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prilocaine

Trade name: citanest

Small moleculeapproved

Approved

Nov 18, 1965

Prilocaine is a local anesthetic that is similar pharmacologically to lidocaine. Prilocaine binds to the intracellular surface of sodium channels which blocks the subsequent influx of sodium into the cell. Action potential propagation and never function is, therefore, prevented. This block is reversible and when the drug diffuses away from the cell, sodium channel function is restored and nerve propagation returns. Prilocaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. Currently, Prilocaine is used most often for infiltration anesthesia in dentistry. — NCATS

Clinical trial activity

151 trials · 143 clinical orgs · 20 marketing orgs

Phase 1
22
Phase 2
33
Phase 3
23
Phase 4
43

Earliest trial started Jan 1, 1996 (NCT00152724)

Timeline

1960s

  1. Nov 18, 1965

    Astra — Earliest FDA Approval

  2. Nov 18, 1965

    AstraZeneca — NDA Secondary Org

  3. Nov 18, 1965

    Dentsply International — NDA Secondary Org

  4. Nov 18, 1965

    Astra — NDA Organization

1990s

  1. Dec 30, 1992

    Teva — NDA Secondary Org

2000s

  1. Jan 1, 2002

    Earliest Phase 3 Sponsor(trial)

  2. Aug 18, 2003

    Fougera — Marketing Organization

  3. Aug 27, 2003

    Tolmar Inc. — Marketing Organization

  4. Aug 27, 2003

    Encube Ethicals Pvt. Ltd. — Marketing Organization

  5. Sep 25, 2003

    Hi Tech Pharmaceuticals — Marketing Organization

  6. Sep 25, 2003

    Akorn, Inc. — Marketing Organization

  7. Sep 25, 2003

    Hikma — Marketing Organization

  8. Jan 1, 2007

    Earliest Phase 1 Sponsor(trial)

  9. Jan 1, 2007

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Sep 29, 2010

    Septodont — Marketing Organization

  2. Sep 29, 2010

    Deproco — Marketing Organization

  3. Jun 29, 2018

    Pharmaceutical Associates — Marketing Organization

  4. Jun 29, 2018

    Teligent Pharmaceuticals — Marketing Organization

2020s

  1. Sep 21, 2020

    Rhodes Pharmaceuticals, L.P. — Marketing Organization

  2. Sep 21, 2020

    Chartwell Pharmaceuticals — Marketing Organization

  3. Jul 27, 2021

    Padagis Us — Marketing Organization

  4. Jul 27, 2021

    Acrux Ltd — Marketing Organization

  5. Apr 8, 2022

    Alembic — Marketing Organization

  6. Dec 17, 2024

    Zydus Discovery DMCC — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • citanest forte dental

    with epinephrine

    Also known as citanest forte

  • emla

    with lidocaine

    Also known as anesthetic neo, emla 1 hour, oraqix

Approval history

  • approvedPriority reviewNov 18, 1965

Chemistry & pharmacology

Loading structure…

SMILES

CCCNC(C)C(=O)Nc1ccccc1C
Mol. weight
220.32 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Parenteral, Topical
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

Yes

Sources

Also known as

  • 2-methyl-alpha-propylaminopropionanilide
  • 2-methyl-alpha-propylaminopropionanilide
  • astra 1512
  • astra 1512
  • citanest
  • citanest
  • citanest
  • citanest
  • citanest plain
  • citanest plain
  • citanest plain dental
  • l-67
  • l-67
  • lidocaine / prilocaine
  • lidocaine / prilocaine
  • n-(2-methylphenyl)-2-(propylamino)propanamide
  • n-(2-methylphenyl)-2-(propylamino)propanamide
  • o-methyl-2-propylaminopropionanilide
  • o-methyl-2-propylaminopropionanilide
  • o-methyl-alpha-propylaminopropionanilide
  • o-methyl-alpha-propylaminopropionanilide
  • prilocain
  • prilocain
  • prilocaina
  • prilocaina
  • prilocaine
  • prilocaine
  • prilocaine
  • prilocaine
  • prilocaine
  • prilocaine
  • prilocaine
  • prilocaine
  • (+/-)-prilocaine
  • prilocaïne
  • prilocaïne
  • prilocaine base
  • prilocaine base
  • prilocaine hcl
  • prilocaine hcl
  • prilocaine hcl
  • prilocaine hydrochloride
  • prilocaine hydrochloride
  • prilocaine hydrochloride
  • prilocaine hydrochloride
  • prilocainum
  • prilocainum
  • propitocaine
  • propitocaine
  • propitocaine
  • propitocaine hcl
  • propitocaine hcl
  • propitocaine hcl
  • propitocaine hydrochloride
  • propitocaine hydrochloride
  • propitocaine hydrochloride
  • propitocaine hydrochloride
  • propitocaine hydrochloride
  • propitocaine hydrochloride

