Generic Name

Paliperidone

Brand Names
Erzofri, Invega HAFYERA, Invega, Invega SUSTENNA, Invega TRINZA
FDA approval date: December 19, 2006
Classification: Atypical Antipsychotic
Form: Injection, Tablet

What is Erzofri (Paliperidone)?

Living with a condition like schizophrenia or schizoaffective disorder, or caring for someone who does, is a journey that requires immense strength, patience and support. The challenges of managing symptoms like hallucinations, disorganized thinking and mood disturbances can feel overwhelming, impacting every aspect of daily life. In this journey, medication is often a critical tool for finding stability and reclaiming a sense of control. One of the key medications used to provide this stability is Paliperidone.

Paliperidone is a prescription medication that belongs to a class of drugs known as second-generation (or atypical) antipsychotics. It is a well-established, first-line treatment option designed to manage the complex symptoms of certain serious mental health conditions. Available as a daily oral tablet or as a long-acting injection given every one to six months, Paliperidone offers flexible treatment plans that can help individuals achieve and maintain recovery, empowering them to lead more fulfilling lives.

What does Paliperidone do?

Paliperidone is approved by the U.S. Food and Drug Administration (FDA) to treat two primary conditions:

  • Schizophrenia: It is used to manage the symptoms of schizophrenia in adults and adolescents (ages 12 and older).
  • Schizoaffective Disorder: It treats adult schizoaffective disorder, which combines schizophrenia symptoms (hallucinations, delusions) with mood disorder symptoms (mania, depression).

Paliperidone aims to reduce psychotic symptoms and stabilize mood. Patients can expect fewer hallucinations, delusions and irrational thoughts, along with improved motivation, social engagement and daily functioning. Clinical studies show its effectiveness in symptom control and relapse prevention, especially with long-acting injections (Janssen Pharmaceuticals, Inc., 2023).

How does Paliperidone work?

The symptoms of schizophrenia and schizoaffective disorder are believed to be caused by an imbalance of natural chemical messengers in the brain called neurotransmitters, particularly dopamine and serotonin. These chemicals are responsible for regulating thoughts, emotions and perceptions.

In these conditions, it is thought that certain dopamine pathways in the brain are overactive, leading to the “positive” symptoms of psychosis like hallucinations and delusions. Paliperidone works by precisely targeting and blocking specific dopamine receptors (known as D2 receptors). Think of these receptors as locks and dopamine as the key; by partially blocking the lock, Paliperidone reduces the effects of excess dopamine, which helps to quiet these psychotic symptoms.

Paliperidone blocks specific serotonin receptors (5-HT2A), improving negative and cognitive symptoms of schizophrenia like emotional withdrawal and lack of motivation. By rebalancing dopamine and serotonin, it restores normal brain function for clearer thinking and emotional stability. It’s the active metabolite of risperidone.

Paliperidone side effects

Like all antipsychotic medications, Paliperidone has potential side effects. Your healthcare provider will work with you to manage any that occur.

Common side effects may include:

  • Drowsiness or sleepiness
  • Restlessness or an inability to sit still (akathisia)
  • Stiffness, tremors, or slow movements (parkinsonism)
  • Increased heart rate (tachycardia)
  • Weight gain
  • Dizziness, especially when standing up (orthostatic hypotension)

Paliperidone can elevate prolactin, potentially causing menstrual irregularities, breast milk production, or sexual side effects in both sexes.

Serious side effects are less common but require immediate medical attention. All antipsychotics, including Paliperidone, have a boxed warning about an increased risk of death in elderly patients with dementia-related psychosis. Other serious risks include:

  • Neuroleptic Malignant Syndrome (NMS): A rare but life-threatening reaction with symptoms like high fever, severe muscle stiffness and confusion.
  • Tardive Dyskinesia (TD): A condition causing uncontrollable, repetitive movements, often of the face and tongue, which can be permanent.
  • Metabolic Changes: An increased risk of high blood sugar, high cholesterol and significant weight gain.

You should contact your doctor right away if you experience a high fever, severe confusion, uncontrollable muscle movements, or fainting.

Paliperidone dosage

Paliperidone comes in two main forms for personalized treatment: once-daily oral extended-release tablets (Invega) and long-acting injections (Invega Sustenna, Invega Trinza, Invega Hafyera). The injections, administered by a healthcare professional every 1, 3, or 6 months, are beneficial for those who struggle with daily pill adherence, ensuring continuous treatment and preventing relapse.

