Adult: As paliperidone palmitate (1 mg paliperidone palmitate is equivalent to approx 0.64 mg paliperidone base): As a monthly inj: 234 mg (150 mg as base) on day 1 then 156 mg (100 mg as base) on day 8. Maintenance: 39-234 mg (25-150 mg as base) monthly, given 5 weeks after the 1st inj. As a 3-monthly inj: Administer only after the patient has been adequately treated with the monthly inj for at least 4 months. Dose is based on the previous monthly inj dose, if the last dose of the monthly inj is 78 mg (50 mg as base), 117 mg (75 mg as base), 156 mg (100 mg as base), and 234 mg (150 mg as base), initiate 3-monthly inj at 273 mg (175 mg as base), 410 mg (263 mg as base), 546 mg (350 mg as base), and 819 mg (525 mg as base), respectively. May adjust dose every 3 months based on tolerability and efficacy. As a 6-monthly inj: Administer only after the patient has been adequately treated with the monthly inj for at least 4 months or the 3-monthly inj for at least one 3-month cycle. Dose is based on the previous monthly inj dose, if the last dose of the monthly inj is 156 mg (100 mg as base) and 234 mg (150 mg as base), initiate 6-monthly inj at 1,092 mg (700 mg as base) and 1,560 mg (1,000 mg as base), respectively; or based on the previous 3-monthly inj dose, if the last dose of 3-monthly inj is 546 mg (350 mg as base) and 819 mg (525 mg as base), initiate 6-monthly inj at 1,092 mg (700 mg as base) and 1,560 mg (1,000 mg as base), respectively. May adjust dose every 6 months based on tolerability and efficacy. Refer to detailed product guidelines for further dosing information including the management of missed dose.
Intramuscular Schizoaffective disorder
Adult: As monotherapy or an adjunct to mood stabilisers or antidepressants: As paliperidone palmitate (1 mg paliperidone palmitate is equivalent to approx 0.64 mg paliperidone base): As a monthly inj: 234 mg (150 mg as base) on day 1 then 156 mg (100 mg as base) on day 8. Maintenance: 78-234 mg (50-150 mg as base) monthly, given 5 weeks after the 1st inj. Refer to detailed product guidelines for further dosing information including the management of missed dose.
Oral Schizophrenia
Adult: As paliperidone base extended-release tab: Initially, 6 mg once daily. If necessary, adjust in increments of 3 mg daily at intervals of >5 days. Usual dosage range: 3-12 mg once daily. Child: 12-17 years As paliperidone base extended-release tab: <51 kg: Initially, 3 mg once daily. Usual dosage range: 3-6 mg daily; ≥51 kg: Initially, 3 mg once daily. Usual dosage range: 3-12 mg daily. If necessary, adjust in increments of 3 mg daily at intervals of ≥5 days. Treatment recommendations may vary among countries or individual products (refer to specific product guidelines).
Oral Schizoaffective disorder
Adult: As monotherapy or an adjunct to mood stabilisers and/or antidepressants: As paliperidone base extended-release tab: Initially, 6 mg once daily. If necessary, adjust in increments of 3 mg daily at intervals of >4 days. Usual dosage range: 3-12 mg once daily.
Suy thận
Oral:
CrCl (mL/min)
Dosage
<10
Not recommended.
≥10-<50
As paliperidone base extended-release tab: Initially, 1.5 mg once daily or 3 mg every other day, may be increased to Max 3 mg once daily if necessary.
≥50-<80
As paliperidone base extended-release tab: Initially, 3 mg once daily, may be increased to Max 6 mg once daily according to response and tolerance.
Intramuscular: Schizophrenia:
CrCl (mL/min)
Dosage
<50
Not recommended.
