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procaine merethoxylline

Small moleculeapproved

Approved

Sep 19, 1952

Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex. — NCATS

Clinical trial activity

8 trials · 8 clinical orgs · 12 marketing orgs

Phase 1
1
Phase 2
5
Phase 3
1
Phase 4
0

Earliest trial started Sep 1, 1997 (NCT00299338)

Timeline

1910s

  1. Jul 1, 1917

    Evidence of US Marketing

1950s

  1. Sep 19, 1952

    Earliest FDA Approval

  2. Sep 19, 1952

    Kodak — NDA Secondary Org

  3. Jan 4, 1954

    Eli Lilly — First NDA Organization

  4. Jan 4, 1954

    Pfizer — Marketing Organization

  5. Jan 4, 1954

    Eli Lilly — NDA Organization

  6. Jul 1, 1954

    Lederle — Marketing Organization

  7. Jul 1, 1954

    American Cyanamid — NDA Secondary Org

1970s

  1. Sep 15, 1972

    Hospira — Marketing Organization

  2. Dec 8, 1972

    Abraxis — Marketing Organization

  3. Oct 12, 1973

    Elkins Sinn — Marketing Organization

  4. Nov 26, 1973

    Belmar Pharmacy — Marketing Organization

  5. Apr 1, 1974

    Watson Pharmaceuticals — Marketing Organization

1990s

  1. Jan 1, 1997

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Jan 1, 2005

    Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2011

    Earliest Phase 3 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

Combination products

Approval history

  • approvedSep 19, 1952
  • approvedJul 1, 1917

Chemistry & pharmacology

Loading structure…

SMILES

CCN(CC)CCOC(=O)c1ccc(N)cc1
Mol. weight
236.31 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Discontinued

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • 2-diethylaminoethyl p-aminobenzoate
  • 2-diethylaminoethyl p-aminobenzoate
  • 4-aminobenzoic acid 2-diethylaminoethyl ester
  • 4-aminobenzoic acid 2-diethylaminoethyl ester
  • dicurin procaine
  • diethylaminoethyl p-aminobenzoate
  • herocaine
  • irocaine
  • isocain
  • isocaine
  • merethoxylline procaine
  • merethoxylline procaine
  • merethoxylline procaine
  • novocain
  • novocain
  • novocain
  • novocaine
  • novocaine
  • p-aminobenzoic acid 2-diethylaminoethyl ester
  • p-aminobenzoic acid 2-diethylaminoethyl ester
  • pasconeural n
  • procain
  • procaina
  • procaina
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine
  • procaine hcl
  • procaine hcl
  • procaine hcl
  • procaine hydrochloride
  • procaine hydrochloride
  • procaine hydrochloride
  • procaine hydrochloride
  • procaine merethoxylline
  • procaine merethoxylline
  • procaine merethoxylline
  • procainum
  • procainum
  • rocaine
  • rocaine
  • sp01a
  • sp01a
  • spinocaine
  • vitamin h3
  • vitamin h3
  • β-(diethylamino)ethyl 4-aminobenzoate
  • β-(diethylamino)ethyl 4-aminobenzoate
  • β-(diethylamino)ethyl p-aminobenzoate
  • β-(diethylamino)ethyl p-aminobenzoate

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT02726620N/AJan 1, 2017Utrecht University, Vanderbilt University
NCT02735317Phase 2Apr 1, 2016Sun Yat-Sen University
NCT02331576N/AJan 1, 2015Chonnam National University
NCT01845532N/AApr 1, 2013Yonsei University
NCT00857688Phase 3May 1, 2011Azidus
NCT00299897Phase 2Mar 1, 2006Samaritan Pharmaceuticals
NCT00113412Phase 2May 1, 2005Samaritan Pharmaceuticals
NCT00299338Phase 1/Phase 2 (Phase 2)Sep 1, 1997AIDS Research Alliance, Samaritan Pharmaceuticals
Showing 8 of 8 trials
Page 1 / 1

Organizations

Research & Development (8)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Samaritan PharmaceuticalsFor profit3311997
AIDS Research AllianceAcademic/Hospital1011997
AzidusFor profit1112011
Chonnam National UniversityAcademic/Hospital1112015
Sun Yat-Sen UniversityAcademic/Hospital1112016
Utrecht UniversityAcademic/Hospital1012017
Vanderbilt UniversityAcademic/Hospital1112017
Yonsei UniversityAcademic/Hospital1112013
8 organizations
Page 1 / 1

Marketing (12)

OrganizationOrg typeRelationshipDate
AbraxisFor profitMKTGDec 8, 1972
American CyanamidFor profitNDA2Jul 1, 1954
Belmar PharmacyFor profitMKTGNov 26, 1973
Eli LillyFor profitNDAJan 4, 1954
Elkins SinnFor profitMKTGOct 12, 1973
G D SearleFor profitMKTG—
HospiraFor profitMKTGSep 15, 1972
KodakFor profitNDA2Sep 19, 1952
LederleFor profitMKTGJul 1, 1954
MilesFor profitMKTG—
PfizerFor profitMKTGJan 4, 1954
Watson PharmaceuticalsFor profitMKTGApr 1, 1974