Paliperidone palmitate

What is Paliperidone palmitate?

• Paliperidone palmitate (Invega Hafyera; Invega Sustenna; Invega Trinza) is an atypical antipsychotic.

What are the uses of this medicine?

Invega Sustenna® is a prescription medicine given by injection by a healthcare professional and used to treat:

• schizophrenia in adults
• schizoaffective disorder in adults either alone or with other medicines such as mood stabilizers or antidepressants

• Invega Trinza is a prescription medicine given by injection by a healthcare professional and used to treat schizophrenia.
• Invega Trinza is used in people who have been treated with Invega Sustenna 1 time a month injections for at least 4 months.

Invega Hafyera is a prescription medicine given by injection by a healthcare provider 1 time every 6 months and used for the treatment of schizophrenia in adults who have been adequately treated with either:

• A 1 time each month paliperidone palmitate extended-release injectable suspension for at least 4 months.
• A 1 time every 3 months paliperidone palmitate extended-release injectable suspension for at least 3 months.

How does this medicine work?

• Paliperidone palmitate is hydrolyzed to paliperidone.
• Paliperidone is the major active metabolite of risperidone.
• The mechanism of action of paliperidone is unclear.
• However, its efficacy in the treatment of schizophrenia could be mediated through a combination of central dopamine D2 and serotonin 5HT2A receptor antagonism.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergic to paliperidone, paliperidone palmitate, risperidone, or any of the ingredients.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Especially tell your doctor if you take:

• other antipsychotic medications such as chlorpromazine, risperidone (Perseris Kit, Risperdal, Risperdal Consta), and thioridazine
• medications for blood pressure
• carbamazepine
• diuretics ('water pills')
• dopamine agonists such as bromocriptine (Cycloset, Parlodel), cabergoline, levodopa and carbidopa (Duopa, Rytary, Sinemet, others), pramipexole (Mirapex), ropinirole (Requip), and rotigotine (Neupro)
• fluoroquinolone antibiotics such as gatifloxacin (Zymar, Zymaxid) and moxifloxacin
• medications for irregular heartbeat such as amiodarone (Nexterone, Pacerone), procainamide, quinidine (in Nuedexta)
• rifampin (Rifadin, Rimactane)
• sotalol (Betapace, Sorine, Sotylize)

Is this medicine FDA approved?

• Oral formulations of paliperidone were approved for use in the United States in 2006 as treatment for schizophrenia and schizoaffective disorder, as extended release tablets of 1.5, 3, 6 and 9 mg under the brand name Invega.
• Subsequently, parenteral formulations of paliperidone palmitate were developed that could be administered every one or three months.
• These palmitate formulations are given intramuscularly in varying doses and are available under the brand names Invega Sustenna and Invega Trinzia.

How should this medicine be used?

Recommended dosage: Invega Sustenna:

• The recommended initiation of Invega Sustenna® is with a dose of 234 mg on treatment day 1 and 156 mg one week later, both administered in the deltoid muscle.
• Following the second initiation dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle.

Initial Invega Hafyera Dose for Adult Patients Switching from a palmitate extended-release injectable suspension (PP1M) Product:

INVEGA HAFYERA Doses for Adults Adequately Treated with Once-a-month paliperidone palmitate extended-release injectable suspension (PP1M)*

If the Last Dose of PP1M is:	Initiate INVEGA HAFYERA at the Following Dose:
156 mg	1,092 mg
234 mg	1,560 mg

Initial Invega Hafyera Dose for Adult Patients Switching from a palmitate injectable suspension (PP3M) Product:

INVEGA HAFYERA Doses for Adults Adequately Treated with Every-three-month paliperidone palmitate injectable suspension (PP3M)*
If the Last Dose of PP3M is:	Initiate INVEGA HAFYERA at the Following Dose:
546 mg	1,092 mg
819 mg	1,560 mg

Invega Trinza® Doses for Adult Patients Adequately Treated with Invega Sustenna:

INVEGA TRINZA® Doses for Adult Patients Adequately Treated with INVEGA SUSTENNA

f the Last Dose of INVEGA SUSTENNA® is:	Initiate INVEGA TRINZA® at the Following Dose:
78 mg	273 mg
117 mg	410 mg
156 mg	546 mg
234 mg	819 mg

