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Paliperidone

Pronunciation

Pronunciation

(pal ee PER i done)

Index Terms

  • 9-hydroxy-risperidone
  • 9-OH-risperidone
  • Paliperidone Palmitate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Suspension, Intramuscular, as palmitate:

Invega Sustenna: 39 mg/0.25 mL (0.25 mL); 78 mg/0.5 mL (0.5 mL); 117 mg/0.75 mL (0.75 mL); 156 mg/mL (1 mL); 234 mg/1.5 mL (1.5 mL) [contains polyethylene glycol]

Invega Trinza: 410 mg/1.315 mL (1.315 mL); 273 mg/0.875 mL (0.875 mL); 546 mg/1.75 mL (1.75 mL); 819 mg/2.625 mL (2.625 mL) [contains polyethylene glycol]

Tablet Extended Release 24 Hour, Oral:

Invega: 1.5 mg, 3 mg, 6 mg, 9 mg

Generic: 1.5 mg, 3 mg, 6 mg, 9 mg

Brand Names: U.S.

  • Invega
  • Invega Sustenna
  • Invega Trinza

Pharmacologic Category

  • Second Generation (Atypical) Antipsychotic

Pharmacology

Paliperidone is considered a benzisoxazole atypical antipsychotic as it is the primary active metabolite of risperidone. As with other atypical antipsychotics, its therapeutic efficacy is believed to result from mixed central serotonergic and dopaminergic antagonism. The addition of serotonin antagonism to dopamine antagonism (classic neuroleptic mechanism) is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side effects. Similar to risperidone, paliperidone demonstrates high affinity to α1, D2, H1, and 5-HT2C receptors, and low affinity for muscarinic and 5-HT1A receptors. In contrast to risperidone, paliperidone displays nearly 10-fold lower affinity for α2 and 5-HT2A receptors, and nearly three- to fivefold less affinity for 5-HT1A and 5-HT1D, respectively.

Absorption

IM: Slow release (Monthly: Begins on day 1 and continues up to 126 days; 3-month: Begins on day 1 and continues up to 18 months)

Distribution

Vd: Oral: 487 L; Monthly IM: 391 L; 3-month IM: 1960 L

Metabolism

Hepatic via CYP2D6 and 3A4 (limited role in elimination); minor metabolism (<10% each) via dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission

Excretion

Urine (80%); feces (11%)

Time to Peak

Oral: ~24 hours; Monthly IM: 13 days; 3-month IM: 30 to 33 days

Half-Life Elimination

Oral: 23 hours; 24 to 51 hours with renal impairment (CrCl <80 mL/minute)

Monthly IM (following a single-dose administration): Range: 25 to 49 days

3-month IM: Deltoid injection range: 84 to 95 days; gluteal injection range: 118 to 139 days

Protein Binding

74%

Special Populations: Renal Function Impairment

Elimination of paliperidone decreased with decreasing estimated creatinine clearance.

Special Populations: Gender

Slower monthly IM absorption observed in women.

Use: Labeled Indications

Schizophrenia: Treatment of schizophrenia

Schizoaffective disorder (oral and monthly IM paliperidone): Treatment of schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers or antidepressants

Use: Unlabeled

Psychosis/agitation related to Alzheimer's dementia

Contraindications

Hypersensitivity to paliperidone, risperidone, or any component of the formulation

Dosage

US labeling:

Schizoaffective disorder: Adults:

Oral: Usual: 6 mg once daily in the morning; titration not required, though some may benefit from lower or higher doses (range: 3 to 12 mg daily). If exceeding 6 mg daily, increases of 3 mg daily are recommended at intervals of more than 4 days, up to a maximum of 12 mg daily.

Monthly IM: Note: Prior to initiation of monthly IM paliperidone, for patients naive to oral paliperidone or oral or injectable risperidone tolerability should be established with oral paliperidone or oral risperidone. Previous oral antipsychotics can be gradually discontinued at the time of initiation of monthly IM paliperidone. Dosing based on paliperidone palmitate.

Initiation of therapy:

Initial: 234 mg on treatment day 1 followed by 156 mg 1 week later with both doses administered in the deltoid muscle. The second dose may be administered 4 days before or after the weekly time point.

Maintenance: Following the 1-week initiation regimen, adjust the dose based on response and tolerability and begin a maintenance dose of 78 to 234 mg every month administered in either the deltoid or gluteal muscle (the 39 mg strength was not studied in schizoaffective disorder trials). The monthly maintenance dose may be administered 7 days before or after the monthly time point.

Conversion from oral paliperidone to monthly IM paliperidone: Initiate monthly IM paliperidone as described using the 1-week initiation regimen. Patients previously stabilized on oral doses can expect similar steady state exposure during maintenance treatment with monthly IM paliperidone using the following conversion:

Oral extended-release dose of 12 mg daily, then IM maintenance dose of 234 mg monthly

Oral extended-release dose of 6 mg daily, then IM maintenance dose of 117 mg monthly

Oral extended-release dose of 3 mg daily, then IM maintenance dose of 39 to 78 mg monthly

Conversion from other oral antipsychotics to monthly IM paliperidone: There is no systematically collected data to address switching patients from other oral antipsychotics to monthly IM paliperidone.

Switching from other long-acting injectable antipsychotics to monthly IM paliperidone: Initiate monthly IM paliperidone in the place of the next scheduled injection and continue at monthly intervals. The 1-week initiation regimen is not required in these patients.

