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QuickView for Droperidol (compound)


PubChem
Name: Droperidol
PubChem Compound ID: 11957508
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)
Molecular formula: C22H22FN3O2
Molecular weight: 379.428 g/mol
Synonyms:
EU-0100346
DrugBank
Identification
Name: Droperidol
Name (isomeric): DB00450
Drug Type: small molecule
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)
Brand: Innovan, Sintodril, McN-JR 4749, Dehidrobenzperidol, Inapsine, Leptofen, Innovar-Vet, Inapsin, Thalamanol, Dehydrobenzperidol, Sintosian, Leptanal, Inopsin, Inoval, Vetkalm, Dridol, Dihidrobenzperidol, Halkan, Deidrobenzperidolo, Properidol, DHBP, Thalamonal, Droleptan, Inappin, Innovar
Brand name mixture: Innovar-Vet Inj(Droperidol + Fentanyl Citrate), Innovar Inj(Droperidol + Fentanyl Citrate)
Category: Adjuvants, Anesthesia, Antiemetics, Dopamine Antagonists, Antipsychotic Agents
CAS number: 548-73-2
Pharmacology
Indication: Droperidol is ssed to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures.
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 proce...
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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 centra...
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Absorption: Completely absorbed following intramuscular administration.
Biotransformation: Extensively metabolized.
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.
Toxicity: The intravenous LD50 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 LD50 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.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
BuprenorphineDroperidol may enhance the CNS depressant effect of CNS Depressants like buprenorphine. Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use.
TacrineThe 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.
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
TriprolidineTriprolidine 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.
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Targets