paliperidone

ROUTE	ONSET	PEAK	DURATION
PO	unknown	24 hr	24 hr
IM—Erzofri	unknown	16–28 days	1 mo
IM—Sustenna	unknown	13 days	1 mo
IM—Trinza	unknown	30–33 days	3 mo
IM—Hafyera	unknown	29–32 days	6 mo

Contraindicated in:

Hypersensitivity to paliperidone or risperidone;
Concurrent use of drugs known to cause QT interval prolongation (including quinidine, procainamide, sotalol, amiodarone, chlorpromazine, thioridazine, moxifloxacin);
History of congenital QTc prolongation or other cardiac arrhythmias;
Bradycardia, hypokalemia, hypomagnesemia (↑ risk of QTc prolongation);
Pre-existing severe GI narrowing (due to nature of tablet formulation);
CCr <50 mL/min (for IM).

Use Cautiously in:

Patients with Parkinson's disease or dementia with Lewy bodies (↑ sensitivity to effects of antipsychotics);
History of suicide attempt;
History of HF, MI, conduction abnormalities, stroke, TIA (↑ risk of orthostatic hypotension and syncope);
Patients at risk for aspiration pneumonia or falls;
History of seizures;
Conditions that may ↑ body temperature (strenuous exercise, exposure to extreme heat, concurrent anticholinergics or risk of dehydration);
↓GI transit time (may ↑ blood levels);
May mask symptoms of some drug overdoses, intestinal obstruction, Reye syndrome, or brain tumor (due to antiemetic effect);
Diabetes mellitus;
Severe hepatic impairment;
Renal impairment (dose ↓ recommended if CCr <80 mL/min);
Low white blood cell count/absolute neutrophil count or history of drug-induced leukopenia/neutropenia (↑ risk of leukopenia/neutropenia);
OB: Neonates at risk for extrapyramidal symptoms and withdrawal after delivery when exposed during the 3rd trimester; use only if maternal benefit outweighs fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Children 12 yr (safety and effectiveness not established);
Geri: Appears on Beers list. risk of stroke, cognitive decline, and mortality in older adults with dementia. Avoid use in older adults, except for schizophrenia.

Adv. Reactions/Side Effects ⬆ ⬇

CV: palpitations, tachycardia (dose related), bradycardia, orthostatic hypotension, QT interval prolongation

EENT: blurred vision

Endo: galactorrhea, gynecomastia, hyperglycemia

GI: abdominal pain, dry mouth, dyspepsia, nausea, swollen tongue

GU: ↓fertility (females), amenorrhea, impotence, priapism

Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia

Metab: dyslipidemia, weight gain

MS: back pain, dystonia (dose related)

Neuro: drowsiness, extrapyramidal disorders (dose related), headache, insomnia, akathisia, anxiety, confusion, dizziness, dysarthria, fatigue, NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES, syncope, tardive dyskinesia, tremor (dose related), weakness

Resp: dyspnea, cough

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

↑risk of CNS depression with other CNS depressants, including alcohol, antihistamines, sedative/hypnotics, or opioid analgesics.
May antagonize the effects of levodopa or other dopamine agonists.
↑risk of orthostatic hypotension with antihypertensives, nitrates, or other agents that lower BP.
Strong CYP3A4 inducers or strong P-glycoprotein inducers, including carbamazepine or rifampin, may ↓ levels/effects; avoid concurrent use with Invega Sustenna; if use of strong CYP3A4 or P-glycoprotein inducer necessary, consider using paliperidone tablets.
Valproic acid may ↑ levels; may need to ↓ dose of paliperidone.

Drug-Natural Products:

St. John's wort may ↓ levels/effects; avoid concurrent use with Invega Sustenna.