Dosage adjustments: Adjustments may be made monthly (full effect from adjustments may not be seen for several months)

Missed second initiation dose:

If <4 weeks have elapsed since the first injection: Administer the missed dose (156 mg) in the deltoid as soon as possible, followed by a third dose of 117 mg in either the deltoid or gluteal muscle 5 weeks after the first injection (regardless of when the second injection was administered), then begin normal monthly maintenance dosing.

If ≥4 weeks and ≤7 weeks have elapsed since the first injection: Administer a dose of 156 mg in the deltoid as soon as possible, followed by another 156 mg dose in the deltoid 1 week later, then begin normal monthly maintenance dosing.

If >7 weeks have elapsed since the first injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Missed maintenance dose:

If ≥4 weeks and ≤6 weeks have elapsed since the last monthly injection: Administer the missed dose as soon as possible and continue therapy at monthly intervals.

If >6 weeks and ≤6 months have elapsed since the last monthly injection:

If the maintenance dose was <234 mg: Administer the same dose the patient was previously stabilized on in the deltoid as soon as possible, followed by a second equivalent dose in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If the maintenance dose was 234 mg: Administer a 156 mg dose in the deltoid as soon as possible, followed by a second dose of 156 mg in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If >6 months have elapsed since last monthly maintenance injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Schizophrenia:

Adolescents 12 to 17 years: Oral: Initial: 3 mg once daily; titration not required (no known benefit to efficacy from higher doses [ie, 6 mg daily for patients <51 kg and 12 mg daily for patients ≥51 kg]). If exceeding 3 mg daily, increases of 3 mg daily are recommended no more frequently than every 5 days.

Adults:

Oral: Usual: 6 mg once daily in the morning; titration not required, though some may benefit from lower or higher doses (range: 3 to 12 mg daily). If exceeding 6 mg daily, increases of 3 mg daily are recommended no more frequently than every 5 days, up to a maximum of 12 mg daily.

IM:

Monthly paliperidone (Invega Sustena):Note: Prior to initiation of monthly IM paliperidone, for patients naive to oral paliperidone or oral or injectable risperidone tolerability should be established with oral paliperidone or oral risperidone. Previous oral antipsychotics can be gradually discontinued at the time of initiation of monthly IM paliperidone. Dosing based on paliperidone palmitate.

Initiation of therapy:

Initial: 234 mg on treatment day 1 followed by 156 mg 1 week later with both doses administered in the deltoid muscle. The second dose may be administered 4 days before or after the weekly time point.

Maintenance: Following the 1-week initiation regimen, begin a maintenance dose of 117 mg every month administered in either the deltoid or gluteal muscle. Some patients may benefit from higher or lower monthly maintenance doses (monthly maintenance dosage range: 39 to 234 mg). The monthly maintenance dose may be administered 7 days before or after the monthly time point.

Conversion from oral paliperidone to monthly IM paliperidone: Initiate monthly IM paliperidone as described using the 1-week initiation regimen. Patients previously stabilized on oral doses can expect similar steady state exposure during maintenance treatment with monthly IM paliperidone using the following conversion:

Oral extended-release dose of 12 mg daily, then IM maintenance dose of 234 mg monthly

Oral extended-release dose of 6 mg daily, then IM maintenance dose of 117 mg monthly

Oral extended-release dose of 3 mg daily, then IM maintenance dose of 39 to 78 mg monthly

Conversion from other oral antipsychotics to monthly IM paliperidone: There is no systematically collected data to address switching patients from other oral antipsychotics to monthly IM paliperidone.

Switching from other long-acting injectable antipsychotics to monthly IM paliperidone: Initiate monthly IM paliperidone in the place of the next scheduled injection and continue at monthly intervals. The 1-week initiation regimen is not required in these patients.

Dosage adjustments: Adjustments may be made monthly (full effect from adjustments may not be seen for several months)

Missed second initiation dose:

If <4 weeks have elapsed since the first injection: Administer the missed dose (156 mg) in the deltoid as soon as possible, followed by a third dose of 117 mg in either the deltoid or gluteal muscle 5 weeks after the first injection (regardless of when the second injection was administered), then begin normal monthly maintenance dosing.

If ≥4 weeks and ≤7 weeks have elapsed since the first injection: Administer a dose of 156 mg in the deltoid as soon as possible, followed by another 156 mg dose in the deltoid 1 week later, then begin normal monthly maintenance dosing.

If >7 weeks has elapsed since the first injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Missed maintenance dose:

If ≥4 weeks and ≤6 weeks have elapsed since the last monthly injection: Administer the missed dose as soon as possible and continue therapy at monthly intervals.

If >6 weeks and ≤6 months have elapsed since the last monthly injection:

If the maintenance dose was <234 mg: Administer the same dose the patient was previously stabilized on in the deltoid as soon as possible, followed by a second equivalent dose in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If the maintenance dose was 234 mg: Administer a 156 mg dose in the deltoid as soon as possible, followed by a second dose of 156 mg in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If >6 months have elapsed since last monthly maintenance injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Three-month paliperidone (Invega Trinza): Note: Three-month IM paliperidone is to be used only after monthly IM paliperidone (Invega Sustenna) has been established as adequate treatment for at least 4 months. The last 2 doses of monthly IM paliperidone should be the same dosage strength before starting 3-month IM paliperidone.

Conversion from monthly injection to 3-month injection: Initiate 3-month IM paliperidone when the next monthly IM paliperidone dose is scheduled. Base the 3-month dose on the previous monthly dose, using the equivalent 3.5 times higher dose. Three-month IM paliperidone may be administered up to 7 days before or after the next monthly dose date. Following the initial injection, administer every 3 months. Patients may be given the injection up to 2 weeks before or after the 3-month time point.

