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

Stem definition	Drug id	CAS RN
	903	5636-83-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: dimetindene maleate dimethindene maleate dimethindene dimetindene	A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies. Molecular weight: 292.43 Formula: C20H24N2 CLOGP: 3.53 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 16.13 ALOGS: -3.88 ROTB: 5

Molecule

Description

Molfile Inchi Smiles

Synonyms:

dimetindene maleate
dimethindene maleate
dimethindene
dimetindene

A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies.

Molecular weight: 292.43
Formula: C20H24N2
CLOGP: 3.53
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 16.13
ALOGS: -3.88
ROTB: 5

Drug dosage:

Dose	Unit	Route
4	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	4.83 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.60 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	2.16 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

None

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
COVID-19	100.16	28.45	70	3770	113033	63372149
Polyneuropathy	80.33	28.45	31	3809	14558	63470624
General physical health deterioration	61.52	28.45	68	3772	201334	63283848
Drug ineffective	48.61	28.45	4	3836	1044761	62440421
Pyrexia	46.14	28.45	93	3747	470385	63014797
Thyroid stimulating immunoglobulin increased	43.53	28.45	7	3833	78	63485104
Leukopenia	42.29	28.45	36	3804	77254	63407928
Chronic hepatitis B	39.35	28.45	8	3832	349	63484833
Glomerulonephritis chronic	39.28	28.45	7	3833	149	63485033
Anti-thyroid antibody positive	37.87	28.45	8	3832	422	63484760

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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
Polyneuropathy	68.41	26.77	26	1647	14870	34940388
COVID-19	47.54	26.77	35	1638	77515	34877743
Flushing	32.78	26.77	20	1653	32400	34922858
Noninfective conjunctivitis	27.36	26.77	4	1669	29	34955229

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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
COVID-19	141.55	24.00	101	5059	157573	79581655
Polyneuropathy	135.58	24.00	53	5107	24098	79715130
General physical health deterioration	64.53	24.00	84	5076	275154	79464074
Coronavirus infection	47.56	24.00	18	5142	7479	79731749
Leukopenia	43.07	24.00	45	5115	116468	79622760
Drug ineffective	42.85	24.00	9	5151	1080904	78658324
Thyroid stimulating immunoglobulin increased	42.28	24.00	7	5153	88	79739140
Blood lactate dehydrogenase increased	39.47	24.00	27	5133	39143	79700085
Pyrexia	37.23	24.00	112	5048	678597	79060631
Chronic hepatitis B	36.94	24.00	8	5152	443	79738785

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FDA Adverse Event Reporting System (Pediatric)

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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
Small for dates baby	12.13	12.06	5	3	2804	86980

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Pharmacologic Action:

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Source	Code	Description
ATC	D04AA13	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use
ATC	R06AB03	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Substituted alkylamines
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
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents

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

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.21	Basic
pKa2	5.05	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	Type	Activity value (-log[M])	Bioact source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	Ki	9.16	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN	Ki	6.58	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	Ki	7.35	CHEMBL
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	Ki	6.72	CHEMBL
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN	Ki	6.39	CHEMBL
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN	Ki	6.10	CHEMBL

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External reference:

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ID	Source
003407	NDDF
004804	NDDF
10101	IUPHAR_LIGAND_ID
1403	INN_ID
21855	PUBCHEM_CID
258334	RXNORM
26122009	SNOMEDCT_US
3614-69-5	SECONDARY_CAS_RN
387142004	SNOMEDCT_US
6LL60J9E0O	UNII

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Pharmaceutical products:

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