pimavanserin (Rx)

Brand and Other Names:Nuplazid
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 34mg

tablet

  • 10mg

Parkinson Disease Psychosis

Indicated for treatment of hallucinations and delusions associated with Parkinson disease psychosis

34 mg PO qDay (without titration)

Dosage Modifications

Coadministration with strong CYP3A4 inhibitors

  • Decrease dose to 10 mg PO qDay

Coadministration with strong CYP3A4 inducers

  • Monitor for reduced efficacy; an increase in pimavanserin dosage may be needed

Renal impairment

  • Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment required
  • Severe (CrCl <30 mL/min) or end stage renal disease: Use with caution

Hepatic impairment

  • No dosage adjustment recommended

Safety and efficacy not established

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death; pimavanserin is not approved for dementia-related psychosis unrelated to Parkinson disease (see Black Box Warnings)

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Interactions

Interaction Checker

and pimavanserin

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            1-10%

            Nausea (7%)

            Peripheral edema (7%)

            Confusional state (6%)

            Hallucinations (5%)

            Constipation (4%)

            Gait disturbance (2%)

            Postmarketing Reports

            Rash

            Urticaria

            Reactions consistent with angioedema (e.g., tongue swelling, circumoral edema, throat tightness, and dyspnea)

            Somnolence, falls

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            Warnings

            Black Box Warnings

            Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death

            Pimavanserin is not approved for the treatment of patients with dementia-related psychosis unrelated to the hallucinations and delusions associated with Parkinson disease psychosis

            Contraindications

            Documented hypersensitivity reaction to drug or components; rash, urticaria, and reactions consistent with angioedema (e.g., tongue swelling, circumoral edema, throat tightness, and dyspnea)

            Cautions

            Antipsychotic drugs increase the all-cause risk of death in elderly patients with dementia-related psychosis (see Black Box Warnings)

            Pimavanserin is a substrate of CYP3A4; strong CYP3A4 inhibitor or inducers affect systemic exposure (see Dosage Modifications and Interactions)

            QT prolongation

            • Prolongs QT interval
            • Avoid use in patients with known QT prolongation or in combination with other drugs known to prolong QT interval, including class 1A antiarrhythmics (eg, quinidine, procainamide) or class 3 antiarrhythmics (eg, amiodarone, sotalol), certain antipsychotic medications (eg, ziprasidone, chlorpromazine, thioridazine), and certain antibiotics (eg, gatifloxacin, moxifloxacin)
            • Avoid with history of cardiac arrhythmias, as well as other circumstances that may increase the risk of the occurrence of torsade de pointes and/or sudden death, including symptomatic bradycardia, hypokalemia, or hypomagnesemia, and the presence of congenital prolongation of the QT interval
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            Pregnancy

            Pregnancy

            There are no data for use in pregnant women that would allow assessment of the drug-associated risk of major congenital malformations or miscarriage

            In animal reproduction studies, no adverse developmental effects were seen when pimavanserin was administered orally to rats or rabbits during the period of organogenesis at doses up to 10 or 12 times the maximum recommended human dose (MRHD) of 34 mg/day, respectively

            Lactation

            Unknown if distributed in human breast milk

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

            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

            Selective serotonin inverse agonist and antagonist activity preferentially targeting 5-HT2A receptors believed to play an important role in psychosis

            Absorption

            Peak plasma time: 6 hr (range 4-24 hr)

            Time to active metabolite formation: 6 hr

            Distribution

            Protein bound: ~95%

            Vd: 2173 L

            Metabolism

            Predominantly metabolized by CYP3A4 and CYP3A5 and to a lesser extent by CYP2J2, CYP2D6, and various other CYP and FMO enzymes

            CYP3A4 is the major enzyme responsible for the formation of its major active metabolite (AC-279)

            Elimination

            Half-life: 57 hr (pimavanserin); 200 hr (active metabolite)

            Excretion (after 10 days): ~0.55 unchanged in urine; 1.53% unchanged in feces; <1% of the administered dose and active metabolite recovered in urine

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            Administration

            Oral Administration

            May take with or without food

            Storage

            Store at controlled room temperature (20-25°C [68-77°F]); excursions permitted between 15-30°C (59-86°F)

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            Formulary

            FormularyPatient Discounts

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            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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.