Monthly IM paliperidone (Invega Sustenna) 78 mg = 3-month IM paliperidone (Invega Trinza) 273 mg

Monthly IM paliperidone (Invega Sustenna) 117 mg = 3-month IM paliperidone (Invega Trinza) 410 mg

Monthly IM paliperidone (Invega Sustenna) 156 mg = 3-month IM paliperidone (Invega Trinza) 546 mg

Monthly IM paliperidone (Invega Sustenna) 234 mg = 3-month IM paliperidone (Invega Trinza) 819 mg

Conversion from 3-month IM paliperidone to monthly IM paliperidone: Initiate monthly IM paliperidone when the next 3-month IM paliperidone dose is scheduled. Base the monthly dose on the previous 3-month dose, using the equivalent 3.5 times lower dose. Following the initial injection, administer once monthly.

3-month IM paliperidone (Invega Trinza) 273 mg = Monthly IM paliperidone (Invega Sustenna) 78 mg

3-month IM paliperidone (Invega Trinza) 410 mg = Monthly IM paliperidone (Invega Sustenna) 117 mg

3-month IM paliperidone (Invega Trinza) 546 mg = Monthly IM paliperidone (Invega Sustenna) 156 mg

3-month IM paliperidone (Invega Trinza) 819 mg = Monthly IM paliperidone (Invega Sustenna) 234 mg

Conversion from 3-month IM paliperidone to paliperidone extended-release tablets: Initiate paliperidone extended release tablets 3 months after the last dose of 3-month IM paliperidone. Base the once daily extended-release tablet dose on the last 3- month injection dose and weeks since last administered. Use the following conversion.

If the last 3-month IM paliperidone dose was:

273 mg: 3 months to >24 weeks since the last dose = 3 mg paliperidone extended-release tablets

410 mg:

3 months to 24 weeks since the last dose = 3 mg paliperidone extended-release tablets

>24 weeks since the last dose = 6 mg paliperidone extended-release tablets

546 mg:

3 months to 18 weeks since the last dose = 3 mg paliperidone extended-release tablets

>18 weeks to 24 weeks since the last dose = 6 mg paliperidone extended-release tablets

>24 weeks since the last dose = 9 mg paliperidone extended-release tablets

819 mg:

3 months to 18 weeks since the last dose = 6 mg paliperidone extended-release tablets

>18 weeks to 24 weeks since the last dose = 9 mg paliperidone extended-release tablets

>24 weeks since the last dose = 12 mg paliperidone extended-release tablets

Dosage adjustments: Dosage adjustments can be made every 3 months in increments within the range of 273 to 819 mg based on response and tolerability. Due to the long-acting nature, the patient’s response to an adjusted dose may not be apparent for several months.

Missed dose 3 ½ months to 4 months since last injection: Administer the previous 3-month dose as soon as possible and continue with normal dosing.

Missed dose 4 months to 9 months since last injection: Do not administer the next 3-month dose. If the last 3-month dose was:

273 mg: Administer 78 mg of monthly IM paliperidone (Invega Sustenna) into the deltoid muscle. Administer a second dose of 78 mg of monthly IM paliperidone (Invega Sustenna) one week later. One month following the second injection, administer 273 mg of 3-month IM paliperidone (Invega Trinza) into the deltoid or gluteal muscle and resume normal dosing at 3-month intervals.

410 mg: Administer 117 mg of monthly IM paliperidone (Invega Sustenna) into the deltoid muscle. Administer a second dose of 117 mg of monthly IM paliperidone (Invega Sustenna) one week later. One month following the second injection, administer 410 mg of 3-month IM paliperidone (Invega Trinza) into the deltoid or gluteal muscle and resume normal dosing at 3-month intervals.

546 mg: Administer 156 mg of monthly IM paliperidone (Invega Sustenna) into the deltoid muscle. Administer a second dose of 156mg of monthly IM paliperidone (Invega Sustenna) one week later. One month following the second injection, administer 546 mg of 3-month IM paliperidone (Invega Trinza) into the deltoid or gluteal muscle and resume normal dosing at 3-month intervals.

819 mg: Administer 156 mg of monthly IM paliperidone (Invega Sustenna) into the deltoid muscle. Administer a second dose of 156mg of monthly IM paliperidone (Invega Sustenna) one week later. One month following the second injection, administer 819 mg of 3-month IM paliperidone (Invega Trinza) into the deltoid or gluteal muscle and resume normal dosing at 3-month intervals.

Missed dose longer than 9 months since last injection: Re-initiate treatment with monthly IM paliperidone (Invega Sustenna). Three-month IM paliperidone can be resumed after the patient has been adequately treated with monthly IM paliperidone for at least 4 months.

Canadian labeling:

Schizoaffective disorder: Adults:

Oral: Usual: 6 mg once daily in the morning; titration not required, though some may benefit from lower or higher doses (range: 3 to 12 mg daily). Dosage adjustments in increments or decrements of 3 mg daily are recommended at intervals of more than 5 days, maximum dose: 12 mg daily.

IM: Monthly paliperidone: Note: In patients naive to oral paliperidone or oral/injectable risperidone, tolerability should be established with oral paliperidone or oral risperidone prior to initiation of monthly IM paliperidone. Previous oral antipsychotics can be gradually discontinued at the time of initiation of monthly IM paliperidone. Dosing based on paliperidone.