Route/Dosage ⬆ ⬇

Schizophrenia

PO (Adults ): 6 mg once daily; may titrate by 3 mg/day at intervals of at least 5 days (range 3–12 mg/day).
PO (Children 12–17 yr): 3 mg once daily; may titrate by 3 mg/day at intervals of at least 5 days (not to exceed 6 mg if <51 kg or 12 mg if ≥51 kg).
IM (Adults ): Erzofri: 351 mg initially, then 117 mg 4 wk later; continue with monthly maintenance dose of 117 mg (range of 39–234 mg based on efficacy and/or tolerability);Invega Sustenna: 234 mg initially, then 156 mg 1 wk later; continue with monthly maintenance dose of 117 mg (range of 39–234 mg based on efficacy and/or tolerability); Invega Trinza: Dose should be based on dose of previous 1-mo injection dose of Invega Sustenna. If last dose of Invega Sustenna was 78 mg: Administer 273 mg of Invega Trinza every 3 mo. If last dose of Invega Sustenna was 117 mg: Administer 410 mg of Invega Trinza every 3 mo. If last dose of Invega Sustenna was 156 mg: Administer 546 mg of Invega Trinza every 3 mo. If last dose of Invega Sustenna was 234 mg: Administer 819 mg of Invega Trinza every 3 mo. May adjust dose based on efficacy and/or tolerability (range: 273–819 mg). Invega Hafyera: Dose should be based on dose of previous 1-mo injection dose of Invega Sustenna or previous every 3-mo dose of Invega Trinza. If last dose of Invega Sustenna was 156 mg: Administer 1,092 mg of Invega Hafyera every 6 mo. If last dose of Invega Sustenna was 234 mg: Administer 1,560 mg of Invega Hafyera every 6 mo. If last dose of Invega Trinza was 546 mg: Administer 1,092 mg of Invega Hafyera every 6 mo. If last dose of Invega Trinza was 819 mg: Administer 1,560 mg of Invega Hafyera every 6 mo.

Renal Impairment

PO (Adults ): CCr 50–79 mL/min: 3 mg/day initially; dose may be ↑ to maximum of 6 mg/day; CCr 10–<50 mL/min: 1.5 mg/day initially; dose may be ↑ to maximum of 3 mg/day.

Renal Impairment

IM (Adults ): CCr 50–79 mL/min:Erzofri: 234 mg initially, then 78 mg 4 wk later; continue with monthly maintenance dose of 78 mg (range of 39–156 mg based on efficacy and/or tolerability); Invega Sustenna: 156 mg initially, then 117 mg 1 wk later; continue with monthly maintenance dose of 78 mg (range of 39–156 mg based on efficacy and/or tolerability); Invega Trinza: once stabilized on Invega Sustenna, can then transition to appropriate dose of Invega Trinza (see above); CCr <50 mL/min: Use not recommended.

Schizoaffective Disorder

PO (Adults ): 6 mg/day; may titrate by 3 mg/day at intervals of at least 4 days (range 3–12 mg/day).
IM (Adults ): Erzofri: 351 mg initially, then 78–234 mg 4 wk later; continue with monthly maintenance dose of 78–234 mg (range based on efficacy and/or tolerability); Invega Sustenna: 234 mg initially, then 156 mg 1 wk later; continue with monthly maintenance dose of 78–234 mg (range based on efficacy and/or tolerability);

Renal Impairment

PO (Adults ): CCr 50–79 mL/min: 3 mg/day initially; dose may be ↑ to maximum of 6 mg/day; CCr 10–<50 mL/min: 1.5 mg/day initially; dose may be ↑ to maximum of 3 mg/day.

Renal Impairment

IM (Adults ): CCr 50–79 mL/min:Erzofri: 234 mg initially, then 78 mg 4 wk later; continue with monthly maintenance dose of 78 mg (range of 39–156 mg based on efficacy and/or tolerability); Invega Sustenna: 156 mg initially, then 117 mg 1 wk later; continue with monthly maintenance dose of 78 mg (range of 39–156 mg based on efficacy and/or tolerability); CCr <50 mL/min: Use not recommended.

