Paliperidone


Concise Prescribing Info
Indications/Uses
Schizophrenia.
Dosage/Direction for Use
Adult : PO Initial: 6 mg once daily in the morning. If necessary, adjust in increments of 3 mg over at least 5 days. Usual range: 3-12 mg/day. IM Initial: 150 mg on day 1, then 100 mg after a wk. Admin the 3rd dose 1 mth after the 2nd initiation dose. Mthly maintenance dose: 75 mg. Usual range: 25-150 mg.
Dosage Details
Intramuscular
Schizophrenia
Adult: Initially, 150 mg on day 1, then 100 mg after a wk. Admin the 3rd dose 1 mth after the 2nd initiation dose. Mthly maintenance dose: 75 mg. Usual range: 25-150 mg.

Oral
Schizophrenia
Adult: Initially, 6 mg once daily in the morning. If necessary, adjust in increments of 3 mg over at least 5 days. Usual range: 3-12 mg daily.
Renal Impairment
Oral:
CrCl (mL/min) Dosage
≥10 to <50 Initially, 1.5 mg once daily, may be increased to 3 mg once daily thereafter.
≥50 to <80 Initially, 3 mg once daily, may be increased to 6 mg once daily, according to response and tolerance.
Intramuscular:
CrCl (mL/min) Dosage
≥50 to <80 Initially, 100 mg on day 1, then 75 mg after a wk. Mthly maintenance dose: 50 mg. Usual range: 25-100 mg.
Administration
May be taken with or without food. Take consistently either always w/ or always w/o food. Swallow whole, do not divide/chew/crush.
Contraindications
Hypersensitivity to paliperidone or risperidone.
Special Precautions
Patient w/ known CV disease or family history of QT prolongation, history of seizures or other conditions that potentially lower the seizure threshold, predisposition to GI obstruction, possible prolactin-dependent tumours, Parkinson's disease. Cataract surgery. Elderly w/ dementia-related psychosis and risk factors for stroke. Renal impairment. Pregnancy and lactation.
Adverse Reactions
Headache, dizziness, somnolence, sedation, agitation, fatigue, constipation, dyspepsia, dry mouth, nausea, vomiting, wt gain, akathisia, dystonia, hypertonia, tremor, tachycardia (including nasopharyngitis), blurred vision, orthostatic hypotension, arthralgia, back pain, pain in extremities, priapism, agranulocytosis, leucopenia, neutropenia. Rarely, tardive dyskinesia, small intestinal obstruction, hyperprolactinaemia resulting in gynaecomastia, menstrual disturbances, amenorrhoea, galactorrhoea.
Potentially Fatal: Neuroleptic malignant syndrome, CVA, transient ischaemic attacks.
IM/Parenteral/PO: C
Patient Counseling Information
This drug may cause somnolence and impairment of judgment, thinking or motor skills, if affected, avoid driving, operating machinery or performing hazardous tasks.
MonitoringParameters
Monitor mental status changes, vital signs, wt, BP, electrolyte, renal and hepatic function. Closely monitor for worsening glucose control in patients w/ pre-existing DM.
Overdosage
Symptoms: Drowsiness, sedation, tachycardia, hypotension, QT prolongation, extrapyramidal symptoms, torsades de pointes, ventricular fibrillation. Management: Symptomatic and supportive treatment. Establish and maintain a clear airway and ensure adequate oxygenation and ventilation. Treat hypotension and circulatory collapse w/ IV fluid and/or sympathomimetic agents. Consider gastric lavage and admin of activated charcoal w/ a laxative. In case of severe extrapyramidal symptoms, admin anticholinergic agents.
Drug Interactions
Increased risk of QT prolongation w/ class IA (e.g. quinidine, disopyramide) and class III (e.g. amiodarone, sotalol) antiarrhythmics. Additive effects w/ drugs that cause orthostatic hypotension (e.g. other antipsychotics, tricyclics). May antagonise actions of levodopa and other dopaminergics. Additive effect w/ drugs known to lower seizure threshold (e.g. phenothiazines or butyrophenones, clozapine, tricyclics or SSRIs, tramadol, mefloquine). May reduce plasma levels w/ carbamazepine. Enhanced central effects w/ other CNS depressants. May increase plasma levels w/ valproate. May affect the absorption w/ metoclopramide.
Food Interaction
Enhanced central effects of alcohol.
Action
Description: Paliperidone is a benzisoxazole atypical antipsychotic which is a main active metabolite of risperidone. It is an antagonist at dopamine D2, serotonin (5-HT2A), adrenergic (α1 and α2), and histamine (H1) receptors.
Pharmacokinetics:
Absorption: Bioavailability: 28%. Time to peak plasma concentration: Approx 24 hr (oral); approx 13 days (IM).
Distribution: Plasma protein binding: 74% (mainly to α1-acid glycoprotein and albumin).
Metabolism: Hepatic by CYP2D6 and CYP3A4 isoenzymes; minor metabolism via dealkylation, hydroxylation, dehydrogenation and benzisoxazole scission.
Excretion: Via urine (80%) and faeces (11%). Elimination half-life: Approx 23 hr (oral); 25-49 days (IM).
Chemical Structure

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Storage
Store below 30°C. Protect from moisture.
MIMS Class
Disclaimer: This information is independently developed by MIMS based on Paliperidone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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