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

Stem definition	Drug id	CAS RN
	1375	51-45-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ceplene histamine 5-imidazoleethylamine eramin ergamine ergotidine histamine dihydrochloride histamine phosphate histamine diphosphate	An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter. Molecular weight: 111.15 Formula: C5H9N3 CLOGP: -0.97 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 54.70 ALOGS: 0.17 ROTB: 2 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ceplene
histamine
5-imidazoleethylamine
eramin
ergamine
ergotidine
histamine dihydrochloride
histamine phosphate
histamine diphosphate

An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.

Molecular weight: 111.15
Formula: C5H9N3
CLOGP: -0.97
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 54.70
ALOGS: 0.17
ROTB: 2

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.50	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
April 25, 1939	FDA	LILLY

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
False negative investigation result	395.29	18.13	50	3072	89	63485811
Exposure to toxic agent	41.34	18.13	14	3108	5573	63480327
Death	30.78	18.13	61	3061	374320	63111580

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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
Exposure to toxic agent	30	20.86	9	1134	3666	34952122

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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
Exposure to toxic agent	69.01	18.47	23	3724	9135	79731506
Death	55.72	18.47	97	3650	566417	79174224

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L03AX14	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSTIMULANTS IMMUNOSTIMULANTS Other immunostimulants
ATC	V04CG03	VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for gastric secretion
CHEBI has role	CHEBI:25512	neurotransmitters
CHEBI has role	CHEBI:75771	Mus musculus metabolites
CHEBI has role	CHEBI:77746	Homo sapiens metabolite
CHEBI has role	CHEBI:35678	histamine agonists
MeSH PA	D018494	Histamine Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D017442	Histamine Agonists

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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
Acute myeloid leukemia, disease	indication	91861009
Hyposensitization to allergens	indication	182678001
Osteoarthritis	indication	396275006
Heart valve disorder	contraindication	368009	DOID:4079
Ocular hypertension	contraindication	4210003	DOID:9282
Alcoholism	contraindication	7200002
Peptic ulcer	contraindication	13200003	DOID:750
Glaucoma	contraindication	23986001	DOID:1686
Feeling agitated	contraindication	24199005
Hyperthyroidism	contraindication	34486009	DOID:7998

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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	13.75	acidic
pKa2	9.89	Basic
pKa3	6.49	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	AGONIST	Ki	4.10	CHEMBL	CHEMBL
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	4.30	CHEMBL
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		Ki	8.10	CHEMBL
Trace amine-associated receptor 1	GPCR	Q96RJ0	TAAR1_HUMAN		Ki	5.51	PDSP
Histamine H3 receptor	GPCR	Q9Y5N1	HRH3_HUMAN		Ki	8.28	CHEMBL
Macrophage migration inhibitory factor	Unclassified	P14174	MIF_HUMAN		Ki	4.21	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		EC50	6.70	CHEMBL
Histamine H2 receptor	GPCR		HRH2_CAVPO		EC50	6	CHEMBL
Histamine H1 receptor	GPCR		HRH1_RAT		EC50	5.35	CHEMBL
Histamine H3 receptor	GPCR		HRH3_RAT		Ki	8.20	CHEMBL

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External reference:

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ID	Source
HSM	PDB_CHEM_ID
003366	NDDF
003599	NDDF
004785	NDDF
1204	IUPHAR_LIGAND_ID
1217222003	SNOMEDCT_US
13994	MMSL
142136	RXNORM
27199	MMSL
4017469	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ActivOn Ultra Strength Arthritis	HUMAN OTC DRUG LABEL	2	51068-501	STICK	0 g	TOPICAL	OTC MONOGRAPH NOT FINAL	15 sections
Alo Therapeutic Massage	HUMAN OTC DRUG LABEL	2	51457-000	CREAM	0.10 g	TOPICAL	OTC monograph not final	10 sections
ALO THERAPEUTIC MASSAGE PAIN RELIEVING	HUMAN OTC DRUG LABEL	2	51457-001	CREAM	0.10 g	TOPICAL	OTC monograph not final	12 sections
Arthritis Pain Relief	HUMAN OTC DRUG LABEL	1	0363-3035	CREAM	0.03 g	TOPICAL	OTC monograph not final	13 sections
Arthritis Pain Relief Cream	HUMAN OTC DRUG LABEL	1	61577-8120	CREAM	0 g	TOPICAL	OTC monograph not final	9 sections
Arthritis Relief	HUMAN OTC DRUG LABEL	2	65121-121	CREAM	0.03 g	TOPICAL	OTC monograph not final	10 sections
Back Pain Cream	HUMAN OTC DRUG LABEL	1	61577-8121	CREAM	0.00 g	TOPICAL	OTC monograph not final	9 sections
Back Pain Cream	HUMAN OTC DRUG LABEL	1	61577-8121	CREAM	0.00 g	TOPICAL	OTC monograph not final	9 sections
BronCare	HUMAN OTC DRUG LABEL	29	55714-4840	PELLET	15 [hp_X]	ORAL	unapproved homeopathic	10 sections
CVS Arthritis Pain Relief	HUMAN OTC DRUG LABEL	1	69842-301	CREAM	0.03 g	TOPICAL	OTC monograph not final	13 sections

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