antazoline indications/contra

Stem definitionDrug idCAS RN
antihistaminics or local vasoconstrictors, antazoline derivatives 224 91-75-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • antazoline mesylate
  • antazoline sulfate
  • antazoline
  • phenazoline
  • antazoline phosphate
  • antazoline hydrochloride
  • antazoline HCl
An ethylenediamine derivative with histamine H1 antagonistic and sedative properties. Antazoline antagonizes histamine H1 receptor and prevents the typical allergic symptoms caused by histamine activities on capillaries, skin, mucous membranes, and gastrointestinal and bronchial smooth muscles. These histamine activities include vasodilation, bronchoconstriction, increased vascular permeability, pain, itching, and spasmodic contractions of gastrointestinal smooth muscles. Antazoline is used to provide symptomatic relieve of allergic symptoms.
  • Molecular weight: 265.36
  • Formula: C17H19N3
  • CLOGP: 4.11
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 27.63
  • ALOGS: -3.37
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.30 g O
0.30 g P

Approvals:

DateAgencyCompanyOrphan
April 30, 1990 FDA NOVARTIS

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC R01AC04 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Antiallergic agents, excl. corticosteroids
ATC R06AX05 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Other antihistamines for systemic use
MeSH PA D018926 Anti-Allergic Agents
CHEBI has role CHEBI:37955 H1-receptor antagonist
CHEBI has role CHEBI:48873 cholinergic antagonist
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Dermatographic urticaria indication 7632005 DOID:743
Vasomotor rhinitis indication 8229003 DOID:4730
Allergic rhinitis indication 61582004
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Red eye indication 75705005
Sneezing indication 76067001
Urticaria indication 126485001
Itching of skin indication 418363000
Allergic conjunctivitis indication 473460002 DOID:11204
Anaphylaxis Adjunct indication
Ocular Itching indication
Ocular hypertension contraindication 4210003 DOID:9282
Peptic ulcer contraindication 13200003 DOID:750
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Chronic idiopathic constipation contraindication 82934008
Eye infection contraindication 128351009
Bladder outflow obstruction contraindication 236645006
Benign prostatic hyperplasia contraindication 266569009 DOID:2883
Retention of urine contraindication 267064002
Injury of eye region contraindication 282752000
Angle-closure glaucoma contraindication 392291006 DOID:13550

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.35 Basic
pKa2 3.96 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST CHEMBL CHEMBL

External reference:

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IDSource
4019615 VUID
N0000147709 NUI
C0003143 UMLSCUI
7116 IUPHAR_LIGAND_ID
D02950 KEGG_DRUG
6T74I07212 UNII
24359-81-7 SECONDARY_CAS_RN
2200 PUBCHEM_CID
4019615 VANDF
865 RXNORM
373544004 SNOMEDCT_US
85408000 SNOMEDCT_US
N0000006006 NDFRT
N0000147709 NDFRT
003378 NDDF
CHEMBL1305 ChEMBL_ID
CHEBI:84115 CHEBI
CHEMBL1200550 ChEMBL_ID
CHEMBL1256819 ChEMBL_ID
1142 INN_ID
DB08799 DRUGBANK_ID
D000865 MESH_DESCRIPTOR_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Nestabs ONE HUMAN PRESCRIPTION DRUG LABEL 9 50967-410 CAPSULE, GELATIN COATED 225 mg ORAL unapproved drug other 12 sections