Chemical: Drug
droperidol

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.



PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

Overview

Generic Names
Trade Names
  • DHBP
  • Dehidrobenzperidol
  • Dehydrobenzperidol
  • Deidrobenzperidolo
  • Dihidrobenzperidol
  • Dridol
  • Droleptan
  • Halkan
  • Inappin
  • Inapsin
  • Inapsine
  • Innovan
  • Innovar
  • Innovar-Vet
  • Inopsin
  • Inoval
  • Leptanal
  • Leptofen
  • McN-JR 4749
  • Properidol
  • Sintodril
  • Sintosian
  • Thalamanol
  • Thalamonal
  • Vetkalm
Brand Mixture Names
  • Innovar Inj (Droperidol + Fentanyl Citrate)
  • Innovar-Vet Inj (Droperidol + Fentanyl Citrate)

PharmGKB Accession Id

PA449422

Type(s):

Drug

Description

A butyrophenone with general properties similar to those of haloperidol. It is used in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593)

Source: Drug Bank

This drug has highly restrictive labeling because of the risk of acquired Long QT Syndrome and fatal torsades de pointes [Article:14999113].

Source: PharmGKB

Indication

Droperidol is ssed to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

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.

Source: Drug Bank

Pharmacology

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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Extensively metabolized.

Source: Drug Bank

Absorption

Completely absorbed following intramuscular administration.

Source: Drug Bank

Half-Life

Biphasic distribution. The rapid distribution phase is 1.4 +/- 0.5 minutes and the slower distribution phase is 14.3 +/- 6.5 minutes. Elimination half-life in adults is 134 +/- 13 minutes and may be increased in geriatric patients. In children, it is 101.5 +/- 26.4 minutes.

Source: Drug Bank

Toxicity

The intravenous LD 50 of droperidol is 20-43 mg/kg in mice; 30 mg/kg in rats; 25 mg/kg in dogs and 11-13 mg/kg in rabbits. The intramuscular LD 50 of droperidol is 195 mg/kg in mice, 104-110 mg/kg in rats; 97 mg/kg in rabbits and 200 mg/kg in guinea pigs. The manifestations of droperidol overdosage are an extension of its pharmacologic actions.

Source: Drug Bank

Chemical Properties

Chemical Formula

C22H22FN3O2

Source: Drug Bank

Isomeric SMILES

c1ccc2c(c1)[nH]c(=O)n2C3=CCN(CC3)CCCC(=O)c4ccc(cc4)F

Source: OpenEye

Canonical SMILES

FC1=CC=C(C=C1)C(=O)CCCN1CCC(=CC1)N1C(=O)NC2=CC=CC=C12

Source: Drug Bank

Average Molecular Weight

379.4274

Source: Drug Bank

Monoisotopic Molecular Weight

379.169605168

Source: Drug Bank

SMILES

FC1=CC=C(C=C1)C(=O)CCCN1CCC(=CC1)N1C(=O)NC2=CC=CC=C12

Source: Drug Bank

InChI String

InChI=1S/C22H22FN3O2/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/h1-2,4-5,7-11H,3,6,12-15H2,(H,24,28)

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Antiarrhythmic Pathway, Pharmacodynamics
    Pharmacodynamic pathway of antiarrhythmic drugs in a stylized cardiac myocyte.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ADRA1A (source: Drug Bank )
DRD2 (source: Drug Bank )

Drug Interactions

Interaction Description
quinupristin - droperidol This combination presents an increased risk of toxicity (source: Drug Bank )
tacrine - droperidol The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Droperidol, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. (source: Drug Bank )
tacrine - droperidol The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Droperidol, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents. (source: Drug Bank )
tetrabenazine - droperidol May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. (source: Drug Bank )
thiothixene - droperidol May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank )
thiothixene - droperidol May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank )
toremifene - droperidol Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. (source: Drug Bank )
trimethobenzamide - droperidol Trimethobenzamide and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank )
trimipramine - droperidol Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. (source: Drug Bank )
triprolidine - droperidol Triprolidine and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. (source: Drug Bank )
triprolidine - droperidol Triprolidine and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects. (source: Drug Bank )
trospium - droperidol Trospium and Droperidol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank )
voriconazole - droperidol Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )
vorinostat - droperidol Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )
ziprasidone - droperidol Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. (source: Drug Bank )
zuclopenthixol - droperidol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). (source: Drug Bank )

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Induces
Contraindicated With

Publications related to droperidol: 3

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The genetics of pro-arrhythmic adverse drug reactions. British journal of clinical pharmacology. 2014. Petropoulou Evmorfia, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug-induced long QT syndrome. Pharmacological reviews. 2010. Kannankeril Prince, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug-induced prolongation of the QT interval. The New England journal of medicine. 2004. Roden Dan M. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
11098-010-01
DrugBank:
DB00450
ChEBI:
4717
KEGG Drug:
D00308
PubChem Compound:
3168
PubChem Substance:
46505291
Drugs Product Database (DPD):
2167832
BindingDB:
50017705
ChemSpider:
3056
Therapeutic Targets Database:
DAP000412
FDA Drug Label at DailyMed:
f4fa5e60-5f70-46d7-8e29-dfcf8b783f2c

Clinical Trials

These are trials that mention droperidol and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, PubChem.