Your doctor will monitor your weight, blood pressure, and family history of diabetes/cholesterol before and during treatment. They’ll order blood tests for sugar/cholesterol, check for abnormal movements, and adjust your dose based on symptoms, side effects, and kidney function.

Does Paliperidone have a generic version?

Yes, the oral extended-release tablet form of Paliperidone is available as a generic medication. The most common brand name for the oral tablet is Invega. The FDA requires that generic medications are bioequivalent to the brand-name product, meaning they are just as safe and effective (FDA, 2021).

The long-acting injectable formulations are newer and are currently only available under their brand names: Invega Sustenna (1-month), Invega Trinza (3-month) and Invega Hafyera (6-month).

Conclusion

Paliperidone is a valuable and effective medication for managing the challenging symptoms of schizophrenia and schizoaffective disorder. By helping to rebalance key brain chemicals, it can reduce psychosis, stabilize mood, and significantly improve a person’s quality of life. The availability of both daily oral and long-acting injectable forms provides flexible options to help ensure consistent treatment, which is the cornerstone of preventing relapse.

While Paliperidone has potential risks and side effects, they can be successfully managed through close collaboration with your healthcare provider. Open communication about your symptoms and any concerns you have is key to finding the right treatment plan. With the right support, Paliperidone can be a powerful tool on the path to long-term stability and recovery.

References

  1. Food and Drug Administration (FDA). (2021). Generic Drug Facts. Retrieved from https://www.fda.gov/drugs/generic-drugs/generic-drug-facts
  2. Janssen Pharmaceuticals, Inc. (2023). INVEGA SUSTENNA® (paliperidone palmitate) Prescribing Information. U.S. Food and Drug Administration. Retrieved from https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/022264s046lbl.pdf
  3. National Institutes of Health. (2022). Paliperidone. MedlinePlus. Retrieved from https://medlineplus.gov/druginfo/meds/a607046.html

