pimozide (Orap)
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Introduction
Tradename: Orap.
Indications
- suppression of severe motor tics & phonic tics in patients with Tourette's syndrome
Contraindications
- simple tics, not due to Tourette's syndrome
- history of cardiac dysrhythmias
- CNS depression
- blood dyscrasias
- depressive disorders
- parkinsonism
Caution:
- treatment imposes serious risks to patient
- benefits must outweigh risks
Dosage
Tabs: 2 mg.
Reduction of dose for hepatic insufficiency
Pharmacokinetics
- oral absorption is 40-50%
- protein-binding is 99%
- metabolized in the liver by cyt P450 3A4
- significant 1st pass metabolism in liver
- elimination 1/2life of 55 hours
- time to peak serum concentration: within 6-8 hours
- metabolites excreted in the urine
elimination via liver
protein binding = 99 %
Adverse effects
- common (> 10%)
- less common (1-10%)
- tardive dyskinesia, diarrhea, anorexia, depression, swelling of the face
- uncommon (< 1%)
- jaundice, blood dyscrasias, neuroleptic malignant syndrome
- other
- tumorogenic in animal studies
- altered mental status
- autonomic instability
- lowers seizure threshold
Drug interactions
- increased effect & toxicity of:
- alfentanil, CNS depressants, guanabenz, MAO inhibitors, agents which prolong the QT interval
- may exacerbate adverse effects of anticholinergic agents
- any drug that inhibits cyt P450 3A4 may increase levels of pimozide
- any drug that induces cyt P450 3A4 may diminish levels of pimozide
- drug interaction(s) of antipsychotics & dopamine receptor agonists
- drug interaction(s) of antipsycotics with benzodiazepines
- drug interaction(s) of citalopram with pimozide
More general terms
Additional terms
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
- Gilles de la Tourette's syndrome