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Look Up > Drugs > Haloperidol
Haloperidol
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Reference Range
Test Interactions
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(ha loe PER i dole)

U.S. Brand Names
Haldol®; Haldol® Decanoate

Generic Available

Yes


Synonyms
Haloperidol Decanoate; Haloperidol Lactate

Pharmacological Index

Antipsychotic Agent, Butyrophenone


Use

Treatment of psychoses; control of tics and vocal utterances of Tourette's disorder in children and adults; severe behavioral problems in children


Pregnancy Risk Factor

C


Contraindications

Hypersensitivity to haloperidol or any component; Parkinson's disease; severe CNS depression, bone marrow suppression, severe cardiac or hepatic disease; coma


Warnings/Precautions

Hypotension may occur, particularly with parenteral administration. Decanoate form should never be administered I.V. Avoid in thyrotoxicosis. May be sedating, use with caution in disorders where CNS depression is a feature. Caution in patients with hemodynamic instability, predisposition to seizures, subcortical brain damage, renal or respiratory disease. Esophageal dysmotility and aspiration have been associated with antipsychotic use - use with caution in patients at risk of pneumonia (ie, Alzheimer's disease). Caution in breast cancer or other prolactin-dependent tumors (may elevate prolactin levels). May alter temperature regulation or mask toxicity of other drugs due to antiemetic effects. May alter cardiac conduction - life-threatening arrhythmias have occurred with therapeutic doses of antipsychotics. Adverse effects of decanoate may be prolonged. May cause orthostatic hypotension - use with caution in patients at risk of this effect or those who would tolerate transient hypotensive episodes (cerebrovascular disease, cardiovascular disease, or other medications which may predispose). Some tablets contain tartrazine.

May cause extrapyramidal reactions, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is high relative to other neuroleptics). May be associated with neuroleptic malignant syndrome (NMS) or pigmentary retinopathy.


Adverse Reactions

Cardiovascular: Hypotension, hypertension, tachycardia, arrhythmias, abnormal T waves with prolonged ventricular repolarization

Central nervous system: Restlessness, anxiety, extrapyramidal reactions, dystonic reactions, pseudoparkinsonian signs and symptoms, tardive dyskinesia, neuroleptic malignant syndrome (NMS), altered central temperature regulation, akathisia, tardive dystonia, insomnia, euphoria, agitation, drowsiness, depression, lethargy, headache, confusion, vertigo, seizures

Dermatologic: Hyperpigmentation, pruritus, rash, contact dermatitis, alopecia, photosensitivity (rare)

Endocrine & metabolic: Amenorrhea, galactorrhea, gynecomastia, sexual dysfunction, lactation, breast engorgement, mastalgia, menstrual irregularities, hyperglycemia, hypoglycemia, hyponatremia

Gastrointestinal: Nausea, vomiting, anorexia, constipation, diarrhea, hypersalivation, dyspepsia, xerostomia

Genitourinary: Urinary retention, priapism

Hematologic: Cholestatic jaundice, obstructive jaundice

Ocular: Blurred vision

Respiratory: Laryngospasm, bronchospasm

Miscellaneous: Heat stroke, diaphoresis


Overdosage/Toxicology

Symptoms of overdose include deep sleep, dystonia, agitation, dysrhythmias, extrapyramidal symptoms

Following initiation of essential overdose management, toxic symptom treatment and supportive treatment should be initiated. Critical cardiac arrhythmias often respond to I.V. lidocaine, while other antiarrhythmics can be used. Neuroleptics often cause extrapyramidal symptoms (eg, dystonic reactions) requiring management with benztropine mesylate I.V. 1-2 mg (adult) may be effective. These agents are generally effective within 2-5 minutes.


Drug Interactions

CYP1A2 enzyme substrate, CYP2D6 enzyme substrate (minor); CYP2D6 enzyme inhibitor CYP2C8 and 3A3/4 enzyme substrate; CYP1A2, 2C, and 3A3/4 inducer

Benztropine (and other anticholinergics) may inhibit the therapeutic response to haloperidol and excess anticholinergic effects may occur

Chloroquine may increase haloperidol concentrations

Cigarette smoking may enhance the hepatic metabolism of haloperidol. Larger doses may be required compared to a nonsmoker.

Concurrent use of haloperidol with an antihypertensive may produce additive hypotensive effects

Concurrent use with TCA may produce increased toxicity or altered therapeutic response

Haloperidol may inhibit the antiparkinsonian effect of levodopa; avoid this combination

Haloperidol plus lithium may rarely produce neurotoxicity

Barbiturates may reduce haloperidol concentrations

Propranolol may increase haloperidol concentrations

Sulfadoxine-pyrimethamine may increase haloperidol concentrations

Haloperidol and CNS depressants (ethanol, narcotics) may produce additive CNS depressant effects

Haloperidol and trazodone may produce additive hypotensive effects

Carbamazepine appears to stimulate the metabolism of haloperidol. Monitor for reduced efficacy

Fluoxetine and paroxetine may inhibit the metabolism of haloperidol resulting in EPS; monitor for EPS