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Brand Information

    Erzofri extended-release (paliperidone palmitate)
    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. ERZOFRI is not approved for use in patients with dementia-related psychosis. [see .
    1INDICATIONS AND USAGE
    ERZOFRI is indicated for the treatment of:
    • Schizophrenia in adults
    • Schizoaffective disorder in adults as monotherapy and as an adjunct to mood stabilizers or antidepressants
    2DOSAGE FORMS AND STRENGTHS
    Extended-release injectable suspension: white to off-white aqueous suspension available in dose strengths of 39 mg/0.25 mL, 78 mg/0.5 mL, 117 mg/0.75 mL, 156 mg/mL, 234 mg/1.5 mL, and 351 mg/2.25 mL paliperidone palmitate.
    Each strength is provided as a kit, which includes: one single-dose prefilled syringe and 2 safety needles (a 1 ½-inch 22 gauge needle and a 1-inch 23 gauge needle).
    3CONTRAINDICATIONS
    ERZOFRI is contraindicated in patients with a known hypersensitivity to either paliperidone or risperidone, or to any of the excipients in the ERZOFRI formulation. Hypersensitivity reactions, including anaphylactic reactions and angioedema, have been reported in patients treated with risperidone and in patients treated with paliperidone
    4ADVERSE REACTIONS
    The following are discussed in more detail in other sections of the labeling:
    • Increased mortality in elderly patients with dementia-related psychosis
    • Cerebrovascular adverse reactions, including stroke, in elderly patients with dementia-related psychosis
    • Neuroleptic malignant syndrome
    • QT prolongation
    • Tardive dyskinesia
    • Metabolic changes
    • Orthostatic hypotension and syncope
    • Falls
    • Leukopenia, neutropenia, and agranulocytosis
    • Hyperprolactinemia
    • Potential for cognitive and motor impairment
    • Seizures
    • Dysphagia
    • Priapism
    • Disruption of body temperature regulation
    4.1Clinical Trials Experience
    Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
    The safety of ERZOFRI for the treatment of schizophrenia in adults and schizoaffective disorder in adults as monotherapy and as an adjunct to mood stabilizers or antidepressants is based upon adequate and well-controlled studies of another once-a-month paliperidone palmitate extended-release injectable suspension (also referred to as "PP1M" in this section). Below is a display of adverse reactions with another PP1M from those adequate and well-controlled studies.
    Injection site reactions for ERZOFRI presented in this section (see "
    4.2Postmarketing Experience
    The following adverse reactions have been identified during post-approval use of paliperidone; because these reactions were reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: angioedema, catatonia, ileus, somnambulism, swollen tongue, thrombotic thrombocytopenic purpura, urinary incontinence, and urinary retention.
    Cases of anaphylactic reaction after injection with another once-a-month paliperidone palmitate extended-release injectable suspension product have been reported during postmarketing experience in patients who have previously tolerated oral risperidone or oral paliperidone.
    Paliperidone is the major active metabolite of risperidone. Adverse reactions reported with oral risperidone and risperidone long-acting injection can be found in the
    5DESCRIPTION
    ERZOFRI (paliperidone palmitate) extended-release injectable suspension contains a racemic mixture of (+)- and (-)- paliperidone palmitate. Paliperidone palmitate, is an atypical antipsychotic belonging to the chemical class of benzisoxazole derivatives. The chemical name is (9
    Chemical Structure
    Paliperidone palmitate is very slightly soluble in ethanol and methanol, practically insoluble in water, and slightly soluble in ethyl acetate.
    ERZOFRI is available as a white to off-white sterile aqueous extended-release suspension for intramuscular injection in the following dose strengths of paliperidone palmitate (deliverable volume) in single-dose prefilled syringes: 39 mg (0.25 mL), 78 mg (0.5 mL), 117 mg (0.75 mL), 156 mg (1 mL), 234 mg (1.5 mL), and 351 mg (2.25 mL). The drug product hydrolyzes in vivo to the active moiety, paliperidone, resulting in dose strengths of 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, and 225 mg of paliperidone, respectively.
    The inactive ingredients are citric acid monohydrate (5 mg/mL), dibasic sodium phosphate anhydrous (5 mg/mL), monobasic sodium phosphate monohydrate (2.5 mg/mL), polyethylene glycol 4000 (30 mg/mL), polysorbate 20 (12 mg/mL), sodium hydroxide to adjust pH, and water for injection. The drug product pH is 6.5 to 7.5.
    6PATIENT COUNSELING INFORMATION
    Advise the patient to read the FDA-approved patient labeling (Patient Information).
    7PRINCIPAL DISPLAY PANEL - 39 mg/0.25 mL Syringe Kit
    NDC 72526-105-11
    Erzofri
    39 mg/0.25 mL
    For Single Use Only.
    FOR INTRAMUSCULAR INJECTION ONLY.
    PRINCIPAL DISPLAY PANEL - 39 mg/0.25 mL Syringe Kit
    8PRINCIPAL DISPLAY PANEL - 78 mg/0.5 mL Syringe Kit
    NDC 72526-106-11
    Erzofri
    78 mg/0.5 mL
    For Single Use Only.
    FOR INTRAMUSCULAR INJECTION ONLY.
    PRINCIPAL DISPLAY PANEL - 78 mg/0.5 mL Syringe Kit
    9PRINCIPAL DISPLAY PANEL - 117 mg/0.75 mL Syringe Kit
    NDC 72526-107-11
    Erzofri
    117 mg/0.75 mL
    For Single Use Only.
    FOR INTRAMUSCULAR INJECTION ONLY.
    PRINCIPAL DISPLAY PANEL - 117 mg/0.75 mL Syringe Kit
    10PRINCIPAL DISPLAY PANEL - 156 mg/mL Syringe Kit
    NDC 72526-108-11
    Erzofri
    156 mg/mL
    For Single Use Only.
    FOR INTRAMUSCULAR INJECTION ONLY.
    PRINCIPAL DISPLAY PANEL - 156 mg/mL Syringe Kit
    11PRINCIPAL DISPLAY PANEL - 234 mg/1.5 mL Syringe Kit
    NDC 72526-109-11
    Erzofri
    234 mg/1.5 mL
    For Single Use Only.
    FOR INTRAMUSCULAR INJECTION ONLY.
    PRINCIPAL DISPLAY PANEL - 234 mg/1.5 mL Syringe Kit
    12PRINCIPAL DISPLAY PANEL - 351 mg/2.25 mL Syringe Kit
    NDC 72526-110-11
    Erzofri
    351 mg/2.25 mL
    For Single Use Only.
    FOR INTRAMUSCULAR INJECTION ONLY.
    PRINCIPAL DISPLAY PANEL - 351 mg/2.25 mL Syringe Kit
    Erzofri has been selected.