Initiation of therapy:

Initial: 150 mg on treatment day 1 followed by 100 mg 1 week later (day 8) with both doses administered in the deltoid. The second dose may be administered up to 4 days before or after the weekly time point.

Maintenance: Following the 1-week initiation regimen, adjust the dose based on response and tolerability and begin a maintenance dose of 50 to 150 mg every month administered in either the deltoid or gluteal muscle. The monthly maintenance dose may be administered 7 days before or after the monthly time point.

Conversion from oral paliperidone to monthly IM paliperidone: Initiate monthly IM paliperidone as described using the 1-week initiation regimen. Patients previously stabilized on oral doses can expect similar steady state exposure during maintenance treatment with monthly IM paliperidone using the following conversion:

Oral extended-release dose of 12 mg daily, then IM maintenance dose of 150 mg monthly

Oral extended-release dose of 6 mg daily, then IM maintenance dose of 75 mg monthly

Oral extended-release dose of 3 mg daily, then IM maintenance dose of 25 to 50 mg monthly

Switching from other long-acting injectable antipsychotics (including Risperdal Consta) to monthly IM paliperidone: Initiate monthly IM paliperidone in the place of the next scheduled injection and continue at monthly intervals. The 1-week initiation regimen is not required in these patients.

Switching from injectable risperidone (Risperdal Consta) to monthly IM paliperidone:

Risperdal Consta dose of 25 mg every 2 weeks, then IM paliperidone maintenance dose of 50 mg monthly

Risperdal Consta dose of 37.5 mg every 2 weeks, then IM paliperidone maintenance dose of 75 mg monthly

Risperdal Consta dose of 50 mg every 2 weeks, then IM paliperidone maintenance dose of 100 mg monthly

Dosage adjustments: Adjustments may be made monthly (full effect from adjustments may not be seen for several months)

Missed second initiation dose:

If <4 weeks has elapsed since first injection: Administer the missed dose (100 mg) in the deltoid as soon as possible followed by a third dose of 75 mg in either the deltoid or gluteal muscle 5 weeks after the first injection (regardless of when the second injection was administered), then begin normal monthly maintenance dosing.

If 4 to 7 weeks have elapsed since first injection: Administer a dose of 100 mg in the deltoid as soon as possible, followed by another 100 mg dose in the deltoid 1 week later, then begin normal monthly maintenance dosing.

If >7 weeks has elapsed since the first injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Missed maintenance dose:

If <6 weeks have elapsed since the last monthly injection: Administer the missed dose as soon as possible and continue therapy at monthly intervals.

If >6 weeks and ≤6 months have elapsed since the last monthly injection:

If the maintenance dose was 25 to 100 mg: Administer the same dose the patient was previously stabilized on in the deltoid as soon as possible, followed by a second equivalent dose in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If the maintenance dose was 150 mg: Administer a 100 mg dose in the deltoid as soon as possible, followed by a second dose of 100 mg in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If >6 months have elapsed since last monthly maintenance injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Schizophrenia: Adults:

Oral: Usual: 6 mg once daily in the morning; titration not required, though some may benefit from lower or higher doses (range: 3 to 12 mg daily). Dosage adjustments in increments or decrements of 3 mg daily are recommended at intervals of more than 5 days, maximum dose: 12 mg daily.

IM: Monthly paliperidone: Note: In patients naive to oral paliperidone or oral/injectable risperidone, tolerability should be established with oral paliperidone or oral risperidone prior to initiation of monthly IM paliperidone. Previous oral antipsychotics can be gradually discontinued at the time of initiation of monthly IM paliperidone. Dosing based on paliperidone.

Initiation of therapy:

Initial: 150 mg on treatment day 1 followed by 100 mg 1 week later (day 8) with both doses administered in the deltoid. The second dose may be administered up to 4 days before or after the weekly time point.

Maintenance: Following the 1-week initiation regimen, begin a maintenance dose of 75 mg every month administered in either the deltoid or gluteal muscle. Some patients may benefit from higher or lower monthly maintenance doses (monthly maintenance dosage range: 25 to 150 mg). The monthly maintenance dose may be administered 7 days before or after the monthly time point.

Conversion from oral paliperidone to monthly IM paliperidone: Initiate monthly IM paliperidone as described using the 1-week initiation regimen. Patients previously stabilized on oral doses can expect similar steady state exposure during maintenance treatment with monthly IM paliperidone using the following conversion:

Oral extended-release dose of 12 mg daily, then IM maintenance dose of 150 mg monthly

Oral extended-release dose of 6 mg daily, then IM maintenance dose of 75 mg monthly

Oral extended-release dose of 3 mg daily, then IM maintenance dose of 25 to 50 mg monthly

Switching from other long-acting injectable antipsychotics (including Risperdal Consta) to monthly IM paliperidone: Initiate monthly IM paliperidone in the place of the next scheduled injection and continue at monthly intervals. The 1-week initiation regimen is not required in these patients.

Switching from injectable risperidone (Risperdal Consta) to monthly IM paliperidone:

Risperdal Consta dose of 25 mg every 2 weeks, then IM paliperidone maintenance dose of 50 mg monthly

Risperdal Consta dose of 37.5 mg every 2 weeks, then IM paliperidone maintenance dose of 75 mg monthly

Risperdal Consta dose of 50 mg every 2 weeks, then IM paliperidone maintenance dose of 100 mg monthly

Dosage adjustments: Adjustments may be made monthly (full effect from adjustments may not be seen for several months)

Missed second initiation dose:

If <4 weeks has elapsed since first injection: Administer the missed dose (100 mg) in the deltoid as soon as possible followed by a third dose of 75 mg in either the deltoid or gluteal muscle 5 weeks after the first injection (regardless of when the second injection was administered), then begin normal monthly maintenance dosing.

