droperidol

Trade name: innovar

Small moleculeapproved

Approved

Jun 11, 1970

Droperidol produces marked tranquilization and sedation. It allays apprehension and provides a state of mental detachment and indifference while maintaining a state of reflex alertness. Droperidol produces an antiemetic effect as evidenced by the antagonism of apomorphine in dogs. It lowers the incidence of nausea and vomiting during surgical procedures and provides antiemetic protection in the postoperative period. Droperidol potentiates other CNS depressants. It produces mild alpha-adrenergic blockade, peripheral vascular dilatation and reduction of the pressor effect of epinephrine. It can produce hypotension and decreased peripheral vascular resistance and may decrease pulmonary arterial pressure (particularly if it is abnormally high). It may reduce the incidence of epinephrine-induced arrhythmias, but it does not prevent other cardiac arrhythmias. The exact mechanism of action is unknown, however, droperidol causes a CNS depression at subcortical levels of the brain, midbrain, and brainstem reticular formation. It may antagonize the actions of glutamic acid within the extrapyramidal system. It may also inhibit cathecolamine receptors and the reuptake of neurotransmiters and has strong central antidopaminergic action and weak central anticholinergic action. It can also produce ganglionic blockade and reduced affective response. The main actions seem to stem from its potent Dopamine (2) receptor antagonism with minor antagonistic effects on alpha-1 adrenergic receptors as well. Droperidol is used to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures. — NCATS

Clinical trial activity

27 trials · 29 clinical orgs · 15 marketing orgs

Phase 1
1
Phase 2
8
Phase 3
7
Phase 4
9

Earliest trial started Oct 1, 2005 (NCT00209885)

Timeline

1970s

  1. Jun 11, 1970

    Akorn, Inc. — Earliest FDA Approval

  2. Jun 11, 1970

    Akorn, Inc. — NDA Secondary Org

  3. Jun 11, 1970

    Johnson and Johnson — NDA Secondary Org

  4. Jun 11, 1970

    Akorn, Inc. — Marketing Organization

  5. Jun 11, 1970

    Rising Pharmaceuticals — Marketing Organization

  6. Jun 11, 1970

    Akorn, Inc. — NDA Organization

1980s

  1. Nov 17, 1986

    Abraxis — Marketing Organization

  2. Feb 29, 1988

    Hospira — Marketing Organization

  3. Sep 6, 1988

    Smith & Nephew — Marketing Organization

  4. Oct 19, 1988

    Teligent Pharmaceuticals — Marketing Organization

  5. Oct 20, 1988

    AstraZeneca — Marketing Organization

  6. Oct 23, 1988

    Lutipold — Marketing Organization

  7. Oct 24, 1988

    Sankyo — Marketing Organization

2000s

  1. Jan 1, 2009

    Earliest Phase 3 Sponsor(trial)

2010s

  1. Dec 14, 2017

    Eurohlth Intl Sarl — Marketing Organization

  2. Dec 14, 2017

    Hikma — Marketing Organization

2020s

  1. Jan 1, 2021

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2025

    Earliest Phase 1 Sponsor(trial)

Indications

Mechanism of action

Combination products

Approval history

  • approvedJun 11, 1970

Chemistry & pharmacology

Loading structure…

SMILES

FC1=CC=C(C=C1)C(=O)CCCN2CCC(=CC2)N3C(=O)NC4=C3C=CC=C4
Mol. weight
379.4274 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warning

Sources

Also known as

  • 1-(1-(3-(p-fluorobenzoyl)propyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • 1-(1-(3-(p-fluorobenzoyl)propyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • 1-{1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl}-2,3-dihydro-1h-benzo[d]imidazol-2-one
  • 1-{1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl}-2,3-dihydro-1h-benzo[d]imidazol-2-one
  • 1-{1-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1,2,3,6-tetrahydro-pyridin-4-yl}-1,3-dihydro-benzoimidazol-2-one
  • 1-{1-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1,2,3,6-tetrahydro-pyridin-4-yl}-1,3-dihydro-benzoimidazol-2-one
  • 1-(1-(4-(p-fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • 1-(1-(4-(p-fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • dehydrobenzperidol
  • dehydrobenzperidol
  • dehydrobenzperidol
  • dridol
  • dridol
  • droleptan
  • droleptan
  • droleptan
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • droperidol
  • dropéridol
  • dropéridol
  • droperidolo
  • droperidolo
  • droperidolum
  • droperidolum
  • inapsin
  • inapsine
  • inapsine
  • inapsine
  • mcn-jr-4749
  • mcn-jr-4749
  • neurolidol
  • r-4749
  • r-4749

