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pimozide (Rx)Brand and Other Names:Orap

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablets

  • 1mg
  • 2mg
more...

Tourette Disorder

Initial 1-2 mg PO qDay ; increase every other day; not to exceed 10 mg/day

Maintenance: <0.2 mg/kg/day or 10 mg/day, choose lowest dose 

Dosage Forms & Strengths

tablets

  • 1mg
  • 2mg
more...

Tourette Disorder

< 2 years

  • Safety & efficacy not established

2-12 years

  • Initial: 0.05 mg/kg/day PO qHS  
  • Can be increased q3Days to 0.2 mg/kg/day PO qHS
  • Maintenance dose: 2-4 mg/day; not to exceed 10 mg/day

>12 years

  • Initial 1-2 mg PO qDay ; increase every other day; not to exceed 10 mg/day
  • Maintenance: <0.2 mg/kg/day or 10 mg/day, choose lowest dose
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Interactions

Interaction Checker

pimozide and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Akinesia (40%)

            Drowsiness (35%)

            EPS (10-15%)

            Sedation (70%)

            Speech disorder (10-15%)

            Visual disturbance (20%)

            Dry mouth (25%)

            Constipation (20%)

            Impotence (10-15%)

            1-10%

            Appetite increase

            Thirst increase

            Dizziness

            Drug-induced tardive dystonia

            Nervousness

            Photosensitivity

            Taste change

            Orthostatic hypotension

            Diminished sweating

            Nasal congestion

            Diarrhea

            Urinary retention

            Retinitis pigmentosa

            Frequency Not Defined

            Ineffective thermoregulation

            Heatstroke or hypothermia (rare)

            Neuroleptic malignant syndrome (rare)

            Seizure (rare)

            Prolonged QT interval

            Torsades de pointes

            Obstipation (rare)

            Paralytic ileus (rare)

            Agranulocytosis (rare)

            Disorder of hematopoietic structure (rare)

            Leukopenia (rare)

            Thrombocytopenia (rare)

            Cholestatic jaundice syndrome (rare)

            Drug-induced lupus erythematosus, systemic (rare)

            Priapism (rare)

            Death

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            Warnings

            Black Box Warnings

            Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature.

            This drug is not approved for the treatment of patients with dementia-related psychosis.

            Contraindications

            Documented hypersensitivity

            CNS depression (including coma), neuroleptic malignant syndrome (NMS), poorly controlled seizure disorder

            Use as first-line treatment

            Tics not associated with Tourette's

            Prolongs QT interval: concurrent QT-prolonging drugs or congenital long QT patients

            Concomitant CYP3A4 or CYP2D6 inhibitors

            Cautions

            FDA Warning regarding off-label use for dementia in elderly

            Avoid grapefruit juice

            Risk of EPS & NMS

            Leukopenia/neutropenia and agranulocytosis reported; possible risk factors for leukopenia/neutropenia include pre-existing low white blood cell count (WBC) and history of drug-induced leukopenia/neutropenia

            If history of clinically significant low WBC or drug-induced leukopenia/neutropenia, monitor complete blood count (CBC) frequently during first few months of therapy; discontinue drug at first sign of a clinically significant decline <1000/mm³ in WBC in absence of other causative factors and continue monitoring WBC until recovery

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            Pregnancy & Lactation

            Pregnancy Category: C

            Neonates exposed to antipsychotic drugs during the 3rd trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery

            These complications vary in severity; in some cases, symptoms have been self-limited, while in other cases neonates have required intensive care unit support and prolonged hospitalization

            Lactation: unknown, avoid

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Phenylbutylpiperadine; potent centrally acting dopamine D2 receptor antagonist

            Absorption

            Bioavailability: 40-50%

            Peak plasma time: 6-8 hr

            Peak plasma concentration: 4-19 ng/mL (dose dependent)

            Metabolism

            Metabolism: Hepatic P450 enzyme CYP3A4 and CYP2D6

            Metabolites: Inactive

            Elimination

            Half-life elimination: 55 hr

            Excretion: Urine

            Dialyzable: Unknown

            Pharmacogenetics

            Poor CYP2D6 metabolizers exhibit higher pimozide concentrations than extensive CYP2D6 metabolizers

            Approximately 7-10% of Caucasians and 3-8% of African Americans lack the capacity to metabolize CYP2D6 substrates and are classified as poor metabolizers (PMs)

            Serum concentrations observed in poor metabolizers are similar to those seen with strong CYP2D6 inhibitors (eg, paroxetine)

            Time to achieve steady state pimozide concentrations is expected to be longer (approximately 2 weeks) in poor metabolizers because of the prolonged half-life

            Alternative dosing strategies are recommended in patients who are genetically poor CYP2D6 metabolizers

            Genetic testing laboratories

            • Genotyping tests for CYP2D6 variants are commercially available through the following companies
            • Applied Biosystems (http://www.appliedbiosystems.com/)
            • GenPath Diagnostics (http://www.genpathdiagnostics.com/)
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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Select a class to view formulary status for similar drugs

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