oxybuprocaine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
local anaesthetics 3016 99-43-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • benoxinate
  • benoxinate hydrochloride
  • oxybucaine
  • oxybuprocaine
  • benoxinate HCl
  • Molecular weight: 308.42
  • Formula: C17H28N2O3
  • CLOGP: 4.36
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 64.79
  • ALOGS: -2.75
  • ROTB: 11
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PLK2,PLK3,PLK4,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 63
kinase-selectivity-class AXL,BRAF,CAMK2D,DYRK1B,MAPK7,NUAK1,PDK4,PRKCD,SIK2,SIK3,STK33,TEK,TTK 13
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
March 9, 2020 FDA BAUSCH

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
Toxic anterior segment syndrome 168.42 119.91 21 92 2229 90626105

FDA Adverse Event Reporting System (Male)

None

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
Toxic anterior segment syndrome 177.05 89.31 24 165 3430 110585680
Aqueous fibrin 123.68 89.31 13 176 201 110588909

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D04AB03 DERMATOLOGICALS
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Anesthetics for topical use
ATC S01HA02 SENSORY ORGANS
OPHTHALMOLOGICALS
LOCAL ANESTHETICS
Local anesthetics
MeSH PA D000777 Anesthetics
MeSH PA D000779 Anesthetics, Local
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:36333 local anaesthetic
CHEBI has role CHEBI:48425 topical anaesthetic
CHEBI has role CHEBI:88188 drug allergen

Related Drugs by ATC class:

D04AB Anesthetics for topical use 6 drugs
benzocainecinchocainelidocainepramocainequinisocainetetracaine
S01HA Local anesthetics 7 drugs
chloroprocainecinchocainecocainelidocaineprocaineproparacainetetracaine

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Topical local anesthetic to eye indication 231346001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.8 Basic
pKa2 2.87 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.4%;0.3% FLUORESCEIN SODIUM AND BENOXINATE HYDROCHLORIDE BAUSCH LOMB IRELAND N211039 March 9, 2020 RX SOLUTION/DROPS OPHTHALMIC 10293047 Nov. 15, 2037 OCULAR EXAMINATION, INTRAOCULAR PRESSURE MEASUREMENT, OR REMOVAL OF FOREIGN BODIES OR SUTURES, IN ADULT AND PEDIATRIC PATIENTS REQUIRING A DISCLOSING AGENT IN COMBINATION WITH A TOPICAL OPHTHALMIC ANESTHETIC
0.4%;0.3% FLUORESCEIN SODIUM AND BENOXINATE HYDROCHLORIDE BAUSCH LOMB IRELAND N211039 March 9, 2020 RX SOLUTION/DROPS OPHTHALMIC 10632197 Nov. 15, 2037 OCULAR EXAMINATION, INTRAOCULAR PRESSURE MEASUREMENT, OR REMOVAL OF FOREIGN BODIES OR SUTURES, IN ADULT AND PEDIATRIC PATIENTS REQUIRING A DISCLOSING AGENT IN COMBINATION WITH A TOPICAL OPHTHALMIC ANESTHETIC
0.4%;0.3% FLUORESCEIN SODIUM AND BENOXINATE HYDROCHLORIDE BAUSCH LOMB IRELAND N211039 March 9, 2020 RX SOLUTION/DROPS OPHTHALMIC 10842872 Nov. 15, 2037 PROCEDURES IN ADULT AND PEDIATRIC PATIENTS REQUIRING A DISCLOSING AGENT IN COMBINATION WITH A TOPICAL OPHTHALMIC ANESTHETIC.

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER DRUGBANK CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel BLOCKER IC50 5.54 CHEMBL CHEMBL

External reference:

IDSource
4019627 VUID
N0000179047 NUI
D08319 KEGG_DRUG
5987-82-6 SECONDARY_CAS_RN
4018751 VANDF
4019627 VANDF
CHEBI:309594 CHEBI
CHEMBL1200 ChEMBL_ID
CHEMBL1200654 ChEMBL_ID
C005298 MESH_SUPPLEMENTAL_RECORD_UI
7123 IUPHAR_LIGAND_ID
DB00892 DRUGBANK_ID
18889 RXNORM
4253 MMSL
001355 NDDF
004569 NDDF
370315001 SNOMEDCT_US
387063004 SNOMEDCT_US
52140009 SNOMEDCT_US
C0053114 UMLSCUI
4633 PUBCHEM_CID
275 INN_ID
AXQ0JYM303 UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Fluorescein Sodium and Benoxinate Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 24208-734 SOLUTION/ DROPS 4.40 mg OPHTHALMIC NDA 21 sections
ALTAFLUOR HUMAN PRESCRIPTION DRUG LABEL 2 59390-218 SOLUTION 4 mg OPHTHALMIC NDA 21 sections
Fluorescein Sodium and Benoxinate Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 82260-734 SOLUTION/ DROPS 4.40 mg OPHTHALMIC NDA authorized generic 21 sections