levocetirizine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihistaminics/cerebral (or peripheral) vasodilators	1566	130018-77-8

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
5	mg	O

ADMET properties:

Property	Value	Reference
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 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
May 25, 2007	FDA	UCB INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.95		WOMBAT-PK	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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