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

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	1605	79794-75-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: loratadine claritin loracert loradex loratidine loratyne	A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness. Molecular weight: 382.89 Formula: C22H23ClN2O2 CLOGP: 5.05 LIPINSKI: 1 HAC: 4 HDO: 0 TPSA: 42.43 ALOGS: -4.46 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

loratadine
claritin
loracert
loradex
loratidine
loratyne

A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.

Molecular weight: 382.89
Formula: C22H23ClN2O2
CLOGP: 5.05
LIPINSKI: 1
HAC: 4
HDO: 0
TPSA: 42.43
ALOGS: -4.46
ROTB: 2

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
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.44 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
April 12, 1993	FDA	BAYER HEALTHCARE LLC

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
Extra dose administered	278.69	9.89	150	91399	6200	63391273
Contraindicated product administered	239.25	9.89	20	91529	217628	63179845
Synovitis	211.56	9.89	15	91534	186903	63210570
Glossodynia	192.33	9.89	18	91531	178858	63218615
Hand deformity	192.03	9.89	9	91540	159448	63238025
Systemic lupus erythematosus	184.96	9.89	38	91511	208880	63188593
Drug ineffective	175.93	9.89	844	90705	1043921	62353552
Accidental exposure to product by child	172.82	9.89	65	91484	1128	63396345
Drug intolerance	171.01	9.89	118	91431	308543	63088930
Wound	163.92	9.89	21	91528	163242	63234231

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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
Accidental exposure to product by child	287.26	10.76	96	42712	1380	34912743
Extra dose administered	209.44	10.76	101	42707	3908	34910215
Drug abuse	81.73	10.76	12	42796	99084	34815039
Failure of child resistant product closure	77.92	10.76	16	42792	21	34914102
Urticaria	71.01	10.76	202	42606	62175	34851948
General physical health deterioration	69.70	10.76	35	42773	128234	34785889
Pruritus	60.87	10.76	338	42470	141643	34772480
Rash	54.63	10.76	462	42346	222290	34691833
Off label use	53.99	10.76	298	42510	419226	34494897
Dermatitis atopic	52.20	10.76	47	42761	5300	34908823

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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
Extra dose administered	514.72	9.73	242	105165	8173	79630808
Accidental exposure to product by child	447.05	9.73	162	105245	2764	79636217
Failure of child resistant product closure	194.13	9.73	39	105368	36	79638945
Urticaria	180.60	9.73	597	104810	184604	79454377
Drug ineffective	151.33	9.73	827	104580	1080086	78558895
Off label use	144.05	9.73	664	104743	906551	78732430
Drug abuse	140.81	9.73	23	105384	162668	79476313
Synovitis	138.12	9.73	18	105389	150716	79488265
Contraindicated product administered	136.95	9.73	22	105385	157516	79481465
Gastrooesophageal reflux disease	133.52	9.73	370	105037	103876	79535105

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AX13	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48873	acetylcholine receptor antagonist
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:176497	geroprotectors
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists

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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
Bone pain after neupogen	off-label use	12584003

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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	4.43	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])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	6.97	WOMBAT-PK	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		Ki	4.94	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.81	DRUG MATRIX
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN		EC50	5.52	CHEMBL
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	7.80	DRUG MATRIX
Potassium channel subfamily K member 9	Ion channel	Q9NPC2	KCNK9_HUMAN		IC50	4.20	CHEMBL
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN		IC50	5.51	CHEMBL
Sodium-dependent neutral amino acid transporter B(0)AT2	Transporter	Q9H2J7	S6A15_HUMAN		IC50	5.40	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.77	WOMBAT-PK
Transient receptor potential cation channel subfamily V member 2	Ion channel	Q9Y5S1	TRPV2_HUMAN	BLOCKER	IC50	5.52	IUPHAR

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External reference:

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ID	Source
003909	NDDF
015760	NDDF
108652002	SNOMEDCT_US
191	MMSL
203576	RXNORM
386884002	SNOMEDCT_US
3957	PUBCHEM_CID
4020716	VUID
4020716	VANDF
45829	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
12 hour allergy and congestion	HUMAN OTC DRUG LABEL	2	0363-1133	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	ANDA	14 sections
Allergy and Congestion Relief	HUMAN OTC DRUG LABEL	2	0113-2007	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	ANDA	14 sections
allergy relief	HUMAN OTC DRUG LABEL	1	0067-6066	TABLET	10 mg	ORAL	NDA	30 sections
allergy relief	HUMAN OTC DRUG LABEL	1	0067-6122	TABLET	10 mg	ORAL	NDA	30 sections
allergy relief	HUMAN OTC DRUG LABEL	1	0363-1612	TABLET	10 mg	ORAL	ANDA	15 sections
allergy relief	HUMAN OTC DRUG LABEL	1	0363-1612	TABLET	10 mg	ORAL	ANDA	15 sections
Basic Care allergy relief	HUMAN OTC DRUG LABEL	1	0113-7612	TABLET	10 mg	ORAL	ANDA	15 sections
basic care childrens allergy relief	HUMAN OTC DRUG LABEL	1	0113-7500	TABLET, CHEWABLE	5 mg	ORAL	ANDA	15 sections
basic care childrens allergy relief	HUMAN OTC DRUG LABEL	1	0113-7500	TABLET, CHEWABLE	5 mg	ORAL	ANDA	15 sections
Basic Care Childrens Allergy Relief	HUMAN OTC DRUG LABEL	1	0113-7671	SOLUTION	5 mg	ORAL	ANDA	14 sections

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