Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C22H22FN3O2.C3H6O3 |
| Molecular Weight | 469.5053 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(O)C(O)=O.FC1=CC=C(C=C1)C(=O)CCCN2CCC(=CC2)N3C(=O)NC4=C3C=CC=C4
InChI
InChIKey=CUYSTLHETVVORS-UHFFFAOYSA-N
InChI=1S/C22H22FN3O2.C3H6O3/c23-17-9-7-16(8-10-17)21(27)6-3-13-25-14-11-18(12-15-25)26-20-5-2-1-4-19(20)24-22(26)28;1-2(4)3(5)6/h1-2,4-5,7-11H,3,6,12-15H2,(H,24,28);2,4H,1H3,(H,5,6)
DescriptionSources: http://www.drugbank.ca/drugs/DB00450Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/pro/droperidol.html
Sources: http://www.drugbank.ca/drugs/DB00450
Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/pro/droperidol.html
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.
CNS Activity
Sources: http://www.drugbank.ca/drugs/DB00450
Curator's Comment: Droperidol causes a CNS depression at subcortical levels of the brain, midbrain, and brainstem reticular formation.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL217 Sources: http://www.drugbank.ca/drugs/DB00450 |
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Target ID: CHEMBL229 Sources: http://www.drugbank.ca/drugs/DB00450 |
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Target ID: CHEMBL240 |
32.2 nM [IC50] | ||
Target ID: CHEMBL224 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Secondary | INAPSINE Approved UseDroperidol injection is indicated to reduce the incidence of nausea and vomiting associated with surgical and diagnostic procedures. Launch Date1970 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
26.6 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30574300/ |
0.02 mg/kg single, intravenous dose: 0.02 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
DROPERIDOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.5 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30574300/ |
0.02 mg/kg single, nasal dose: 0.02 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
DROPERIDOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
40 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30574300/ |
0.02 mg/kg single, intravenous dose: 0.02 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
DROPERIDOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
18.7 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30574300/ |
0.02 mg/kg single, nasal dose: 0.02 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
DROPERIDOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30574300/ |
0.02 mg/kg single, intravenous dose: 0.02 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
DROPERIDOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30574300/ |
0.02 mg/kg single, nasal dose: 0.02 mg/kg route of administration: Nasal experiment type: SINGLE co-administered: |
DROPERIDOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
0.4 mg/kg multiple, oral Dose: 0.4 mg/kg Route: oral Route: multiple Dose: 0.4 mg/kg Sources: |
unhealthy, 2-9 years Health Status: unhealthy Age Group: 2-9 years Sources: |
Disc. AE: QT interval prolonged... AEs leading to discontinuation/dose reduction: QT interval prolonged Sources: |
8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
Other AEs: Asthenia, Chills... Other AEs: Asthenia (24.6%) Sources: Chills (3.3%) Anorexia (3.3%) Akathisia (16.4%) Anxiety (27.9%) Confusion (3.3%) Dizziness (9.8%) Dry mouth (9.8%) Nervousness (4.9%) Paresthesia (3.3%) Somnolence (24.6%) Tremor (1.6%) Pharyngitis (4.9%) Rhinitis (4.9%) Sweaty (8.2%) |
2.5 mg multiple, intravenous Dose: 2.5 mg Route: intravenous Route: multiple Dose: 2.5 mg Sources: |
unhealthy |
Disc. AE: Torsades de pointes... AEs leading to discontinuation/dose reduction: Torsades de pointes Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| QT interval prolonged | Disc. AE | 0.4 mg/kg multiple, oral Dose: 0.4 mg/kg Route: oral Route: multiple Dose: 0.4 mg/kg Sources: |
unhealthy, 2-9 years Health Status: unhealthy Age Group: 2-9 years Sources: |
| Tremor | 1.6% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Akathisia | 16.4% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Asthenia | 24.6% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Somnolence | 24.6% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Anxiety | 27.9% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Anorexia | 3.3% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Chills | 3.3% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Confusion | 3.3% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Paresthesia | 3.3% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Nervousness | 4.9% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Pharyngitis | 4.9% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Rhinitis | 4.9% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Sweaty | 8.2% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Dizziness | 9.8% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Dry mouth | 9.8% | 8.25 mg single, intramuscular Highest studied dose Dose: 8.25 mg Route: intramuscular Route: single Dose: 8.25 mg Sources: |
unhealthy, 42 ± 10.0 years Health Status: unhealthy Age Group: 42 ± 10.0 years Sex: M+F Sources: |
| Torsades de pointes | Disc. AE | 2.5 mg multiple, intravenous Dose: 2.5 mg Route: intravenous Route: multiple Dose: 2.5 mg Sources: |
unhealthy |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| major | ||||
| major |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| The effects of ketamine and of Innovar anesthesia on digitalis tolerance in dogs. | 1975 Jan-Feb |
|
| Rapid induction of acute dyskinesia by droperidol. | 1975 Jul |
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| [Postoperative nausea and vomiting--still a problem?]. | 2001 |
|
| Ondansetron: a review of its use as an antiemetic in children. | 2001 |
|
| Placebo-controlled comparison of dolasetron and metoclopramide in preventing postoperative nausea and vomiting in patients undergoing hysterectomy. | 2001 Apr |
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| Patient-controlled epidural analgesia versus continuous epidural analgesia after total knee arthroplasty. | 2001 Apr |
