CDEK
← All drugs Report issue

proparacaine

Trade name: ophthaine

Small moleculeapproved

Approved

Jul 1, 1953

Proparacaine is a topical anesthetic drug of the amino ester group. It is available as its hydrochloride salt in ophthalmic solutions at a concentration of 0.5%. Proparacaine hydrochloride ophthalmic solution is indicated for procedures in which a topical ophthalmic anesthetic is indicated: corneal anesthesia of short duration, e.g. tonometry, gonioscopy, removal of corneal foreign bodies, and for short corneal and conjunctival procedures. Proparacaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. More specifically, proparacaine appears to bind or antagonize the function of voltage gated sodium channels. The exact mechanism whereby proparacaine and other local anesthetics influence the permeability of the cell membrane is unknown; however, several studies indicate that local anesthetics may limit sodium ion permeability through the lipid layer of the nerve cell membrane. Proparacaine may alter epithelial sodium channels through interaction with channel protein residues. This limitation prevents the fundamental change necessary for the generation of the action potential. — NCATS

Clinical trial activity

20 trials · 28 clinical orgs · 13 marketing orgs

Phase 1
1
Phase 2
2
Phase 3
2
Phase 4
5

Earliest trial started Oct 1, 2005 (NCT00620997)

Timeline

1950s

  1. Jul 1, 1953

    Squibb — Earliest FDA Approval

  2. Jul 1, 1953

    Apothecon — NDA Secondary Org

  3. Jul 1, 1953

    Squibb — NDA Organization

1960s

  1. Jan 23, 1961

    Allergan — NDA Secondary Org

1970s

  1. Dec 22, 1971

    Alcon — Marketing Organization

  2. Nov 1, 1974

    Johnson and Johnson — Marketing Organization

1980s

  1. Aug 5, 1982

    Optopics — Marketing Organization

  2. Jun 7, 1983

    Pharmafair — Marketing Organization

1990s

  1. Sep 29, 1995

    Bausch & Lomb — Marketing Organization

2000s

  1. Mar 16, 2000

    Akorn, Inc. — Marketing Organization

  2. Mar 16, 2000

    Rising Pharmaceuticals — Marketing Organization

  3. Jan 1, 2005

    Earliest Phase 1 Sponsor(trial)

  4. Jan 1, 2009

    Earliest Phase 3 Sponsor(trial)

2020s

  1. Aug 9, 2024

    Somerset Pharmaceuticals — Marketing Organization

  2. May 21, 2025

    Mankind Pharma — Marketing Organization

  3. Oct 20, 2025

    Micro Labs Ltd India — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedJul 1, 1953

Chemistry & pharmacology

Loading structure…

SMILES

CCCOc1ccc(C(=O)OCCN(CC)CC)cc1N
Mol. weight
294.39 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Topical
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

Yes

Sources

Also known as

  • 2-(diethylamino)ethyl 3-amino-4-propoxybenzoate
  • 2-(diethylamino)ethyl 3-amino-4-propoxybenzoate monohydrochloride
  • 3-amino-4-propoxybenzoic acid 2-(diethylamino)ethyl ester
  • ak-taine
  • alcaine
  • alcaine
  • alcaine
  • benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester
  • benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, monohydrochloride*benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, monohydrochloride
  • chibro-kerakain
  • kainair
  • kainair
  • kainair
  • kéracaine
  • minims proxymetacaine hydrochloride
  • ocu-caine
  • ophthaine
  • ophthaine
  • ophthaine
  • ophthaine
  • ophthaine
  • ophthetic
  • ophthetic
  • ophthetic
  • paracaine
  • paracaine
  • parcaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine
  • proparacaine hcl
  • proparacaine hcl
  • proparacaine hcl
  • proparacaine hcl
  • proparacaine hydrochloride
  • proparacaine hydrochloride
  • proparacaine hydrochloride
  • proparacaine hydrochloride
  • proparacaine hydrochloride
  • proparacaine, ophthaine
  • proparakain-pos
  • proximetacaina
  • proximetacaina
  • proxymetacaine
  • proxymetacaine
  • proxymetacaine
  • proxymetacaine
  • proxymetacaine
  • proxymetacaine
  • proxymetacaine
  • proxymetacaine hydrochloride
  • proxymetacaine monohydrochloride
  • proxymetacainum
  • proxymetacainum
  • proxymethacaine

