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

Stem definition	Drug id	CAS RN
diphenylmethyl piperazine derivatives	581	83881-51-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cetirizine cetirizine hydrochloride cetirizine dihydrochloride cetirizine HCl	A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects. 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:

cetirizine
cetirizine hydrochloride
cetirizine dihydrochloride
cetirizine HCl

A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.

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
10	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	50 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	5 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.37 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Dec. 8, 1995	FDA	J AND J CONSUMER 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
Pemphigus	3062.39	10.69	4344	340231	179382	62965065
Systemic lupus erythematosus	2728.03	10.69	4409	340166	204509	62939938
Glossodynia	2642.16	10.69	3996	340579	174880	62969567
Hand deformity	1985.60	10.69	3296	341279	156161	62988286
Abdominal discomfort	1842.18	10.69	4820	339755	316065	62828382
Alopecia	1837.68	10.69	4971	339604	332565	62811882
Wound	1732.49	10.69	3145	341430	160118	62984329
Swelling	1707.81	10.69	4260	340315	271118	62873329
Pericarditis	1509.01	10.69	2623	341952	128956	63015491
Discomfort	1417.98	10.69	2932	341643	164442	62980005

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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
Asthma	317.85	10.52	401	66881	42255	34847394
Pruritus	296.54	10.52	764	66518	141217	34748432
Urticaria	270.77	10.52	454	66828	61923	34827726
Dermatitis atopic	238.48	10.52	141	67141	5206	34884443
Sleep terror	231.18	10.52	105	67177	2213	34887436
Pruritus genital	141.85	10.52	74	67208	2130	34887519
Cardiospasm	133.75	10.52	64	67218	1524	34888125
Eye pruritus	132.12	10.52	112	67170	7377	34882272
Lip swelling	130.65	10.52	158	67124	15922	34873727
Dry skin	122.86	10.52	218	67064	31069	34858580

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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
Pemphigus	1830.40	10.08	2081	304362	97501	79340444
Glossodynia	1641.21	10.08	2004	304439	101333	79336612
Systemic lupus erythematosus	1615.84	10.08	2154	304289	118995	79318950
Hand deformity	1480.74	10.08	1909	304534	102010	79335935
Pericarditis	1415.45	10.08	1870	304573	102366	79335579
Anti-cyclic citrullinated peptide antibody positive	1226.14	10.08	1554	304889	81589	79356356
Wound	1164.62	10.08	1804	304639	114375	79323570
Alopecia	1155.97	10.08	2666	303777	228689	79209256
Hypersensitivity	1122.02	10.08	2846	303597	259393	79178552
Swelling	1121.08	10.08	2532	303911	214179	79223766

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AE07	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Piperazine derivatives
ATC	S01GX12	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics
CHEBI has role	CHEBI:35703	Xenobiotic
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:78298	environmental contaminants
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D018494	Histamine 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
Vasomotor rhinitis	indication	8229003	DOID:4730
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Sneezing	indication	76067001
Common cold	indication	82272006	DOID:10459
Chronic idiopathic urticaria	indication	302162004
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204
Atopic dermatitis	off-label use	24079001	DOID:3310

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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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG/ML (10MG/ML)	QUZYTTIR	JDP	N211415	Oct. 4, 2019	RX	SOLUTION	INTRAVENOUS	8513259	Feb. 11, 2030	METHOD OF INCREASING PEAK PLASMA OR ONSET OF PLASMA CONCENTRATION BY INTRAVENOUS INJECTION IN INDIVIDUALS IN NEED OF TREATMENT FOR ACUTE URTICARIA
10MG/ML (10MG/ML)	QUZYTTIR	JDP	N211415	Oct. 4, 2019	RX	SOLUTION	INTRAVENOUS	9119771	Feb. 11, 2030	TREATMENT OF ACUTE URTICARIA
10MG/ML (10MG/ML)	QUZYTTIR	JDP	N211415	Oct. 4, 2019	RX	SOLUTION	INTRAVENOUS	9180090	Feb. 11, 2030	TREATMENT OF ACUTE URTICARIA
10MG/ML (10MG/ML)	QUZYTTIR	JDP	N211415	Oct. 4, 2019	RX	SOLUTION	INTRAVENOUS	8263581	Feb. 28, 2030	TREATMENT OF ACUTE URTICARIA
10MG/ML (10MG/ML)	QUZYTTIR	JDP	N211415	Oct. 4, 2019	RX	SOLUTION	INTRAVENOUS	8314083	Feb. 28, 2030	METHOD OF TREATMENT IN PATIENTS WITH CONCOMITANT ANGIOEDEMA
EQ 0.24% BASE	ZERVIATE	EYEVANCE	N208694	May 30, 2017	RX	SOLUTION/DROPS	OPHTHALMIC	8829005	March 15, 2030	TREATMENT OF OCULAR ITCHING ASSOCIATED WITH ALLERGIC CONJUNCTIVITIS
EQ 0.24% BASE	ZERVIATE	EYEVANCE	N208694	May 30, 2017	RX	SOLUTION/DROPS	OPHTHALMIC	9993471	March 15, 2030	TREATMENT OF OCULAR ITCHING ASSOCIATED WITH ALLERGIC CONJUNCTIVITIS

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.91	WOMBAT-PK	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.52	CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	4.05	CHEMBL

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External reference:

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ID	Source
003803	NDDF
003804	NDDF
108655000	SNOMEDCT_US
108656004	SNOMEDCT_US
1222	IUPHAR_LIGAND_ID
130140	MMSL
203150	RXNORM
2678	PUBCHEM_CID
372523007	SNOMEDCT_US
38293	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
24 HOUR ALLERGY	HUMAN OTC DRUG LABEL	1	0363-1219	CAPSULE	10 mg	ORAL	NDA	17 sections
24 HOUR ALLERGY	HUMAN OTC DRUG LABEL	1	0363-1219	CAPSULE	10 mg	ORAL	NDA	17 sections
All Day Allergy-D	HUMAN OTC DRUG LABEL	2	0113-2176	TABLET, EXTENDED RELEASE	5 mg	ORAL	ANDA	16 sections
Basic Care All Day Allergy	HUMAN OTC DRUG LABEL	1	0113-7002	TABLET, FILM COATED	10 mg	ORAL	ANDA	16 sections
BASIC CARE ALL DAY ALLERGY	HUMAN OTC DRUG LABEL	1	0113-7036	CAPSULE, LIQUID FILLED	10 mg	ORAL	ANDA	16 sections
basic care childrens all day allergy	HUMAN OTC DRUG LABEL	1	0113-7189	SOLUTION	5 mg	ORAL	ANDA	16 sections
basic care childrens all day allergy	HUMAN OTC DRUG LABEL	1	0113-7475	SOLUTION	5 mg	ORAL	ANDA	16 sections
Cetirizine	HUMAN OTC DRUG LABEL	1	0363-1040	CAPSULE, LIQUID FILLED	10 mg	ORAL	ANDA	16 sections
Cetirizine Hydrochloride	HUMAN OTC DRUG LABEL	1	0121-4780	SYRUP	5 mg	ORAL	ANDA	34 sections
Cetirizine Hydrochloride	Human OTC Drug Label	1	0363-0471	TABLET, ORALLY DISINTEGRATING	10 mg	ORAL	ANDA	14 sections

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