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

Stem definitionDrug idCAS RN
local anaesthetics 2294 499-67-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • proparacaine
  • proparacaine hydrochloride
  • ophthaine
  • proxymetacaine
  • proparacaine HCl
  • Molecular weight: 294.40
  • Formula: C16H26N2O3
  • CLOGP: 3.83
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 64.79
  • ALOGS: -2.33
  • ROTB: 10
  • 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,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,MAP3K1,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,TTK,ULK1 62
kinase-selectivity-class AXL,BRAF,GRK2,PDK4,STK33 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
July 1, 1953 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
Retinopathy of prematurity 180.52 82.18 23 789 351 90627284
Endophthalmitis 97.45 82.18 19 793 4666 90622969
Visual acuity reduced 85.57 82.18 23 789 23387 90604248

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
Conjunctival hyperaemia 226.72 105.54 42 919 3134 42617240
Hypopyon 220.82 105.54 32 929 503 42619871
Corneal epithelium defect 212.17 105.54 30 931 392 42619982
Corneal oedema 193.71 105.54 33 928 1515 42618859
Ulcerative keratitis 190.45 105.54 34 927 2054 42618320
Keratopathy 159.61 105.54 25 936 673 42619701
Eye pain 156.48 105.54 42 919 16988 42603386
Corneal infiltrates 133.63 105.54 18 943 159 42620215
Photophobia 108.39 105.54 27 934 8092 42612282

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
Corneal epithelium defect 299.20 80.49 42 1489 870 110586898
Conjunctival hyperaemia 285.31 80.49 52 1479 5779 110581989
Hypopyon 264.71 80.49 40 1491 1400 110586368
Corneal oedema 253.77 80.49 43 1488 3130 110584638
Keratopathy 221.03 80.49 34 1497 1339 110586429
Ulcerative keratitis 210.46 80.49 39 1492 4727 110583041
Eye pain 169.71 80.49 51 1480 50048 110537720
Corneal infiltrates 145.75 80.49 20 1511 346 110587422
Endophthalmitis 143.38 80.49 31 1500 8156 110579612
Visual acuity reduced 127.41 80.49 37 1494 32136 110555632
Persistent corneal epithelial defect 113.71 80.49 14 1517 97 110587671
Ciliary hyperaemia 109.04 80.49 13 1518 66 110587702
Photophobia 103.60 80.49 30 1501 25741 110562027
Corneal opacity 100.23 80.49 17 1514 1234 110586534
Toxic anterior segment syndrome 94.88 80.49 19 1512 3435 110584333
Drug abuse 91.87 80.49 46 1485 177365 110410403
Lacrimation increased 89.71 80.49 28 1503 30922 110556846
Off label use 86.64 80.49 104 1427 1500081 109087687
Retinal disorder 83.15 80.49 16 1515 2354 110585414
Vitreous floaters 81.53 80.49 20 1511 9114 110578654

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01HA04 SENSORY ORGANS
OPHTHALMOLOGICALS
LOCAL ANESTHETICS
Local anesthetics
FDA EPC N0000175539 Local Anesthetic
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
FDA PE N0000175976 Local Anesthesia
CHEBI has role CHEBI:35480 analgesic

Related Drugs by ATC class:

S01HA Local anesthetics 7 drugs
chloroprocainecinchocainecocainelidocaineoxybuprocaineprocainetetracaine

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

DiseaseRelationSNOMED_IDDOID
Administration of Corneal Anesthesia indication
Local Anesthesia for Ophthalmologic Procedure indication
Hyperthyroidism contraindication 34486009 DOID:7998
Heart disease contraindication 56265001 DOID:114
Eye infection contraindication 128351009
Uveitis contraindication 128473001 DOID:13141




🐶 Veterinary Drug Use

SpeciesUseRelation
Multiple Species Ophthalmic anesthetic Indication
Multiple Species Anesthetic in cauterization of corneal ulcers, minor surgery, removal of sutures from the cornea, removal of foreign bodies cornea Indication
Multiple Species For examination and treatment of painful otitis, and prior to catheterization Indication
Multiple Species For removal of foreign bodies from eye, ear, and nose Indication

🐶 Veterinary products

ProductApplicantIngredients
Ophthaine Solution Zoetis Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.8 Basic
pKa2 3.76 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
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 5.72 CHEMBL CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7 DRUG MATRIX
Amine oxidase [flavin-containing] A Enzyme IC50 5.75 DRUG MATRIX

External reference:

IDSource
4019913 VUID
N0000179224 NUI
D02098 KEGG_DRUG
5875-06-9 SECONDARY_CAS_RN
4017727 VANDF
4019913 VANDF
C0072510 UMLSCUI
CHEBI:8485 CHEBI
CHEMBL1196 ChEMBL_ID
DB00807 DRUGBANK_ID
CHEMBL1200464 ChEMBL_ID
4935 PUBCHEM_CID
7283 IUPHAR_LIGAND_ID
C005717 MESH_SUPPLEMENTAL_RECORD_UI
540 INN_ID
B4OB0JHI1X UNII
203759 RXNORM
3827 MMSL
39893 MMSL
5370 MMSL
7955 MMSL
001360 NDDF
004572 NDDF
30424002 SNOMEDCT_US
349837002 SNOMEDCT_US
373465008 SNOMEDCT_US
B4OB0JHI1X INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alcaine HUMAN PRESCRIPTION DRUG LABEL 1 0998-0016 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 15 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 13985-611 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 17 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 16590-195 SOLUTION 5 mg OPHTHALMIC ANDA 10 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-263 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 18 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 21695-530 SOLUTION 5 mg OPHTHALMIC ANDA 18 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24208-730 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42571-497 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 17 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-0259 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 17 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-1923 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-1931 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 52959-705 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Fluorescein Sodium and Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 2 59390-205 SOLUTION/ DROPS 5 mg OPHTHALMIC unapproved drug other 10 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 61314-016 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-4368 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
proparacaine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-5139 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 15 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70069-601 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 15 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70518-3408 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70756-193 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 10 sections
Mydriatic-4 HUMAN PRESCRIPTION DRUG LABEL 4 71384-632 SOLUTION/ DROPS 5 mg OPHTHALMIC unapproved drug other 2 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 85766-039 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 15 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 85766-056 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 85766-057 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections