droperidol
Trade name: innovar
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
Earliest trial started Oct 1, 2005 (NCT00209885)
Timeline
1970s
- Jun 11, 1970
Akorn, Inc. — Earliest FDA Approval
- Jun 11, 1970
Akorn, Inc. — NDA Secondary Org
- Jun 11, 1970
Johnson and Johnson — NDA Secondary Org
- Jun 11, 1970
Akorn, Inc. — Marketing Organization
- Jun 11, 1970
Rising Pharmaceuticals — Marketing Organization
- Jun 11, 1970
Akorn, Inc. — NDA Organization
1980s
- Nov 17, 1986
Abraxis — Marketing Organization
- Feb 29, 1988
Hospira — Marketing Organization
- Sep 6, 1988
Smith & Nephew — Marketing Organization
- Oct 19, 1988
Teligent Pharmaceuticals — Marketing Organization
- Oct 20, 1988
AstraZeneca — Marketing Organization
- Oct 23, 1988
Lutipold — Marketing Organization
- Oct 24, 1988
Sankyo — Marketing Organization
2000s
- Jan 1, 2009
Earliest Phase 3 Sponsor(trial)
2010s
- Dec 14, 2017
Eurohlth Intl Sarl — Marketing Organization
- Dec 14, 2017
Hikma — Marketing Organization
Indications
Studied for
- Arthropathy, Neurogenic · Phase 4
- Cannabis · Phase 3
- Cholecystolithiasis · Phase 4
- Colonic Neoplasms · Phase 4
- Dental Care for Persons with Disabilities · Phase 4
- Drug Interactions · Phase 3
- Fractures, Bone · Phase 4
- Genital Neoplasms, Female · Phase 4
- Hallux Valgus · Phase 4
- Heart Diseases · Phase 4
- Hernia, Inguinal · Phase 4
- Kidney Neoplasms · Phase 4
- Liver Neoplasms · Phase 4
- Mental Health · Phase 3
- Nausea · Phase 4
- Pain · Phase 3
- Postoperative Nausea and Vomiting · Phase 4
- Postoperative Pain · Phase 4
- Prostatic Neoplasms · Phase 4
- Psychomotor Agitation · Phase 3
- Rectal Neoplasms · Phase 4
- Sigmoid Neoplasms · Phase 4
- Stomach Neoplasms · Phase 4
- Urinary Bladder Neoplasms · Phase 4
- Vomiting · Phase 4
Mechanism of action
- Serotonin 2a (5-HT2a) receptorANTAGONIST
HTR2A antagonist
- D2-like dopamine receptorANTAGONIST
D2-like dopamine receptor antagonist
Combination products
innovar
with fentanyl
Approval history
- approvedJun 11, 1970
Chemistry & pharmacology
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
Sources
- WikipediaDroperidol ↗
- NCATSO9U0F09D5X ↗
- ChEMBLCHEMBL2104603 ↗
- ChEMBLCHEMBL1108 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07015528 | Early Phase 1 (Phase 1) | Sep 1, 2025 | Stanford University |
| NCT05401058 | N/A | Oct 10, 2022 | Jiao Tong University |
| NCT05244460 | Phase 3 | Dec 2, 2021 | Lake Erie College of Osteopathic Medicine, Mercy Health Partners, Cincinnati |
| NCT05068180 | Phase 4 | Oct 5, 2021 | Jiao Tong University |
| NCT05065567 | Phase 2 | Aug 30, 2021 | The Spectrum Health Group |
| NCT03944681 | N/A | Apr 23, 2019 | Medical University of Gdansk |
| NCT04411069 | Phase 3 | Feb 20, 2019 | Instituto do Cancer do Estado de São Paulo |
| NCT03677323 | N/A | Oct 31, 2018 | Clinique Saint Jean, Montpellier |
| NCT03546088 | N/A | Feb 20, 2018 | Iuliu Hatieganu University of Medicine and Pharmacy |
| NCT03036514 | N/A | Apr 5, 2017 | University of Antwerp |
| NCT03023462 | Phase 4 | Apr 1, 2017 | Ostfold University |
| NCT02625181 | N/A | Jul 1, 2016 | University of Washington, Vanderbilt University |
| NCT02744495 | Phase 3 | Feb 1, 2016 | Hôpital Privé de Parly II - Le Chesnay |
| NCT02282956 | Phase 4 | Oct 1, 2014 | Spitalregion Rheintal, Werdenberg, Sarganserland |
| NCT02078336 | Phase 4 | Dec 1, 2013 | Katholieke Universiteit Leuven |
| NCT01942343 | Phase 3 | Oct 1, 2013 | University of Strasbourg |
| NCT01765829 | Phase 3 | Nov 1, 2012 | Government of Spain, Universidad Carlos III Madrid |
| NCT01432977 | Phase 3 | Sep 1, 2011 | University of Limoges |
| NCT01406860 | N/A | Jul 1, 2011 | University of Iowa |
| NCT01819857 | Phase 4 | Jun 1, 2011 | Medical University of Gdansk |
Organizations
Research & Development (29)
Marketing (17)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Abraxis | For profit | MKTG | Nov 17, 1986 |
| Akorn, Inc. | For profit | NDA2 | Jun 11, 1970 |
| Akorn, Inc. | For profit | MKTG | Jun 11, 1970 |
| Akorn, Inc. | For profit | NDA | Jun 11, 1970 |
| AstraZeneca | For profit | MKTG | Oct 20, 1988 |
| Athenex, Inc. | For profit | MKTG | — |
| Eurohlth Intl Sarl | For profit | MKTG | Dec 14, 2017 |
| Hikma | For profit | MKTG | Dec 14, 2017 |
| Hospira | For profit | MKTG | Feb 29, 1988 |
| Johnson and Johnson | For profit | NDA2 | Jun 11, 1970 |
| Lutipold | For profit | MKTG | Oct 23, 1988 |
| Rising Pharmaceuticals | For profit | MKTG | Jun 11, 1970 |
| SOLOPAK | For profit | MKTG | — |
| Sankyo | For profit | MKTG | Oct 24, 1988 |
| Smith & Nephew | For profit | MKTG | Sep 6, 1988 |
| Teligent Pharmaceuticals | For profit | MKTG | Oct 19, 1988 |
| Watson Pharmaceuticals | For profit | MKTG | — |