proparacaine 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)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01HA04 SENSORY ORGANS
OPHTHALMOLOGICALS
LOCAL ANESTHETICS
Local anesthetics
FDA PE N0000175976 Local Anesthesia
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

Drug Use (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

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
C0072510 UMLSCUI
D02098 KEGG_DRUG
349837002 SNOMEDCT_US
373465008 SNOMEDCT_US
34905 RXNORM
004572 NDDF
4019913 VANDF
B4OB0JHI1X UNII
540 INN_ID
CHEBI:8485 CHEBI
CHEMBL1196 ChEMBL_ID
DB00807 DRUGBANK_ID
CHEMBL1200464 ChEMBL_ID
5875-06-9 SECONDARY_CAS_RN
4935 PUBCHEM_CID
7283 IUPHAR_LIGAND_ID
C005717 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0404-7199 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 11 sections
Alcaine HUMAN PRESCRIPTION DRUG LABEL 1 0998-0016 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 13 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 13985-611 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 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 11 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 21695-530 SOLUTION 5 mg OPHTHALMIC ANDA 11 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 24208-730 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 11 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50090-1923 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 52959-705 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 sections
FLUCAINE HUMAN PRESCRIPTION DRUG LABEL 2 54799-507 SOLUTION/ DROPS 5 mg OPHTHALMIC unapproved drug other 11 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 11 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-1332 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-4368 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 12 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-4701 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 11 sections
proparacaine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68071-5139 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 13 sections
Proparacaine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 70518-2056 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 11 sections
Mydriatic-4 HUMAN PRESCRIPTION DRUG LABEL 4 71384-632 SOLUTION/ DROPS 5 mg OPHTHALMIC unapproved drug other 1 sections