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
  • 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


Austria: Orap; Belgium: Orap; Cyprus: Orap; Czech Republic: Orap; Denmark: Orap; France: Orap; Germany: Orap; Greece: Pirium; Ireland: Orap; Italy: Orap; Luxembourg: Orap; Netherlands: Orap; Portugal: Orap; Spain: Orap; UK: Orap.

North America

Canada: Orap, Pimozide; USA: Orap.

Latin America

Argentina: Orap, Pimozida; Brazil: Orap.


Japan: Orap.

Drug combinations


Pimozide: C~28~H~29~F~2~N~3~O. Mw: 461.55. (1) 2H-Benzimidazol-2-one, 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-; (2) 1-[1-[4,4-Bis(p-fluorophenyl)butyl]-4-piperidyl]-2-benzimidazolinone. CAS-2062-78-4 (1967).

Pharmacologic Category

Antipsychotics, Miscellaneous. (ATC-Code: N05AG02).

Mechanism of action

Pimozide, a diphenylbutylperidine antipsychotic, is a potent centrally-acting dopamine-receptor antagonist resulting in its characteristic neuroleptic effects.

Therapeutic use

Suppression of severe motor and phonic tics in Tourette’s disorder.

Pregnancy and lactiation implications

Use caution during pregnancy or lactation.

Unlabeled use

Psychosis. Reported use in delusions focused on physical symptoms (e.g. preoccupation with parasitic infestation). Huntington’s chorea. Psychosis/agitation related to Alzheimer’s dementia.


Hypersensitivity to pimozide or any component of the formulation. Severe CNS depression. Coma. History of dysrhythmia. Prolonged QT syndrome. Concurrent use with QTc-prolonging agents. Hypokalemia or hypomagnesemia. Concurrent use of drugs which inhibit CYP3A4, including concurrent use of azole antifungals, fluvoxamine, macrolide antibiotics (such as clarithromycin or erythromycin, mesoridazine, nefazodone, protease inhibitors (e.g. atazanavir, indinavir, nelfinavir, ritonavir, saquinavir), sertraline, thioridazine, zileuton, and ziprasidone). Simple tics other than Tourette’s.

Warnings and precautions

May alter cardiac conduction (avoid use in underlying QT prolongation, in patients taking medicines which prolong QT interval, or cause polymorphic ventricular tachycardia). May cause anticholinergic effects (use with caution in decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, or visual problems). Myelosuppression (e.g. leukopenia, agranulocytosis) observed with antipsychotic use. Antipsychotic use associated with esophageal dysmotility and aspiration (use with caution in risk of pneumonia). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Use may be associated with neuroleptic malignant syndrome (risk may be increased in Parkinson’s disease or Lewy body dementia). May cause orthostatic hypotension (use with caution in cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia). May be associated with pigmentary retinopathy. May be sedating. Impaired core body temperature regulation may occur. Use with caution in severe cardiovascular disease. Pimozide not approved for treatment of dementia-related psychosis (increased incidence of cerebrovascular adverse events, including fatalities). Use with caution in narrow-angle glaucoma (may be exacerbated by cholinergic blockade), in hepatic impairment, in myasthenia gravis (may be exacerbated by cholinergic blockade), and in Parkinson’s disease (may be more sensitive to adverse effects). Use with caution in breast cancer or other prolactin-dependent tumors (elevates prolactin levels), in renal impairment, in respiratory disease, and in risk of seizures, including patients with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects.



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