【藥品性質提示】 根據 2019 AGS Beers Criteria，本藥品為【潛在不適當用藥 (PIM)】，不建議用於老年人 (除非用於思覺失調、雙極症、或化療止吐)。 #特殊劑型：不建議磨粉、管灌藥品

思覺失調症 Schizoaffective disorder, Schizophrenia

Second Generation (Atypical) Antipsychotic
Paliperidone is the major active metabolite of risperidone. While the mechanism of action is unknown, its proposed therapeutic activity is antagonism of both the central D2 and 5HT2A receptors. It also has antagonistic effects on the alpha-1 adrenergic, alpha-2 adrenergic, and H1 histaminergic receptors.

Absorption
1. Time to peak: approximately 24 hr
2. Bioavailability: 28%
3. Effect of food: increase Cmax by 60% and AUC by 54%
Distribution
1. Vd: 487 L
2. Protein binding: 74%
Metabolism
1. Hepatic: limited
2. Metabolic pathways: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission; less than 10% each
Excretion
1. Renal clearance: 53.1 mL/min
2. Fecal (solution, healthy volunteers): not detected
Elimination Half Life
1.Approximately 23 h
2. Mild renal impairment: 24 h
3. Moderate renal impairment: 40 h
4. Severe renal impairment: 51 hr

Hypersensitivity to paliperidone, risperidone, or to any product component

Fetal risk cannot be ruled out.

Infant risk cannot be ruled out.

Common
Cardiovascular: Tachycardia
Endocrine metabolic: Hyperprolactinemia, Weight gain
Gastrointestinal: Constipation, Indigestion
Neurologic: Akathisia, Dyskinesia, Dystonia, Extrapyramidal disease, Parkinsonism, Somnolence, Tremor
Psychiatric: Anxiety
Respiratory: Nasopharyngitis
Serious
Cardiovascular: Prolonged QT interval
Hematologic: Agranulocytosis, Leukopenia
Neurologic: Dysphagia, Tardive dyskinesia
Reproductive: Priapism

Bipolar I disorder, Acute manic and mixed episodes: (Off-label use)
1. Initial: 6 mg QD
2. Dosage adjustment: based on efficacy and tolerance with 3 mg/day increments or decrements to remain within the range of 3 to 12 mg/day
Schizoaffective disorder:
1. Initial: 6 mg QD
2. Dosage titration: may increase by 3 mg/day increments at intervals of more than 4 days, only after clinical reassessment.
3. Maintenance dosage: 3 to 12 mg QD
4. Maximum dosage: 12 mg QD
Schizophrenia
1. Initial: 6 mg QD; 3 mg/day may be sufficient in some patients
2. Dosage titration: May increase by 3-mg/day increments; increases above 6 mg/day should occur only after clinical reassessment and at intervals of more than 5 days
3. Maintenance dosage: 3 to 12 mg QD
4. Maximum dosage: 12 mg QD

[Schizophrenia]
12 to 17 years, ≥51 kg:
1. Initial 3 mg orally once daily
2. Maintenance dosage ranges from 3 to 12 mg/day; may increase by 3-mg/day increments at intervals of more than 5 days; MAX 12 mg/day
12 to 17 years, <51 kg:
1. Initial 3 mg orally once daily
2. Maintenance dosage ranges from 3 to 6 mg/day; may increase by 3-mg/day increments at intervals of more than 5 days; MAX 6 mg/day

1. CrCl 50-80 mL/min: Initial, 3 mg once daily; MAX 6 mg once daily
2. CrCl 10-50 mL/min: Initial, 1.5 mg once daily; MAX 3 mg once daily
3. CrCl <10 mL/min: Use not recommended

Child-Pugh Class A and B: Adjustment not necessary.

May be taken without regard to meals, and must be swallowed whole with liquid; do not chew, divide, or crush.
Store paliperidone extended-release tablets at 25 degrees Celsius, with excursions permitted to 15 to 30 degrees Celsius; protect from moisture.