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

Stem definitionDrug idCAS RN
1201 3385-03-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • flunisolide
  • nasalide
  • bronalide
corticosteroid prescribed as treatment for allergic rhinitis
  • Molecular weight: 434.50
  • Formula: C24H31FO6
  • CLOGP: 2.41
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 93.06
  • ALOGS: -4.07
  • ROTB: 2

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.15 mg N
1 mg Inhal.aerosol

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.07 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 6.70 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.08 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.24 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.68 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 24, 1981 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
Nasal discomfort 55.03 27.05 11 342 4175 53344538

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
Nasal discomfort 55.45 22.75 13 1723 1256 32510534
International normalised ratio increased 23.37 22.75 20 1716 49015 32462775
Throat irritation 23.08 22.75 11 1725 9767 32502023

Pharmacologic Action:

SourceCodeDescription
ATC R01AD04 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R03BA03 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Glucocorticoids
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D019141 Respiratory System Agents
CHEBI has role CHEBI:35472 anti-inflammatory drugs
CHEBI has role CHEBI:35705 immunosuppressant
CHEBI has role CHEBI:49167 anti-asthmatic agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Asthma indication 195967001 DOID:2841
Asthma management indication 406162001
Allergic Rhinitis Prevention indication
Chronic Non-Allergic Rhinitis indication
Severe chronic obstructive pulmonary disease off-label use 313299006
Mycosis contraindication 3218000 DOID:1564
Inactive tuberculosis contraindication 11999007
Epistaxis contraindication 12441001
Measles contraindication 14189004 DOID:8622
Disease caused by parasite contraindication 17322007
Glaucoma contraindication 23986001 DOID:1686
Acute tuberculosis contraindication 25629007
Perforation of nasal septum contraindication 80142000
Bacterial infectious disease contraindication 87628006
Operation on nose contraindication 88733004
Bilateral cataracts contraindication 95722004
Ophthalmic herpes simplex contraindication 186542001
Disease of liver contraindication 235856003 DOID:409
Varicella-zoster virus infection contraindication 309465005
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Exposure to varicella contraindication 444453009
Oropharyngeal Candidiasis contraindication
Nasal Septal Ulcers contraindication
Nasal Trauma contraindication
Uncontrolled Bacterial Infections contraindication
Nasal Candidiasis contraindication
Untreated Fungal Infection contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.78 acidic
pKa2 12.78 acidic

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
Glucocorticoid receptor Nuclear hormone receptor AGONIST EC50 9.10 WOMBAT-PK CHEMBL
Progesterone receptor Transcription factor Ki 7.33 DRUG MATRIX

External reference:

IDSource
4018433 VUID
N0000146759 NUI
D00324 KEGG_DRUG
4018433 VANDF
C0060501 UMLSCUI
CHEBI:5106 CHEBI
CHEMBL1512 ChEMBL_ID
DB00180 DRUGBANK_ID
C007734 MESH_SUPPLEMENTAL_RECORD_UI
82153 PUBCHEM_CID
7076 IUPHAR_LIGAND_ID
77326-96-6 SECONDARY_CAS_RN
QK4DYS664X UNII
218620 RXNORM
2119 MMSL
43033 MMSL
4737 MMSL
d00761 MMSL
002195 NDDF
116588001 SNOMEDCT_US
43879000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Flunisolide HUMAN PRESCRIPTION DRUG LABEL 1 24208-344 SOLUTION 0.25 mg NASAL ANDA 13 sections
Flunisolide HUMAN PRESCRIPTION DRUG LABEL 1 54868-4799 SOLUTION 0.25 mg NASAL ANDA 18 sections
Flunisolide Human Prescription Drug Label 1 64980-510 SPRAY, METERED 0.25 mg NASAL ANDA 19 sections
Flunisolide HUMAN PRESCRIPTION DRUG LABEL 1 70518-0671 SOLUTION 0.25 mg NASAL ANDA 17 sections