Medical term:
Invega
paliperidone
paliperidone palmitate
Pharmacologic class: Benzisoxazole derivative
Therapeutic class: Antipsychotic
Pregnancy risk category C
FDA Box Warning
• Elderly patients with dementia-related psychosis are at increased risk for death. Over course of 10-week controlled trial, death rate in drug-treated patients was about 4.5%, compared to about 2.6% in placebo group. Although causes of death varied, most appeared to be cardiovascular or infectious. Don't give drug to patients with dementia-related psychosis.
Action
Unknown. In schizophrenia, therapeutic activity may be mediated through combination of central serotonin2-and dopamine2-receptor antagonism. Drug is a major active metabolite of risperidone.
Availability
Injection (paliperidone palmitate): 39 mg, 78 mg, 117 mg, 156 mg, 234 mg in prefilled syringes
Tablets (extended-release): 1.5 mg, 3 mg, 6 mg, 9 mg
Indications and dosages
➣ Schizophrenia
Adults: 6 mg P.O. once daily. Some patients may benefit from daily dosages as high as 12 mg or as low as 3 mg. If indicated, increase in increments of 3 mg/day at intervals of more than 5 days. Or initially, 234 mg I.M. (paliperidone palmitate) on treatment day 1 and 156 mg I.M. 1 week later. Recommended monthly maintenance dose is 117 mg; some patients may benefit from lower or higher maintenance doses within recommended range of 39 to 234 mg. Adjustment of maintenance dosage may be made monthly. When making dosage adjustments, consider paliperidone palmitate's prolonged-release characteristics, as the full effect of the dosage adjustment may not be evident for several months.
Adolescents ages 12 to 17 weighing 51 kg (112 lb) or more: 3 mg P.O. daily; increase dosage, if necessary, only after clinical reassessment at increments of 3 mg/day at intervals of more than 5 days up to a maximum of 12 mg/day.
Adolescents ages 12 to 17 weighing less than 51 kg (112 lb): 3 mg P.O. daily; increase dosage, if necessary, only after clinical reassessment at increments of 3 mg/day at intervals of more than 5 days up to a maximum of 6 mg/day.
➣ Schizoaffective disorder
Adults: 6 mg P.O. once daily. Some patients may benefit from dosages as high as 12 mg or as low as 3 mg. Maximum recommended dosage is 12 mg/day.
Dosage adjustment
• Renal impairment
Contraindications
• Hypersensitivity to drug, its components, or risperidone
Precautions
Use cautiously in:
• GI strictures (use should be avoided), cardiovascular or cerebrovascular disease, diabetes mellitus, Parkinson's disease, or conditions that raise body temperature (such as exercise, exposure to extreme heat, and concomitant anticholinergics use)
• increased risk of hypotension (as from dehydration, hypovolemia, or antihypertensives), aspiration pneumonia, or suicide attempt
• increased risk of metabolic changes (including hyperglycemia, dyslipidemia, weight gain)
• concurrent use of other drugs that are centrally acting or prolong the QT interval (use should be avoided)
• history of seizures or breast cancer
• elderly patients with dementia-related psychosis
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).
Administration
• Give tablets in morning with or without food.
• Administer tablets whole. Ensure that patient doesn't chew, divide, or crush them.
☞ Administer paliperidone palmitate by deep I.M. injection only as a single injection. Don't give in divided injections. Don't administer I.V. or subcutaneously.
☞ For first and second I.M. doses, give in the deltoid muscle using 1½-inch 22G needle for patients 90 kg (198 lb) or more or 1-inch 23G needle for patients less than 90 kg. After the second dose, monthly maintenance doses may be given in either the deltoid or gluteal muscle. For gluteal injection, use 1½-inch 22G needle regardless of patient weight.
