema 20.67 10.38 12 39296 1940 90587199
Lip dry 20.56 10.38 9 39299 100946 90488193
Injection site erythema 20.56 10.38 91 39217 98411 90490728
Therapeutic response shortened 20.32 10.38 36 39272 22843 90566296
Prescribed overdose 20.23 10.38 90 39218 97535 90491604
Hemianopia 19.95 10.38 12 39296 2070 90587069
Joint range of motion decreased 19.54 10.38 18 39290 135625 90453514
Bursitis 19.53 10.38 17 39291 131637 90457502
Rash 19.49 10.38 467 38841 795633 89793506
Urine glucose/creatinine ratio increased 19.45 10.38 6 39302 196 90588943
Myocardial infarction 19.25 10.38 11 39297 105961 90483178
Rheumatoid factor positive 19.25 10.38 134 39174 171516 90417623
Hereditary angioedema 19.23 10.38 22 39286 9343 90579796
Pleural effusion 18.69 10.38 97 39211 111894 90477245
Retinitis 18.38 10.38 47 39261 38411 90550728
C-reactive protein abnormal 18.25 10.38 17 39291 127412 90461727
Injection site urticaria 18.19 10.38 30 39278 17981 90571158
Injection site swelling 17.96 10.38 62 39246 59777 90529362
Hyponatraemia 17.76 10.38 19 39289 133519 90455620
Gastrointestinal disorder 17.59 10.38 55 39253 256632 90332507
Erythema multiforme 17.51 10.38 24 39284 12222 90576917
Drug abuse 17.32 10.38 7 39301 82340 90506799
Wheelchair user 17.20 10.38 19 39289 7766 90581373
Intentional product use issue 17.03 10.38 156 39152 216736 90372403
Infusion site swelling 16.81 10.38 23 39285 11697 90577442
Fixed eruption 16.65 10.38 10 39298 1720 90587419
Upper-airway cough syndrome 16.36 10.38 26 39282 15109 90574030
Oculomucocutaneous syndrome 16.22 10.38 5 39303 163 90588976
Helicobacter infection 15.97 10.38 48 39260 226802 90362337
Hepatitis cholestatic 15.74 10.38 19 39289 8542 90580597
Skin haemorrhage 15.69 10.38 31 39277 21349 90567790
Anaemia vitamin B12 deficiency 15.54 10.38 7 39301 665 90588474
Duodenal ulcer perforation 15.45 10.38 47 39261 221241 90367898
Hepatic encephalopathy 15.36 10.38 24 39284 13748 90575391
Alopecia areata 15.25 10.38 10 39298 2005 90587134
Lung disorder 15.20 10.38 26 39282 149857 90439282
Cardiac arrest 15.02 10.38 14 39294 104921 90484218
Cerebrovascular accident 14.90 10.38 19 39289 123514 90465625
Ocular hyperaemia 14.82 10.38 40 39268 33758 90555381
Sensitive skin 14.69 10.38 12 39296 3369 90585770
Drug interaction 14.54 10.38 66 39242 276387 90312752
Gastrointestinal haemorrhage 14.19 10.38 11 39297 90237 90498902
Erythema 14.19 10.38 157 39151 229089 90360050
Infusion site erythema 14.11 10.38 23 39285 13647 90575492
Prescribed underdose 13.95 10.38 67 39241 74952 90514187
Blood pressure systolic increased 13.93 10.38 4 39304 58341 90530798
Cholangiocarcinoma 13.77 10.38 8 39300 1295 90587844
Accidental exposure to product 13.69 10.38 45 39263 42321 90546818
Drug eruption 13.66 10.38 40 39268 35367 90553772
Breast cancer stage III 13.65 10.38 10 39298 84437 90504702
Stomatitis 13.61 10.38 67 39241 274631 90314508
Papule 13.48 10.38 17 39291 7985 90581154
Muscle oedema 13.44 10.38 3 39305 26 90589113
Septic shock 13.43 10.38 72 39236 84088 90505051
Asthenia 13.22 10.38 158 39150 533593 90055546
Inflammation 13.14 10.38 37 39271 178555 90410584
Visual impairment 12.93 10.38 100 39208 132265 90456874
Nasal obstruction 12.91 10.38 10 39298 2602 90586537
Cytogenetic analysis abnormal 12.84 10.38 7 39301 1003 90588136
Gait inability 12.60 10.38 28 39280 146428 90442711
Multiple organ dysfunction syndrome 12.54 10.38 7 39301 68329 90520810
Nail disorder 12.46 10.38 5 39303 59062 90530077
Exposure during pregnancy 12.43 10.38 158 39150 238252 90350887