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07015528Early Phase 1 (Phase 1)Sep 1, 2025Stanford University
NCT05401058N/AOct 10, 2022Jiao Tong University
NCT05244460Phase 3Dec 2, 2021Lake Erie College of Osteopathic Medicine, Mercy Health Partners, Cincinnati
NCT05068180Phase 4Oct 5, 2021Jiao Tong University
NCT05065567Phase 2Aug 30, 2021The Spectrum Health Group
NCT03944681N/AApr 23, 2019Medical University of Gdansk
NCT04411069Phase 3Feb 20, 2019Instituto do Cancer do Estado de São Paulo
NCT03677323N/AOct 31, 2018Clinique Saint Jean, Montpellier
NCT03546088N/AFeb 20, 2018Iuliu Hatieganu University of Medicine and Pharmacy
NCT03036514N/AApr 5, 2017University of Antwerp
NCT03023462Phase 4Apr 1, 2017Ostfold University
NCT02625181N/AJul 1, 2016University of Washington, Vanderbilt University
NCT02744495Phase 3Feb 1, 2016Hôpital Privé de Parly II - Le Chesnay
NCT02282956Phase 4Oct 1, 2014Spitalregion Rheintal, Werdenberg, Sarganserland
NCT02078336Phase 4Dec 1, 2013Katholieke Universiteit Leuven
NCT01942343Phase 3Oct 1, 2013University of Strasbourg
NCT01765829Phase 3Nov 1, 2012Government of Spain, Universidad Carlos III Madrid
NCT01432977Phase 3Sep 1, 2011University of Limoges
NCT01406860N/AJul 1, 2011University of Iowa
NCT01819857Phase 4Jun 1, 2011Medical University of Gdansk
Showing 20 of 27 trials
Page 1 / 2

Organizations

Research & Development (29)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Jiao Tong UniversityAcademic/Hospital2222021
Medical University of GdanskAcademic/Hospital2222011
Aristotle University of ThessalonikiAcademic/Hospital1112008
Clinique Saint Jean, MontpellierAcademic/Hospital1112018
Government of SpainGovernment1112012
Hôpital Privé de Parly II - Le ChesnayAcademic/Hospital1112016
Instituto do Cancer do Estado de São PauloAcademic/Hospital1112019
Iuliu Hatieganu University of Medicine and PharmacyAcademic/Hospital1112018
Katholieke Universiteit LeuvenAcademic/Hospital1112013
Lake Erie College of Osteopathic MedicineAcademic/Hospital1012021
Mercy Health Partners, CincinnatiAcademic/Hospital1112021
Ostfold UniversityAcademic/Hospital1112017
ProStrakenFor profit1012007
Spitalregion Rheintal, Werdenberg, SarganserlandAcademic/Hospital1112014
Stanford UniversityAcademic/Hospital1112025
The Spectrum Health GroupAcademic/Hospital1112021
Universidad Carlos III MadridAcademic/Hospital1012012
University of AntwerpAcademic/Hospital1112017
University of BordeauxAcademic/Hospital1112007
University of British ColumbiaAcademic/Hospital1112008
29 organizations
Page 1 / 2

Marketing (17)

OrganizationOrg typeRelationshipDate
AbraxisFor profitMKTGNov 17, 1986
Akorn, Inc.For profitNDA2Jun 11, 1970
Akorn, Inc.For profitMKTGJun 11, 1970
Akorn, Inc.For profitNDAJun 11, 1970
AstraZenecaFor profitMKTGOct 20, 1988
Athenex, Inc.For profitMKTG
Eurohlth Intl SarlFor profitMKTGDec 14, 2017
HikmaFor profitMKTGDec 14, 2017
HospiraFor profitMKTGFeb 29, 1988
Johnson and JohnsonFor profitNDA2Jun 11, 1970
LutipoldFor profitMKTGOct 23, 1988
Rising PharmaceuticalsFor profitMKTGJun 11, 1970
SOLOPAKFor profitMKTG
SankyoFor profitMKTGOct 24, 1988
Smith & NephewFor profitMKTGSep 6, 1988
Teligent PharmaceuticalsFor profitMKTGOct 19, 1988
Watson PharmaceuticalsFor profitMKTG