If 4 to 7 weeks have elapsed since first injection: Administer a dose of 100 mg in the deltoid as soon as possible, followed by another 100 mg dose in the deltoid 1 week later, then begin normal monthly maintenance dosing.

If >7 weeks has elapsed since the first injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Missed maintenance dose:

If <6 weeks have elapsed since the last monthly injection: Administer the missed dose as soon as possible and continue therapy at monthly intervals.

If >6 weeks and ≤6 months have elapsed since the last monthly injection:

If the maintenance dose was 25 to 100 mg: Administer the same dose the patient was previously stabilized on in the deltoid as soon as possible, followed by a second equivalent dose in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If the maintenance dose was 150 mg: Administer a 100 mg dose in the deltoid as soon as possible, followed by a second dose of 100 mg in the deltoid 1 week later, then resume maintenance dose at monthly intervals.

If >6 months have elapsed since last monthly maintenance injection: Therapy must be reinitiated following dosing recommendations for initiation of therapy.

Dosage adjustment in renal impairment: Clearance is decreased in renal impairment; adjust dose according to renal function:

Oral:

Mild impairment (CrCl 50 to 79 mL/minute): Initial dose: 3 mg once daily; maximum dose: 6 mg once daily

Moderate to severe impairment (CrCl 10 to 49 mL/minute): Initial dose: 1.5 mg once daily; maximum dose: 3 mg once daily

Severe impairment (CrCl <10 mL/minute): Use not recommended (has not been studied).

IM:

US labeling:

Mild impairment (CrCl 50 to 79 mL/minute):

Monthly IM paliperidone (Invega Sustenna): Initiation of therapy: 156 mg on treatment day 1, followed by 117 mg 1 week later with both doses administered in the deltoid, followed by a maintenance dose of 78 mg every month (administered in the deltoid or gluteal muscle)

Three-month IM paliperidone (Invega Trinza): Adjust dosage and stabilize the patient using the monthly IM injection, then transition to the 3-month IM injection.

Moderate to severe impairment (CrCl <50 mL/minute): Use not recommended

Canadian labeling:

Mild impairment (CrCl 50 to 79 mL/minute): Initiation of therapy: 100 mg on treatment day 1, followed by 75 mg 1 week later with both doses administered in the deltoid, followed by a maintenance dose of 50 mg every month (administered in the deltoid or gluteal muscle). Based on tolerability and/or response, maintenance dose may be adjusted within range of 25 to 100 mg.

Moderate to severe impairment (CrCl <50 mL/minute): Use not recommended

Dosage adjustment in hepatic impairment: Oral, IM (monthly, 3-month):

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Administration

Oral: Administer in the morning without regard to meals. Extended release tablets should be swallowed whole with liquids; do not crush, chew, or divide.

IM Injection: Administer by IM route only as a single injection (do not divide); do not administer by any other route. Avoid inadvertent injection into vasculature.

Monthly paliperidone (Invega Sustenna): Prior to injection, shake syringe for at least 10 seconds to ensure a homogenous suspension. The 2 initial injections should be administered in the deltoid muscle using a 11/2 inch, 22-gauge needle for patients ≥90 kg, and a 1 inch, 23-gauge needle for patients <90 kg. The 2 initial deltoid intramuscular injections help attain therapeutic concentrations rapidly. Alternate deltoid injections (right and left deltoid muscle). The second dose may be administered 4 days before or after the weekly time point. Monthly maintenance doses can be administered in either the deltoid or gluteal muscle. Administer injections in the gluteal muscle using a 11/2 inch, 22-gauge needle (regardless of patient weight) in the upper-outer quadrant of the gluteal area. Alternate gluteal injections (right and left gluteal muscle). The monthly maintenance dose may be administered 7 days before or after the monthly time point.

Three-month paliperidone (Invega Trinza): Prior to injection, shake syringe for at least 15 seconds to ensure a homogenous suspension. Inject within 5 minutes of shaking vigorously. Inject slowly, deep into the deltoid or gluteal muscle. Must be administered using only the thin wall needles that are provided in the pack. Do not use needles from monthly IM paliperidone or other commercially-available needles to reduce the risk of blockage. Administer into the center of the deltoid muscle using a 11/2 inch, 22-gauge thin wall needle for patients ≥90 kg, and a 1 inch, 22-gauge thin wall needle for patients <90 kg. Alternate deltoid injections (right and left deltoid muscle). Administer injections in the gluteal muscle using a 11/2 inch, 22-gauge thin wall needle (regardless of patient weight) in the upper-outer quadrant of the gluteal area. Alternate gluteal injections (right and left gluteal muscle). In the event of an incompletely administered dose, do not re-inject the dose remaining in the syringe and do not administer another dose. Closely monitor and treat the patient with oral supplementation as clinically appropriate until the next scheduled 3-month injection.

Storage

Oral, Monthly IM: Store at ≤25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect tablets from moisture.

