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droperidol (Dridol / Xomolix)

✓ Approved

Kyowa Kirin Co., Ltd. · DRD2 · Small Molecule

What is droperidol?

droperidol is a small molecule developed by Kyowa Kirin Co., Ltd.. It is approved for therapeutic indications via injectable (others) or intravenous (iv).

Drug Profile

Brand NamesDridol, Xomolix
CompanyKyowa Kirin Co., Ltd.
Drug ClassSmall Molecule
Molecular TargetDRD2
RouteInjectable (Others), Intravenous (IV)
StatusApproved

Mechanism of Action

Molecular Targets

droperidol acts on 1 molecular target:

DRD2dopamine receptor D2 (D2DR, D2R)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

droperidol is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Surgical and medical proceduresProphylaxis of nausea and vomiting✓ Approved

Related Research Articles

PubMedClinical neuropharmacology2026-09-24

Cytotoxic Lesion of the Corpus Callosum After Hospital-Administered Intravenous Fentanyl for Trigeminal Neuralgia: A Case Report and Focused Review.

Benito-León Julián J

Fentanyl-associated neurotoxicity is increasingly recognized across illicit, inhalational, transdermal, pediatric, and delayed posthypoxic exposures, but isolated splenial CLOCC after hospital-administered intravenous fentanyl has not been well characterized. This is a single-patient case report with a focused review of fentanyl-associated neurotoxic syndromes and proposed mechanisms. A 41-year-old woman with trigeminal neuralgia presented with severe facial pain. After droperidol, metoclopramide, and metamizole failed to control symptoms, intravenous fentanyl (75 μg) was administered. Soon afterward, she developed dizziness, nausea, vomiting, left-sided paresthesias, hypoesthesia, and mild weakness. Initial computed tomography was unrevealing, and cerebrospinal fluid findings were normal. Brain magnetic resonance imaging (MRI) obtained 8 days later showed a 6-mm midline splenial lesion that was hyperintense on T2-weighted and FLAIR sequences, restricted on diffusion-weighted imaging, and nonenhancing, consistent with CLOCC. Follow-up MRI showed complete radiologic resolution, but serial assessments documented persistent deficits in the left upper and lower extremities, including impaired fine motor control, dysdiadochokinesia, arm and leg weakness, foot drag, and gait imbalance; somatosensory-evoked potentials showed mild dysfunction of the left lower-extremity pathway. Review of comparable fentanyl-associated cases shows a spectrum ranging from isolated callosal injury to diffuse, cerebellar, and delayed leukoencephalopathic phenotypes. This case expands the neuroimaging spectrum of fentanyl-associated brain injury and supports a toxic-metabolic pathogenesis in which splenial CLOCC may represent a focal manifestation of broader opioid-related white-matter vulnerability.

PubMedMethods and protocols2026-09-23

Comparison of the Utility of Amplitude-Spectral and Coherence Features of Psychotropic Drugs' Action on ECoG Signal for Pharmaco-EEG Based Drug Screening in Rats.

