Details About Overdose or Poisoning Generic Salt ::  Haloperidol And Droperidol

Haloperidol and Droperidol

    

Drug Pharmacology ::

I. Pharmacology. Haloperidoland droperidol are butyrophenone neuroleptic drugs that are useful forthe management of acutely agitated psychotic patients and asantiemetics. They have strong central antidopaminergic activity andweak anticholinergic and anti–alpha-adrenergic effects. Haloperidol iswell absorbed from the GI tract and by the intramuscular route.Droperidol is available only for parenteral use and is also wellabsorbed by the intramuscular route. Droperidol has a more predictableand rapid onset of 3–10 minutes, and both have peak pharmacologiceffects that occur within 30–40 minutes of an intramuscular injection.Both drugs are metabolized principally by the liver. The serumhalf-life for haloperidol is 12–24 hours.

Drug Indications ::

Indications

   

Haloperidolis used for the management of acute agitated functional psychosis orextreme agitation induced by stimulants or hallucinogenic drugs,especially when drug-induced agitation has not responded to abenzodiazepine.

Droperidolhad been recognized to a have more rapid onset and greater efficacythan haloperidol (for agitation and psychosis as well as an antiemeticfor drug- or toxin-induced nausea and vomiting). However, its role inroutine therapy is uncertain because of reports of deaths and a new”black box” warning about QT prolongation (see IV.D, below). Therefore,other antiemetic drugs (eg, metoclopramide, see Metoclopramide, andondansetron, see Ondansetron) should be considered as first-line drugsto control persistent nausea and vomiting.

Drug Contra-Indications ::

III. Contraindications./b>

   

Severe CNS depression in the absence of airway and ventilatory control.

Severe parkinsonism.

Known hypersensitivity to haloperidol or droperidol.

Prolonged QTc interval (prior to droperidol administration, a 12-lead ECG is recommended).

Drug Adverse Effects ::

IV. Adverse effects

   

Haloperidoland droperidol produce less sedation and less hypotension thanchlorpromazine but are associated with a higher incidence ofextrapyramidal side effects.

Rigidity,diaphoresis, and hyperpyrexia may be a manifestation of neurolepticmalignant syndrome (see Neuroleptic malignant syndrome) induced byhaloperidol, droperidol, and other neuroleptic agents.

Haloperidollowers the seizure threshold and should be used with caution inpatients with known seizure disorder or those who have ingested aconvulsant drug.

Largedoses of haloperidol can prolong the QT interval and cause torsade depointes (see Ventricular arrhythmias). The FDA recently added a black box warning for droperidol that QT prolongation and torsade de pointes have occurred at or below recommended doses.

E. Both drugs may cause orthostatic hypotension and tachycardia.

F. Some oral haloperidol tablets contain tartrazine dye, which may precipitate allergic reactions in susceptible patients.

G. Use in pregnancy. FDAcategory C (indeterminate). These drugs are teratogenic and fetotoxicin animals and cross the placenta. Their safety in human pregnancy hasnot been established (see Table III–1).

Drug Lab Interactions ::

Drug or laboratory interactions

   

Haloperidoland droperidol potentiate CNS–depressant effects of opioids,antidepressants, phenothiazines, ethanol, barbiturates, and othersedatives.

Combined therapy with lithium may increase the risk of neuroleptic malignant syndrome (see Hyperthermia).

Drug Dose Management ::

Dosage and method of administration

   

Oral. Give2–5 mg of haloperidol PO; repeat once if necessary; usual daily dose is3–5 mg two to three times daily (children 3 years old, 0.05–0.15mg/kg/day or 0.5 mg in two to three divided doses).

Parenteral. Caution: Monitor the QT interval continuously and treat torsade de pointes if it occurs (see Ventricular arrhythmias).

   

1. Haloperidol. Give2–5 mg of haloperidol IM; may repeat once after 20–30 minutes andhourly if necessary (children 3 years old, same as orally). Haloperidolis not approved for intravenous use in the United States, but thatroute has been used widely and is apparently safe (except the decanoatesalt formulation, which is a depo product for monthly deep IMinjections only).

2. Droperidol.Usual adult dose for delirium is 5 mg IM, and sedative dose is 2.5–5.0mg IM (initial maximum dose of 2.5 mg with additional 1.25-mg dosestitrated to desired effect). For antiemetic effects, usually given30–60 minutes as a premedication, 2.5–10 mg (children 0.088–0.165mg/kg) slowly IV or IM. Note: See warnings above; use alternativeantiemetics as first-line therapy.

Drug Chemical Formulations ::

Formulations

   

Haloperidol

   

1. Oral. Haloperidol(Haldol), 0.5-, 1-, 2-, 5-, 10-, and 20-mg tablets, 2-mg (aslactate)/mL concentrate in 15 and 120 mL, and 5- and 10-mL unit dose.

2. Parenteral. Haloperidol (Haldol), 5 (as lactate) mg/mL, 1-mL ampules, syringes, and vials, and 2-, 2.5-, and 10-mL vials.

Droperidol (Inapsine, others), 2.5 mg/mL, 1- and 2-mL ampules or vials.

The suggested minimum stocking levelto treat a 70-kg adult for the first 24 hours is two vials ofhaloperidol (5 mg/mL, 10 mL each) and three vials of droperidol (2.5mg/mL, 2 mL each).

Disclaimer ::

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