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paliperidone (Rx)Brand and Other Names:Invega, Invega Sustenna, more...Invega Trinza

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, extended release

  • 1.5mg
  • 3mg
  • 6mg
  • 9mg

IM injectable suspension prefilled syringe (once monthly, Invega Sustenna)

  • 39mg
  • 78mg
  • 117mg
  • 156mg
  • 234mg

IM injectable suspension prefilled syringe (q3month, Invega Trinza)

  • 273mg
  • 410mg
  • 546mg
  • 819mg
more...

Schizophrenia

PO

  • 6 mg PO qAM; may be titrated upward or downward in increments of 3 mg/day at intervals ≥5 days; not to exceed 12 mg/day

IM, sustained-released 1-month (Invega Sustenna)

  • 234 mg in deltoid on treatment day 1, then 156 mg 1 week later (day 8)
  • Recommended maintenance dose is 117 mg IM once monthly, although some patients may require lower or higher dosages (monthly dose range 39-234 mg)

IM, sustained-released 3-months (Invega Trinza)

  • Patients must be adequately treated with Invega Sustenna (1-month paliperidone) for at least 4 months before initiating Invega Trinza
  • Dose initiation dependent on once-monthly Invega Sustenna dose
  • Initiate Invega Trinza when the next 1-month paliperidone dose is scheduled with an Invega Trinza dose based on the previous 1-month injection dose (see below)
  • Conversion from monthly injection to 3-month injection
    • Invega Sustenna 78 mg/month: Initiate Invega Trinza at 273 mg IM q3mo
    • Invega Sustenna 117 mg/month: Initiate Invega Trinza at 410 mg IM q3mo
    • Invega Sustenna 156 mg/month: Initiate Invega Trinza at 546 mg IM q3mo
    • Invega Sustenna 234 mg/month: Initiate Invega Trinza at 819 mg IM q3mo
  • Conversoin from 3-month IM injection to extended-release tablets
    • 273 mg IM (last 3 months to 24wk): 3 mg ER tab
    • 410 mg IM (last 3 months to 24wk): 3 mg ER tab; 6 mg if >24wk
    • 546 mg IM (last 3 months to 18 wk): 3 mg ER tab; 6 mg if 18-24 wk; 9 mg if >24 wk
    • 819 mg IM (last 3 months to 18 wk): 6 mg ER tab; 9 mg if 18-24 wk; 12 mg if >24 wk

Schizoaffective Disorder

Indicated for schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers or antidepressants

6 mg PO qDay in am (range 3-12 mg); titration may not be necessary; if exceeding 6 mg/day, increases of 3 mg/day recommended at intervals of 4 days of more; not to exceed 12 mg/day

IM (initial): 234 mg in deltoid on treatment day 1, then 156 mg 1 week later (day 8)

IM (maintenance): Administer once each month IM in deltoid or gluteal muscle; adjust dose based on tolerability and/or efficacy using available strengths; maintenance dose ranges between 78-234 mg once monthly

Dosing Modifications

Renal impairment, PO

  • CrCl 50-79 mL/min: 3 mg/day initially; not to exceed 6 mg/day
  • CrCl 10-49 mL/min: 1.5 mg/day initially; not to exceed 3 mg/day
  • CrCl <10 mL/min: Not recommended

Renal impairment, IM

  • Moderate-to-severe (CrCl <50 mL/min): Not recommended
  • Mild (CrCl 50-79 mL/min)
    • Invega Sustenna: 156 mg IM in deltoid on treatment day 1, then 117 mg 1 week later; maintenance: 78 mg IM monthly
    • Invega Trinza: Adjust dosage and stabilize the patient using the 1-month paliperidone palmitate extended-release injectable suspension (Invega Sustenna), then transition to Invega Trinza

Dosage Forms & Strengths

tablet, extended-release

  • 1.5mg
  • 3mg
  • 6mg
  • 9mg
more...