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06899724N/AJun 1, 2025Dr. John A. Thiel Medical Professional Corporation, University of Saskatchewan
NCT05325853Phase 3Apr 6, 2022American Genomics, LLC
NCT05238233Phase 4Apr 1, 2022Prisma Health
NCT05663684Phase 4Jun 30, 2020Louisiana State University
NCT04346095Phase 4Jun 30, 2020Rocky Vista University
NCT04229771Phase 4Mar 1, 2020Oakland University
NCT04283331Phase 4Feb 29, 2020Thomas Jefferson University
NCT02951351N/AOct 1, 2016Mayo Clinic
NCT02925832N/AOct 1, 2016Government Medical College, Haldwani
NCT03049163N/AOct 1, 2016Wenzhou Medical University
NCT02528123N/AApr 1, 2016London Vision Clinic
NCT02973581N/AFeb 1, 2016Silesian University of Medicine
NCT02613013N/AOct 1, 2015Capital Medical University, Central South University, Harbin Medical University, Hebei University, He University, Huazhong University of Science and Technology, People's Liberation Army of China, Sun Yat-Sen University, The Third Hospital of HanDan, Wenzhou Medical University
NCT02895074N/AAug 1, 2014Government of China, Sun Yat-Sen University
NCT02609997N/ASep 1, 2012Sun Yat-Sen University
NCT01640171N/AJul 1, 2012Retina Vitreous Associates of Florida
NCT01266824N/ADec 1, 2010University of Pennsylvania
NCT01027611Phase 3Oct 1, 2009Illinois Retina Associates
NCT00769392N/ASep 1, 2008Tufts University
NCT00620997Phase 1Oct 1, 2005University of Western Ontario
Showing 20 of 20 trials
Page 1 / 1

Organizations

Research & Development (28)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Sun Yat-Sen UniversityAcademic/Hospital3312012
Wenzhou Medical UniversityAcademic/Hospital2112015
American Genomics, LLCAcademic/Hospital1112022
Capital Medical UniversityAcademic/Hospital1012015
Central South UniversityAcademic/Hospital1012015
Dr. John A. Thiel Medical Professional CorporationAcademic/Hospital1112025
Government Medical College, HaldwaniAcademic/Hospital1112016
Government of ChinaGovernment1012014
Harbin Medical UniversityAcademic/Hospital1012015
Hebei UniversityAcademic/Hospital1012015
He UniversityAcademic/Hospital1012015
Huazhong University of Science and TechnologyAcademic/Hospital1012015
Illinois Retina AssociatesAcademic/Hospital1112009
London Vision ClinicAcademic/Hospital1112016
Louisiana State UniversityAcademic/Hospital1112020
Mayo ClinicAcademic/Hospital1112016
Oakland UniversityAcademic/Hospital1112020
People's Liberation Army of ChinaGovernment1012015
Prisma HealthAcademic/Hospital1112022
Retina Vitreous Associates of FloridaAcademic/Hospital1112012
28 organizations
Page 1 / 2

Marketing (15)

OrganizationOrg typeRelationshipDate
Akorn, Inc.For profitSYNMar 16, 2000
Akorn, Inc.For profitMKTGMar 16, 2000
AlconFor profitMKTGDec 22, 1971
AllerganFor profitNDA2Jan 23, 1961
ApotheconFor profitNDA2Jul 1, 1953
Bausch & LombFor profitMKTGSep 29, 1995
Bausch & LombFor profitSYNSep 29, 1995
Johnson and JohnsonFor profitMKTGNov 1, 1974
Mankind PharmaFor profitMKTGMay 21, 2025
Micro Labs Ltd IndiaFor profitMKTGOct 20, 2025
OptopicsAcademic/HospitalMKTGAug 5, 1982
PharmafairFor profitMKTGJun 7, 1983
Rising PharmaceuticalsFor profitMKTGMar 16, 2000
Somerset PharmaceuticalsFor profitMKTGAug 9, 2024
SquibbFor profitNDAJul 1, 1953