Active Ingredient: Paliperidone
For this indication, competent medicine agencies globally authorize below treatments:
For:
Oral, between 3 milligrams paliperidone and 12 milligrams paliperidone, once daily at morning.
The recommended dose of paliperidone for the treatment of schizophrenia in adults is 6 mg once daily, administered in the morning. Initial dose titration is not required. Some patients may benefit from lower or higher doses within the recommended range of 3 mg to 12 mg once daily. Dosage adjustment, if indicated, should occur only after clinical reassessment. When dose increases are indicated, increments of 3 mg/day are recommended and generally should occur at intervals of more than 5 days.
Dosing recommendations for elderly patients with normal renal function (≥80 mL/min) are the same as for adults with normal renal function. However, because elderly patients may have diminished renal function, dose adjustments may be required according to their renal function status. Paliperidone should be used with caution in elderly patients with dementia with risk factors for stroke.
There are no systematically collected data to specifically address switching patients from paliperidone to other antipsychotic medicinal products. Due to different pharmacodynamic and pharmacokinetic profiles among antipsychotic medicinal products, supervision by a clinician is needed when switching to another antipsychotic product is considered medically appropriate.
It should be taken in the morning. It must be swallowed with liquid.
The administration of paliperidone should be standardised in relation to food intake. The patient should be instructed to always take paliperidone in the fasting state or always take it together with breakfast and not to alternate between administration in the fasting state or in the fed state.
For:
Regimen A: In case that patient weight is ≤ 51 kg, oral, 3 milligrams paliperidone, once daily. The maximum allowed total dose is 6 milligrams paliperidone daily.
Regimen B: In case that patient weight is ≥ 51 kg, oral, 3 milligrams paliperidone, once daily. The maximum allowed total dose is 12 milligrams paliperidone daily.
The recommended starting dose of paliperidone for the treatment of schizophrenia in adolescents 15 years and older is 3 mg once daily, administered in the morning.
Adolescents weighing <51 kg: the maximum recommended daily dose of paliperidone is 6 mg.
Adolescents weighing ≥51 kg: the maximum recommended daily dose of paliperidone is 12 mg.
Dosage adjustment, if indicated, should occur only after clinical reassessment based on the individual need of the patient. When dose increases are indicated, increments of 3 mg/day are recommended and generally should occur at intervals of 5 days or more. The safety and efficacy of paliperidone in the treatment of schizophrenia in adolescents between 12 and 14 years old has not been established.
There are no systematically collected data to specifically address switching patients from paliperidone to other antipsychotic medicinal products. Due to different pharmacodynamic and pharmacokinetic profiles among antipsychotic medicinal products, supervision by a clinician is needed when switching to another antipsychotic product is considered medically appropriate.
It should be taken in the morning. It must be swallowed with liquid.
The administration of paliperidone should be standardised in relation to food intake. The patient should be instructed to always take paliperidone in the fasting state or always take it together with breakfast and not to alternate between administration in the fasting state or in the fed state.
For:
Intramuscular, 150 milligrams paliperidone, one dose, over the duration of 7 days. Afterwards, intramuscular, 100 milligrams paliperidone, one dose, over the duration of 1 month. Afterwards, intramuscular, between 25 milligrams paliperidone and 150 milligrams paliperidone, once monthly.
Paliperidone prolonged release suspension for injection is indicated for maintenance treatment of schizophrenia in adult patients stabilised with paliperidone or risperidone.
In selected adult patients with schizophrenia and previous responsiveness to oral paliperidone or risperidone, paliperidone prolonged release suspension for injection may be used without prior stabilisation with oral treatment if psychotic symptoms are mild to moderate and a long-acting injectable treatment is needed.
Recommended initiation of paliperidone prolonged release suspension for injection is with a dose of 150 mg on treatment day 1 and 100 mg one week later (day 8), both administered in the deltoid muscle in order to attain therapeutic concentrations rapidly. 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. Patients who are overweight or obese may require doses in the upper range. 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. When making dose adjustments, the prolonged release characteristics of paliperidone injection should be considered, as the full effect of maintenance doses may not be evident for several months.
Paliperidone prolonged release suspension for injection should be initiated as described above. During monthly maintenance treatment, patients previously stabilised on different doses of paliperidone prolonged release tablets can attain similar paliperdone steady-state exposure by injection. The paliperidone injection maintenance doses needed to attain similar steady-state exposure are shown as follows:
Doses of paliperidone prolonged release tablets and paliperidone prolonged release suspension for injection needed to attain similar steady-state paliperidone exposure during maintenance treatment:
| Previous paliperidone prolonged release tablet dose | Paliperidone 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 paliperidone injection. Some patients may benefit from gradual withdrawal. Some patients switching from higher paliperidone oral doses (e.g. 9-12 mg daily) to gluteal injections with paliperidone 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.
It is recommended that the second initiation dose of paliperidone injection be given one week after the first dose. To avoid a missed dose, patients may be given the second dose 4 days before or after the one-week (day 8) time point. Similarly, the third and subsequent injections after the initiation regimen are recommended to be given monthly. To avoid a missed monthly dose, patients may be given the injection up to 7 days before or after the monthly time point.
If the target date for the second paliperidone injection (day 8 ± 4 days) is missed, the recommended reinitiation depends on the length of time which has elapsed since the patient’s first injection.
It should be injected slowly, deep into the deltoid or gluteal muscle.
The day 1 and day 8 initiation doses must each be administered in the deltoid muscle in order to attain therapeutic concentrations rapidly. Following the second initiation dose, monthly maintenance doses can be administered in either the deltoid or gluteal muscle. A switch from gluteal to deltoid (and vice versa) should be considered in the event of injection site pain if the injection site discomfort is not well tolerated. It is also recommended to alternate between left and right sides.
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