Inapsine
Inapsine Uses, Dosage, Side Effects, Food Interaction and all others data.
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)
Inapsine produces marked tranquilization and sedation. It allays apprehension and provides a state of mental detachment and indifference while maintaining a state of reflex alertness. Inapsine 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. Inapsine 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.
| Trade Name | Inapsine |
| Availability | Prescription only |
| Generic | Droperidol |
| Droperidol Other Names | Droperidol, Dropéridol, Droperidolo, Droperidolum |
| Related Drugs | hydroxyzine, lorazepam, ondansetron, Zofran, meclizine, promethazine, metoclopramide, Reglan, amisulpride, Zofran ODT |
| Weight | 2.5mg/ml, |
| Type | Injectable solution |
| Formula | C22H22FN3O2 |
| Weight | Average: 379.4274 Monoisotopic: 379.169605168 |
| Groups | Approved, Vet approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Inapsine is a butyrophenone derivative and dopamine antagonist used to prevent and treat postoperative nausea and vomiting.
Inapsine is ssed to produce tranquilization and to reduce the incidence of nausea and vomiting in surgical and diagnostic procedures.
Inapsine is also used to associated treatment for these conditions: Agitation, Chemotherapy-Induced Nausea and Vomiting (CINV), Delirium, Nausea and vomiting, Sedation
How Inapsine works
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.
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.
Food Interaction
No interactions found.Inapsine Alcohol interaction
[Major] MONITOR CLOSELY:
The use of droperidol has been associated with QT interval prolongation, torsade de pointes and other serious arrhythmias, and sudden death.
The concurrent administration of agents that can produce hypokalemia and/or hypomagnesemia (e.g., potassium-wasting diuretics, amphotericin B, cation exchange resins), drugs known to increase the QT interval (e.g., phenothiazines, tricyclic antidepressants, antiarrhythmic agents, etc.), certain other drugs (benzodiazepines, volatile anesthetics, intravenous opiates), or alcohol abuse may increase the risk of prolonged QT syndrome.
In addition, central nervous system- and/or respiratory-depressant effects may be additively or synergistically increased in patients taking droperidol with certain other drugs that cause these effects, especially in elderly or debilitated patients.
The manufacturer recommends extreme caution if droperidol must be given concomitantly with these agents.
The dosage of droperidol should be individualized and titrated to the desired effect.
Routine vital sign and ECG monitoring is recommended.
When droperidol is used in combination with other drugs that cause CNS and/or respiratory depression, patients should be monitored for potentially excessive or prolonged CNS and respiratory depression.
Ambulatory patients should be counseled to avoid hazardous activities requiring mental alertness and motor coordination until they know how these agents affect them, and to notify their doctor if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Inapsine Drug Interaction
Major: lorazepam, lorazepam, promethazine, promethazine, metoclopramide, metoclopramide, ondansetron, ondansetronModerate: duloxetine, duloxetineUnknown: glucose, glucose, diltiazem, diltiazem, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Inapsine Disease Interaction
Major: cardiovascular, QT prolongationModerate: hepatic/renal dysfunction, pheochromocytoma
Elimination Route
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.
Innovators Monograph
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