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

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	814	100643-71-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: SCH-34117 SCH 34117 desloratadine azomyr delopedil descarboethoxyloratadine descarboethoxyloratidine neoclarityn	major metabolite of loratadine Molecular weight: 310.83 Formula: C19H19ClN2 CLOGP: 3.83 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 24.92 ALOGS: -4.90 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

SCH-34117
SCH 34117
desloratadine
azomyr
delopedil
descarboethoxyloratadine
descarboethoxyloratidine
neoclarityn

major metabolite of loratadine

Molecular weight: 310.83
Formula: C19H19ClN2
CLOGP: 3.83
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 24.92
ALOGS: -4.90
ROTB: 0

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)	5 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.23 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.15 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 21, 2001	FDA	MERCK SHARP DOHME

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
Angioedema	179.66	12.58	128	16853	47837	63424204
Urticaria	100.57	12.58	168	16813	165634	63306407
Endocrine ophthalmopathy	74.46	12.58	20	16961	651	63471390
Nasal ulcer	68.21	12.58	25	16956	2279	63469762
Intentional overdose	61.60	12.58	87	16894	74065	63397976
Toxic shock syndrome	61.10	12.58	18	16963	824	63471217
Drug reaction with eosinophilia and systemic symptoms	58.87	12.58	58	16923	33778	63438263
Pruritus	53.94	12.58	215	16766	361238	63110803
Allergy test positive	52.75	12.58	15	16966	605	63471436
Erythema	52.55	12.58	133	16848	175618	63296423

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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
Troponin T increased	55.44	14.04	21	8341	2350	34946219
Eosinophilia	54.03	14.04	47	8315	26175	34922394
Toxic skin eruption	52.10	14.04	33	8329	11352	34937217
Rash maculo-papular	46.89	14.04	45	8317	28406	34920163
Dermatitis bullous	44.55	14.04	25	8337	6897	34941672
Death	44.35	14.04	20	8342	398029	34550540
Hepatic haematoma	41.02	14.04	11	8351	399	34948170
N-terminal prohormone brain natriuretic peptide increased	39.17	14.04	17	8345	2698	34945871
Hyperkaliuria	38.21	14.04	8	8354	96	34948473
Xerosis	36.81	14.04	11	8351	593	34947976

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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
Angioedema	158.12	12.24	145	21599	75890	79646754
Urticaria	123.53	12.24	198	21546	185003	79537641
Pruritus	83.83	12.24	267	21477	394381	79328263
Toxic skin eruption	83.52	12.24	60	21684	22233	79700411
Dermatitis bullous	76.62	12.24	48	21696	14197	79708447
Endocrine ophthalmopathy	72.46	12.24	20	21724	708	79721936
Nasal ulcer	69.54	12.24	25	21719	2115	79720529
Eosinophilia	63.80	12.24	70	21674	45275	79677369
Rash maculo-papular	62.85	12.24	77	21667	56001	79666643
Eczema	60.91	12.24	65	21679	40753	79681891

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AX27	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:49103	drug metabolites
CHEBI has role	CHEBI:50857	anti-allergic drugs
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D018680	Cholinergic Antagonists
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 urticaria	indication	40178009	DOID:10612
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

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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	8.92	Basic
pKa2	2.48	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	9.40	WOMBAT-PK	CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.91	DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.96	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.03	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.55	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.80	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.00	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.01	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.19	DRUG MATRIX
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.97	DRUG MATRIX

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External reference:

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ID	Source
009081	NDDF
124087	PUBCHEM_CID
134506008	SNOMEDCT_US
16243	MMSL
275635	RXNORM
396015008	SNOMEDCT_US
4021292	VUID
4021292	VANDF
42606	MMSL
51632	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	21695-815	TABLET, FILM COATED	5 mg	ORAL	NDA	23 sections
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	50090-0765	TABLET, FILM COATED	5 mg	ORAL	NDA	29 sections
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4624	TABLET, FILM COATED	5 mg	ORAL	NDA	12 sections
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	78206-119	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	78206-119	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	78206-119	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections
Clarinex	HUMAN PRESCRIPTION DRUG LABEL	1	78206-188	TABLET, FILM COATED	5 mg	ORAL	NDA	30 sections
Clarinex-D 12 Hour	HUMAN PRESCRIPTION DRUG LABEL	2	54868-5708	TABLET, EXTENDED RELEASE	2.50 mg	ORAL	NDA	29 sections
CLARINEX-D 12 HOUR	HUMAN PRESCRIPTION DRUG LABEL	2	78206-120	TABLET, EXTENDED RELEASE	2.50 mg	ORAL	NDA	29 sections
CLARINEX-D 12 HOUR	HUMAN PRESCRIPTION DRUG LABEL	2	78206-120	TABLET, EXTENDED RELEASE	2.50 mg	ORAL	NDA	29 sections

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