Idiopathic urticaria 12.42 10.38 5 39303 360 90588779
Mast cell activation syndrome 12.28 10.38 8 39300 1586 90587553
Abortion induced 12.27 10.38 20 39288 11868 90577271
Neutropenia 12.24 10.38 53 39255 224851 90364288
Renal artery stenosis 12.24 10.38 9 39299 2168 90586971
Laryngitis 12.23 10.38 49 39259 50704 90538435
General physical health deterioration 12.21 10.38 97 39211 355018 90234121
Condition aggravated 12.10 10.38 341 38967 595204 89993935
Liver injury 12.05 10.38 120 39188 170447 90418692
Dyspepsia 11.85 10.38 45 39263 198115 90391024
Frequent bowel movements 11.71 10.38 5 39303 56930 90532209
Haemoglobin decreased 11.59 10.38 34 39274 161922 90427217
Alopecia totalis 11.54 10.38 5 39303 433 90588706
Contusion 11.47 10.38 63 39245 251153 90337986
Histone antibody positive 11.43 10.38 4 39304 195 90588944
Chronic spontaneous urticaria 11.32 10.38 8 39300 1812 90587327
Fibromyalgia 11.31 10.38 138 39170 206131 90383008
Facet joint syndrome 10.99 10.38 16 39292 98373 90490766
Enzyme level increased 10.93 10.38 5 39303 493 90588646
Hyperventilation 10.87 10.38 14 39294 6714 90582425
Seronegative arthritis 10.55 10.38 24 39284 18210 90570929
Lupus vulgaris 10.46 10.38 43 39265 45016 90544123
Disease progression 10.41 10.38 34 39274 156581 90432558
Drug-induced liver injury 10.41 10.38 71 39237 90247 90498892
Blood pressure increased 10.40 10.38 131 39177 197086 90392053
Blood pressure orthostatic 10.38 10.38 3 39305 78 90589061

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
Dermatitis atopic 108.91 14.01 59 12493 12345 42596438
Pruritus 91.28 14.01 183 12369 188588 42420195
Foetal malformation 79.98 14.01 17 12535 176 42608607
Asthma 57.77 14.01 81 12471 62233 42546550
Trisomy 18 54.68 14.01 17 12535 848 42607935
Fixed eruption 50.49 14.01 21 12531 2433 42606350
Erythema 43.78 14.01 98 12454 108695 42500088
Sinusitis 41.64 14.01 60 12492 47232 42561551
Injection site pain 39.21 14.01 65 12487 57733 42551050
Urticaria 38.34 14.01 74 12478 73962 42534821
Alopecia areata 35.86 14.01 10 12542 340 42608443
Drug-induced liver injury 34.34 14.01 49 12503 38224 42570559
Eczema 34.11 14.01 46 12506 34040 42574743
Dry skin 33.64 14.01 55 12497 48283 42560500
Febrile convulsion 28.90 14.01 10 12542 699 42608084
No adverse event 27.96 14.01 45 12507 38976 42569807
Hypothermia 26.56 14.01 25 12527 12490 42596293
Middle ear inflammation 26.30 14.01 7 12545 199 42608584
Neonatal hyponatraemia 26.18 14.01 6 12546 90 42608693
Product use in unapproved indication 25.72 14.01 115 12437 184341 42424442
Rash 25.65 14.01 154 12398 276800 42331983
Skin fissures 23.81 14.01 21 12531 9655 42599128
Drug eruption 22.87 14.01 31 12521 23044 42585739
Cough 22.58 14.01 108 12444 177995 42430788
Generalised bullous fixed drug eruption 20.95 14.01 7 12545 440 42608343
Anaphylactic reaction 20.04 14.01 41 12511 42702 42566081
Eyelid oedema 19.55 14.01 15 12537 5680 42603103
Erythema multiforme 19.42 14.01 19 12533 9958 42598825
Impetigo 19.38 14.01 9 12543 1357 42607426
Death 19.05 14.01 73 12479 471112 42137671
Pemphigoid 18.96 14.01 20 12532 11447 42597336
Drug abuse 18.71 14.01 4 12548 104767 42504016
Skin weeping 18.13 14.01 9 12543 1570 42607213
Congenital inguinal hernia 17.73 14.01 5 12547 177 42608606
Toxicity to various agents 17.73 14.01 25 12527 229111 42379672
Impaired quality of life 17.11 14.01 21 12531 14156 42594627
Exposure via skin contact 16.70 14.01 13 12539 5025 42603758
Periportal oedema 16.56 14.01 4 12548 76 42608707
Neonatal seizure 16.01 14.01 6 12546 528 42608255
