Names and pronunciation
(pim-a-van′ser-in) Nuplazid
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Drug reference
(pim-a-van′ser-in) Nuplazid
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Func. class.: Atypical antipsychotic
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ACTION: The exact mechanism of action is unknown; may be mediated through inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at 5-HT2C receptors
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USES: The treatment of hallucinations and delusions associated with Parkinson’s disease psychosis
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CONTRAINDICATIONS: Hyper sensitivity Precautions: Alcoholism, bradycardia, breastfeeding, cardiac arrhythmias, car- diac disease, children, coronary artery disease, diabetes mellitus, females, geri- atric patients, heart failure, hepatic dis- ease, hypertension, hypocalcemia, hypo- kalemia, hypomagnesemia, long QT syndrome, malnutrition, myocardial infarction, pregnancy, QT prolongation, renal failure, renal impairment, stroke, thyroid disease
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Black Box Warning: Dementia-related psychosis Black Box Warning: Dementia-related psychosis: at increased risk of death, avoid using • Swallowing of medication; check for hoarding, giving product to other pa- tients • AIMS assessment, neurologic function, LFTs, serum electrolytes, creatinine monthly • Constipation daily; if this occurs, in- crease bulk, water in diet; stool soften- ers, laxatives may be needed • QT prolongation: avoid in those with cardiac disease or other risk factors for QT prolongation, torsades de pointes (TdP), and/or sudden death such as cardiac arrhythmias, congenital long QT syndrome, heart failure, bradycardia, myocardial infarction, hypertension, coronary artery disease, hypomagnese- mia, hypokalemia, hypocalcemia, or in patients receiving medications known to prolong the QT interval. Females, el- derly patients, patients with diabetes mellitus, thyroid disease, malnutrition, alcoholism, or hepatic impairment may also be at increased risk for QT prolon- gation • Stroke: avoid antipsychotics to treat delirium- or dementia-related behavioral problems unless nonpharmacologic op- tions have failed and the patient is a substantial threat to self or others; avoid use in those with a history of falls or fractures • Hyponatremia: product can cause hy- ponatremia and SIADH and elderly pa- tients are at increased risk; sodium levels should be closely monitored when start- ing or changing dosages of antipsychotics in older adults
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SIDE EFFECTS CNS: Confusion, hallucinations, fatigue, stroke, dizziness GI: Nausea, constipation MISC: Peripheral edema, infection, QT prolongation
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INTERACTIONS Increase: effects of pimavanserin—CYP3A4 inhibitors (ketoconazole, erythromycin), CYP2D6 inhibitors (quiNIDine, FLUoxetine, PARoxetine); reduce dose of pimavanserin Increase: sedation—other CNS depressants Increase: QT prolongation—products that cause QT prolongation Decrease: pimavanserin effects—famoti- dine, valproate, CYP3A4 inducers (carbamazepine) Decrease: pimavanserin effect—St. John’s wort
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DOSAGE AND ROUTES • Adult: PO 34 mg daily
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Available forms: Capsule 34 mg; tablet 10 mg
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Administer: • Give without regard to food • Do not split, chew capsules • Capsules may be opened and sprinkled on soft food
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Assess:
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Evaluate: • Therapeutic response: decrease in hal- lucinations, delusions, paranoia; reorga- nization of patterns of thought and speech Patient and caregiver information: • To avoid hazardous activities until re- sponse is known, dizziness may occur • That compliance with dose is needed • To avoid OTC products unless ap- proved by prescriber
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CLINICAL CONSIDERATIONS
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PHARMACOKINETICS Protein binding 95%, hepatic metabolism occurs through CYP3A4 and CYP3A5 and to a lesser extent CYP2J2, CYP2D6 with a major active metabolite; peak 6 hr, plasma half-lives of drug and metabolite are 57 hr and 200 hr, 0.55% eliminated unchanged in the urine and 1.53% was eliminated in feces after 10 days
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• Adult: PO 34 mg daily
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