Availability ⬆ ⬇

(Generic available)

Extended-release tablets (Invega): 1.5 mg; 3 mg; 6 mg; 9 mg
Extended-release intramuscular injection (Erzofri): 39 mg/0.25 mL; 78 mg/0.5 mL; 117 mg/0.75 mL; 156 mg/mL; 234 mg/1.5 mL; 351 mg/2.25 mL
Extended-release intramuscular injection (Invega Sustenna): 39 mg/0.25 mL; 50 mg/0.5 mL; 75 mg/0.75 mL; 78 mg/0.5 mL; 100 mg/mL; 117 mg/0.75 mL; 150 mg/1.5 mL; 156 mg/mL; 234 mg/1.5 mL
Extended-release intramuscular injection (Invega Trinza): 175 mg/0.875 mL; 263 mg/1.315 mL; 273 mg/0.875 mL; 350 mg/1.75 mL; 410 mg/1.315 mL; 525 mg/2.625 mL; 546 mg/1.75 mL; 819 mg/2.625 mL
Extended-release intramuscular injection (Invega Hafyera): 1,092 mg/3.5 mL; 1,560 mg/5 mL

Assessment ⬆ ⬇

Monitor patient’s mental status (orientation, mood, behavior) before and periodically during therapy. Monitor closely for notable changes in behavior that could indicate the emergence or worsening of suicidal thoughts or behavior or depression, especially during early therapy. Restrict amount of drug available to patient.
Assess weight and BMI initially and throughout therapy. Refer as appropriate for nutritional/weight and medical management.
Obtain ECG at baseline. Monitor orthostatic BP (sitting, standing, lying down) and HR before and periodically during therapy. May cause prolonged QT interval, tachycardia, hypertension, and orthostatic hypotension. Protect patient from falls.
Monitor for signs and symptoms of hyperglycemia such as polydipsia, polyuria, polyphagia, nausea, and weakness during treatment.
Observe patient when administering medication to ensure that medication is actually swallowed and not hoarded or cheeked.
Monitor patient for onset of extrapyramidal side effects (akathisia: restlessness; dystonia: muscle spasms and twisting motions; or pseudoparkinsonism: mask-like face, rigidity, tremors, drooling, shuffling gait, dysphagia). Report these symptoms; reduction of dose or discontinuation of medication may be necessary.
Monitor for tardive dyskinesia (involuntary rhythmic movement of mouth, face, and extremities). Report immediately; may be irreversible.
Monitor for development of neuroleptic malignant syndrome (fever, muscle rigidity, delirium, respiratory distress, tachycardia, seizures, diaphoresis, hypertension or hypotension, cardiac arrhythmia, pallor, tiredness). Discontinue paliperidone and notify health care professional immediately if these symptoms occur.
Monitor for symptoms related to hyperprolactinemia (menstrual abnormalities, galactorrhea, sexual dysfunction, changes in libido, erectile or ejaculatory dysfunction).
Assess for falls risk. Drowsiness, orthostatic hypotension, and motor and sensory instability ↑ risk. Institute prevention if indicated.

Lab Test Considerations:

Monitor fasting blood glucose at baseline, at wk 12, and annually in all patients; monitor more frequently for patients with risk factors for diabetes mellitus; patients with diabetes should be closely monitored for worsening glucose control.
- Monitor cholesterol levels at baseline, at wk 12, and every 5 yr thereafter.
- Monitor serum prolactin prior to and periodically during therapy. May cause ↑ serum prolactin levels.
- Monitor CBC frequently during initial mo of therapy in patients with pre-existing or history of low WBC. May cause leukopenia, neutropenia, or agranulocytosis. Discontinue therapy if this occurs.