Skin exfoliation 15.11 14.01 36 12516 41517 42567266
Therapeutic response shortened 14.65 14.01 19 12533 13535 42595248
Injection site swelling 14.15 14.01 21 12531 16952 42591831
Dry eye 14.12 14.01 20 12532 15486 42593297

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
Dermatitis atopic 209.05 11.27 128 42967 25413 110520791
Pruritus 119.98 11.27 496 42599 581064 109965140
Asthma 96.73 11.27 264 42831 250027 110296177
Joint destruction 95.08 11.27 57 43038 10886 110535318
Drug tolerance 89.24 11.27 64 43031 16521 110529683
Product use in unapproved indication 79.46 11.27 365 42730 447012 110099192
Polyarthritis 77.30 11.27 62 43033 18901 110527303
Toxicity to various agents 74.15 11.27 48 43047 480507 110065697
Urticaria 68.79 11.27 276 42819 318581 110227623
Dry skin 67.19 11.27 137 42958 107516 110438688
Fixed eruption 61.61 11.27 31 43064 4201 110542003
Skin fissures 58.12 11.27 59 43036 24399 110521805
Eczema 57.47 11.27 102 42993 72191 110474013
Injection site pain 56.49 11.27 175 42920 177747 110368457
Adrenal insufficiency 55.03 11.27 75 43020 42315 110503889
Death 54.26 11.27 120 42975 698749 109847455
Psoriasis 53.37 11.27 147 42948 139846 110406358
Immunodeficiency 52.38 11.27 70 43025 38768 110507436
Foot deformity 51.53 11.27 78 43017 48402 110497802
Febrile convulsion 49.55 11.27 18 43077 1092 110545112
Exposure via skin contact 49.41 11.27 41 43054 13106 110533098
Anaphylactic reaction 47.57 11.27 124 42971 114176 110432028
Alopecia areata 43.97 11.27 20 43075 2167 110544037
Prescribed overdose 41.68 11.27 100 42995 87481 110458723
Skin exfoliation 41.63 11.27 100 42995 87551 110458653
Impaired quality of life 40.32 11.27 54 43041 29963 110516241
Angioedema 40.11 11.27 106 42989 98394 110447810
Dermatitis contact 39.40 11.27 37 43058 13916 110532288
Confusional state 38.40 11.27 78 43017 468602 110077602
Ankle arthroplasty 38.06 11.27 19 43076 2532 110543672
Drug abuse 37.95 11.27 11 43084 177400 110368804
Lower respiratory tract infection 37.84 11.27 24 43071 243082 110303122
COVID-19 37.70 11.27 192 42903 244868 110301336
Rash 37.46 11.27 486 42609 820478 109725726
Drug-induced liver injury 37.08 11.27 117 42978 119950 110426254
Amaurosis fugax 36.24 11.27 18 43077 2372 110543832
Gastroenteritis viral 35.71 11.27 52 43043 31174 110515030
Upper respiratory tract infection 35.22 11.27 122 42973 131206 110414998
Completed suicide 34.97 11.27 26 43069 242355 110303849
Cough 34.00 11.27 301 42794 461340 110084864
Dry eye 33.62 11.27 70 43025 55723 110490481
Bronchitis 33.07 11.27 135 42960 156897 110389307
Face oedema 32.98 11.27 52 43043 33417 110512787
Erythema 32.76 11.27 210 42885 291237 110254967
Ear infection 31.34 11.27 73 43022 62659 110483545
Drug eruption 30.80 11.27 66 43029 53593 110492611
Foot operation 30.00 11.27 24 43071 7289 110538915
Product use issue 29.34 11.27 215 42880 311480 110234724
Retinitis 28.82 11.27 48 43047 32279 110513925
Nail growth abnormal 28.73 11.27 10 43085 535 110545669
Eye pruritus 28.34 11.27 48 43047 32727 110513477
Illness 27.16 11.27 82 43013 82089 110464115
Nasal congestion 26.96 11.27 92 43003 98190 110448014
Product dose omission issue 26.95 11.27 216 42879 321566 110224638
Erythema multiforme 26.89 11.27 37 43058 21060 110525144
Sleep disorder due to a general medical condition 26.42 11.27 61 43034 52051 110494153
Injection site swelling 25.67 11.27 67 43028 61723 110484481
Product dose omission in error 25.23 11.27 38 43057 23474 110522730
Drug interaction 25.06 11.27 105 42990 500078 110046126