Schizophrenia

<12 years: Safety and efficacy not established

≥12 years (<51 kg): 3 mg/day PO initially; may be increased if necessary in increments of 3 mg/day at intervals ≥5 days; not to exceed 6 mg/day

≥12 years (≥51 kg): 3 mg/day PO initially; may be increased if necessary in increments of 3 mg/day at intervals ≥5 days; not to exceed 12 mg/day

Schizoaffective Disorder

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

paliperidone 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%

            Akathisia

            Somnolence

            Insomnia

            Parkinsonism

            Tachycardia

            Hyperprolactinemia

            Others similar to placebo (eg, headache)

            <10% (selected)

            Cough

            Dystonia

            Extrapyramidal symptoms (EPS)

            Orthostatic hypotension

            QT prolongation

            Sialorrhea

            Priapism

            Weight gain

            Constipation

            Indigestion

            Amenorrhea

            Galactorrhea

            Nausea

            Dyspepsia

            Salivation

            Xerostomia

            Myalgia

            Extremity pain

            Nasopharyngitis

            Postmarketing Reports

            Angioedema, swollen tongue

            Ileus

            Thrombotic thrombocytopenic purpura

            Urinary incontinence, urinary retention

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            Warnings

            Black Box Warnings

            Not approved for dementia-related psychosis; patients with dementia-related psychosis who are treated with antipsychotic drugs are at increased risk of death, as shown in short-term controlled trials; deaths in these trials appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature

            Contraindications

            Documented hypersensitivity to paliperidone or risperidone

            Cautions

            Avoid use in severe preexisting GI stenosis

            Avoid overheating and dehydration, medications with anticholinergic side effects being taken concomitantly, and strenuous exercise; impaired core body temperature regulation may occur

            Rare cases of priapism reported

            Rare cases of intraoperative floppy iris syndrome reported with risperidone in patients undergoing cataract surgery; paliperidone is active metabolite of risperidone; use caution; benefits or risks of interrupting paliperidone or risperidone use prior to cataract surgery not established

            If tardive dyskinesia develops discontinue drug if clinically appropriate

            Hyperprolactinemia occurs and persists during long-term administration

            Prolongs QT interval modestly; avoid use with drugs that also increase QT interval and in patients with risk factors for prolonged QT interval

            Potential risk of neuroleptic malignant syndrome (NMS); manage with immediate discontinuation of drug and close monitoring

            Risk of orthostatic hypotension; use with caution in patients with known cardiovascular or cerebrovascular disease and patients predisposed to hypotension

            Increased incidence of cerebrovascular adverse reactions (e.g. stroke, transient ischemic attack, including fatalities) reported

            Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold

            Patients with Parkinson disease may be more sensitive to CNS and extrapyramidal effects

            May mask toxicity of other drugs or conditions (eg, intestinal obstruction) due to antiemetic effects

            FDA warning regarding off-label use for dementia in elderly

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

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

            May cause CNS depression, which may impair abilities to perform tasks requiring mental alertness, including operating heavy machinery

            Antipsychotic use has been associated with esophageal dysmotility and aspiration; use with caution in patients at risk of aspiration pneumonia; not for use in patients unable to swallow the tablet whole

            Use caution in patients with history of suicidal ideation or any form of psychotic illnes; may increase risk of suicide attempt

            Metabolic changes

            • Atypical antipsychotic drugs have been associated with metabolic changes that may increase cardiovascular or cerebrovascular risk (eg, hyperglycemia, dyslipidemia, hyperprolactinemia, body weight gain)
            • In some cases, hyperglycemia concomitant with use of atypical antipsychotics has been associated with ketoacidosis, hyperosmolar coma, or death
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            Pregnancy & Lactation

            Pregnancy category: C

            Neonates exposed to antipsychotic drugs during 3rd trimester of pregnancy are at risk for EPS or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU support and prolonged hospitalization

            Lactation: Drug excreted in breast milk; do not nurse

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Major metabolite of risperidone; improves negative symptoms of psychoses and reduces incidence of EPS

            Has high affinity for serotonin type 2 (5-HT2) receptors; binds to dopamine D2 receptors with 20 times lower affinity than that for 5-HT2 receptors; antagonizes alpha1-adrenergic, alpha2-adrenergic, and histaminergic receptors; has moderate affinity for serotonin type 1 (5-HT1C, 5-HT1D, 5-HT1A) receptors; has weak affinity for dopamine D1 receptors; has no affinity for muscarinic, beta1-adrenergic, and beta2-adrenergic receptors

            Absorption

            Bioavailability: 28%

            Peak plasma time: PO, 24 hr; IM, 13 days

            Distribution

            Protein bound: 74%

            Vd: 390-487 L

            Metabolism

            Metabolized by CYP2D6 and CYP3A4

            Elimination

            Half-life: PO, 23 hr; IM, 25-49 days

            Excretion: Urine (80%), feces (11%)

