Pimozide
Orap
First-Generation AntipsychoticGeneric availableTDM data
Clinical Pharmacology Pimozide is an orally active antipsychotic agent which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system. Although its exact mode of action has not been established, the ability of pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be a function of its dopaminergic blocking activity.
Compare Pimozide →FDA-Approved Indications
- Suppression of motor and phonic tics in Tourette's disorder — second-line, when development/daily function is severely compromised and standard treatment has failed
What Sets This Drug Apart
- Only FGA with FDA-approved indication for Tourette syndrome (tic suppression) — a unique niche among antipsychotics
- Also approved for delusional disorder (atypical and somatic subtypes) — another unique indication
- Significant QTc prolongation risk: mandatory baseline ECG and periodic monitoring; contraindicated with other QT-prolonging drugs including most SSRIs
- Lowest starting dose among FGAs (1-2 mg/day, titrate 1 mg every 2-7 days) due to narrow therapeutic window; max 10 mg/day
- Very long half-life (~55 hours); steady-state effects are slow to develop and persist after discontinuation
- CYP3A4 and CYP1A2 substrate — strong CYP3A4 inhibitors are contraindicated due to QTc risk from elevated pimozide levels