≥50-<80
As a monthly inj: As paliperidone palmitate (1 mg paliperidone palmitate is equivalent to approx 0.64 mg paliperidone base): 156 mg (100 mg as base) on day 1 then 117 mg (75 mg as base) on day 8, followed by monthly inj of 78 mg (50 mg as base). As a 3-monthly inj: Adjust dose and stabilise patient using the monthly inj then transition to the 3-monthly inj. As a 6-monthly inj: Not recommended.
Schizoaffective disorder:
CrCl (mL/min)
Dosage
<50
Not recommended.
≥50-<80
As a monthly inj: As paliperidone palmitate (1 mg paliperidone palmitate is equivalent to approx 0.64 mg paliperidone base): 156 mg (100 mg as base) on day 1 then 117 mg (75 mg as base) on day 8, followed by monthly inj of 78 mg (50 mg as base).
Cách dùng
extended-release tab: May be taken with or without food. Swallow whole w/ liqd, do not chew/divide/crush.
Chống chỉ định
Hypersensitivity to paliperidone or risperidone. Lactation.
Thận trọng
Patient with known CV disease (e.g. heart failure, history of MI or ischaemia), cerebrovascular disease, conditions that may predispose to hypotension (e.g. dehydration, hypovolaemia), diabetes mellitus or risk factors for diabetes (e.g. obesity, family history of diabetes), at risk for aspiration pneumonia, history of seizures or other conditions that may lower the seizure threshold, history of clinically significant low WBC/absolute neutrophil count or drug-induced leucopenia or neutropenia, possible prolactin-dependent tumours, Parkinson's disease. Patient undergoing cataract surgery. Patient who will be experiencing conditions that may cause elevation in core body temperature (e.g. strenuous exercise, exposure to extreme heat). Not indicated for the treatment of dementia-related psychosis. Avoid use in patients with congenital long QT syndrome or history of cardiac arrhythmias. Renal and severe hepatic impairment. Children and elderly. Pregnancy.
Tác dụng không mong muốn
Significant: QT prolongation, extrapyramidal symptoms (including tardive dyskinesia), dyslipidaemia, significant weight gain, hyperprolactinaemia, orthostatic hypotension, syncope, leucopenia, neutropenia, agranulocytosis, somnolence, motor and sensory instability, seizures, priapism, oesophageal dysmotility/aspiration, hyperglycaemia, diabetes mellitus (including exacerbation of pre-existing diabetes; ketoacidosis [very rarely], and diabetic coma [rarely]), impaired core body temperature regulation, hypersensitivity reactions (including anaphylactic reactions and angioedema). Cardiac disorders: Tachycardia, bradycardia, atrioventricular block, conduction disorder. Eye disorders: Blurred vision. Gastrointestinal disorders: Abdominal pain or discomfort, nausea, vomiting, constipation, diarrhoea, dyspepsia, toothache, dry mouth. General disorders and administration site conditions: Pyrexia, asthenia, fatigue; inj site reactions (IM). Infections and infestations: Influenza. Investigations: Decreased weight, increased transaminases. Metabolism and nutrition disorders: Decreased or increased appetite. Musculoskeletal and connective tissue disorders: Musculoskeletal pain, back pain, arthralgia. Nervous system disorders: Sedation, dizziness, tremor, headache. Psychiatric disorders: Insomnia, agitation, anxiety, depression, mania. Renal and urinary disorders: UTI. Reproductive system and breast disorders: Amenorrhoea, galactorrhoea. Respiratory, thoracic and mediastinal disorders: Cough, nasal congestion, upper respiratory tract infection, bronchitis, sinusitis, pharyngolaryngeal pain. Skin and subcutaneous tissue disorders: Pruritus, rash. Vascular disorders: Hypertension. Potentially Fatal: Neuroleptic malignant syndrome (NMS).