Haloperidol in combination with indomethacin may result in drowsiness, tiredness, and confusion; monitor for adverse effects

Quinidine appears to increase haloperidol concentrations; monitor for EPS


Stability

Protect oral dosage forms from light

Haloperidol lactate injection should be stored at controlled room temperature and protected from light, freezing and temperatures >40°C; exposure to light may cause discoloration and the development of a grayish-red precipitate over several weeks

Haloperidol lactate may be administered IVPB or I.V. infusion in D5W solutions; NS solutions should not be used due to reports of decreased stability and incompatibility

Standardized dose: 0.5-100 mg/50-100 mL D5W

Stability of standardized solutions is 38 days at room temperature (24°C)


Mechanism of Action

Blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones; believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis


Pharmacodynamics/Kinetics

Onset of sedation: I.V.: Within 1 hour

Duration of action: ~3 weeks for decanoate form

Distribution: Crosses the placenta; appears in breast milk

Protein binding: 90%

Metabolism: In the liver to inactive compounds

Bioavailability: Oral: 60%

Half-life: 20 hours

Time to peak serum concentration: 20 minutes

Elimination: 33% to 40% excreted in urine within 5 days; an additional 15% excreted in feces


Usual Dosage

Children: 3-12 years (15-40 kg): Oral:

Initial: 0.05 mg/kg/day or 0.25-0.5 mg/day given in 2-3 divided doses; increase by 0.25-0.5 mg every 5-7 days; maximum: 0.15 mg/kg/day

Usual maintenance:

Agitation or hyperkinesia: 0.01-0.03 mg/kg/day once daily

Nonpsychotic disorders: 0.05-0.075 mg/kg/day in 2-3 divided doses

Psychotic disorders: 0.05-0.15 mg/kg/day in 2-3 divided doses

Children 6-12 years: I.M. (as lactate): 1-3 mg/dose every 4-8 hours to a maximum of 0.15 mg/kg/day; change over to oral therapy as soon as able

Adults:

Oral: 0.5-5 mg 2-3 times/day; usual maximum: 30 mg/day

I.M. (as lactate): 2-5 mg every 4-8 hours as needed

I.M. (as decanoate): Initial: 10-20 times the daily oral dose administered at 4-week intervals

Maintenance dose: 10-15 times initial oral dose; used to stabilize psychiatric symptoms

Sedation in the Intensive Care Unit:

I.M./IVP/IVPB: May repeat bolus doses after 30 minutes until calm achieved then administer 50% of the maximum dose every 6 hours

Mild agitation: 0.5-2 mg

Moderate agitation: 2.5-5 mg

Severe agitation: 10-20 mg

Oral: Agitation: 5-10 mg

Continuous intravenous infusion (100 mg/100 mL D5W): Rates of 1-40 mg/hour have been used

Rapid tranquilization of agitated patient (administer every 30-60 minutes):

Oral: 10 mg

I.M.: 5 mg

Average total dose for tranquilization: 30-60 mg

Elderly (nonpsychotic patients, dementia behavior):

Initial: Oral: 0.25-0.5 mg 1-2 times/day; increase dose at 4- to 7-day intervals by 0.25-0.5 mg/day; increase dosing intervals (twice daily, 3 times/day, etc) as necessary to control response or side effects

Hemodialysis/peritoneal dialysis: Supplemental dose is not necessary


Dietary Considerations

Alcohol: Additive CNS effect, avoid use


Monitoring Parameters

Monitor orthostatic blood pressures 3-5 days after initiation of therapy or a dose increase; observe for tremor and abnormal movement or posturing (extrapyramidal symptoms)


Reference Range

Therapeutic: 5-15 ng/mL (SI: 10-30 nmol/L) (psychotic disorders - less for Tourette's and mania)

Toxic: >42 ng/mL (SI: >84 nmol/L)


Test Interactions

cholesterol (S)


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

Manufacturer's information states that haloperidol may block vasopressor activity of epinephrine. This has not been observed during use of epinephrine as a vasoconstrictor in local anesthesia.


Dental Health: Effects on Dental Treatment

Orthostatic hypotension and nasal congestion possible in dental patients. Since the drug is a dopamine antagonist, extrapyramidal symptoms of the TMJ a possibility.


Patient Information

Use exactly as directed (do not increase dose or frequency); may cause physical and/or psychological dependence. It may take 2-3 weeks to achieve desired results; do not discontinue without consulting prescriber. Dilute oral concentration with water or juice. Do not take within 2 hours of any antacid. Store away from light. Avoid excess alcohol or caffeine and other prescription or OTC medications not approved by prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Avoid skin contact with medication; may cause contact dermatitis (wash immediately with warm, soapy water). You may experience excess drowsiness, restlessness, dizziness, or blurred vision (use caution driving or when engaging in tasks requiring alertness until response to drug is known); nausea, vomiting (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help); postural hypotension (use caution climbing stairs or when changing position from lying or sitting to standing); urinary retention (void before taking medication); decreased perspiration (avoid strenuous exercise in hot environments). Report persistent CNS effects (eg, trembling fingers, altered gait or balance, excessive sedation, seizures, unusual movements, anxiety, abnormal thoughts, confusion, personality changes); chest pain, palpitations, rapid heartbeat, severe dizziness; unresolved urinary retention or changes in urinary pattern; vision changes; skin rash or yellowing of skin; difficulty breathing; or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.