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06891794N/AAug 4, 2025Oregon Health and Science University
NCT06913855N/AApr 5, 2025Istanbul Medeniyet University
NCT06769204Phase 3Feb 10, 2025Cairo University
NCT06767085Phase 4Feb 5, 2025Cairo University
NCT06857890Phase 1Dec 9, 2024Valenta Pharm JSC
NCT06703580Phase 3Nov 30, 2024Cairo University
NCT06680167Early Phase 1 (Phase 1)Oct 9, 2024Sohag University
NCT06600048N/ASep 17, 2024Tanta University
NCT07262398Phase 4Aug 3, 2024Cairo University
NCT06290583N/AMay 31, 2024South Valley University
NCT07288021Phase 4Feb 5, 2024Bnai Zion Medical Center
NCT06242977Phase 3Jan 25, 2024University of Manitoba
NCT06165679Phase 3Dec 15, 2023Cairo University
NCT06133881Phase 4Dec 1, 2023Cairo University
NCT06023368Phase 4Nov 15, 2023University of Kentucky
NCT05877690N/AOct 31, 2023Assiut University
NCT06416111N/AOct 22, 2023Ankara Yildirim Beyazıt University
NCT05970354Phase 4Sep 15, 2023CAMC Health System
NCT05891132N/ASep 1, 2023Cairo University
NCT05834647Phase 4Aug 1, 2023Universitas Sebelas Maret
Showing 20 of 151 trials
Page 1 / 8

Organizations

Research & Development (143)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Cairo UniversityAcademic/Hospital121232017
Dong-A UniversityAcademic/Hospital6622011
Free University of BrusselsAcademic/Hospital5542014
Assiut UniversityAcademic/Hospital4442016
Medical University of GrazAcademic/Hospital4122018
Plethora Solutions LtdFor profit4422007
Izmir Bozyaka Training and Research HospitalAcademic/Hospital3312016
Joanneum Research Forschungsgesellschaft mbHAcademic/Hospital3312018
ShionogiFor profit3022007
University of AntwerpAcademic/Hospital3221996
University of RostockAcademic/Hospital3322009
Aga Khan UniversityAcademic/Hospital2212019
Ain Shams UniversityAcademic/Hospital2222014
Ankara Yildirim Beyazıt UniversityAcademic/Hospital2222012
Bakirkoy Dr. Sadi Konuk Research and Training HospitalAcademic/Hospital2212022
Biolab Sanus FarmaceuticaFor profit2022014
CAMC Health SystemAcademic/Hospital2212019
Consorci Sanitari de TerrassaAcademic/Hospital2212007
Federal University of Minas GeraisAcademic/Hospital2212008
Galeno Desenvolvimento de PesquisasAcademic/Hospital2222014
143 organizations
Page 1 / 8

Marketing (22)

OrganizationOrg typeRelationshipDate
Acrux LtdFor profitMKTGJul 27, 2021
Akorn, Inc.For profitMKTGSep 25, 2003
AlembicFor profitMKTGApr 8, 2022
AlembicFor profitSYNApr 8, 2022
AstraFor profitNDANov 18, 1965
AstraZenecaFor profitNDA2Nov 18, 1965
Chartwell PharmaceuticalsFor profitMKTGSep 21, 2020
Dentsply InternationalFor profitNDA2Nov 18, 1965
DeprocoFor profitMKTGSep 29, 2010
Encube Ethicals Pvt. Ltd.For profitMKTGAug 27, 2003
FougeraFor profitMKTGAug 18, 2003
Hi Tech PharmaceuticalsFor profitMKTGSep 25, 2003
HikmaFor profitMKTGSep 25, 2003
Padagis UsFor profitMKTGJul 27, 2021
Pharmaceutical AssociatesFor profitMKTGJun 29, 2018
Rhodes Pharmaceuticals, L.P.For profitMKTGSep 21, 2020
SeptodontFor profitMKTGSep 29, 2010
Teligent PharmaceuticalsFor profitMKTGJun 29, 2018
Teligent PharmaceuticalsFor profitSYNJun 29, 2018
TevaFor profitNDA2Dec 30, 1992
Tolmar Inc.For profitMKTGAug 27, 2003
Zydus Discovery DMCCFor profitMKTGDec 17, 2024