Cardiac arrest 24.83 11.27 24 43071 196729 110349475
Hyponatraemia 24.73 11.27 29 43066 217624 110328580
Neutropenia 24.60 11.27 70 43025 374550 110171654
No adverse event 23.76 11.27 73 43022 73766 110472438
Multiple organ dysfunction syndrome 23.57 11.27 15 43080 151695 110394509
Limb discomfort 23.16 11.27 50 43045 40804 110505400
Cerebrovascular accident 23.01 11.27 22 43073 181262 110364942
Middle ear inflammation 22.94 11.27 7 43088 246 110545958
Injection site erythema 22.28 11.27 84 43011 94092 110452112
Blood pressure systolic increased 22.22 11.27 3 43092 82988 110463216
Nodule 22.12 11.27 43 43052 32588 110513616
Urinary tract disorder 21.49 11.27 18 43077 5826 110540378
Eye oedema 21.37 11.27 13 43082 2549 110543655
Loss of consciousness 21.16 11.27 140 42955 196166 110350038
Acute kidney injury 21.06 11.27 153 42942 635277 109910927
Prescribed underdose 20.57 11.27 64 43031 65110 110481094
Impaired healing 20.49 11.27 28 43067 196689 110349515
Red blood cell sedimentation rate abnormal 20.01 11.27 35 43060 24474 110521730
Gastrointestinal haemorrhage 19.96 11.27 21 43074 165497 110380707
Therapeutic product effect decreased 19.91 11.27 163 42932 244153 110302051
Injection site rash 19.85 11.27 34 43061 23385 110522819
Lupus vulgaris 19.82 11.27 42 43053 33841 110512363
Laryngitis 19.72 11.27 48 43047 42363 110503841
Seronegative arthritis 19.71 11.27 25 43070 13152 110533052
Joint swelling 19.18 11.27 98 42997 442747 110103457
Muscle injury 19.17 11.27 16 43079 140791 110405413
Skin weeping 19.15 11.27 14 43081 3721 110542483
Fibromyalgia 19.09 11.27 123 42972 170786 110375418
Cerebral disorder 19.08 11.27 18 43077 6808 110539396
Disease progression 18.81 11.27 42 43053 243992 110302212
Wheelchair user 18.78 11.27 19 43076 7823 110538381
Arthritis 18.35 11.27 120 42975 167466 110378738
Hepatitis chronic active 17.81 11.27 6 43089 291 110545913
Visual impairment 17.72 11.27 101 42994 134327 110411877
Altered state of consciousness 17.64 11.27 56 43039 57570 110488634
Respiratory failure 17.47 11.27 36 43059 215296 110330908
Ocular discomfort 17.44 11.27 19 43076 8514 110537690
Infusion related reaction 17.28 11.27 83 43012 381079 110165125
Underdose 17.00 11.27 59 43036 63495 110482709
Anti-cyclic citrullinated peptide antibody 16.94 11.27 29 43066 19935 110526269
Liver injury 16.65 11.27 108 42987 150305 110395899
Hepatic cirrhosis 16.56 11.27 61 43034 67565 110478639
Therapeutic response shortened 16.53 11.27 36 43059 29547 110516657
Hepatic encephalopathy 16.49 11.27 35 43060 28221 110517983
C-reactive protein abnormal 16.15 11.27 16 43079 129679 110416525
Mast cell activation syndrome 16.04 11.27 9 43086 1519 110544685
Ocular hyperaemia 15.71 11.27 42 43053 39244 110506960
Myocardial infarction 15.68 11.27 32 43063 192051 110354153
Lymphorrhoea 15.60 11.27 5 43090 207 110545997
Lip dry 15.40 11.27 10 43085 100073 110446131
Pneumococcal sepsis 15.37 11.27 10 43085 2202 110544002
Metabolic acidosis 15.30 11.27 10 43085 99734 110446470
Hemianopia 15.27 11.27 11 43084 2857 110543347
Haemoglobin decreased 15.22 11.27 48 43047 248679 110297525
Bursitis 15.09 11.27 17 43078 129901 110416303
Generalised bullous fixed drug eruption 15.06 11.27 7 43088 797 110545407
Infusion site rash 14.85 11.27 10 43085 2333 110543871
Sensitive skin 14.84 11.27 12 43083 3700 110542504
Accidental exposure to product 14.77 11.27 48 43047 49960 110496244
Upper-airway cough syndrome 14.75 11.27 24 43071 15833 110530371
Enzyme level increased 14.67 11.27 6 43089 502 110545702