3-month IM: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Acetylcholinesterase Inhibitors (Central): May enhance the neurotoxic (central) effect of Antipsychotic Agents. Severe extrapyramidal symptoms have occurred in some patients. Monitor therapy

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy

Amisulpride: Antipsychotic Agents may enhance the adverse/toxic effect of Amisulpride. Avoid combination

Amphetamines: Antipsychotic Agents may diminish the stimulatory effect of Amphetamines. Monitor therapy

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Anti-Parkinson's Agents (Dopamine Agonist): Antipsychotic Agents (Second Generation [Atypical]) may diminish the therapeutic effect of Anti-Parkinson's Agents (Dopamine Agonist). Management: Consider using an alternative antipsychotic agent when possible in patients with Parkinson's disease. If an atypical antipsychotic is necessary, consider using clozapine or quetiapine, which may convey the lowest interaction risk. Consider therapy modification

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

Blood Pressure Lowering Agents: May enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

CarBAMazepine: May decrease the serum concentration of Paliperidone. Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Highest Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of other Highest Risk QTc-Prolonging Agents. Avoid combination

Hydrocodone: CNS Depressants may enhance the CNS depressant effect of Hydrocodone. Management: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification

Inducers of CYP3A4 (Strong) and P-glycoprotein: May decrease the serum concentration of Paliperidone. Management: Avoid using the 3-month extended-release injectable suspension (Invega Trinza) with inducers of both CYP3A4 and P-glycoprotein during the 3-month dosing interval if possible. If combination is necessary, consider using extended-release tablets. Consider therapy modification

Itraconazole: May enhance the QTc-prolonging effect of Paliperidone. Itraconazole may decrease the metabolism of Paliperidone. Consider therapy modification

Ivabradine: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Lumacaftor: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. Lumacaftor may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification

Methylphenidate: Antipsychotic Agents may enhance the adverse/toxic effect of Methylphenidate. Methylphenidate may enhance the adverse/toxic effect of Antipsychotic Agents. Monitor therapy

Metoclopramide: May enhance the adverse/toxic effect of Antipsychotic Agents. Avoid combination

Metyrosine: CNS Depressants may enhance the sedative effect of Metyrosine. Monitor therapy

Metyrosine: May enhance the adverse/toxic effect of Antipsychotic Agents. Monitor therapy

Mifepristone: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Moderate Risk QTc-Prolonging Agents: May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Avoid combination

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying): May enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Quinagolide: Antipsychotic Agents may diminish the therapeutic effect of Quinagolide. Monitor therapy

RisperiDONE: May enhance the adverse/toxic effect of Paliperidone. Management: Additive paliperidone exposure is expected with this combination. Consider using an alternative combination when possible. Consider therapy modification

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy

Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy

Serotonin Modulators: May enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Consider therapy modification

St Johns Wort: May decrease the serum concentration of Paliperidone. Management: Avoid using the 3-month extended-release injectable suspension (Invega Trinza) with inducers of both CYP3A4 and P-glycoprotein during the 3-month dosing interval if possible. If combination is necessary, consider using extended-release tablets. Consider therapy modification

Sulpiride: Antipsychotic Agents may enhance the adverse/toxic effect of Sulpiride. Avoid combination

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination

Valproate Products: May increase the serum concentration of Paliperidone. Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification

Adverse Reactions

Unless otherwise noted, frequency of adverse effects is reported for the oral/IM formulation in adults. Frequency not always defined.

Cardiovascular: Tachycardia (3% to 14%), orthostatic hypotension (2% to 4%; dose dependent), bundle branch block (≤3%)

Central nervous system: Extrapyramidal reaction (adolescents 18% to 40%; adults ≤3% to 26%; dose dependent), drowsiness (adolescents 13% to 26%; adults 4% to 12%; dose dependent), parkinsonian-like syndrome (1% to 18%; dose dependent), akathisia (3% to 17%; dose dependent), headache (6% to 15%), dystonia (1% to 14%; dose dependent), agitation (≤10%), anxiety (≤9%), dizziness (2% to 6%), dysarthria (1% to 4%; dose dependent), fatigue (≤2% to 3%), lethargy (≤3%), sleep disorder (≤3%), tonic-clonic seizures

Dermatologic: Papular rash

Endocrine & metabolic: Increased serum prolactin (males: 42% to 46%; females: 27% to 32%), decreased HDL cholesterol (14%), abnormal triglycerides (5% to 13%), altered serum glucose (4% to 11%), blood cholesterol abnormal (4% to 11%), weight gain (6% to 19%; dose dependent), amenorrhea (≤6%), galactorrhea (≤4%), gynecomastia (≤3%)

Gastrointestinal: Vomiting (≤11%), nausea (4% to 8%), dyspepsia (5% to 6%), sialorrhea (≤6%; dose dependent), constipation (4% to 5%), abdominal pain (≤2% to 4%), increased appetite (2% to 3%), toothache (2% to 3%), xerostomia (2% to 3%), diarrhea (≤3%), swollen tongue (≤3%)

Genitourinary: Urinary tract infection (≤2% to 3%)

Hematologic & oncologic: Change in HDL (15% to 29%), change in LDL (4% to 14%)

Local: Injection site reaction (≤12%)

Neuromuscular & skeletal: Hyperkinesia (2% to 17%; dose dependent), tremor (3% to 12%), dyskinesia (adolescents and adults <1% to 9%), myalgia (≤4%; dose dependent), weakness (≤4%), back pain (1% to 3%), limb pain (≤3%), tongue paralysis (adolescents: ≤3%)

Ophthalmic: Blurred vision (≤3%)

Respiratory: Upper respiratory tract infection (2% to 10%), nasopharyngitis (adolescents and adults 2% to 5%; dose dependent), cough (2% to 3%; dose dependent), rhinitis (1% to 3%; dose dependent)

