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) 0.10 mg/mL Benet LZ, Broccatelli F, Oprea TI
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
Urticaria 75.27 12.52 131 13822 129430 50461741
Pruritus 59.15 12.52 192 13761 283376 50307795
Asthma 48.83 12.52 88 13865 89249 50501922
Drug-induced liver injury 45.54 12.52 47 13906 28048 50563123
Angioedema 45.47 12.52 54 13899 37622 50553549
Anaphylactic reaction 42.80 12.52 63 13890 53992 50537179
Product use in unapproved indication 40.65 12.52 95 13858 115724 50475447
Sinusitis 38.69 12.52 119 13834 170439 50420732
Dermatitis contact 36.16 12.52 25 13928 8621 50582550
Nail growth abnormal 33.36 12.52 10 13943 471 50590700
Joint swelling 33.30 12.52 13 13940 245273 50345898
Eye oedema 30.12 12.52 12 13941 1331 50589840
Hepatitis chronic active 29.09 12.52 6 13947 57 50591114
Product dose omission issue 28.42 12.52 113 13840 183725 50407446
Contraindicated product administered 27.80 12.52 4 13949 148954 50442217
Arthropathy 27.77 12.52 5 13948 157901 50433270
Face oedema 27.39 12.52 29 13924 17810 50573361
Abortion induced 25.65 12.52 21 13932 9323 50581848
Hepatic encephalopathy 25.08 12.52 21 13932 9615 50581556
Fixed eruption 24.18 12.52 9 13944 830 50590341
Dermatitis atopic 24.10 12.52 14 13939 3572 50587599
Lymphorrhoea 23.92 12.52 5 13948 51 50591120
Completed suicide 23.57 12.52 4 13949 131885 50459286
Psoriasis 21.40 12.52 54 13899 68946 50522225
Bronchitis 21.15 12.52 70 13883 104089 50487082
Cough 21.13 12.52 126 13827 241138 50350033
Nasal congestion 20.22 12.52 44 13909 51076 50540095
Glossodynia 19.59 12.52 4 13949 115565 50475606
Drug intolerance 19.50 12.52 19 13934 219085 50372086
Infusion site swelling 19.43 12.52 16 13937 7160 50584011
Cholangiocarcinoma 18.86 12.52 8 13945 1040 50590131
Rash morbilliform 18.83 12.52 11 13942 2835 50588336
Cytogenetic analysis abnormal 17.90 12.52 7 13946 739 50590432
Chest discomfort 17.66 12.52 61 13892 92661 50498510
Swelling face 17.19 12.52 42 13911 52553 50538618
Infusion site erythema 16.73 12.52 16 13937 8711 50582460
Hereditary angioedema 16.57 12.52 13 13940 5429 50585742
Abortion spontaneous 16.57 12.52 36 13917 41736 50549435
Ear infection 16.01 12.52 27 13926 25943 50565228
Foreign body in throat 15.49 12.52 4 13949 108 50591063
Infusion site pain 15.39 12.52 18 13935 12328 50578843
Alopecia totalis 15.25 12.52 5 13948 317 50590854
Death 15.17 12.52 43 13910 325336 50265835
Analgesic drug level increased 15.03 12.52 8 13945 1723 50589448
Upper respiratory tract infection 14.93 12.52 46 13907 65852 50525319
Arrhythmia 14.82 12.52 30 13923 33102 50558069
Dry skin 14.66 12.52 35 13918 43156 50548015
Eczema 14.53 12.52 24 13929 22678 50568493
Jaundice 14.37 12.52 26 13927 26403 50564768
Serotonin syndrome 14.32 12.52 25 13928 24688 50566483
Cross sensitivity reaction 14.07 12.52 8 13945 1961 50589210
Headache 13.88 12.52 206 13747 506329 50084842
Alopecia areata 13.83 12.52 7 13946 1361 50589810
Exposure during pregnancy 13.82 12.52 68 13885 120947 50470224
Wound 13.70 12.52 6 13947 105788 50485383
Vascular injury 13.59 12.52 6 13947 859 50590312
Laryngopharyngitis 13.54 12.52 3 13950 41 50591130
Coronavirus infection 13.51 12.52 9 13944 2920 50588251