Sysoev Yuriy I YI, Kurmazov Nikita S NS, Shitc Darya D DD, Okovityi Sergey V SV

A naive Bayesian classifier (NBC) combined with principal component analysis (PCA) effectively differentiates the dose-dependent effects of certain groups of psychoactive drugs based on their impact on the amplitude-spectral characteristics of electrocorticograms (ECoG) in rats. This approach has been shown to be useful for pharmacological screening of agents with unknown or poorly understood activity. Despite previously obtained optimistic results, classification determination for some drugs was inaccurate, necessitating the search for possible ways to improve the predictive effectiveness of the proposed algorithm. One possible approach would be to use as input quantitative data not only the impact of the psychoactive drugs studied on the amplitude-spectral characteristics of ECoG but also connectivity changes, including the average coherence power of different pairs of leads. The aim of this study was to compare the accuracy of NBC in classifying the pharmacological mechanism of action of agents with well-known mechanisms (test set) using pharmaco-EEG data on changes in the amplitude-spectral characteristics of ECoG, coherence, and the combined use of two data sets. Materials and methods. Experiments were performed on Wistar rats with chronically implanted ECoG electrodes. The training set, relative to which the effects of the pharmacological agents from the test set were classified, were the matrices of effects of 12 pharmacological agents: the NMDA antagonist dizocilpine, the D2/D3 antagonists haloperidol and sulpiride, the M-anticholinergic tropicamide, the H1/5HT2A receptor blocker hydroxyzine, the acetylcholinesterase inhibitor galantamine, the alpha-2 adrenergic agonist dexmedetomidine, the alpha-2 adrenergic antagonist atipamezole, the adenosine receptor blocker caffeine and the GABA-mimetics aminophenylbutyric acid (phenibut), bromdihydrochlorophenylbenzodiazepine (phenazepam) and 5-ethyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione. The test set included various drugs with tropism for the targets of the training set drugs: dopamine receptor antagonists chlorpromazine, droperidol, tiapride and raclopride, H1-histamine blockers diphenhydramine and promethazine, 5-HT2-receptor blockers ritanserin and glemenserin, acetylcholinesterase inhibitor ipidacrine, alpha2-adrenergic receptor antagonist yohimbine, alpha2-adrenergic agonists medetomidine and xylazine, GABA-mimetics 5-ethyl-5-(1-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrione and chloral hydrate. The analysis of the ECoG signal included the calculation of 132 amplitude-spectral characteristics and 75 coherence indicators, which, using the PCA, led to new integrative indicators used for further classification of the NBC. Results and discussion. For each drug in the test set, the median similarity probability with a particular group from the training set was calculated, which was used to assess the classification quality. It was found that, when using the amplitude-spectral characteristics of ECoG, the proposed methodological approach allows for the identification of the ECoG effects of several groups of psychoactive drugs, including D2/D3-dopamine, M-cholinergic, H1-histamine, and 5-HT2-serotonin receptor blockers, AChE inhibitors, GABA-mimetics, and alpha-2-adrenergic receptor agonists and antagonists. This approach enabled the correct classification of 18 of 24 groups in the test set. When using changes in coherence indices as the initial data, the classification accuracy also amounted to 18 of 24 groups. When combining the two data sets, the number of correctly identified NBC groups was 20 of 24 groups. When comparing the classification during training (confusion matrix), it was found that coherence data or adding coherence data to the data based on changes in amplitude-spectral characteristics leads to a statistically significant (p < 0.01 in both cases) increase in accuracy. Conclusions. The obtained data demonstrated high accuracy in classifying the pharmacological activity of the test sample drugs using any of the three compared approaches. Despite the lack of statistically significant differences between them, classification based on the combined dataset demonstrated a higher number of "correct" similarities. This allows us to recommend the approach based on combined data of drug effects on amplitude-spectral characteristics and coherence as the most promising for further studies using pharmaco-EEG screening.

PubMedThe American journal of emergency medicine2026-09-13

QTc interval changes following low-dose droperidol administration in the emergency department.

Bartoe Aaron A, Berkvens Laura L, Solano Aimee A, Hacnik Justin J et al.

PubMedAnnals of medicine and surgery (2012)2026-09-11

Addition of lidocaine to prophylactic ondansetron and dexamethasone in high-risk adults for postoperative nausea and vomiting: a randomized, controlled, double-blinded study.

Yi Ke-Xin KX, Du Ming-Cheng MC, Zheng Jia J, Long Xiang X et al.

A triple combination of dexamethasone, ondansetron, and droperidol is recommended as prophylaxis to prevent postoperative nausea and vomiting in high-risk patients. However, the administration of droperidol is controversial owing to its fatal side effects. Considering the antiemetic effect of lidocaine, the aim of this study was to determine if its incorporation could mitigate postoperative nausea and vomiting in adults at high risk. This randomized, controlled, double-blind study was conducted from 10 June 2023 to 31 October 2023. Based on a preliminary experiment, 260 patients were enrolled in the trial, with 130 in group C (saline) and 130 in group L (lidocaine). The primary outcome was the incidence of postoperative nausea and vomiting at 24 hours postoperatively. The secondary outcomes were the Quality of Recovery-40 (QoR-40) score at 24 hours postoperatively and the time to extubation. Adverse events that occurred during the study were recorded. The incidence of postoperative nausea and vomiting differed between the groups, with 26.6% (33 patients) in group C and 16.4% (21 patients) in group L (P = 0.0484). The QoR-40 score was 176.45 ± 10.87 in group C and 186.59 ± 9.79 in group L (P < 0.001). No adverse events were observed during the trial. In high-risk patients, the addition of lidocaine to ondansetron and dexamethasone effectively reduced the incidence of postoperative nausea and vomiting and improved the quality of recovery.

