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

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 179.28 89.61 23 605 336 63488058

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 228.48 127.81 41 815 2361 34953714
Hypopyon 227.87 127.81 32 824 364 34955711
Corneal epithelium defect 188.78 127.81 27 829 352 34955723
Corneal oedema 188.62 127.81 32 824 1319 34954756
Ulcerative keratitis 180.74 127.81 32 824 1697 34954378
Eye pain 134.04 127.81 36 820 13426 34942649
Corneal infiltrates 133.87 127.81 18 838 143 34955932
Keratopathy 130.32 127.81 21 835 624 34955451

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
Conjunctival hyperaemia 280.16 104.55 50 1202 4363 79738773
Hypopyon 269.07 104.55 40 1212 1102 79742034
Corneal epithelium defect 263.07 104.55 37 1215 682 79742454
Corneal oedema 235.88 104.55 40 1212 2580 79740556
Ulcerative keratitis 196.14 104.55 36 1216 3653 79739483
Keratopathy 176.99 104.55 28 1224 1166 79741970
Endophthalmitis 152.80 104.55 32 1220 6396 79736740
Corneal infiltrates 146.59 104.55 20 1232 290 79742846
Eye pain 138.43 104.55 42 1210 37536 79705600
Visual acuity reduced 121.73 104.55 36 1216 29433 79713703
Ciliary hyperaemia 108.09 104.55 13 1239 62 79743074

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

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
C005717 MESH_SUPPLEMENTAL_RECORD_UI
4935 PUBCHEM_CID
7283 IUPHAR_LIGAND_ID
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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0404-7199 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Alcaine HUMAN PRESCRIPTION DRUG LABEL 1 0998-0016 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 15 sections
Alcaine HUMAN PRESCRIPTION DRUG LABEL 1 0998-0016 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 15 sections
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 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 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
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 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 68071-4368 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-4701 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 70518-3408 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70518-3408 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 16 sections
Mydriatic-4 HUMAN PRESCRIPTION DRUG LABEL 4 71384-632 SOLUTION/ DROPS 5 mg OPHTHALMIC unapproved drug other 2 sections