Treatment failure 13.35 12.52 11 13942 137626 50453545
Hepatitis cholestatic 13.24 12.52 12 13941 6105 50585066
Toxicity to various agents 13.21 12.52 24 13929 212475 50378696
COVID-19 12.91 12.52 35 13918 46627 50544544
Abortion missed 12.84 12.52 7 13946 1581 50589590
Bronchospasm 12.75 12.52 18 13935 14836 50576335
Systemic lupus erythematosus 12.73 12.52 12 13941 140610 50450561

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
Foetal malformation 66.13 14.93 13 6338 125 29568051
Trisomy 18 61.58 14.93 13 6338 183 29567993
Drug-induced liver injury 48.68 14.93 39 6312 21616 29546560
Sinusitis 40.28 14.93 43 6308 34307 29533869
Alopecia areata 39.15 14.93 9 6342 191 29567985
Fixed eruption 38.22 14.93 13 6338 1189 29566987
Product use in unapproved indication 32.48 14.93 63 6288 86812 29481364
Febrile convulsion 30.21 14.93 9 6342 536 29567640
Neonatal hyponatraemia 29.23 14.93 6 6345 73 29568103
Pruritus 29.16 14.93 72 6279 116777 29451399
Erythema 28.46 14.93 55 6296 75551 29492625
Anaphylactic reaction 27.97 14.93 32 6319 27541 29540635
Hypothermia 25.93 14.93 19 6332 9220 29558956
Asthma 25.78 14.93 34 6317 33815 29534361
Dermatitis atopic 24.02 14.93 11 6340 2208 29565968
Pemphigoid 22.21 14.93 16 6335 7565 29560611
Urticaria 20.84 14.93 40 6311 54620 29513556
Congenital inguinal hernia 19.85 14.93 5 6346 158 29568018
Periportal oedema 18.97 14.93 4 6347 56 29568120
Hypogammaglobulinaemia 18.53 14.93 13 6338 5894 29562282
Neonatal seizure 18.44 14.93 6 6345 478 29567698
Rash maculo-papular 17.88 14.93 24 6327 24265 29543911
Erythema multiforme 17.54 14.93 14 6337 7703 29560473
Renal aplasia 16.57 14.93 6 6345 660 29567516
Eyelid oedema 16.43 14.93 11 6340 4625 29563551
Facial discomfort 16.11 14.93 3 6348 21 29568155
Face oedema 15.96 14.93 15 6336 10268 29557908
Suspected suicide attempt 15.95 14.93 4 6347 124 29568052
Trigeminal nerve disorder 15.34 14.93 3 6348 28 29568148
Carbuncle 15.24 14.93 3 6348 29 29568147
Idiosyncratic drug reaction 15.10 14.93 5 6346 421 29567755

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
Drug-induced liver injury 87.69 12.56 83 16623 47560 64434466
Pruritus 86.65 12.56 225 16481 312175 64169851
Urticaria 81.77 12.56 141 16565 147176 64334850
Fixed eruption 59.36 12.56 22 16684 2137 64479889
Febrile convulsion 57.83 12.56 17 16689 798 64481228
Product use in unapproved indication 55.99 12.56 134 16572 176484 64305542
Anaphylactic reaction 55.21 12.56 78 16628 68586 64413440
Angioedema 52.34 12.56 72 16634 61749 64420277
Asthma 47.45 12.56 87 16619 95138 64386888
Dermatitis contact 46.46 12.56 29 16677 8971 64473055
Alopecia areata 43.60 12.56 16 16690 1512 64480514
Face oedema 41.51 12.56 41 16665 24720 64457306
Completed suicide 36.39 12.56 7 16699 224407 64257619
Dermatitis atopic 32.11 12.56 17 16689 3859 64478167
Eye oedema 30.93 12.56 13 16693 1760 64480266
Nail growth abnormal 30.20 12.56 9 16697 443 64481583
Toxicity to various agents 27.74 12.56 32 16674 363481 64118545
Erythema 26.32 12.56 107 16599 186963 64295063
Cough 26.01 12.56 150 16556 301998 64180028
Joint swelling 25.41 12.56 12 16694 215370 64266656
Hepatic encephalopathy 24.92 12.56 29 16677 21037 64460989
Swelling face 23.31 12.56 49 16657 59117 64422909
