Pimozide
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| Clinical data | |
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| Trade names | Orap |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a686018 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 40-50% |
| Metabolism | CYP3A4, CYP1A2 and CYP2D6 |
| Biological half-life | 55 hours (adults), 66 hours (children) |
| Excretion | Urine |
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| ECHA InfoCard | 100.016.520 |
| Chemical and physical data | |
| Formula | C28H29F2N3O |
| Molar mass | 461.56 g/mol |
| 3D model (Jmol) | |
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Pimozide (Orap) is an antipsychotic drug of the diphenylbutylpiperidine class. It was discovered at Janssen Pharmaceutica in 1963. It has a high potency compared to chlorpromazine (ratio 50-70:1). On a weight basis it is even more potent than haloperidol. It also has special neurologic indications for Tourette syndrome and resistant tics. The side effects include akathisia, tardive dyskinesia, and, more rarely, neuroleptic malignant syndrome and prolongation of the QT interval.
Pimozide is used in its oral preparation in schizophrenia and chronic psychosis (on-label indications in Europe only), Tourette syndrome and resistant tics (Europe, USA and Canada).
Pimozide has been used in the treatment of delusional disorder and paranoid personality disorder. It has also been used for delusions of parasitosis.
Use as an antibiotic for Listeria monocytogenes has been described.
Very common (>10% frequency) side effects include:
It is contraindicated in individuals with either acquired, congenital or a family history of QT interval prolongation. Its use is advised against in individuals with people with either a personal or a family history of arrhythmias or torsades de pointes. Likewise its use is also advised against in individuals with uncorrected hypokalaemia and hypomagnesaemia or clinical significant cardiac disorders (e.g. a recent myocardial infarction or bradycardia. It is also contraindicated in individuals being cotreated with SSRIs or in those with a known hypersensitivity to pimozide or other diphenylbutyl-piperidine derivatives. Likewise its use is contraindicated in individuals receiving treatment with CYP3A4, CYP1A2, or CYP2D6 inhibitors.
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