levocetirizine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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 122.61 11.97 61 20647 9663 63458651
Urticaria 64.67 11.97 157 20551 165645 63302669
Pruritus 64.02 11.97 260 20448 361193 63107121
COVID-19 58.60 11.97 120 20588 112983 63355331
Asthma 57.63 11.97 128 20580 127433 63340881
Product use in unapproved indication 51.99 11.97 152 20556 178928 63289386
Product dose omission issue 41.75 11.97 169 20539 234144 63234170
Joint swelling 41.52 11.97 28 20680 327638 63140676
Sinusitis 40 11.97 163 20545 226490 63241824
Prescribed overdose 39.30 11.97 52 20656 34101 63434213
Cerebral disorder 38.92 11.97 22 20686 4504 63463810
Anaphylactic reaction 37.66 11.97 73 20635 66027 63402287
Drug-induced liver injury 36.99 11.97 55 20653 40167 63428147
Angioedema 35.01 11.97 59 20649 47906 63420408
Completed suicide 33.66 11.97 4 20704 145669 63322645
Ear infection 33.36 11.97 51 20657 38162 63430152
Dermatitis contact 33.12 11.97 28 20680 10980 63457334
Infusion site erythema 31.68 11.97 28 20680 11651 63456663
Nail growth abnormal 30.48 11.97 10 20698 535 63467779
Infusion site swelling 29.70 11.97 25 20683 9745 63458569
Seasonal allergy 29.03 11.97 35 20673 20915 63447399
Bronchitis 28.83 11.97 98 20610 124837 63343477
Liver injury 28.74 11.97 62 20646 60458 63407856
Death 28.50 11.97 49 20659 374332 63093982
Hepatitis chronic active 28.08 11.97 6 20702 57 63468257
Psoriatic arthropathy 27.80 11.97 79 20629 91441 63376873
Underdose 27.36 11.97 39 20669 27417 63440897
Eye oedema 26.74 11.97 12 20696 1508 63466806
Toxicity to various agents 26.44 11.97 25 20683 247225 63221089
Skin exfoliation 26.27 11.97 49 20659 43053 63425261
Fibromyalgia 25.98 11.97 71 20637 80349 63387965
Psoriasis 25.38 11.97 74 20634 86883 63381431
Eczema 25.28 11.97 41 20667 32250 63436064
Dry skin 24.45 11.97 56 20652 56831 63411483
Impaired quality of life 24.14 11.97 26 20682 13757 63454557
Upper respiratory tract infection 24.12 11.97 70 20638 81977 63386337
Confusional state 24.01 11.97 25 20683 236355 63231959
Prescribed underdose 23.66 11.97 38 20670 29651 63438663
Infusion site pain 23.07 11.97 28 20680 16841 63451473
Lymphorrhoea 22.34 11.97 5 20703 60 63468254
Face oedema 22.06 11.97 30 20678 20182 63448132
Abortion induced 20.95 11.97 21 20687 10221 63458093
Hereditary angioedema 20.25 11.97 18 20690 7544 63460770
Fixed eruption 19.87 11.97 9 20699 1155 63467159
Cough 19.77 11.97 163 20545 292580 63175734
Alopecia areata 19.56 11.97 10 20698 1675 63466639
Hepatic encephalopathy 19.26 11.97 21 20687 11261 63457053
Lower respiratory tract infection 18.56 11.97 10 20698 132297 63336017
Nasal congestion 18.32 11.97 55 20653 65605 63402709
Cholangiocarcinoma 16.57 11.97 8 20700 1186 63467128
Dry eye 16.28 11.97 39 20669 40722 63427592
Skin fissures 15.73 11.97 19 20689 11369 63456945
Rash morbilliform 15.57 11.97 11 20697 3314 63465000
Illness 15.53 11.97 43 20665 49016 63419298
Cytogenetic analysis abnormal 15.35 11.97 7 20701 913 63467401
Oedema 13.98 11.97 66 20642 97556 63370758
Respiratory tract infection 13.77 11.97 37 20671 41446 63426868
Hepatic cirrhosis 13.69 11.97 27 20681 24707 63443607
Arrhythmia 13.66 11.97 35 20673 38105 63430209
Alopecia totalis 13.65 11.97 5 20703 372 63467942
Anti-cyclic citrullinated peptide antibody positive 13.31 11.97 11 20697 116201 63352113
Exposure during pregnancy 12.94 11.97 91 20617 155456 63312858
Multiple allergies 12.87 11.97 19 20689 13783 63454531
Cerebrovascular accident 12.66 11.97 10 20698 108014 63360300
Treatment failure 12.58 11.97 29 20679 199014 63269300
Condition aggravated 12.40 11.97 192 20516 402025 63066289
Hepatic enzyme increased 12.37 11.97 30 20678 202298 63266016
Swelling face 12.25 11.97 47 20661 63428 63404886
Laryngopharyngitis 12.22 11.97 3 20705 55 63468259
Cross sensitivity reaction 12.14 11.97 8 20700 2154 63466160

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 67.34 15 30 7948 5317 34943636
Foetal malformation 65.34 15 13 7965 125 34948828
