Paliperidone Exeltis (Paliperidone Palmitate)

Paliperidone Exeltis is an atypical antipsychotic used in the schizophrenia treatment pathway.

• Schizophrenia: Improves psychotic symptoms and reduces risk of relapse when administered as a monthly injection.
• Schizoaffective disorder: Stabilises mood and psychotic features as part of a maintenance regimen.
• Bipolar I disorder (maintenance): Provides long‑term mood stabilization to prevent manic or depressive episodes.
• Psychotic relapse prevention: Maintains therapeutic plasma levels to minimise breakthrough psychosis.
• Adjunct to oral antipsychotics: Allows dose reduction of oral agents during transition to long‑acting therapy.

• Paliperidone palmitate is a pro‑drug of paliperidone that, after intramuscular administration, is slowly hydrolysed to release paliperidone. The active moiety antagonises dopamine D2 and serotonin 5‑HT2A receptors, modulating dopaminergic and serotonergic neurotransmission implicated in psychosis and mood regulation. This receptor blockade reduces positive and negative symptoms of schizophrenia and stabilises mood in related disorders.

Paliperidone Exeltis may cause a range of adverse reactions, most of which are dose‑dependent and reversible.

Common Side Effects

• Injection site pain: Discomfort at the site of administration.
• Weight gain: Increase in body weight over time.
• Akathisia: Restlessness or an urge to move.
• Sedation: Drowsiness or reduced alertness.
• Hyperprolactinemia: Elevated prolactin levels, potentially causing menstrual changes.
• Constipation: Reduced bowel motility.

Serious or Rare Side Effects

• Neuroleptic malignant syndrome: Potentially life‑threatening reaction with fever and rigidity.
• Tardive dyskinesia: Involuntary, repetitive movements.
• Seizures: Increased risk, especially in predisposed individuals.
• Orthostatic hypotension: Marked blood pressure drop on standing.
• Cardiac arrhythmias: QT‑interval prolongation.
• Severe allergic reactions: Anaphylaxis or angio‑edema.

When prescribing Paliperidone Exeltis, clinicians should consider several safety aspects.

• Cardiovascular assessment: Evaluate for history of arrhythmias or QT prolongation.
• Metabolic monitoring: Track weight, glucose, and lipid levels regularly.
• Prolactin surveillance: Monitor for menstrual disturbances or galactorrhoea.
• CNS effects: Observe for signs of sedation, akathisia, or extrapyramidal symptoms.
• Pregnancy and lactation: Use only if benefits outweigh risks; discuss with patient.
• Store at ambient temperature: Keep in original packaging, protect from moisture and direct sunlight.

Paliperidone Exeltis can interact with several drug classes; awareness helps avoid adverse outcomes.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors: May increase paliperidone levels, raising toxicity risk.
• QT‑prolonging agents: Combined use can exacerbate cardiac repolarisation delays.
• CNS depressants: Additive sedation or respiratory depression.

Moderate Interactions (Monitor Closely)

• Antihypertensives: May enhance orthostatic hypotension.
• Anticholinergic drugs: Can worsen cognitive side effects.
• CYP2D6 substrates: Potential for altered metabolism of co‑administered medications.