Xeplion

2). The third dose should be administered one month after the second initiation dose. The recommended monthly maintenance dose is 75 mg; some patients may benefit from lower or higher doses within the recommended range of 25 to 150 mg based on individual patient tolerability and/or efficacy.

2). Following the second initiation dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle. Adjustment of the maintenance dose may be made monthly. 2), as the full effect of maintenance doses may not be evident for several months.

2 above. During monthly maintenance treatment with Xeplion, patients previously stabilised on different doses of paliperidone prolonged release tablets can attain similar paliperdone steady-state exposure by injection. The Xeplion maintenance doses needed to attain similar steady-state exposure are shown as follows: Doses of paliperidone prolonged release tablets and Xeplion needed to attain similar steady- state paliperidone exposure during maintenance treatment Previous paliperidone prolonged release tablet dose Xeplion injection 3 mg daily 25-50 mg monthly 6 mg daily 75 mg monthly 9 mg daily 100 mg monthly 12 mg daily 150 mg monthly Previous oral paliperidone or oral risperidone can be discontinued at the time of initiation of treatment with Xeplion.

Some patients may benefit from gradual withdrawal. , 9-12 mg daily) to gluteal injections with Xeplion may have lower plasma exposure during the first 6 months after the switch. Therefore, alternatively, it could be considered to give deltoid injections for the first 6 months.

Switching from risperidone long acting injection to Xeplion When switching patients from risperidone long acting injection, initiate Xeplion therapy in place of the next scheduled injection. Xeplion should then be continued at monthly intervals.

2 above is not required. 5 mg every 2 weeks 75 mg monthly 50 mg every 2 weeks 100 mg monthly Discontinuation of antipsychotic medicinal products should be made in accordance with appropriate prescribing information. If Xeplion is discontinued, its prolonged release characteristics must be considered.

The need for continuing existing extrapyramidal symptoms (EPS) medicine should be re-evaluated periodically. 4 Missed doses Avoiding missed doses It is recommended that the second initiation dose of Xeplion be given one week after the first dose.

Summary of the safety profile The adverse reactions most frequently reported in clinical trials were insomnia, headache, anxiety, upper respiratory tract infection, injection site reaction, parkinsonism, weight increased, akathisia, agitation, sedation/somnolence, nausea, constipation, dizziness, musculoskeletal pain, tachycardia, tremor, abdominal pain, vomiting, diarrhoea, fatigue, and dystonia.

Of these, akathisia and sedation/somnolence appeared to be dose-related. Tabulated list of adverse reactions The following are all adverse reactions that were reported with paliperidone by frequency category estimated from paliperidone palmitate clinical trials.

The following terms and frequencies are applied: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1 000 to < 1/100); rare (≥ 1/10 000 to < 1/1 000); very rare (< 1/10 000); and not known (cannot be estimated from the available data).

6) Reproductive system and breast disorders amenorrhoea erectile dysfunction, ejaculation disorder, menstrual disordere, gynaecomastia, galactorrhoea, sexual dysfunction, breast pain priapism, breast discomfort, breast engorgement, breast enlargement, vaginal discharge General disorders and administration site conditions pyrexia, asthenia, fatigue, injection site reaction face oedema, oedemae, body temperature increased, gait abnormal, chest pain, chest discomfort, malaise, induration hypothermia, chills, thirst, drug withdrawal syndrome, injection site abscess, injection site cellulitis, injection site cyst, injection site haematoma body temperature decreased, injection site necrosis, injection site ulcer Injury, poisoning and procedural complications fall a The frequency of adverse reactions is qualified as “not known” because they were not observed in paliperidone palmitate clinical trials.

They were either derived from spontaneous post-marketing reports and frequency cannot be determined, or they were derived from risperidone (any formulation) or oral paliperidone clinical trials data and/or post-marketing reports. b Refer to ‘Hyperprolactinaemia’ below.

Use in patients who are in an acutely agitated or severely psychotic state Xeplion should not be used to manage acutely agitated or severely psychotic states when immediate symptom control is warranted. QT interval Caution should be exercised when paliperidone is prescribed in patients with known cardiovascular disease or family history of QT prolongation, and in concomitant use with other medicinal products thought to prolong the QT interval.

Neuroleptic malignant syndrome Neuroleptic Malignant Syndrome (NMS), characterised by hyperthermia, muscle rigidity, autonomic instability, altered consciousness, and elevated serum creatine phosphokinase levels has been reported to occur with paliperidone.

Additional clinical signs may include myoglobinuria (rhabdomyolysis) and acute renal failure. If a patient develops signs or symptoms indicative of NMS, paliperidone should be discontinued. Tardive dyskinesia/extrapyramidal symptoms Medicinal products with dopamine receptor antagonistic properties have been associated with the induction of tardive dyskinesia characterised by rhythmical, involuntary movements, predominantly of the tongue and/or face.

If signs and symptoms of tardive dyskinesia appear, the discontinuation of all antipsychotics, including paliperidone, should be considered. , methylphenidate) and paliperidone concomitantly, as extrapyramidal symptoms could emerge when adjusting one or both medications.

5). Leucopenia, neutropenia, and agranulocytosis Events of leucopenia, neutropenia, and agranulocytosis have been reported with Xeplion. Agranulocytosis has been reported very rarely (< 1/10,000 patients) during post-marketing surveillance.

Patients with a history of a clinically significant low white blood cell count (WBC) or a drug-induced leucopenia/neutropenia should be monitored during the first few months of therapy and discontinuation of Xeplion should be considered at the first sign of a clinically significant decline in WBC in the absence of other causative factors.

1.