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

Stem definitionDrug idCAS RN
antihistaminics or local vasoconstrictors, antazoline derivatives 3658 526-36-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • xylometazoline
  • rhinoxilin
  • otrivine
  • xylometazoline hydrochloride
  • xylometazoline HCl
nasal decongestant
  • Molecular weight: 244.38
  • Formula: C16H24N2
  • CLOGP: 5.38
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 1
  • TPSA: 24.39
  • ALOGS: -4.44
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.80 mg N

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None FDA

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
Reversible cerebral vasoconstriction syndrome 143.64 34.42 24 519 2095 50602486
Thunderclap headache 102.96 34.42 13 530 151 50604430
Rebound nasal congestion 84.17 34.42 9 534 18 50604563
Anticholinergic syndrome 46.42 34.42 9 534 1786 50602795
Cerebral artery stenosis 37.43 34.42 6 537 398 50604183

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
Appendicolith 61.26 55.59 14 546 3466 29570501

FDA Adverse Event Reporting System (Geriatric)

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
Reversible cerebral vasoconstriction syndrome 164.31 35.02 29 1004 2313 64495386
Thunderclap headache 93.51 35.02 13 1020 213 64497486
Rebound nasal congestion 90.17 35.02 10 1023 18 64497681
Appendicolith 63.56 35.02 14 1019 3455 64494244
Appendicitis 44.63 35.02 14 1019 13555 64484144
Anticholinergic syndrome 39.23 35.02 9 1024 2660 64495039
Ascites 35.29 35.02 18 1015 61983 64435716

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R01AA07 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Sympathomimetics, plain
ATC R01AB06 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Sympathomimetics, combinations excl. corticosteroids
ATC S01GA03 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Sympathomimetics used as decongestants
ATC S01GA53 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Sympathomimetics used as decongestants
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014663 Nasal Decongestants
MeSH PA D019141 Respiratory System Agents
MeSH PA D014662 Vasoconstrictor Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Heart disease contraindication 56265001 DOID:114
Diabetes mellitus contraindication 73211009 DOID:9351
Transsphenoidal hypophysectomy contraindication 171948002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.95 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
Alpha-2B adrenergic receptor GPCR AGONIST Ki 5.98 PDSP SCIENTIFIC LITERATURE
Alpha-1A adrenergic receptor GPCR Ki 7.04 CHEMBL
5-hydroxytryptamine receptor 1B GPCR Ki 7.89 CHEMBL
5-hydroxytryptamine receptor 1D GPCR Ki 9.15 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 7.82 PDSP
Alpha-2C adrenergic receptor GPCR Ki 6.89 PDSP
Adrenergic receptor alpha-2 GPCR IC50 7.64 CHEMBL
Adrenergic receptor alpha-1 GPCR IC50 6.24 CHEMBL
Adrenergic receptor alpha GPCR Ki 8.32 CHEMBL

External reference:

IDSource
4020518 VUID
N0000148237 NUI
D00757 KEGG_DRUG
1218-35-5 SECONDARY_CAS_RN
4020500 VANDF
4020518 VANDF
C0078643 UMLSCUI
CHEBI:10082 CHEBI
CHEMBL312448 ChEMBL_ID
DB06694 DRUGBANK_ID
CHEMBL1256400 ChEMBL_ID
C009695 MESH_SUPPLEMENTAL_RECORD_UI
5709 PUBCHEM_CID
517 IUPHAR_LIGAND_ID
809 INN_ID
WPY40FTH8K UNII
226046 RXNORM
12647 MMSL
5697 MMSL
001804 NDDF
004727 NDDF
372841007 SNOMEDCT_US
75327003 SNOMEDCT_US
76289007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SinosilNasal Decongestant HUMAN OTC DRUG LABEL 1 44237-007 SPRAY 0.02 mL NASAL OTC monograph final 14 sections
Aqua Maris Fast Acting Decongestant HUMAN OTC DRUG LABEL 1 76260-106 SPRAY 10 mg NASAL OTC monograph final 13 sections
Aqua Maris Kids Fast Acting Decongestant HUMAN OTC DRUG LABEL 1 76260-107 SPRAY 0.05 mg NASAL OTC monograph final 12 sections