Brands, Medical Use, Clinical Data
Drug Category
- Adjuvants, Anesthesia
- Antiemetics
- Antipsychotic Agents
- Dopamine Antagonists
Dosage Forms
Brands / Synonyms
Dehidrobenzperidol; Dehydrobenzperidol; Deidrobenzperidolo; DHBP; Dihidrobenzperidol; Dridol; Droleptan; Droperidol; Halkan; Inappin; Inapsin; Inapsine; Innovan; Innovar; Innovar-Vet; Inopsin; Inoval; Leptanal; Leptofen; McN-JR 4749; Properidol; Sintodril; Sintosian; Thalamanol; Thalamonal; Vetkalm
Indications
Used 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.
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, may antagonize the actions of glutamic acid within the extrapyramidal system, may inhibit cathecolamine receptors and the reuptake of neurotransmiters, has strong central antidopaminergic action and weak central anticholinergic action, produces ganglionic blockade and reduces affective response.
Absorption
Completely absorbed following intramuscular administration.
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.
Biotrnasformation / Drug Metabolism
Extensively metabolized.
Contraindications
INAPSINE (droperidol) is contraindicated in patients with known hypersensitivity to the drug.
Drug Interactions
Other CNS depressant drugs (e.g. barbiturates, tranquilizers, opioids and general anesthetics) have additive or
potentiating effects with INAPSINE. When patients have received such drugs, the dose of INAPSINE required will be
less than usual. Following the administration of INAPSINE, the dose of other CNS depressant drugs should be
reduced.
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