Administration:

• Paliperidone extended-release injections come as a suspension to be injected into a muscle by a healthcare provider.
• There are three different types of paliperidone extended release injection products: Invega Sustenna, Invega Trinza, and Invega Hafyera.
• Your doctor will start you with a single dose of paliperidone extended-release injection Invega Sustenna.
• After you receive your first dose, you will receive a second dose usually 1 week after the first and then once every month after that.
• After at least 4 months of treatment with paliperidone extended-release injection Invega Sustenna and you have responded to your treatment, your doctor may switch you to paliperidone extended-release injection Invega Trinza.
• Paliperidone extended-release injection Invega Trinza is usually injected into a muscle by a healthcare provider once every 3 months.
• After at least 4 months of treatment with paliperidone extended-release injection Invega Sustenna or after at least one 3-month injection of paliperidone extended-release injection Invega Trinza and you have responded to either treatment, your doctor may switch you to paliperidone extended-release injection (Invega Hafyera).
• Paliperidone extended-release injection Invega Hafyera is usually injected into a muscle by a healthcare provider once every 6 months.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-release injectable suspension

This medicine is available in fallowing brand namesː

• Invega Sustenna, Invega Trinza, and Invega Hafyera

What side effects can this medication cause?

The most common side effects of Invega Hafyera include:

• upper respiratory tract infections
• weight gain
• feeling restlessness or difficulty sitting still
• tremors
• shuffling walk
• injection site reactions
• headache
• slow movements
• stiffness

The most common side effects of Invega Sustenna® include:

• injection site reactions, sleepiness or drowsiness, dizziness, feeling restlessness or needing to be constantly moving, abnormal muscle movements including tremor (shaking), shuffling, uncontrolled involuntary movements, and abnormal movements of your eyes.

The most common side effects of Invega Trinza® include:

• injection site reactions, weight gain, headache, upper respiratory tract infections, feeling restlessness or difficulty sitting still, slow movements, tremors, stiffness and shuffling walk.

Paliperidone extended-release injections may cause serious side effects which may include:

• Increased risk of death in elderly people who are confused, have memory loss and have lost touch with reality (dementia-related psychosis)
• stroke in elderly people (cerebrovascular problems) that can lead to death
• Neuroleptic Malignant Syndrome (NMS)
• problems with your heartbeat
• tardive dyskinesia
• hyperglycemia
• dyslipidemia
• weight gain
• low blood pressure and fainting
• changes in your blood cell counts
• hyperprolactinemia
• problems thinking clearly and moving your body
• seizures
• difficulty swallowing that can cause food or liquid to get into your lungs
• prolonged or painful erection lasting more than 4 hours
• problems with control of your body temperature

What special precautions should I follow?

• Counsel patients about a potentially fatal adverse reaction, Neuroleptic Malignant Syndrome (NMS), that has been reported in association with administration of antipsychotic drugs. Advise patients, family members, or caregivers to contact their healthcare provider or report to the emergency room if they experience signs and symptoms of NMS, including hyperpyrexia, muscle rigidity, altered mental status including delirium, and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia).
• Counsel patients on the signs and symptoms of tardive dyskinesia and to contact their healthcare provider if these abnormal movements occur.
• Educate patients about the risk of metabolic changes, how to recognize symptoms of hyperglycemia and diabetes mellitus, and the need for specific monitoring, including blood glucose, lipids, and weight.
• Educate patients about the risk of orthostatic hypotension and syncope, particularly at the time of initiating treatment, re-initiating treatment, or increasing the dose.
• Advise patients with a pre-existing low WBC or a history of drug induced leukopenia/neutropenia that they should have their CBC monitored while taking Paliperidone extended-release injections.
• Caution patients about performing activities requiring mental alertness, such as operating hazardous machinery, or operating a motor vehicle until they are reasonably certain that Paliperidone extended-release injections therapy does not affect them adversely
• Advise patients of the possibility of painful or prolonged penile erections (priapism). Instruct the patient to seek immediate medical attention in the event of priapism.
• Counsel patients regarding appropriate care in avoiding overheating and dehydration.
• Advise patients to inform their healthcare providers if they are taking, or plan to take any prescription or over-the-counter medications, because there is a potential for clinically significant interactions.
• Advise patients to avoid alcohol during treatment with Paliperidone extended-release injections.
• Advise breastfeeding women using Paliperidone extended-release injections to monitor infants for somnolence, failure to thrive, jitteriness, and extrapyramidal symptoms (tremors and abnormal muscle movements) and to seek medical care if they notice these signs.
• Advise females of reproductive potential that Paliperidone extended-release injections may impair fertility due to an increase in serum prolactin levels. The effects on fertility are reversible.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• extrapyramidal symptoms
• gait unsteadiness
• drowsiness
• somnolence
• tachycardia
• hypotension
• QT prolongation
• Torsade de pointes
• ventricular fibrillation