Fixed eruption 47.67 15 17 7961 1683 34947270
Pruritus 46.52 15 101 7877 141880 34807073
Trisomy 18 43.12 15 13 7965 758 34948195
Drug-induced liver injury 42.51 15 42 7936 28790 34920163
Alopecia areata 37.05 15 9 7969 229 34948724
Sinusitis 36.34 15 46 7932 41356 34907597
Product use in unapproved indication 35.54 15 81 7897 117418 34831535
Asthma 35.25 15 46 7932 42610 34906343
Erythema 33.53 15 67 7911 88713 34860240
Febrile convulsion 32.62 15 10 7968 617 34948336
Neonatal hyponatraemia 28.22 15 6 7972 82 34948871
Urticaria 27.13 15 50 7928 62327 34886626
Anaphylactic reaction 25.39 15 34 7944 32267 34916686
Pemphigoid 23.75 15 18 7960 8648 34940305
Hypothermia 22.37 15 19 7959 10729 34938224
Toxicity to various agents 20.61 15 10 7968 200352 34748601
Congenital inguinal hernia 18.94 15 5 7973 179 34948774
Cough 18.92 15 76 7902 150064 34798889
Periportal oedema 18.59 15 4 7974 58 34948895
Neonatal seizure 17.84 15 6 7972 498 34948455
Eyelid oedema 17.12 15 12 7966 5112 34943841
Eczema 16.99 15 21 7957 18415 34930538
COVID-19 16.66 15 47 7931 77503 34871450
Erythema multiforme 15.41 15 14 7964 8635 34940318
Renal aplasia 15.39 15 6 7972 760 34948193
Suspected suicide attempt 15.32 15 4 7974 137 34948816

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 112.16 11.61 56 23199 10000 79711133
Pruritus 100.37 11.61 297 22958 394351 79326782
Drug-induced liver injury 74.31 11.61 94 23161 66023 79655110
Urticaria 72.43 11.61 164 23091 185037 79536096
Product use in unapproved indication 65.03 11.61 190 23065 250169 79470964
Asthma 64.78 11.61 130 23125 134965 79586168
Fixed eruption 63.46 11.61 26 23229 2928 79718205
Febrile convulsion 57.49 11.61 18 23237 928 79720205
Alopecia areata 49.29 11.61 19 23236 1824 79719309
Prescribed overdose 49.27 11.61 58 23197 37825 79683308
Completed suicide 48.48 11.61 7 23248 245760 79475373
Anaphylactic reaction 48.04 11.61 87 23168 83656 79637477
Toxicity to various agents 46.71 11.61 33 23222 421507 79299626
COVID-19 45.13 11.61 124 23131 157550 79563583
Dermatitis contact 44.74 11.61 32 23223 11001 79710132
Angioedema 42.35 11.61 78 23177 75957 79645176
Face oedema 34.81 11.61 42 23213 28094 79693039
Nail growth abnormal 32.35 11.61 10 23245 494 79720639
Cerebral disorder 29.46 11.61 19 23236 5519 79715614
Psoriatic arthropathy 29.26 11.61 68 23187 77931 79643202
Product dose omission issue 29.14 11.61 146 23109 247391 79473742
Eczema 28.11 11.61 46 23209 40772 79680361
Eye oedema 27.56 11.61 13 23242 2050 79719083
Ear infection 26.74 11.61 41 23214 34391 79686742
Death 26.63 11.61 81 23174 566433 79154700
Impaired quality of life 25.63 11.61 26 23229 14360 79706773
Joint swelling 25.42 11.61 28 23227 288618 79432515
Liver injury 25.36 11.61 53 23202 56561 79664572
Dry skin 25.20 11.61 59 23196 67936 79653197
Erythema 25.09 11.61 130 23125 223160 79497973
Product use issue 24.86 11.61 124 23131 209698 79511435
Cough 24.57 11.61 187 23068 366602 79354531
Psoriasis 24.18 11.61 69 23186 89518 79631615
Fibromyalgia 22.94 11.61 55 23200 64285 79656848
Skin exfoliation 22.85 11.61 50 23205 55050 79666083
Prescribed underdose 22.72 11.61 35 23220 29479 79691654
Drug abuse 21.90 11.61 10 23245 162681 79558452
Hepatitis chronic active 21.57 11.61 6 23249 204 79720929
Rash 21.37 11.61 260 22995 578098 79143035
Hepatic cirrhosis 20.95 11.61 37 23218 34869 79686264
Sinusitis 20.70 11.61 112 23143 195389 79525744
Upper respiratory tract infection 20.63 11.61 66 23189 91102 79630031
Bronchitis 19.77 11.61 83 23172 130561 79590572
Hepatic encephalopathy 19.08 11.61 29 23226 24137 79696996
Lymphorrhoea 18.48 11.61 5 23250 153 79720980
Erythema multiforme 18.11 11.61 24 23231 17627 79703506
Seasonal allergy 17.91 11.61 23 23232 16383 79704750
Pemphigoid 17.55 11.61 22 23233 15293 79705840
Infusion site pain 17.27 11.61 21 23234 14155 79706978
Underdose 17.20 11.61 33 23222 33118 79688015
Skin fissures 16.97 11.61 20 23235 13053 79708080
Infusion site erythema 16.68 11.61 17 23238 9443 79711690
