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Pimozide (Orap)


Pimozide is used in the hospital and outpatient treatment of schizophrenia, paranoid states, psychotic and neurotic states with paranoid symptoms and Tourette's syndrome. In the outpatient setting it is used for maintenance therapy in patients previously treated with antipsychotic drugs. The preparation is not applied to press for relief of aggression and agitation in acute psychoses, as it offers no sedative influence. In acute mental illness treatment it is recommended to start with neuroleptic providing sedation, and then gradually reducing the dose, switch to pimozide.

The medication is appointed to be taken pereorally (with food), starting at a dose of 0.001 g (1 mg) 1 times a day, following a gradual increase. Therefore, an average daily dose equals 0.005 g (0.008 g). The drug can be used in combination with other antipsychotic drugs.

When applying pimozide extrapyramidal disorders may occur; in this case antiparkinsonian medications are prescribed. In the first days of treatment (mainly upon discontinuance of the previously used neuroleptics with sedative effect) aggressiveness may increase. Furthermore, the occurrence of arrhythmias and allergic reactions is possible.

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Pimozide: pharmacology

Pimozide is typically produced in the form of white crystalline powder, which is almost insoluble in water. Along the spectrum of action similar to haloperidol, has a pronounced antipsychotic influence. Compared with other antipsychotics, Pimozide is more specific blocker of D2-receptors. The peculiarity of the product is a relatively long-lasting effect after the first administered (maximum effect usually develops within 2 hours, lasts about 6 hours, and dissolves after 24 hours).

When a dose is ingested it is absorbed by 50%, while the maximum concentration builds in 6-8 hours. The preparation is subjected to intense biotransformation in the liver, excreted mainly in the urine and partly with faeces.

Pimozide: contraindications

The medication must not be used in case of hypersensitivity to the preparation (including hypersensitivity to other neuroleptics), Parkinson's disease, arrhythmias, severe CNS depression, coma, breast cancer (may increase the concentration of prolactin in the blood serum and deterioration) functional disorders of the liver and kidneys and hypokalemia.

The treatment requires careful monitoring of ECG, careful observation aimed at detecting the early symptoms of tardive dyskinesia (especially in the elderly and in patients receiving high-dose or long-term maintenance treatment) or late dystonia. At the first signs of these symptoms pimozide course should be ceased immediately.

Extrapyramidal effects may occur within the very first days of treatment and extremely low doses, though effects are characterized by mild or moderate in nature. Elderly patients may need correction of dosing regimen. The remedy is not recommended to be used in children, except for Tourette's syndrome. Moreover an efficient pimozide dose for kids under 12 years is not established. The fact should be underlined that children are generally more sensitive to the drug.

Pimozide: dosage and administration methods

The remedy is taken orally. In Tourette syndrome the initial dose equals 1-2 mg on a daily basis, if necessary, given the tolerance dose, it can be gradually increased. The max dosage must not exceed 10 mg each 24 hours. In psychotic disorders the initial dose is 2-4 mg 1 time/day, though, if necessary, it can be increased up to 2-4 mg/day at an intervals of 1 week; the average maintenance dose is 6 mg/day. In all the rest cases exceeding the 20mg is strongly prohibited.

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