PubMedFederal practitioner : for the health care professionals of the VA, DoD, and PHS2026-09-10

Effectiveness and Safety of Droperidol Use in the VA Greater Los Angeles Healthcare System Emergency Department.

Minoda Emily E, Kono Shogo S, Pham My-Phuong MP, Acharya Hemang H et al.

Droperidol, a butyrophenone antipsychotic, is used for postoperative nausea and vomiting and as a sedative, anxiolytic, and analgesic. Concerns about potential QTc (corrected QT interval) prolongation led the US Food and Drug Administration (FDA) to issue a boxed warning and halt manufacturing. However, recent studies have supported droperidol's safety and it was reintroduced in 2019. Given the limited available options for managing acute agitation at the Veterans Affairs Greater Los Angeles Healthcare System (VAGLAHS), there has been interest in re-evaluating the risks associated with droperidol use for sedation, anxiolysis, analgesia, and as an antiemetic. This retrospective chart review examined patients who received droperidol in the VAGLAHS emergency department (ED) from February 2021 to April 2023. The primary outcome was all-cause mortality after droperidol administration within 24 hours. Secondary outcomes included the efficacy of droperidol, incidence of QT prolongation, incidence of extrapyramidal symptoms (EPS) such as akathisia, dystonia, parkinsonism or tardive dyskinesia, and incidence of respiratory depression. Of 207 patients receiving droperidol, 38 (18.4%) were adults aged ≥ 65 years. Droperidol was used for acute agitation in 183 patients (88.4%) and as an antiemetic in 24 (11.6%) patients. No deaths were observed following droperidol administration in a 24-hour period. The need for rescue medication occurred in 15 patients (7.3%). EPS such as tardive dyskinesia and dystonia occurred in 2 (1.0%) patients. No arrhythmias or respiratory depression were observed within 24 hours of administration. No clinically relevant QTc prolongation was observed. No fatalities were seen among patients who received droperidol in the VAGLAHS ED. Despite the boxed warning issued by the FDA, these findings suggest droperidol is safe and effective in managing agitation and as an antiemetic.

PubMedInternational clinical psychopharmacology2026-08-25

Efficacy and safety of intramuscular and intravenous midazolam for acute agitation in emergency settings: a systematic review.

Bottaro Federico F, Nosari Guido G, Tesic Isidora I, Brambilla Paolo P et al.

Acute agitation often requires parenteral sedation in emergency care. Midazolam is widely used for its rapid onset, short duration of action, and availability for intramuscular and intravenous administration, but its efficacy and safety across emergency settings remain incompletely understood. Following Preferred Reporting Items for Systematic reviews and Meta-Analyses 2020 guidelines, we searched PubMed, Scopus, and Web of Science for original studies evaluating intramuscular or intravenous midazolam, as monotherapy or in combination regimens, for acute agitation in emergency department (ED), psychiatric emergency service (PES), and prehospital emergency medical service (EMS) settings. Twenty-three studies met the inclusion criteria. Intramuscular midazolam was generally associated with rapid early sedation in ED studies, although this advantage was sometimes offset by less sustained clinical effects and higher need for rescue or additional sedation. Intravenous midazolam monotherapy showed a greater need for active airway management in its main direct comparison with intravenous droperidol. Midazolam-droperidol combinations showed more consistent advantages for rapid early sedation in monitored ED settings. In PES and EMS, midazolam's role was more dependent on clinical context, operational constraints and postsedation monitoring. Midazolam appears a useful rapid-onset option, but should not be considered a consistently superior standalone strategy. Future multicenter studies should better elucidate its safest and most effective use.

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