Adverse reactions
CNS: dizziness, headache, akathisia, tardive dyskinesia, dystonia, extrapyramidal disorder, hypertonia, parkinsonism, sedation, somnolence, tremor, anxiety, asthenia, fatigue, seizure, stroke (in elderly patients with dementia-related psychosis), neuroleptic malignant syndrome (NMS)
CV: first-degree atrioventricular block, bundle-branch block, sinus arrhythmia, tachycardia, hypertension, orthostatic hypotension, prolonged QT interval, abnormal T wave, palpitations
EENT: blurred vision
GI: upper abdominal pain, dyspepsia, nausea, antiemetic effect, esophageal dysmotility, salivary hypersecretion, dry mouth
GU: hyperprolactinemia
Hematologic: leukopenia, neutropenia, agranulocytosis
Musculoskeletal: back pain, extremity pain
Respiratory: cough, dyspnea, aspiration pneumonia
Other: fever, weight gain, possible drug tolerance or dependency
Interactions
Drug-drug. Antihypertensives: increased risk of hypotension Centrally acting drugs with sedative effect: increased sedation Class IA antiarrhythmics (such as procainamide, quinidine), Class III antiarrhythmics (such as amiodarone, sotalol), anti-infectives (such as gatifloxacin, moxifloxacin), other antipsychotics (such as chlorpromazine, thioridazine), other drugs that prolong the QT interval: increased risk of prolonged QT interval
Dopamine agonists (such as levodopa): antagonized effects of these drugs
Drug-diagnostic tests. Blood glucose, serum prolactin: increased levels Granulocytes, leukocytes, neutrophils: decreased counts
Drug-food. Any food: possibly increased paliperidone effects
Drug-behaviors. Alcohol use: increased sedation
Patient monitoring
• Closely monitor patient at risk for suicide attempts.
• Monitor patient with diabetes regularly for signs and symptoms of worsening glycemic control.
• Stay alert for orthostatic hypotension.
☞ Monitor patient for signs and symptoms of NMS (extremely high fever, muscle rigidity, altered mental status, irregular pulse or blood pressure, tachycardia, diaphoresis, arrhythmias). Immediately discontinue drug and take appropriate measures if NMS occurs.
☞ Closely monitor CBC with differential, especially during first few months of therapy; discontinue drug if severe neutropenia occurs.
• Consider discontinuing drug if tardive dyskinesia occurs.
• Watch for signs and symptoms of drug tolerance, dependency, and abuse.
Patient teaching
• Inform patient he may take drug with or without food.
• Teach patient to take tablets whole and not to chew, divide, or crush them.
• Inform patient that tablet shell doesn't dissolve and may look like a complete tablet in stool.
☞ Instruct patient to immediately discontinue drug and report signs or symptoms of NMS (such as high fever, muscle rigidity, altered mental status, irregular pulse or blood pressure, fast heart rate, or excessive sweating).
• Instruct patient to report fever or other signs and symptoms of infection.
• Tell patient drug may cause temporary blood pressure decrease if he stands or sits up suddenly. Instruct him to rise slowly and carefully.
• Advise patient to take precautions against dehydration and overheating.
• Caution patient not to consume alcohol during therapy.
• Caution patient to avoid hazardous activities until drug's effects on concentration, coordination, vision, and alertness are known.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.