Implementation ⬆ ⬇

Do not confuse Invega Sustenna with Invega Trinza. Do no confuse Invega with Intuniv.
PO: Administer once daily in the morning without regard to food. DNC: Tablets should be swallowed whole; do not crush, break, or chew.
IM: Erzofri: Prior to administration, shake the prefilled syringe vigorously for ≥10 sec within 5 min prior to administration to ensure a homogeneous suspension. Administer as a single injection; do not administer as a divided injection; use only the needles provided within the dose kit. Administer initial and 2nd doses in deltoid using a 1½-inch 22-gauge needle for patients ≥90 kg (≥200 lb) or 1-inch 23-gauge needle for patients <90 kg (<200 lb). Monthly maintenance doses can be administered in either deltoid or gluteal sites. For gluteal injection, use 1½-inch 22-gauge needle regardless of patient weight. Monthly doses may be given up to 7 days before or after the monthly time point. After 1st mo, if missed dose is within 4–6 wk of scheduled dose,resume regular monthly dosing as soon as possible at the patient's previously stabilized dose, followed by return to normal monthly injections in either deltoid or gluteal muscle. If > 6 wk–6 mo since 1st injection,resume at same dose the patient was previously stabilized on (unless patient was stabilized on a dose of 234 mg—then the first 2 injections should be 156 mg each). Administer a deltoid injection as soon as possible, administer a second deltoid injection 1 wk later at the same dose, and thereafter resume previously stabilized dose 1 mo after the second injection in deltoid or gluteal sites. If >6 mo since scheduled dose, restart dosing with initial dose of 351 mg deltoid injection on day 1 and thereafter resume previously stabilized dose 1 mo after the initial injection.
IM: Invega Sustenna: Administer initial and 2nd doses in deltoid using a 1½-inch 22-gauge needle for patients ≥90 kg (≥200 lb) or 1-inch 23-gauge needle for patients <90 kg (<200 lb). Monthly maintenance doses can be administered in either deltoid or gluteal sites. For gluteal injection, use 1½-inch 22-gauge needle regardless of patient weight. To avoid missed dose, may give 2nd dose 4 days before or after the 1-wk time point. Monthly doses may be given up to 7 days before or after the monthly time point. After 1st mo, if missed dose is within 4 wk of scheduled dose, administer 2nd dose of 156 mg as soon as possible. Give 3rd dose of 117 mg in either deltoid or gluteal muscle 5 wk after 1st injection (regardless of timing of 2nd injection). Then return to normal monthly injections in either deltoid or gluteal muscle. If >4 wk and <7 wk since 1st injection, resume by administering 156 mg dose in deltoid as soon as possible, a 2nd 156 mg dose in deltoid in 1 wk, followed by monthly doses in deltoid or gluteal sites. If >7 mo since scheduled dose, administer using initial dosing schedule. During regular monthly dose schedule, if <6 wk since last injection, administer previously stabilized dose as soon as possible, then monthly. If >6 wk since last injection, resume dose previously stabilized on, unless stabilized on 234 mg (then 1st two injections should be 156 mg). Administer one dose in deltoid as soon as possible, then another deltoid injection of same dose 1 wk later; then resume regular monthly schedule. If >6 mo since last injection, administer using initial dosing schedule.
IM: Invega Trinza: Use only after ≥4 mo of monthly Invega Sustenna therapy. Prior to administration, shake the prefilled syringe vigorously for ≥15 sec within 5 min prior to administration to ensure a homogeneous suspension. Deltoid injection: For patients weighing <90 kg, use the 1-inch 22-gauge thin wall needle. For patients weighing ≥90 kg, use the 1½-inch 22-gauge thin wall needle. Gluteal injection: Regardless of patient weight, use 1½-inch 22-gauge thin wall needle. Initiate Invega Trinza when next 1-mo paliperidone dose is scheduled. Avoid missed doses; dose may be given 2 wk before or after 3 mo scheduled dose. If more than 3½ mo (up to but <4 mo) since last dose, administer previously administered dose as soon as possible; then continue with 3-mo injections. If 4 mo up to and including 9 mo since last dose, do NOT administer next dose. If last dose was 273 mg, administer 2 doses of 78 mg of Invega Sustenna one wk apart into deltoid muscle, then one dose of Invega Trinza 273 mg 1 mo after 2nd dose of Invega Sustenna. If last dose was 410 mg, administer 2 doses of 117 mg of Invega Sustenna 1 wk apart into deltoid muscle, then one dose of Invega Trinza 410 mg 1 mo after 2nd dose of Invega Sustenna. If last dose was 819 mg, administer 2 doses of 156 mg of Invega Sustenna 1 wk apart into deltoid muscle, then one dose of Invega Trinza 819 mg 1 mo after 2nd dose of Invega Sustenna. If >9 mo have elapsed since last injection of Invega Trinza, reinitiate treatment with Invega Sustenna. Then resume Invega Trinza after at least 4 mo of Invega Sustenna.
