Dehidrobenzperidol - General Information
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)
Pharmacology of Dehidrobenzperidol
Dehidrobenzperidol produces marked tranquilization and sedation. It allays apprehension and provides a state of mental detachment and indifference while maintaining a state of reflex alertness. Dehidrobenzperidol 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. Dehidrobenzperidol 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.
Dehidrobenzperidol for patients
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.
INAPSINE (droperidol) is contraindicated in patients with known hypersensitivity to the drug.
Additional information about Dehidrobenzperidol
Dehidrobenzperidol Indication: Used to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures.
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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Droperidol
Synonyms: Not Available
Drug Category: Adjuvants, Anesthesia; Antiemetics; Antipsychotic Agents; Dopamine Antagonists
Drug Type: Small Molecule; Approved
Absorption: Completely absorbed following intramuscular administration.
Toxicity (Overdose): 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.
Protein Binding: Not Available
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.
Dosage Forms of Dehidrobenzperidol: Solution Intramuscular
Chemical IUPAC Name: 3-[1-[4-(4-fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-benzimidazol-2-one
Chemical Formula: C22H22FN3O2
Droperidol on Wikipedia: https://en.wikipedia.org/wiki/Droperidol
Organisms Affected: Humans and other mammals