Haloperidol

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Haldol; Belgium: Haldol; Bulgaria: Haloperidol; Cyprus: Haemaccel, Haldol, Haloxen, Serenace; Czech Republic: Haloperidol; Denmark: Serenase; Estonia: Haloperidol; Finland: Serenase; France: Haldol, Haloperidol; Germany: Haldol, Haloper, Haloperidol; Greece: Aloperidin; Hungary: Haloperidol; Ireland: Haldol, Haloperidol, Serenace; Italy: Aloperid, Haldol, Serenase; Latvia: Haloperidol; Lithuania: Haloperidol; Luxembourg: Haldol, Haloperidol; Malta: Avant, Haldol, Haloperidol, Serenace; Netherlands: Haldol, Haloperidol; Poland: Decaldol, Haloperidol; Portugal: Haldol, Haloperidol; Romania: Haldol, Haloperidol; Slovakia: Haloperidol; Slovenia: Haldol; Spain: Haloperidol; Sweden: Haldol; UK: Dozic, Haldol.

North America

Canada: Haloperidol; USA: Haldol, Haloperidol.

Latin America

Argentina: Enabran, Haloperidol, Halopidol, Halozen, Limerix, Neupram; Brazil: Haldol, Halo, Haloper, Haloperidol, Loperidol; Mexico: Haldol, Haloperil, Hispadol, Kepsidol, Pulsit.

Asia

Japan: Cosminal, Esextin, Halojust, Halomidol, Halomonth, Haloperidol, Halosten, Lemonamin, Linton, Neoperidol, Peluces, Serenace, Suirolin, Youperidol.

Drug combinations

Chemistry

Haloperidol: C~21~H~23~ClFNO~2~. Mw: 375.86. (1) 1-Butanone, 4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]-1-(4-fluorophenyl)-; (2) 4-[4-(p-Chlorophenyl)-4-hydroxypiperidino]-4′-fluorobutyrophenone. CAS-52-86-8 (1965).

Haloperidol Decanoate: C~31~H~41~ClFNO~3~. Mw: 530.11. Decanoic acid, 4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]-4-piperidinyl ester. CAS-74050-97-8 (1980).

Pharmacologic Category

Antipsychotics; Butyrophenones. Conventional Antipsychotic. First-Generation Antipsychotic. Typical Antipsychotic. (ATC-Code: N05AD01).

Mechanism of action

Haloperidol is a butyrophenone antipsychotic which blocks postsynaptic mesolimbic dopaminergic D~1~ and D~2~ receptors in brain. Depresses release of hypothalamic and hypophyseal hormones. Believed to depress reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.

Therapeutic use

Used for symptomatic management of psychotic disorders. Control of tics and vocal utterances of Tourette’s disorder in children and adults. Severe behavioral problems in children. Schizophrenia.

Pregnancy and lactiation implications

Haloperidol should be used during pregnancy or in women likely to become pregnant only when potential benefits justify possible risks to fetus. Haloperidol is distributed into milk.

Unlabeled use

Treatment of non-schizophrenia psychosis. May be used for emergency sedation of severely-agitated or delirious patients. Adjunctive treatment of ethanol dependence. Antiemetic. Psychosis/agitation related to Alzheimer’s dementia. Delirium.

Contraindications

Hypersensitivity to haloperidol or any component of the formulation. Parkinson’s disease. Severe CNS depression. Bone marrow suppression. Severe cardiac or hepatic disease. Coma.

Warnings and precautions

May alter cardiac conduction and prolong QT interval. Use with caution or avoid use in electrolyte abnormalities (e.g. hypokalemia, hypomagnesemia), hypothyroidism, familial long QT syndrome, concomitant medications which may augment QT prolongation, or any underlying cardiac abnormality which may also potentiate risk. May cause anticholinergic effects (constipation, blurred vision, urinary retention, xerostomia). Use with caution in decreased GI motility, paralytic ileus, urinary retention, BPH, xerostomia, or visual problems. Myelosuppression (e.g. leukopenia, agranulocytosis) observed with antipsychotic use. Use contraindicated in bone marrow suppression. Antipsychotic use associated with esophageal dysmotility and aspiration. Use with caution in risk of pneumonia (e.g. Alzheimer’s disease). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is high relative to other neuroleptics). Neuroleptic malignant syndrome possible. May cause orthostatic hypotension. May be associated with pigmentary retinopathy. May be sedating. Impaired core body temperature regulation may occur. Use with caution in severe cardiovascular disease. Haloperidol not approved for treatment of dementia-related psychosis in elderly patients. Use with caution in narrow-angle glaucoma, myasthenia gravis (condition may be exacerbated by cholinergic blockade). Use with caution in Parkinson’s disease. Use with caution in breast cancer or other prolactin-dependent tumors (elevates prolactin levels). Use with caution in renal impairment, and in respiratory disease. Use with caution in risk of seizures. Avoid use in thyrotoxicosis. May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects. Some tablets contain tartrazine. Hypotension may occur, particularly with parenteral administration. Risk of QT prolongation, torsade de pointes, and sudden death appear to be increased with I.V. administration, particularly at higher doses. Although short-acting form (lactate) is used clinically intravenously, I.V. use of injection is not an FDA-approved route of administration. The decanoate form should never be administered intravenously.

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