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Namespace Prefixes

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Statements

Subject Item
n2:DB00450
rdf:type
n3:Drug
n3: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)
n3:dosage
n12:271B5224-363D-11E5-9242-09173F13E4C5 n12:271B5225-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3:halfLife
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.
n3:indication
Droperidol is ssed to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures.
n3:manufacturer
n14:271B5219-363D-11E5-9242-09173F13E4C5 n14:271B521A-363D-11E5-9242-09173F13E4C5 n14:271B521F-363D-11E5-9242-09173F13E4C5 n14:271B5220-363D-11E5-9242-09173F13E4C5 n14:271B521D-363D-11E5-9242-09173F13E4C5 n14:271B521E-363D-11E5-9242-09173F13E4C5 n14:271B521B-363D-11E5-9242-09173F13E4C5 n14:271B521C-363D-11E5-9242-09173F13E4C5
owl:sameAs
n9:DB00450 n21:DB00450
dcterms:title
Droperidol
adms:identifier
n6:3168 n7:46505291 n10:11098-010-01 n11:PA449422 n22:Droperidol n24:D00308 n25:3056 n26:DB00450 n27:50017705 n29:4717
n3:mechanismOfAction
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.
n3:packager
n14:271B5213-363D-11E5-9242-09173F13E4C5 n14:271B5214-363D-11E5-9242-09173F13E4C5 n14:271B5211-363D-11E5-9242-09173F13E4C5 n14:271B5212-363D-11E5-9242-09173F13E4C5 n14:271B5215-363D-11E5-9242-09173F13E4C5 n14:271B5216-363D-11E5-9242-09173F13E4C5 n14:271B5217-363D-11E5-9242-09173F13E4C5 n14:271B5218-363D-11E5-9242-09173F13E4C5
n3:synonym
Dropéridol 1-(1-(4-(P-Fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone 1-{1-[4-(4-fluoro-phenyl)-4-oxo-butyl]-1,2,3,6-tetrahydro-pyridin-4-yl}-1,3-dihydro-benzoimidazol-2-one Droperidolum Droperidol 1-{1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl}-2,3-dihydro-1H-benzo[D]imidazol-2-one Droperidolo 1-(1-(3-(P-Fluorobenzoyl)propyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
n3:toxicity
The intravenous LD<sub>50</sub> 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<sub>50</sub> 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.
n18:hasAHFSCode
n19:28-24-92
n3:mixture
n20:271B5210-363D-11E5-9242-09173F13E4C5
n3:synthesisReference
Janssen, P.A.J. and Gardocki, J.F.; U.S. Patent 3,141,823; July 21, 1964; assigned to Research Laboratorium Dr. C. Janssen NV, Belgium. Januen, P.A.J.; U.S. Patent 3,161,645; December 15,1964: assigned to Research Laboratorium Dr. C. Janssen NV, Belgium.
foaf:page
n17:droperidol.htm n28:droperidol.html
n3:IUPAC-Name
n4:271B522A-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5230-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B522F-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B522C-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B522D-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B522E-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5228-363D-11E5-9242-09173F13E4C5 n4:271B5240-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5242-363D-11E5-9242-09173F13E4C5 n4:271B5226-363D-11E5-9242-09173F13E4C5 n4:271B5229-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5227-363D-11E5-9242-09173F13E4C5
n3:pKa
n4:271B5243-363D-11E5-9242-09173F13E4C5
n18:hasATCCode
n23:N05AD08
n3:H-Bond-Acceptor-Count
n4:271B5236-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5237-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5231-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5232-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5234-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5233-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5235-363D-11E5-9242-09173F13E4C5
n3:absorption
Completely absorbed following intramuscular administration.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
548-73-2
n3:category
n3:containedIn
n15:271B5223-363D-11E5-9242-09173F13E4C5 n15:271B5221-363D-11E5-9242-09173F13E4C5 n15:271B5222-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B523C-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B523E-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B523F-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B5241-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B523B-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B523A-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B523D-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B522B-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5238-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5239-363D-11E5-9242-09173F13E4C5