≤2% (Limited to important or life-threatening): Agranulocytosis, alopecia, anaphylaxis, antiemetic effect, aspiration pneumonia, atrial fibrillation, cerebrovascular accident, convulsions, deep vein thrombosis, diabetes mellitus, diabetic ketoacidosis, edema, epistaxis, erectile dysfunction, first degree atrioventricular block, hyperprolactinemia, hypertension, hypertonia, hypothermia, increased serum ALT, increased serum AST, insomnia, intestinal obstruction, intraoperative floppy iris syndrome, ischemia, jaundice, mania, neck stiffness, neuroleptic malignant syndrome, orthostatic dizziness, pancreatitis, postural orthostatic tachycardia, priapism, psychomotor agitation, pulmonary embolism, retrograde ejaculation, sedation, seizure, SIADH, sinus arrhythmia, sleep apnea, suicidal ideation, syncope, tardive dyskinesia, thrombocytopenia, thrombotic thrombocytopenic purpura, trismus, urinary incontinence, urinary retention, venous thromboembolism

ALERT: U.S. Boxed Warning

Increased mortality in elderly patients with dementia-related psychosis:

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Paliperidone is not approved for the treatment of patients with dementia-related psychosis.

Warnings/Precautions

Concerns related to adverse effects:

• Altered cardiac conduction: May alter cardiac conduction and prolong the QTc interval; life-threatening arrhythmias have occurred with therapeutic doses of antipsychotics. Risk may be increased by conditions or concomitant medications which cause bradycardia, hypokalemia, and/or hypomagnesemia. Avoid use in combination with QTc-prolonging drugs. Avoid use in patients with congenital long QT syndrome and in patients with history of cardiac arrhythmia.

• Antiemetic effects: May mask toxicity of other drugs or conditions (eg, intestinal obstruction, Reye's syndrome, brain tumor) due to antiemetic effects.

• Blood dyscrasias: Leukopenia, neutropenia, and agranulocytosis (sometimes fatal) have been reported in clinical trials and postmarketing reports with antipsychotic use; presence of risk factors (eg, preexisting low WBC or history of drug-induced leuko-/neutropenia) should prompt periodic blood count assessment. Discontinue therapy at first signs of blood dyscrasias or if absolute neutrophil count <1,000/mm3.

• Cerebrovascular effects: An increased incidence of cerebrovascular adverse effects (eg, transient ischemic attack, stroke), including fatalities, has been reported in placebo-controlled trials of risperidone (paliperidone is the primary active metabolite of risperidone) for the unapproved use in elderly patients with dementia-related psychosis.

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

• Dyslipidemia: Increased cholesterol and triglycerides and decreased HDL have been noted. Use with caution in patients with a pre-existing abnormal lipid profile.

• Esophageal dysmotility/aspiration: Antipsychotic use has been associated with esophageal dysmotility and aspiration; use with caution in patients at risk of aspiration pneumonia (eg, Alzheimer disease). Do not use in patients unable to swallow the tablet whole.

• Extrapyramidal symptoms: May cause extrapyramidal symptoms (EPS), including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is generally much lower relative to typical/conventional antipsychotics). Risk of tardive dyskinesia may be increased in the elderly, particularly women. Symptoms may be masked by antipsychotic treatment. Risk of dystonia (and probably other EPS) may be greater with increased doses, use of conventional antipsychotics, males, and younger patients.

• Hyperglycemia: Atypical antipsychotics have been associated with development of hyperglycemia; in some cases, may be extreme and associated with ketoacidosis, hyperosmolar coma, or death. All patients should be monitored for symptoms of hyperglycemia (eg, polydipsia, polyuria, polyphagia, weakness). Use with caution in patients with diabetes (or risk factors) or other disorders of glucose regulation; monitor for worsening of glucose control. Patients with risk factors for diabetes (eg, obesity or family history) should have a baseline fasting blood sugar (FBS) and periodically during treatment.

• Hyperprolactinemia: Use is associated with increased prolactin levels; clinical significance of hyperprolactinemia in patients with breast cancer or other prolactin-dependent tumors is unknown.

• Hypersensitivity: Hypersensitivity reactions, including anaphylactic reactions and angioedema, have been reported.

• Intraoperative floppy iris syndrome (IFIS): Few case reports describe IFIS in patients receiving risperidone and undergoing cataract surgery (Ford, 2011). IFIS has not been reported with paliperidone but caution is advised since it is the active metabolite of risperidone. Prior to cataract surgery, evaluate for prior or current paliperidone or risperidone use. The benefits or risks of interrupting paliperidone or risperidone prior to surgery have not been established; clinicians are advised to proceed with surgery cautiously.

• Neuroleptic malignant syndrome (NMS): Use may be associated with NMS; monitor for mental status changes, fever, muscle rigidity, and/or autonomic instability (risk may be increased in patients with Parkinson disease or Lewy body dementia).

• Orthostatic hypotension: May cause orthostatic hypotension and syncope; use with caution in patients with known cardiovascular disease (heart failure, history of myocardial infarction or ischemia, conduction abnormalities), cerebrovascular disease, or conditions that predispose the patient to hypotension (dehydration, hypovolemia, and treatment with antihypertensive medications).

• Priapism: Rare cases of priapism have been reported.

• Suicidal ideation: The possibility of a suicide attempt is inherent in psychotic illness or bipolar disorder; use with caution in high-risk patients during initiation of therapy. Prescriptions should be written for the smallest quantity consistent with good patient care.

• Temperature regulation: Impaired core body temperature regulation may occur; caution with strenuous exercise, heat exposure, dehydration, and concomitant medication possessing anticholinergic effects.