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            Administration

            Oral administration

            May be taken with or without food

            Swallow tablet whole with liquids; do not chew, crush or divide

            The tablet shell, along with insoluble core components, is eliminated from the body; patients should not be concerned if they occasionally notice in their stool, something that looks like a tablet

            IM administration

            Each IM injection must be administered only by a healthcare professional

            Prior to administration, shake the prefilled syringe vigorously for at least 15 seconds within 5 minutes prior to administration to ensure a homogeneous suspension

            Once monthly IM injection

            • Before initiating once monthly IM therapy, establish PO tolerability with paliperidone or risperidone
            • First 2 doses are injected into deltoid; maintenance doses may be injected into either deltoid or gluteal muscle

            Every 3-months IM administration

            • Before initiating q3mo IM therapy, establish tolerability with once-monthly paliperidone for at least 4 months
            • Initiate Invega Trinza when the next 1-month paliperidone dose is scheduled with an Invega Trinza dose based on the previous 1-month injection dose (see Adult Dosing)

            Needle length and gauge

            • Deltoid injection: If patient ≥90 kg, use 1.5-in. 22-gauge needle; if patient <90 kg, use 1-in. 23-gauge needle
            • Gluteal injection: Use 1.5-in. 22-gauge needle regardless of patient weight

            Missed Doses

            Invega Sustenna

            • Second dose
              • To avoid a missed dose, patients may be given the second dose 4 days before or after the one-week time point
              • <4 wk since first injection: Administer second initiation dose of 156 mg IM in deltoid muscle as soon as possible, then administer a third injection of 117 mg IM (deltoid or gluteal) 5 weeks afterwards; thereafter resume regular monthly dosing
              • 4-7 wk since first injection: Resume dose with 2 injections of 156 mg IM in deltoid muscle 1 week apart; thereafter, resume regular monthly dosing
              • >7 wk since first injection: Restart with recommended initiation (see Adult Dosing)
            • Third and subsequent doses
              • To avoid a missed dose, patients may be give the injection 7 days before or after the monthly time point
              • 4-6 wk since last injection: Resume regular monthly dosing as soon as possible at previous stabilized dose; followed in monthly injections
              • >6 wk to 6 months since last injection: Resume same dose as previously stabilized, unless stabilized on 234 mg/month, then the first 2 injections should each be 156 mg given 1 wk apart; thereafter, resume previously stabilized dose 1 month later
              • >6 months since last injection: Administer 234 mg IM in deltoid on Day 1, then 156 mg IM in deltoid on Day 8; thereafter, resume administration 1 month after Day 8 at the previously stabilized dose (deltoid or gluteal)

            Invega Trinza

            • If necessary, patients may be given the injection up to 2 weeks before or after the 3-month time point
            • Missed dose >9 months since last injection: Must reinitiate with the 1-month paliperidone as previously described (see Adult Dosing)
            • Missed dose 3.5-4 months since last injection: Administer the patient’s regular dose as soon as possible, then continue with the 3-month injection following this dose
            • Missed dose 4-9 months since last injection: Do not administer the next dose, instead use reinitiation schedule
            • Reinitiation schedule based on last dose of Invega Trinza
              • Administer Invega Sustenna, 2 doses given 1 week apart into deltoid muscle (ie, Day 1 and Day 8), then administer Invega Trinza 1 month after Day 8 (in deltoid or gluteal muscle)
              • Last dose 273 mg: Invega Sustenna 78 mg IM on Days 1 and 8, then Invega Trinza 273 mg IM 1 month after Day 8
              • Last dose 410 mg: Invega Sustenna 117 mg IM on Days 1 and 8, then Invega Trinza 410 mg IM 1 month after Day 8
              • Last dose 546 mg: Invega Sustenna 156 mg IM on Days 1 and 8, then Invega Trinza 546 mg IM 1 month after Day 8
              • Last dose 819 mg: Invega Sustenna 156 mg IM on Days 1 and 8, then Invega Trinza 819 mg IM 1 month after Day 8

            Storage

            IM: Store at room temperature 20-25°C (68-77°F); excursions between 15-30°C (59-86°F) are permitted

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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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