paliperidone
(pa-li-per-i-done) ,Invega
(trade name),Invega Sustenna
(trade name)Classification
Therapeutic: antipsychoticsPharmacologic: benzisoxazoles
Indications
Action
Therapeutic effects
Pharmacokinetics
Time/action profile (blood levels)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO | unknown | 24 hr | 24 hr |
| IM | unknown | 13 days | 1 mo |
Contraindications/Precautions
Adverse Reactions/Side Effects
Central nervous system
- neuroleptic malignant syndrome (life-threatening)
- suicidal thoughts (life-threatening)
- drowsiness (most frequent)
- extrapyramidal disorders (dose related) (most frequent)
- headache (most frequent)
- insomnia (most frequent)
- anxiety
- confusion
- dizziness
- dysarthria
- fatigue
- syncope
- tardive dyskinesia
- weakness
Ear, Eye, Nose, Throat
- blurred vision
Respiratory
- dyspnea (most frequent)
- cough
Cardiovascular
- palpitations (most frequent)
- tachycardia (dose related) (most frequent)
- bradycardia
- orthostatic hypotension
- QTc interval prolongation
Gastrointestinal
- abdominal pain (most frequent)
- dry mouth
- dyspepsia
- nausea
- swollen tongue
Genitourinary
- impotence
- priapism
Endocrinologic
- amenorrhea
- dyslipidemia
- galactorrhea
- gynecomastia
- hyperglycemia
- weight gain
Hematologic
- agranulocytosis (life-threatening)
- leukopenia
- neutropenia
Musculoskeletal
- back pain
- dystonia (dose related)
Neurologic
- akathisia
- dyskinesia
- tremor (dose related)
Miscellaneous
- fever
Interactions
Drug-Drug interaction
↑ 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.Carbamazepine may ↓ levels/effects.Route/Dosage
Schizophrenia
Renal Impairment
Oral (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
Intramuscular (Adults) CCr 50–79 mL/min—156 mg initially, then 117 mg one week later; continue with monthly maintenance dose of 78 mg; CCr <50 mL/min—Contraindicated.Schizoaffective Disorder
Renal Impairment
Oral (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.Availability
Nursing implications
Nursing 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.
- Monitor BP (sitting, standing, lying down) and pulse before and periodically during therapy. May cause prolonged QT interval, tachycardia, and orthostatic hypotension.
- 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, respiratory distress, tachycardia, seizures, diaphoresis, hypertension or hypotension, 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).
- Lab Test Considerations: Monitor fasting blood glucose and cholesterol levels before and periodically during therapy.
- Monitor serum prolactin prior to and periodically during therapy. May cause ↑ serum prolactin levels.
- Monitor CBC frequently during initial months of therapy in patients with pre-existing or history of low WBC. May cause leukopenia, neutropenia, or agranulocytosis. Discontinue therapy if this occurs.
Potential Nursing Diagnoses
Risk for self-directed violence (Indications, Adverse Reactions)Disturbed sensory perception (specify: visual, auditory, kinesthetic, gustatory, tactile, olfactory) (Indications)
Implementation
- Oral: Administer once daily in the morning without regard to food. Tablets should be swallowed whole; do not crush, break or chew.
- Intramuscular: Administer initial and second doses in deltoid using a 1 1/2-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 1 1/2-inch, 22 gauge needle regardless of patient weight. To avoid missed dose, may give second dose 4 days before or after the 1-wk timepoint. Monthly doses may be given up to 7 days before or after the monthly timepoint. After 1st month, 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 first 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 second 156 mg dose in deltoid in 1 wk, followed by monthly doses in deltoid or gluteal sites. If > 7 months since scheduled dose, administer using initial dosing schedule. During regular monthly dose schedule, if <6 wks since last injection, administer previously stabilized dose as soon as possible, then monthly. If >6 wks since last injection, resume dose previously stabilized on, unless stabilized on 234 mg (then 1st two injections should be 156 mg). Administer 1 dose in deltoid as soon as possible, then another deltoid injection of same dose 1 wk later, then resume regular monthly schedule. If >6 months since last injection, administer using initial dosing schedule.
Patient/Family Teaching
- Instruct patient to take medication as directed. Advise patient that appearance of tablets in stool is normal and not of concern.
- Inform patient of the possibility of extrapyramidal symptoms. Instruct patient to report these symptoms immediately to health care professional.
- Advise patient to change positions slowly to minimize orthostatic hypotension.
- May cause drowsiness. 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 increase in activity and talking, 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 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.
- Advise female patients to notify health care professional if pregnancy is planned or suspected, or if breast feeding or planning to breast feed.
- Emphasize the importance of routine follow-up exams to monitor side effects and continued participation in psychotherapy to improve coping skills.
Evaluation/Desired Outcomes
- Decrease in excited, manic behavior.
- Decrease in positive symptoms (delusions, hallucinations) of schizophrenia.
- Decrease in negative symptoms (social withdrawal, flat, blunted affect) of schizophrenia.
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