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)	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

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
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 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
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 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
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:

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 | Suggest Off label Use Form| |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
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