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| [The influence of age on hemodynamics and the dose requirements of propofol and buprenorphine in total intravenous anesthesia combined with continuous epidural anesthesia]. | 2001 Aug |
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| Warnings strengthened on tranquilizer inapsine (Droperidol). | 2001 Dec 18 |
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| Preparation, premedication, and surveillance. | 2001 Feb |
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| [Prevention of postoperative nausea and vomiting in gynecologic surgery with 3 fixed doses of metoclopramide, droperidol or placebo]. | 2001 Feb |
|
| The effect of betahistine on vestibular habituation: comparison of rotatory and sway habituation training. | 2001 Jul |
|
| [Prophylaxis of nausea and vomiting after thyroid surgery: comparison of oral and intravenous dolasetron with intravenous droperidol and placebo]. | 2001 Jul |
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| Droperidol: an effective adjuvant for difficult cases of conscious sedation? | 2001 Jul |
|
| Combination of droperidol and ondansetron reduces PONV after pediatric strabismus surgery more than single drug therapy. | 2001 Jul |
|
| Outpatient laparoscopic adrenalectomy in patients with Conn's syndrome. | 2001 Jun |
|
| Plasma glucocorticoid concentrations after fentanyl-droperidol, ketamine-xylazine and ketamine-diazepam anaesthesia in New Zealand white rabbits. | 2001 Jun 23 |
|
| Optimising management of delirium. Withdrawal of Droleptan (droperidol). | 2001 Jun 30 |
|
| Small doses of propofol, droperidol, and metoclopramide for the prevention of postoperative nausea and vomiting after thyroidectomy. | 2001 Mar |
|
| Dexamethasone for preventing nausea and vomiting associated with epidural morphine: a dose-ranging study. | 2001 Mar |
|
| In vitro neuromuscular effects of droperidol in rats. | 2001 May |
|
| Evaluation of droperidol in the acutely agitated child or adolescent. | 2001 Nov |
|
| Antipsychotic drugs: prolonged QTc interval, torsade de pointes, and sudden death. | 2001 Nov |
|
| IM droperidol as premedication attenuates intraoperative hypothermia. | 2001 Oct |
|
| Whose drug is it anyway? | 2001 Oct 13 |
|
| [Therapy of angina pectoris pain: morphine or thalamonal?]. | 2001 Oct 26 |
|
| [Postoperative nausea--still a problem]. | 2001 Oct 3 |
|
| Prehospital sedation with intramuscular droperidol: a one-year pilot. | 2001 Oct-Dec |
|
| Antipsychotic-related QTc prolongation, torsade de pointes and sudden death. | 2002 |
|
| Current practices in managing acutely disturbed patients at three hospitals in Rio de Janeiro-Brazil: a prevalence study. | 2002 |
|
| Use of sevoflurane during cardiopulmonary bypass decreases incidence of awareness. | 2002 Apr |
|
| The black box warning. | 2002 Fall |
|
| [Continuous epidural administration of droperidol to prevent postoperative nausea and vomiting]. | 2002 Feb |
|
| [Prophylaxis of Postoperative Nausea and Vomiting FollowingGynaecological Laparoscopy]. | 2002 Jan |
|
| A randomized clinical trial to assess the efficacy of intramuscular droperidol for the treatment of acute migraine headache. | 2002 Jan |
|
| Effects of sevoflurane on electrocorticography in patients with intractable temporal lobe epilepsy. | 2002 Jan |
|
| Monocomponent chemoembolization in oral and oropharyngeal cancer using an aqueous crystal suspension of cisplatin. | 2002 Jan 21 |
|
| Dolasetron decreases postoperative nausea and vomiting after breast surgery. | 2002 Jul-Aug |
|
| Four-step local anesthesia and sedation for thoracoscopic diagnosis and management of pleural diseases. | 2002 Jun |
|
| Droperidol--behind the black box warning. | 2002 Jun |
|
| Derivative spectrophotometric determination of droperidol in presence of parabens. | 2002 Jun 20 |
|
| Continuous epidural, not intravenous, droperidol inhibits pruritus, nausea, and vomiting during epidural morphine analgesia. | 2002 Mar |
|
| Treatment patterns of isolated benign headache in US emergency departments. | 2002 Mar |
|
| Comparison of granisetron and ramosetron for the prevention of nausea and vomiting after thyroidectomy. | 2002 May |
|
| Using imprecise probabilities to address the questions of inference and decision in randomized clinical trials. | 2002 May |
|
| Oral ondansetron, tropisetron or metoclopramide to prevent postoperative nausea and vomiting: a comparison in high-risk patients undergoing thyroid or parathyroid surgery. | 2002 May |
|
| Effect of intravenous droperidol on intraocular pressure and retrobulbar hemodynamics. | 2002 May-Jun |
|
| Acute dystonia by droperidol during intravenous patient-controlled analgesia in young patients. | 2002 Oct |
|
| Droperidol: a cost-effective antiemetic for over thirty years. | 2002 Oct |
|
| Effects of anesthesia on efferent-mediated adaptation of the DPOAE. | 2002 Sep |
|
| The addition of antiemetics to the morphine solution in patient controlled analgesia syringes used by children after an appendicectomy does not reduce the incidence of postoperative nausea and vomiting. | 2002 Sep |
Patents
Sample Use Guides
Dosage: The dosage should be individualized. Factors to be considered in determining dose are age, body weight, physical status, underlying pathological condition, use of other drugs, the type of anesthesia to be used, and the surgical procedure involved. Vital signs and ECG should be monitored closely.
Maximum Dosage: The maximum recommended initial dose is 2.5 mg IM or slow IV. Additional 1.25 mg doses of droperidol may be administered to achieve the desired effect. The additional doses should be administered with caution and only if the potential benefit outweighs the potential risk.
Route of Administration:
Intravenous
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SUB01839MIG
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9956314
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09NO5N37E0
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100000087719
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ACTIVE MOIETY
SUBSTANCE RECORD