Blood creatinine increased 14.48 11.27 31 43064 182858 110363346
Cardiac failure congestive 14.25 11.27 23 43072 150977 110395227
Cough variant asthma 14.08 11.27 3 43092 23 110546181
Injection site pruritus 14.07 11.27 48 43047 51210 110494994
Rheumatoid factor positive 13.65 11.27 93 43002 131547 110414657
Skin haemorrhage 13.63 11.27 30 43065 24797 110521407
Folliculitis 13.62 11.27 28 43067 167625 110378579
Hypothermia 13.56 11.27 31 43064 26271 110519933
Oedema 13.46 11.27 133 42962 209843 110336361
Contraindicated product administered 13.45 11.27 152 42943 248115 110298089
Sleep disorder due to general medical condition, insomnia type 13.19 11.27 13 43082 105630 110440574
Hereditary angioedema 13.10 11.27 15 43080 7099 110539105
Urine glucose/creatinine ratio increased 13.04 11.27 4 43091 143 110546061
Haemorrhagic stroke 13.00 11.27 21 43074 13768 110532436
Suspected suicide attempt 12.95 11.27 5 43090 359 110545845
Head discomfort 12.83 11.27 25 43070 18975 110527229
Eyelid oedema 12.73 11.27 22 43073 15240 110530964
Gestational diabetes 12.64 11.27 15 43080 7374 110538830
Frequent bowel movements 12.62 11.27 6 43089 71384 110474820
Maternal exposure during pregnancy 12.46 11.27 153 42942 254730 110291474
Periportal oedema 12.45 11.27 4 43091 167 110546037
Histone antibody positive 12.45 11.27 4 43091 167 110546037
Nasal polyps 12.31 11.27 20 43075 13180 110533024
Lung disorder 12.29 11.27 33 43062 180014 110366190
Anaemia vitamin B12 deficiency 12.27 11.27 7 43088 1220 110544984
Pemphigoid 12.19 11.27 25 43070 19682 110526522
Joint dislocation 12.13 11.27 35 43060 34155 110512049
Injection site urticaria 12.05 11.27 23 43072 17192 110529012
Joint range of motion decreased 12.03 11.27 18 43077 121814 110424390
Joint stiffness 11.99 11.27 55 43040 67188 110479016
Lupus-like syndrome 11.90 11.27 39 43056 40753 110505451
Infusion site pain 11.86 11.27 23 43072 17396 110528808
Obsessive thoughts 11.85 11.27 7 43088 1300 110544904
Psoriatic arthropathy 11.83 11.27 123 42972 196638 110349566
Eosinophilic oesophagitis 11.83 11.27 7 43088 1305 110544899
Mucosal inflammation 11.81 11.27 12 43083 96129 110450075
Alopecia totalis 11.79 11.27 5 43090 458 110545746
Intentional product use issue 11.77 11.27 148 42947 247758 110298446
Papule 11.77 11.27 17 43078 10116 110536088
Injection site discolouration 11.65 11.27 16 43079 9087 110537117
Skin swelling 11.57 11.27 15 43080 8065 110538139
Pemphigus 11.46 11.27 131 42964 214439 110331765
Generalised oedema 11.45 11.27 32 43063 30672 110515532
Chronic spontaneous urticaria 11.44 11.27 8 43087 1985 110544219
Rhinitis allergic 11.40 11.27 23 43072 17899 110528305
Myelosuppression 11.34 11.27 12 43083 94328 110451876
Irritable bowel syndrome 11.28 11.27 30 43065 164185 110382019

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AE09 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Piperazine derivatives
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 D039563 Histamine H1 Antagonists, Non-Sedating
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
CHEBI has role CHEBI:50857 anti-allergic agent
CHEBI has role CHEBI:51177 antitussive

Related Drugs by ATC class:

R06AE Piperazine derivatives 6 drugs
buclizinecetirizinechlorcyclizinecyclizinemeclozineoxatomide

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

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Chronic idiopathic urticaria indication 302162004
Seasonal allergic rhinitis indication 367498001
Atopic dermatitis off-label use 24079001 DOID:3310