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Treatment should consist of general measures employed in the management of overdosage with any drug.
• Consider the possibility of multiple drug overdosage.
• Ensure an adequate airway, oxygenation, and ventilation.
• Monitor cardiac rhythm and vital signs.
• Use supportive and symptomatic measures.
• There is no specific antidote to paliperidone.

Can this medicine be used in pregnancy?

• Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery.
• Overall, available data from published epidemiologic studies of pregnant women exposed to paliperidone have not established a drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes

Can this medicine be used in children?

• Safety and effectiveness of Paliperidone extended-release injections in patients less than 18 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Invega Hafyera:

• Active ingredient: paliperidone palmitate
• Inactive ingredients: polysorbate 20, polyethylene glycol 4000, citric acid monohydrate, sodium dihydrogen phosphate monohydrate, sodium hydroxide, and water for injection

Invega Trinza:

• Active ingredient: paliperidone palmitate
• Inactive ingredients: polysorbate 20, polyethylene glycol 4000, citric acid monohydrate, sodium dihydrogen phosphate monohydrate, sodium hydroxide, and water for injection

Invega Sustenna:

• Active ingredient: paliperidone palmitate
• Inactive ingredients: polysorbate 20, polyethylene glycol 4000, citric acid monohydrate, sodium dihydrogen phosphate monohydrate, sodium hydroxide, and water for injection

Who manufactures and distributes this medicine?

Invega Hafyera:

• Manufactured by: Janssen Pharmaceutica N.V. Beerse, Belgium
• Manufactured for: Janssen Pharmaceuticals, Inc. Titusville, NJ

Invega Trinza:

• Manufactured by: Janssen Pharmaceutica NV Beerse, Belgium
• Manufactured for: Janssen Pharmaceuticals, Inc. Titusville, NJ

Invega Sustenna:

• Manufactured by: Janssen Pharmaceutica NV, Beerse, Belgium
• Manufactured for: Janssen Pharmaceuticals, Inc., Titusville, NJ

What should I know about storage and disposal of this medication?

Invega Hafyera:

• Store at room temperature 20°C to 25°C (68°F to 77°F); excursions between 15°C and 30°C (59°F and 86°F) are permitted. Do not mix with any other product or diluent.
• Ship and store in a horizontal position.

Invega Trinza:

• Store at room temperature 20°C to 25°C (68°F to 77°F); excursions between 15°C and 30°C (59°F and 86°F) are permitted. Do not mix with any other product or diluent.

Invega Sustenna:

• Store at room temperature (25°C, 77°F); excursions between 15°C and 30°C (between 59°F and 86°F) are permitted.
• Do not mix with any other product or diluent.

Antipsychotic agents

First Generation

• Phenothiazines
  • Chlorpromazine, Fluphenazine, Perphenazine, Prochlorperazine, Thioridazine, Trifluoperazine

• Other
  • Haloperidol, Lithium, Loxapine, Molindone, Pimozide

Second Generation (Atypicals)

• Aripiprazole, Asenapine, Brexpiprazole, Cariprazine, Clozapine, Iloperidone, Lurasidone, Olanzapine, Paliperidone, Pimavanserin, Quetiapine, Risperidone, Ziprasidone

• Dailymed label info on Paliperidone palmitate
• FDA Paliperidone palmitate

Paliperidone palmitate Resources
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