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

Stem definitionDrug idCAS RN
1375 51-45-6

Description:

MoleculeDescription

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:

DoseUnitRoute
0.50 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 25, 1939 FDA LILLY

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Death 138.78 101.40 35 35 81433 2276582

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC L03AX14 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSTIMULANTS
IMMUNOSTIMULANTS
Other immunostimulants
ATC V04CG03 VARIOUS
DIAGNOSTIC AGENTS
OTHER DIAGNOSTIC AGENTS
Tests for gastric secretion
MeSH PA D018494 Histamine Agents
MeSH PA D017442 Histamine Agonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
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
Hypertensive disorder contraindication 38341003 DOID:10763
Mild pre-eclampsia contraindication 41114007
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Diabetes mellitus type 1 contraindication 46635009 DOID:9744
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Acute nephropathy contraindication 58574008
Substance abuse contraindication 66214007
Psychotic disorder contraindication 69322001
Abnormal vasomotor function contraindication 70670009
Pulmonary hypertension contraindication 70995007 DOID:6432
Diabetes mellitus contraindication 73211009 DOID:9351
Chronic idiopathic constipation contraindication 82934008
Secondary glaucoma contraindication 95717004
Angina pectoris contraindication 194828000
Asthma contraindication 195967001 DOID:2841
Bladder outflow obstruction contraindication 236645006
Benign prostatic hyperplasia contraindication 266569009
Edema contraindication 267038008
Retention of urine contraindication 267064002
Syncope contraindication 271594007
Arteriosclerosis obliterans contraindication 361133006 DOID:5160
Angle-closure glaucoma contraindication 392291006 DOID:13550
Respiratory insufficiency contraindication 409623005
Hypertensive urgency contraindication 443482000
Acute exacerbation of asthma contraindication 708038006
Severe Cardiac Disease contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR AGONIST Ki 4.10 CHEMBL CHEMBL
Histamine H4 receptor GPCR Ki 8.10 CHEMBL
Histamine H3 receptor GPCR Ki 8.28 CHEMBL
Trace amine-associated receptor 1 GPCR Ki 5.51 PDSP
Histamine H2 receptor GPCR Ki 4.30 CHEMBL
Histamine H2 receptor GPCR EC50 6 CHEMBL
Histamine H4 receptor GPCR Ki 7.10 CHEMBL
Histamine H3 receptor GPCR Ki 7.17 CHEMBL
Histamine H4 receptor GPCR Ki 7.20 CHEMBL
Histamine H1 receptor GPCR EC50 6.70 CHEMBL
Histamine H1 receptor GPCR EC50 5.35 CHEMBL
Histamine H4 receptor Unclassified Ki 8.22 CHEMBL
Histamine H3 receptor Unclassified Ki 9.84 CHEMBL
Histamine H3 receptor GPCR Ki 8.20 CHEMBL

External reference:

IDSource
D006632 MESH_DESCRIPTOR_UI
4019776 VUID
N0000147867 NUI
C0019588 UMLSCUI
D04444 KEGG_DRUG
3POA0Q644U UNII
56-92-8 SECONDARY_CAS_RN
768672006 SNOMEDCT_US
5333 RXNORM
54235008 SNOMEDCT_US
4019776 VANDF
004785 NDDF
774 PUBCHEM_CID
CHEBI:18295 CHEBI
CHEMBL90 ChEMBL_ID
CHEMBL535166 ChEMBL_ID
HSM PDB_CHEM_ID
DB05381 DRUGBANK_ID
CHEMBL1533310 ChEMBL_ID
C027556 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL3989520 ChEMBL_ID
1204 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Histamine Positive HUMAN PRESCRIPTION DRUG LABEL 1 0268-0247 SOLUTION 2.75 mg PERCUTANEOUS BLA 13 sections
histamine positive HUMAN PRESCRIPTION DRUG LABEL 1 0268-0248 INJECTION, SOLUTION 0.28 mg INTRADERMAL BLA 13 sections
ActivOn Ultra Strength Arthritis HUMAN OTC DRUG LABEL 1 51068-501 STICK 0.00 g TOPICAL OTC MONOGRAPH NOT FINAL 9 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 8 sections
Glucosamine Cream EXTRA STRENGTH HUMAN OTC DRUG LABEL 1 52099-0008 CREAM 0.05 g TOPICAL OTC monograph not final 9 sections
PainMD Max HUMAN OTC DRUG LABEL 2 55992-404 CREAM 3.50 mg TOPICAL OTC monograph not final 9 sections
Arthritis Pain Relief Cream HUMAN OTC DRUG LABEL 1 61577-8120 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
Hand and Wrist Pain Cream HUMAN OTC DRUG LABEL 1 61577-8122 CREAM 0.00 g TOPICAL OTC monograph not final 9 sections
Positive Skin Test Control - Histamine HUMAN PRESCRIPTION DRUG LABEL 1 65044-9998 INJECTION 6 mg PERCUTANEOUS BLA 14 sections
Arthritis Relief HUMAN OTC DRUG LABEL 2 65121-121 CREAM 0.03 g TOPICAL OTC monograph not final 8 sections
Dr. Freds MIRACLE RUB HUMAN OTC DRUG LABEL 1 65121-403 CREAM 0.25 mg TOPICAL OTC monograph not final 8 sections
MANCORE MUSCLE MEND ROLL-ON PAIN RELIEVER HUMAN OTC DRUG LABEL 1 69198-700 LOTION 0.60 mg TOPICAL OTC monograph not final 8 sections
Simanix HUMAN PRESCRIPTION DRUG LABEL 3 69379-001 CREAM 0.04 g TOPICAL unapproved drug other 5 sections
Rematex HUMAN OTC DRUG LABEL 3 69379-012 CREAM 0.04 g TOPICAL OTC monograph not final 8 sections
Simanix HUMAN PRESCRIPTION DRUG LABEL 3 69379-013 CREAM 0.04 g TOPICAL unapproved drug other 5 sections
Royal Labs Hemp Recover HUMAN OTC DRUG LABEL 1 69580-400 CREAM 0.05 mg TOPICAL OTC monograph not final 8 sections
CVS Arthritis Pain Relief HUMAN OTC DRUG LABEL 1 69842-301 CREAM 0.03 g TOPICAL OTC monograph not final 13 sections
Histamine DHCl 0.10 Percent HUMAN OTC DRUG LABEL 1 70645-264 SPRAY 0.10 g TOPICAL OTC MONOGRAPH NOT FINAL 9 sections
Histamine DHCl 0.10 Percent and Menthol 2 Percent HUMAN OTC DRUG LABEL 2 70645-265 SPRAY 0.10 g TOPICAL OTC MONOGRAPH NOT FINAL 9 sections
Abee Med HUMAN OTC DRUG LABEL 2 70724-748 CREAM 0.50 mg TOPICAL OTC monograph not final 7 sections
Raging Kakapo Pain Relieve HUMAN OTC DRUG LABEL 2 70984-001 CREAM 0.75 mg TOPICAL OTC MONOGRAPH NOT FINAL 9 sections
Alo Therapeutic Massage HUMAN OTC DRUG LABEL 2 71061-763 CREAM 1 mg TOPICAL OTC monograph not final 7 sections
Alo Therapeutic Massage HUMAN OTC DRUG LABEL 2 71061-764 CREAM 1 mg TOPICAL OTC monograph not final 7 sections
Alo Therapeutic Massage HUMAN OTC DRUG LABEL 2 71061-765 CREAM 1 mg TOPICAL OTC monograph not final 7 sections
Alo Therapeutic Massage HUMAN OTC DRUG LABEL 2 71061-766 CREAM 1 mg TOPICAL OTC monograph not final 7 sections
PONOS NATURAL PAIN RELIEF HUMAN OTC DRUG LABEL 2 71067-767 CREAM 0.50 mg TOPICAL OTC monograph not final 7 sections
Pain Relieving Arthritis HUMAN OTC DRUG LABEL 1 71301-004 CREAM 0.03 g TOPICAL OTC monograph not final 13 sections
TerraFreeze Pain Relief HUMAN OTC DRUG LABEL 3 71805-855 CREAM 0.50 mg TOPICAL OTC monograph not final 8 sections