Urticaria off-label use 126485001
Chronic renal failure syndrome contraindication 90688005
Kidney disease contraindication 90708001 DOID:557
Drowsy contraindication 271782001
Hemodialysis with High-Flux Membrane contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.03 acidic
pKa2 8.21 Basic
pKa3 3.72 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 7.95 WOMBAT-PK CHEMBL

External reference:

IDSource
D07402 KEGG_DRUG
823178-28-5 SECONDARY_CAS_RN
130018-87-0 SECONDARY_CAS_RN
4026739 VANDF
4026740 VANDF
C1174893 UMLSCUI
CHEBI:94559 CHEBI
CHEMBL1201191 ChEMBL_ID
CHEMBL1201190 ChEMBL_ID
DB06282 DRUGBANK_ID
C472067 MESH_SUPPLEMENTAL_RECORD_UI
1549000 PUBCHEM_CID
7700 INN_ID
6U5EA9RT2O UNII
356887 RXNORM
178562 MMSL
18517 MMSL
83855 MMSL
d05851 MMSL
009491 NDDF
009492 NDDF
391595003 SNOMEDCT_US
421889003 SNOMEDCT_US
425461004 SNOMEDCT_US
LCR PDB_CHEM_ID
6U5EA9RT2O INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-7701 TABLET, FILM COATED 5 mg ORAL ANDA 26 sections
good sense levocetirizine HUMAN OTC DRUG LABEL 1 0113-0241 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
allergy relief HUMAN OTC DRUG LABEL 1 0363-3901 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 0363-5529 TABLET, COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0615-8565 TABLET 5 mg ORAL ANDA 24 sections
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-639 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 11673-847 TABLET, COATED 5 mg ORAL ANDA 15 sections
allergy relief HUMAN OTC DRUG LABEL 1 11822-0241 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
allergy relief HUMAN OTC DRUG LABEL 1 11822-0241 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 11822-5252 TABLET, COATED 5 mg ORAL ANDA 15 sections
Allergy Relief HUMAN OTC DRUG LABEL 1 21130-732 TABLET, COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 30142-717 TABLET, COATED 5 mg ORAL ANDA 15 sections
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-551 TABLET 5 mg ORAL ANDA 25 sections
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-551 TABLET 5 mg ORAL ANDA 25 sections
levocetirizine dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 31722-659 SOLUTION 2.50 mg ORAL ANDA 26 sections
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 33261-947 TABLET, FILM COATED 5 mg ORAL ANDA 27 sections
LEVOCETIRIZINE DIHYDROCHLORIDE Human Prescription Drug Label 1 33342-200 TABLET, FILM COATED 5 mg ORAL ANDA 26 sections
Topcare All Day Allergy HUMAN OTC DRUG LABEL 1 36800-241 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 37808-126 TABLET, COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 41163-938 TABLET, COATED 5 mg ORAL ANDA 15 sections
Xyzal Allergy 24HR HUMAN OTC DRUG LABEL 1 41167-3510 TABLET 5 mg ORAL NDA 15 sections
Xyzal Allergy 24HR HUMAN OTC DRUG LABEL 1 41167-3511 TABLET 5 mg ORAL NDA 15 sections
Xyzal Allergy 24HR HUMAN OTC DRUG LABEL 1 41167-3513 TABLET 5 mg ORAL NDA 15 sections
Childrens Xyzal Allergy HUMAN OTC DRUG LABEL 1 41167-3530 SOLUTION 2.50 mg ORAL NDA 15 sections
Childrens Xyzal Allergy HUMAN OTC DRUG LABEL 1 41167-3533 SOLUTION 2.50 mg ORAL NDA 15 sections
Childrens Xyzal Allergy HUMAN OTC DRUG LABEL 1 41167-3535 SOLUTION 2.50 mg ORAL NDA 15 sections
Xyzal HUMAN PRESCRIPTION DRUG LABEL 1 41167-5803 TABLET, FILM COATED 5 mg ORAL NDA 30 sections
Xyzal HUMAN PRESCRIPTION DRUG LABEL 1 41167-5804 SOLUTION 0.50 mg ORAL NDA 30 sections
Allergy Relief HUMAN OTC DRUG LABEL 1 41250-488 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42543-712 TABLET 5 mg ORAL ANDA 26 sections