Nursing Implications

Avoid skin contact with oral suspension or solution; may cause contact dermatitis


Dosage Forms

Concentrate, oral, as lactate: 2 mg/mL (5 mL, 10 mL, 15 mL, 120 mL, 240 mL)

Injection, as decanoate: 50 mg/mL (1 mL, 5 mL); 100 mg/mL (1 mL, 5 mL)

Injection, as lactate: 5 mg/mL (1 mL, 2 mL, 2.5 mL, 10 mL)

Tablet: 0.5 mg, 1 mg, 2 mg, 5 mg, 10 mg, 20 mg


References

Aunsholt NA, "Prolonged Q-T Interval and Hypokalemia Caused by Haloperidol," Acta Psychiatr Scand, 1989, 79(4):411-2.

Bauer M, "Concurrent Agranulocytosis and Acute Hepatitis Resulting From Combination of Classic Neuroleptics and Subsequent Successful Clozapine Treatment," Pharmacopsychiatry, 1995, 28(1):29-31.

Cole RM, Robinson F, Harvey L, et al, "Successful Control of Intractable Nausea and Vomiting Requiring Combined Ondansetron and Haloperidol in a Patient With Advanced Cancer," J Pain Symptom Manage, 1994, 9(1):48-50.

Di Salvo TG and O'Gara PT, "Torsade de Pointes Caused by High-Dose Intravenous Haloperidol in Cardiac Patients," Clin Cardiol, 1995, 18(5):285-90.

Doenecke AL and Heuermann RC, "Treatment of Haloperidol Abuse With Diphenhydramine," Am J Psychiatry, 1980, 137(4):487-8.

Fisher H, "A New Approach to Emergency Department Therapy of Migraine Headache With Intravenous Haloperidol: A Case Series," J Emerg Med, 1995, 13(1):119-22.

Harada H, Igarashi M, Sugae S, et al, "A Schizophrenic Patient Who Developed Extreme Hypothermia After an Increase in the Dose of Haloperidol: A Case Report," Jpn J Psychiatry Neurol, 1994, 48(3):595-8.

Kubota T, Ishikura T, and Jibiki I, "Alopecia Areata Associated With Haloperidol," Jpn J Psychiatry Neurol, 1994, 48(3):579-81.

Mahutte CK, Nakasato SK, and Light RW, "Haloperidol and Sudden Death Due to Pulmonary Edema," Arch Intern Med, 1982, 142(10):1951-2.

Peabody CA, Warner MD, Whiteford HA, et al, "Neuroleptics and the Elderly," J Am Geriatr Soc, 1987, 35(3):233-8.

Plotkin DA, Plotkin D, and Okun R, "Haloperidol in the Treatment of Nausea and Vomiting Due to Cytotoxic Drug Administration," Curr Ther Res Clin Exp,1973, 15(9):599-602.

Riker RR, Fraser GL, and Cox PM, "Continuous Infusion of Haloperidol Controls Agitation in Critically Ill Patients," Crit Care Med, 1994, 22(3):433-40.

Risse SC and Barnes R, "Pharmacologic Treatment of Agitation Associated With Dementia," J Am Geriatr Soc, 1986, 34(5):368-76.

Saltz BL, Woerner MG, Kane JM, et al, "Prospective Study of Tardive Dyskinesia Incidence in the Elderly," JAMA, 1991, 266(17):2402-6.

Schwartz M, Weller B, Erdreich M, et al, "Rabbit Syndrome and Tardive Dyskinesia: Two Complications of Chronic Neuroleptic Treatment," J Clin Psychiatry, 1995, 56(5):212.

Seifert RD, "Therapeutic Drug Monitoring: Psychotropic Drugs," J Pharm Pract, 1984, 6:403-16.

Serrano AC, "Haloperidol - Its Use in Children," J Clin Psychiatry, 1981, 42(4):154-6.

Silvey L, Carpenter JT Jr, Wheeler RH, et al, "A Randomized Comparison of Haloperidol Plus Dexamethasone Versus Prochlorperazine Plus Dexamethasone in Preventing Nausea and Vomiting in Patients Receiving Chemotherapy for Breast Cancer," J Clin Oncol, 1988, 6(9):1397-400.

Spencer EK, Kafantaris V, Padron-Gayol MV, et al, "Haloperidol in Schizophrenic Children: Early Findings From a Study in Progress," Psychopharmacol Bull, 1992, 28(2):183-6.

Wilt JL, Minnema AM, Johnson RF, et al, "Torsade de Pointes Associated With the Use of Intravenous Haloperidol," Ann Intern Med, 1993, 119(5):391-4.


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