Rash morbilliform 16.57 11.61 14 23241 6136 79714997
Swelling face 16.52 11.61 52 23203 71160 79649973
Drug interaction 16.34 11.61 64 23191 415119 79306014
Hereditary angioedema 16.16 11.61 13 23242 5322 79715811
Cerebrovascular accident 16.08 11.61 13 23242 155279 79565854
Eosinophilic granulomatosis with polyangiitis 15.73 11.61 11 23244 3649 79717484
Product quality issue 15.46 11.61 32 23223 33908 79687225
Knee arthroplasty 15.45 11.61 37 23218 43211 79677922
Periportal oedema 15.34 11.61 4 23251 106 79721027
Skin weeping 15.23 11.61 7 23248 1040 79720093
Suspected suicide attempt 14.73 11.61 5 23250 333 79720800
Obsessive thoughts 14.71 11.61 7 23248 1125 79720008
Eyelid oedema 14.64 11.61 19 23236 13668 79707465
Respiratory tract infection 14.62 11.61 39 23216 48650 79672483
Lower respiratory tract infection 14.43 11.61 10 23245 129210 79591923
Activated partial thromboplastin time prolonged 14.06 11.61 19 23236 14209 79706924
Alopecia totalis 14.02 11.61 5 23250 386 79720747
Drug eruption 14.02 11.61 36 23219 43899 79677234
Abortion missed 13.88 11.61 7 23248 1276 79719857
Laryngitis 13.74 11.61 20 23235 16019 79705114
Dry eye 13.63 11.61 32 23223 36899 79684234
Hypothermia 13.50 11.61 24 23231 22722 79698411
Hip arthroplasty 13.21 11.61 31 23224 35725 79685408
Bronchospasm 13.21 11.61 25 23230 24834 79696299
Confusional state 13.17 11.61 48 23207 317949 79403184
Rash maculo-papular 13.05 11.61 41 23214 56037 79665096
Foreign body in throat 13.03 11.61 5 23250 474 79720659
Metabolic acidosis 12.90 11.61 4 23251 82525 79638608
Nasal congestion 12.66 11.61 50 23205 76502 79644631
Stevens-Johnson syndrome 12.40 11.61 32 23223 39134 79681999
Gastrointestinal haemorrhage 12.27 11.61 15 23240 147704 79573429
Interstitial lung disease 12.24 11.61 65 23190 112535 79608598
Infusion site rash 12.02 11.61 7 23248 1695 79719438
Pulmonary radiation injury 11.99 11.61 3 23252 67 79721066
Lupus vulgaris 11.97 11.61 9 23246 3337 79717796
Product dose omission in error 11.95 11.61 13 23242 7775 79713358
Intraductal proliferative breast lesion 11.92 11.61 8 23247 2483 79718650
Infusion site swelling 11.90 11.61 13 23242 7813 79713320
Hyponatraemia 11.90 11.61 21 23234 177827 79543306
Hyperventilation 11.80 11.61 13 23242 7886 79713247

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
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
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
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




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 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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0093-7701 TABLET, FILM COATED 5 mg ORAL ANDA 26 sections
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
levocetirizine HUMAN OTC DRUG LABEL 1 0363-2241 TABLET, FILM COATED 5 mg ORAL ANDA 15 sections
levocetirizine HUMAN OTC DRUG LABEL 1 0363-2241 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 0363-5528 TABLET, 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 0527-1917 SOLUTION 0.50 mg ORAL ANDA 25 sections
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0527-1917 SOLUTION 0.50 mg ORAL ANDA 25 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 0536-1144 TABLET, COATED 5 mg ORAL ANDA 15 sections
levocetirizine dihydrochloride HUMAN OTC DRUG LABEL 1 0536-1144 TABLET, COATED 5 mg ORAL ANDA 15 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 24 sections
levocetirizine dihydrochloride Human Prescription Drug Label 1 31722-659 SOLUTION 2.50 mg ORAL ANDA 25 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 25 sections
LEVOCETIRIZINE DIHYDROCHLORIDE Human Prescription Drug Label 1 33342-200 TABLET, FILM COATED 5 mg ORAL ANDA 25 sections
Topcare All Day Allergy HUMAN OTC DRUG LABEL 1 36800-241 TABLET, FILM COATED 5 mg ORAL ANDA 15 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 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 14 sections
Xyzal Allergy 24HR HUMAN OTC DRUG LABEL 1 41167-3510 TABLET 5 mg ORAL NDA 15 sections