Hepatitis chronic active 22.97 12.56 6 16700 181 64481845
Erythema multiforme 22.68 12.56 24 16682 15677 64466349
Sinusitis 22.57 12.56 86 16620 145842 64336184
Drug eruption 20.54 12.56 35 16671 36101 64445925
Rash morbilliform 20.27 12.56 14 16692 5127 64476899
Lymphorrhoea 20.11 12.56 5 16701 123 64481903
Pyrexia 19.22 12.56 225 16481 558419 63923607
Psoriasis 19.12 12.56 51 16655 71652 64410374
Rash maculo-papular 18.59 12.56 39 16667 46987 64435039
Prescribed overdose 17.68 12.56 24 16682 20307 64461719
Activated partial thromboplastin time prolonged 17.46 12.56 19 16687 12812 64469214
Rash 16.79 12.56 187 16519 458362 64023664
Bronchospasm 16.49 12.56 24 16682 21658 64460368
Eyelid oedema 16.39 12.56 18 16688 12261 64469765
Product dose omission issue 16.28 12.56 96 16610 194651 64287375
Suspected suicide attempt 16.26 12.56 5 16701 274 64481752
Obsessive thoughts 16.22 12.56 7 16699 1010 64481016
Drug abuse 16.19 12.56 7 16699 132367 64349659
Drug intolerance 16.06 12.56 15 16691 187977 64294049
Periportal oedema 15.88 12.56 4 16702 104 64481922
Eczema 15.87 12.56 28 16678 29692 64452334
Alopecia totalis 15.71 12.56 5 16701 307 64481719
Cerebrovascular accident 15.71 12.56 8 16698 137575 64344451
Pemphigoid 15.56 12.56 18 16688 12968 64469058
Interstitial lung disease 15.43 12.56 58 16648 97674 64384352
Abortion missed 15.27 12.56 7 16699 1165 64480861
Hypothermia 15.13 12.56 22 16684 19834 64462192
Hyperventilation 14.69 12.56 13 16693 6827 64475199
Altered state of consciousness 14.48 12.56 31 16675 37871 64444155
Eosinophilia 14.38 12.56 31 16675 38045 64443981
Eosinophilic granulomatosis with polyangiitis 14.16 12.56 9 16697 2873 64479153
Intraductal proliferative breast lesion 13.87 12.56 8 16698 2143 64479883
Arthropathy 13.86 12.56 7 16699 120960 64361066
Analgesic drug level increased 13.47 12.56 8 16698 2262 64479764
Foreign body in throat 13.30 12.56 4 16702 203 64481823
Acute hepatic failure 13.17 12.56 24 16682 26088 64455938
Facial discomfort 13.12 12.56 3 16703 51 64481975
Stevens-Johnson syndrome 13.07 12.56 28 16678 34221 64447805
Laryngopharyngitis 12.96 12.56 3 16703 54 64481972
Death 12.83 12.56 73 16633 482632 63999394
Acoustic neuroma 12.77 12.56 4 16702 233 64481793
Nasal congestion 12.58 12.56 39 16667 59619 64422407

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 (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
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
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 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
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
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 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
Childrens Xyzal Allergy HUMAN OTC DRUG LABEL 1 41167-3530 SOLUTION 0.50 mg ORAL NDA 14 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 42291-386 TABLET 5 mg ORAL ANDA 18 sections
levocetirizine dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42543-712 TABLET 5 mg ORAL ANDA 26 sections
Levocetirizine Dihydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42571-122 TABLET, FILM COATED 5 mg ORAL ANDA 25 sections
Levocetirizine Dihydrochloride HUMAN OTC DRUG LABEL 1 42571-312 TABLET 5 mg ORAL ANDA 16 sections