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:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	71 %	Benet LZ, Broccatelli F, Oprea TI
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
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.18 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
May 25, 2007	FDA	UCB INC

FDA Adverse Event Reporting System (Female)

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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

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FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AE09	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Piperazine derivatives
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
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

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

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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

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🐶 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:

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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

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External reference:

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ID	Source
009491	NDDF
009492	NDDF
130018-87-0	SECONDARY_CAS_RN
1549000	PUBCHEM_CID
178562	MMSL
18517	MMSL
356887	RXNORM
391595003	SNOMEDCT_US
4026739	VANDF
4026740	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
allergy relief	HUMAN OTC DRUG LABEL	1	0363-3901	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
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	21130-732	TABLET, COATED	5 mg	ORAL	ANDA	15 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
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
levocetirizine dihydrochloride	HUMAN OTC DRUG LABEL	1	0363-5528	TABLET, COATED	5 mg	ORAL	ANDA	15 sections

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