• Weight gain: Significant weight gain has been observed with antipsychotic therapy; incidence varies with product. Monitor waist circumference and BMI.

Disease-related concerns:

• Dementia: [US Boxed Warning]: Elderly patients with dementia-related psychosis treated with antipsychotics are at an increased risk of death compared to placebo. Most deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Paliperidone is not approved for the treatment of dementia-related psychosis. In addition, patients with Lewy body dementia (LBD) may be more sensitive to CNS-related and extrapyramidal effects.

• Parkinson disease: Use with caution in patients with Parkinson disease; may be more sensitive to CNS-related and extrapyramidal effects.

• Renal impairment: Use with caution in patients with mild renal disease; dosage reduction is recommended. Not recommended in patients with moderate to severe impairment.

• Seizures: Use with caution in patients at risk of seizures, including those with a history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. Elderly patients may be at increased risk of seizures due to an increased prevalence of predisposing factors.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Elderly: Use in patients with dementia is associated with an increased risk of mortality and cerebrovascular accidents; avoid antipsychotic use for behavioral problems associated with dementia unless alternative nonpharmacologic therapies have failed and patient may harm self or others. Paliperidone is not approved for the treatment of dementia-related psychosis. In addition, use may cause or exacerbate syndrome of inappropriate antidiuretic hormone secretion or hyponatremia; monitor sodium closely with initiation or dosage adjustments in older adults (Beers Criteria).

Dosage form specific issues:

• Extended-release tablet: Use is not recommended in patients with preexisting severe gastrointestinal narrowing disorders (nondeformable controlled release formulation). Patients with upper GI tract alterations in transit time may have increased or decreased bioavailability of paliperidone. Formulation consists of drug within a nonabsorbable shell; following drug release/absorption, the shell is expelled in the stool.

Monitoring Parameters

Mental status; vital signs (as clinically indicated); blood pressure (baseline; repeat 3 months after antipsychotic initiation, then yearly); weight, height, BMI, waist circumference (baseline; repeat at 4, 8, and 12 weeks after initiating or changing therapy, then quarterly; consider switching to a different antipsychotic for a weight gain ≥5% of initial weight); CBC (as clinically indicated; monitor frequently during the first few months of therapy in patients with preexisting low WBC or history of drug-induced leukopenia/neutropenia); electrolytes, renal and liver function (annually and as clinically indicated); personal and family history of obesity, diabetes, dyslipidemia, hypertension, or cardiovascular disease (baseline; repeat annually); fasting plasma glucose level/HbA1c (baseline; repeat 3 months after starting antipsychotic, then yearly); fasting lipid panel (baseline; repeat 3 months after initiation of antipsychotic; if LDL level is normal repeat at 2-5 year intervals or more frequently if clinical indicated); changes in menstruation, libido, development of galactorrhea, erectile and ejaculatory function (at each visit for the first 12 weeks after the antipsychotic is initiated or until the dose is stable, then yearly); abnormal involuntary movements or parkinsonian signs (baseline; repeat weekly until dose stabilized for at least 2 weeks after introduction and for 2 weeks after any significant dose increase); tardive dyskinesia (every 12 months; high-risk patients every 6 months); ocular examination (yearly in patients >40 years; every 2 years in younger patients) (ADA, 2004; Lehman, 2004; Marder, 2004).

Pregnancy Risk Factor

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Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. Antipsychotic use during the third trimester of pregnancy has a risk for extrapyramidal symptoms (EPS) and/or withdrawal symptoms in newborns following delivery. Symptoms in the newborn may include agitation, feeding disorder, hypertonia, hypotonia, respiratory distress, somnolence, and tremor. These effects may be self-limiting and allow recovery within hours or days with no specific treatment, or they may be severe requiring prolonged hospitalization.

Paliperidone may cause hyperprolactinemia, which may decrease reproductive function in both males and females. Paliperidone is the active metabolite of risperidone; refer to Risperidone monograph for additional information.

The ACOG recommends that therapy during pregnancy be individualized; treatment with psychiatric medications during pregnancy should incorporate the clinical expertise of the mental health clinician, obstetrician, primary healthcare provider, and pediatrician. Safety data related to atypical antipsychotics during pregnancy is limited and routine use is not recommended. However, if a woman is inadvertently exposed to an atypical antipsychotic while pregnant, continuing therapy may be preferable to switching to a typical antipsychotic that the fetus has not yet been exposed to; consider risk:benefit (ACOG, 2008).

Healthcare providers are encouraged to enroll women 18 to 45 years of age exposed to paliperidone during pregnancy in the Atypical Antipsychotics Pregnancy Registry (1-866-961-2388 or http://www.womensmentalhealth.org/pregnancyregistry).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache, weight gain, constipation, fatigue, nausea, rhinitis, pharyngitis, akathisia, asthenia, or tablet shell in stool. Have patient report immediately to prescriber severe injection site irritation, signs of hyperglycemia, strength differences from one side to another, difficulty speaking or thinking, change in balance, blurred vision, suicidal ideation, angina, tachycardia, considerable dizziness, syncope, arrhythmia, behavioral changes, mood changes, tremors, difficulty moving, rigidity, bradycardia, dysphagia, difficulty focusing, vision changes, dyspnea, sialorrhea, ecchymosis, hemorrhaging, involuntary eye movements, macromastia, sexual dysfunction, nipple discharge, amenorrhea, priapism, signs of neuroleptic malignant syndrome, or signs of tardive dyskinesia (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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