IM: Invega Hafyera must be administered as a gluteal IM injection by a health care professional once every 6 mo. After shaking, solution is uniform, thick, and milky white; do not inject if discolored or contains particulate matter. Do not use needles from Invega Sustenna or Invega Trinza; may develop blockage. Begin Invega Hafyera only after therapy has been established with either once-a-month Invega Sustenna for ≥4 mo OR every-3-mo Invega Trinza for at least one 3-mo injection cycle. Begin within 1 wk before or after next scheduled dose for Invega Sustenna or 2 wk before or after Invega Trinza dose. May give Invega Hafyera injection up to 2 wk before or 3 wk after the scheduled 6-mo dose to avoid a missed dose. If >6 mo and 3 wk but <8 mo since last dose of Invega Hafyera, restart with Invega Sustenna. If last dose of Invega Hafyera was 1092 mg, administer Invega Sustenna 156 mg into deltoid muscle on Day 1. Then 1 mo after Day 1, administer Invega Hafyera 1092 mg into gluteal muscle. If last dose of Invega Hafyera was 1560 mg, administer Invega Sustenna 234 mg into deltoid muscle on Day 1. Then 1 mo after Day 1, administer Invega Hafyera 1560 mg into gluteal muscle. If 8 mo up to and including 11 mo since last dose of Invega Hafyera, restart with Invega Sustenna. If last dose of Invega Hafyera was 1092 mg, administer Invega Sustenna 156 mg into deltoid muscle on Day 1 and 156 mg on Day 8. Then 1 mo after Day 8, administer Invega Hafyera 1092 mg into gluteal muscle. If last dose of Invega Hafyera was 1560 mg, administer Invega Sustenna 156 mg into deltoid muscle on Day 1 and 156 mg on Day 8. Then 1 mo after Day 1, administer Invega Hafyera 1560 mg into gluteal muscle. If >11 mo since the last dose of Invega Hafyera, restart therapy with Invega Sustenna. Invega Hafyera can be resumed after therapy with Invega Sustenna for at least 4 mo.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of paliperidone to patient. Instruct them to take medication as directed. Do not share medication with others, even if they have similar symptoms; may be harmful. Keep out of children's reach. Appearance of tablets in stool is normal and not of concern. Advise patient to read Patient Informationbefore starting and with each Rx refill in case of changes.
Emphasize the importance of routine follow-up exams and lab tests to monitor side effects and continued participation in psychotherapy to improve coping skills.
Inform patient of the possibility of extrapyramidal symptoms, neuroleptic malignant syndrome, and tardive dyskinesia. Instruct patient to report these symptoms immediately to health care professional.
Instruct patients with diabetes to monitor blood glucose more closely; advise patients without diabetes of symptoms of high blood glucose such as ↑ thirst, hunger, and urination.
Advise patient to change positions slowly to minimize orthostatic hypotension. Protect from falls.
May cause drowsiness and dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient and family to notify health care professional if thoughts about suicide or dying, attempts to commit suicide, new or worse depression, new or worse anxiety, feeling very agitated or restless, panic attacks, trouble sleeping, new or worse irritability, acting aggressive, being angry or violent, acting on dangerous impulses, an extreme ↑ in activity and talking, or other unusual changes in behavior or mood occur.
Advise patient that extremes in temperature should also be avoided; this drug impairs body temperature regulation.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's wort and alcohol.
Advise patient to seek nutritional, weight, or medical management as needed for weight gain or cholesterol elevation.
Instruct patient to notify health care professional promptly if sore throat, fever, unusual bleeding or bruising, rash, tremors, menstrual abnormalities, galactorrhea, or sexual dysfunction occur.
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Encourage women who become pregnant while taking paliperidone to enroll in the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/. Monitor neonates for extrapyramidal and/or withdrawal symptoms (agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, feeding disorder) and manage symptoms appropriately. Monitor infants exposed to paliperidone through breast milk for excess sedation, failure to thrive, jitteriness, and extrapyramidal symptoms (tremors and abnormal muscle movements). May temporarily cause female infertility.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