This drug may cause somnolence, dizziness or blurred vision, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor mental status; vital signs (as clinically indicated); blood pressure (at baseline, 3 months after treatment initiation, then yearly); weight (at baseline then repeat as clinically indicated); CBC (as clinically indicated); electrolytes, renal and liver function (annually and as clinically indicated); fasting plasma glucose level/HbA1c (at baseline, 3 months after starting therapy, then yearly); fasting lipid panel (at baseline then 3 months after initiation of therapy). Monitor for signs and symptoms of tardive dyskinesia (every 12 months; every 6 months for high-risk patients), neuroleptic malignant syndrome, autonomic instability (e.g. tachycardia, cardiac dysrhythmia). Perform ocular examination yearly in patients >40 years or every 2 years in younger patients.
Quá liều
Symptoms: Extrapyramidal symptoms, gait unsteadiness, drowsiness, somnolence, tachycardia, hypotension, QT prolongation. Torsades de pointes and ventricular fibrillation may also occur. Management: Supportive and symptomatic treatment. For acute overdose, establish and maintain clear airway and ensure adequate oxygenation and ventilation. Initiate CV monitoring (e.g. ECG) immediately. Consider administration of activated charcoal together with a laxative. Hypotension and circulatory collapse may be treated with IV fluids and/or sympathomimetic agents (do not use epinephrine and dopamine). Administer an anticholinergic agent in cases of severe extrapyramidal symptoms.
Tương tác
Increased risk of QT prolongation with class IA (e.g. quinidine, procainamide) or class III (e.g. amiodarone, sotalol) antiarrhythmics, other antipsychotics (e.g. chlorpromazine, thioridazine), antibiotics (e.g. gatifloxacin, moxifloxacin), or any other class of medications known to prolong the QT interval; avoid concomitant use. May result in additive paliperidone exposure when administered concomitantly with risperidone. Enhanced CNS effects with centrally acting drugs. Concomitant use with psychostimulants (e.g. methylphenidate) may result in extrapyramidal symptoms upon change of either or both treatments. May antagonise the effect of levodopa and other dopamine agonists. Strong CYP3A4/P-glycoprotein (P-gp) inducers (e.g. carbamazepine) may reduce paliperidone concentration. Co-administration of valproate semisodium increases the concentration of oral paliperidone. Additive hypotensive effect may occur when given with drugs that have potential for inducing orthostatic hypotension.
Tương tác với thức ăn
Enhanced CNS effects with alcohol.
Tác dụng
Description: Mechanism of Action: Paliperidone is a benzisoxazole derivative atypical antipsychotic, which is the major active metabolite of risperidone. The exact mechanism for its antipsychotic action is unclear but may involve mixed central dopaminergic (D2 receptor) and serotonergic (5-HT2A receptor) antagonism. It is also an active antagonist at adrenergic (α1 and α2) and histaminergic (H1) receptors.
Synonym: 9-hydroxyrisperidone. Pharmacokinetics: Absorption: Bioavailability: 28% (oral). Time to peak plasma concentrations: Oral: Approx 24 hours; IM: Approx 13 days (monthly inj), 30-33 days (3-monthly inj), 29-32 days (6-monthly inj). Distribution: Enters breast milk. Volume of distribution: Oral: 487 L; IM: 391 L (monthly inj), 1,960 L (3- and 6-monthly inj). Plasma protein binding: 74%, mainly to α1-acid glycoprotein and albumin. Metabolism: Undergoes dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Excretion: Via urine (approx 80%; approx 59% as unchanged drug, 32% as metabolites); faeces (11%). Elimination half-life: Oral: Approx 23 hours; IM: 25-49 days (monthly inj); 84-95 days (3-monthly inj [deltoid]), 118-139 days (3-monthly inj [gluteal]); 148-159 days (6-monthly inj).
Đặc tính
Paliperidone Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 115237, Paliperidone. https://pubchem.ncbi.nlm.nih.gov/compound/Paliperidone. Accessed Mar. 31, 2022.
Bảo quản
Store between 15-30°C. Protect from moisture (tab). Store the 6-monthly inj in a horizontal position.
Đăng xuất
