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histamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1375 | 51-45-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.50 | mg | P |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK7,CDK9,CHEK1,CLK2,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK1,GRK2,GRK3,HASPIN,IRAK1,IRAK4,ITK,JAK1,JAK3,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK12,MAPK7,MAPK9,MARK4,NTRK1,NTRK2,PDK2,PIM2,PRKACA,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ULK1,ULK2 | 52 | |||
| kinase-selectivity-class | AKT2,AKT3,AXL,BRAF,CAMK2B,CAMK2D,CHEK1,EIF2AK3,MARK4,MELK,PRKCD,SIK2,STK33,SYK | 14 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 25, 1939 | FDA | LILLY |
FDA Adverse Event Reporting System (Female)
| 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 | 390.83 | 16.99 | 50 | 3568 | 137 | 90624692 |
| Product dose omission issue | 29.00 | 16.99 | 46 | 3572 | 291641 | 90333188 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Testicular haemorrhage | 26.54 | 22.73 | 5 | 1511 | 252 | 42619567 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Therapeutic reaction time decreased | 32.42 | 17.45 | 11 | 4534 | 5268 | 110579486 |
| Product dose omission issue | 25.95 | 17.45 | 47 | 4498 | 321735 | 110263019 |
| Testicular haemorrhage | 25.89 | 17.45 | 5 | 4540 | 248 | 110584506 |
| Diarrhoea | 20.74 | 17.45 | 97 | 4448 | 1139408 | 109445346 |
| Back pain | 20.15 | 17.45 | 46 | 4499 | 370950 | 110213804 |
| Penile haemorrhage | 19.53 | 17.45 | 5 | 4540 | 903 | 110583851 |
| Groin infection | 18.72 | 17.45 | 5 | 4540 | 1065 | 110583689 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| 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 |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D017442 | Histamine Agonists |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| CHEBI has role | CHEBI:25512 | neurotransmitter |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35705 | immunosuppressive agent |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
| CHEBI has role | CHEBI:75771 | mouse metabolite |
| CHEBI has role | CHEBI:77746 | human metabolite |
| CHEBI has role | CHEBI:35678 | histamine agonist |
Related Drugs by ATC class:
L03AX Other immunostimulants 15 drugs
V04CG Tests for gastric secretion 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 |
| 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 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | AGONIST | Ki | 4.10 | CHEMBL | CHEMBL | |||
| Histamine H2 receptor | GPCR | Ki | 4.30 | CHEMBL | |||||
| Histamine H4 receptor | GPCR | Ki | 8.10 | CHEMBL | |||||
| Trace amine-associated receptor 1 | GPCR | Ki | 5.51 | PDSP | |||||
| Histamine H3 receptor | GPCR | Ki | 8.28 | CHEMBL | |||||
| Macrophage migration inhibitory factor | Cytokine | Ki | 4.21 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | EC50 | 6.70 | CHEMBL | |||||
| Histamine H2 receptor | GPCR | EC50 | 6 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | EC50 | 5.35 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 8.20 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 7.17 | CHEMBL | |||||
| Histamine H4 receptor | GPCR | Ki | 7.10 | CHEMBL | |||||
| Histamine H4 receptor | GPCR | Ki | 7.20 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 9.84 | CHEMBL | |||||
| Histamine H4 receptor | GPCR | Ki | 8.22 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 820484N8I3 | UNII |
| 4019776 | VUID |
| N0000147867 | NUI |
| D04444 | KEGG_DRUG |
| 56-92-8 | SECONDARY_CAS_RN |
| 51-74-1 | SECONDARY_CAS_RN |
| 4017469 | VANDF |
| 4019776 | VANDF |
| 4034665 | VANDF |
| C0019588 | UMLSCUI |
| CHEBI:18295 | CHEBI |
| HSM | PDB_CHEM_ID |
| CHEMBL90 | ChEMBL_ID |
| 774 | PUBCHEM_CID |
| DB05381 | DRUGBANK_ID |
| CHEMBL1533310 | ChEMBL_ID |
| CHEMBL3989520 | ChEMBL_ID |
| D006632 | MESH_DESCRIPTOR_UI |
