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Droperidol

Catalog No. DB00450 Name DrugBank
CAS Number 548-73-2 Website http://www.ualberta.ca/
M. F. C22H22FN3O2 Telephone (780) 492-3111
M. W. 379.4273832 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 333

SYNONYMS

IUPAC name
1-{1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydropyridin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
IUPAC Traditional name
halkan
Brand Name
Dridol
Halkan
Inoval
Inopsin
Innovan
Inapsin
DHBP
Deidrobenzperidolo
Innovar
Innovar-Vet
Leptanal
Leptofen
McN-JR 4749
Sintodril
Sintosian
Thalamonal
Vetkalm
Dehidrobenzperidol
Dehydrobenzperidol
Dihidrobenzperidol
Droleptan
Inappin
Inapsine
Properidol
Thalamanol

DATABASE IDS

PubChem SID 46505291
PubChem CID 3168
CAS Number 548-73-2

PROPERTIES

Hydrophobicity(logP) 2.8
Solubility 4.21 mg/L

DETAILS

Description (English)
Item Information
Drug Groups approved
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)
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 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.
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
Biotransformation Extensively metabolized.
Absorption Completely absorbed following intramuscular administration.
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.
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REFERENCES