| 1204 | IUPHAR_LIGAND_ID |
| C027556 | MESH_SUPPLEMENTAL_RECORD_UI |
| 142136 | RXNORM |
| 13994 | MMSL |
| 27199 | MMSL |
| 4827 | MMSL |
| d03892 | MMSL |
| 003366 | NDDF |
| 003599 | NDDF |
| 004785 | NDDF |
| 1217222003 | SNOMEDCT_US |
| 54235008 | SNOMEDCT_US |
| 62666006 | SNOMEDCT_US |
| 768672006 | SNOMEDCT_US |
| 820484N8I3 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Histamine PositiveSkin Test Control | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0268-0247 | SOLUTION | 2.75 mg | PERCUTANEOUS | BLA | 19 sections |
| histamine positiveskin test control | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0268-0248 | INJECTION, SOLUTION | 0.28 mg | INTRADERMAL | BLA | 19 sections |
| Walgreens Arthritis Pain Relief Cream | HUMAN OTC DRUG LABEL | 1 | 0363-5301 | CREAM | 0 g | TOPICAL | OTC Monograph Drug | 12 sections |
| 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 Drug | 10 sections |
| ALO THERAPEUTIC MASSAGE PAIN RELIEVING | HUMAN OTC DRUG LABEL | 2 | 51457-001 | CREAM | 0.10 g | TOPICAL | OTC Monograph Drug | 12 sections |
| Glucosamine Cream EXTRA STRENGTH | HUMAN OTC DRUG LABEL | 1 | 52099-0008 | CREAM | 0.05 g | TOPICAL | OTC monograph not final | 9 sections |
| Hay Fever | HUMAN OTC DRUG LABEL | 55 | 55714-2562 | LIQUID | 15 [hp_X] | ORAL | unapproved homeopathic | 10 sections |
| BronCare | HUMAN OTC DRUG LABEL | 29 | 55714-4840 | PELLET | 15 [hp_X] | ORAL | unapproved homeopathic | 10 sections |
| PainMD Max | HUMAN OTC DRUG LABEL | 2 | 55992-404 | CREAM | 3.50 mg | TOPICAL | OTC monograph not final | 10 sections |
| Sombra Max | HUMAN OTC DRUG LABEL | 5 | 61577-3440 | CREAM | 0.03 g | TOPICAL | OTC Monograph Drug | 9 sections |
| Arthritis Pain Relief Cream | HUMAN OTC DRUG LABEL | 1 | 61577-8120 | CREAM | 0 g | TOPICAL | OTC monograph not final | 9 sections |
| Arthritis Pain Relief Cream | HUMAN OTC DRUG LABEL | 1 | 61577-8120 | CREAM | 0 g | TOPICAL | OTC monograph not final | 9 sections |
| Australian Dream Back Pain | HUMAN OTC DRUG LABEL | 1 | 61577-8121 | CREAM | 0.00 g | TOPICAL | OTC Monograph Drug | 9 sections |
| Australian Dream Back Pain | HUMAN OTC DRUG LABEL | 1 | 61577-8121 | CREAM | 0.00 g | TOPICAL | OTC Monograph Drug | 9 sections |
| Hand and Wrist Pain Cream | HUMAN OTC DRUG LABEL | 1 | 61577-8122 | CREAM | 0 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 | 20 sections |
| Simanix | HUMAN PRESCRIPTION DRUG LABEL | 3 | 69379-001 | CREAM | 0.04 g | TOPICAL | unapproved drug other | 6 sections |
| Rematex | HUMAN OTC DRUG LABEL | 3 | 69379-012 | CREAM | 0.04 g | TOPICAL | OTC monograph not final | 10 sections |
| Simanix | HUMAN PRESCRIPTION DRUG LABEL | 3 | 69379-013 | CREAM | 0.04 g | TOPICAL | unapproved drug other | 6 sections |
| CVS Arthritis Pain Relief | HUMAN OTC DRUG LABEL | 1 | 69842-301 | CREAM | 0.03 g | TOPICAL | OTC Monograph Drug | 13 sections |
| Raging Kakapo Pain Relieve | HUMAN OTC DRUG LABEL | 2 | 70984-001 | CREAM | 0.75 mg | TOPICAL | OTC MONOGRAPH NOT FINAL | 14 sections |
| Alo Therapeutic Massage | HUMAN OTC DRUG LABEL | 2 | 71061-763 | CREAM | 1 mg | TOPICAL | OTC Monograph Drug | 11 sections |
| Alo Therapeutic Massage | HUMAN OTC DRUG LABEL | 2 | 71061-764 | CREAM | 1 mg | TOPICAL | OTC Monograph Drug | 11 sections |
| Alo Therapeutic Massage | HUMAN OTC DRUG LABEL | 2 | 71061-765 | CREAM | 1 mg | TOPICAL | OTC Monograph Drug | 11 sections |
| Alo Therapeutic Massage | HUMAN OTC DRUG LABEL | 2 | 71061-766 | CREAM | 1 mg | TOPICAL | OTC Monograph Drug | 11 sections |
| DR. MIKES Ponos Pain Relief Cream Roll-On | HUMAN OTC DRUG LABEL | 2 | 71067-359 | CREAM | 0.30 mg | TOPICAL | OTC Monograph Drug | 13 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 Drug | 13 sections |
| MD SCIENCE CANNABIDIOL | HUMAN OTC DRUG LABEL | 2 | 73615-101 | CREAM | 0.04 mg | TOPICAL | OTC monograph not final | 13 sections |