Adult Dosing & Uses
Dosing Forms & Strengths
tablet, extended-release
- 1.5mg
- 3mg
- 6mg
- 9mg
IM injectable suspension prefilled syringe
- 39mg
- 78mg
- 117mg
- 156mg
- 234mg
Schizophrenia
Oral
- 6 mg PO qAM; may titrate up or down, not to exceed 12 mg/day
- Titrate by dose increment of 3 mg/day at intervals of at least 5 days
IM
- Initial: 234 mg IM in deltoid muscle on treatment day 1, THEN 156 mg 1 week later
- Maintenance: 117 mg IM qMonth, some patients may require lower or higher doses (dose range 39-234 mg/month)
Renal Impairment
Oral
- CrCl 50-79 mL/min: No more than 6 mg/day
- CrCl 10-49 mL/min: No more than 3 mg/day
IM
- CrCl 50-79 mL/min: 156 mg IM in deltoid muscle on treatment day 1, THEN 117 mg 1 week later, THEN maintenance of 78 mg qMonth thereafter
- CrCl <50 mL/min: Use not recommended
Administration
Oral
- May take with or without food
- Swallow tablet whole with liquids, do not chew, crush or divide
IM
- Administer first 2 doses in deltoid muscle
- Maintenance dose may be administered in deltoid muscle or gluteal muscle
- Deltoid injection: use 1.5-in 22-ga needle for 90 kg or 1-in 23-ga needle if <90 kg
- Gluteal injection: use 1.5-in 22-ga needle regardless of patient weight
Pediatric Dosing & Uses
Dosing Forms & Strengths
tablet, extended-release
- 1.5mg
- 3mg
- 6mg
- 9mg
Schizophrenia
<12 years: Safety and efficacy not established
12-17 years (<51 kg): 3 mg PO qDay initially; may increase dose if needed, not to exceed 6 mg/day
12-17 years (51 kg or more): 3 mg PO qDay initially; may increase dose if needed, not to exceed 12 mg/day
Schizoaffective Disorder
<18 years: Safety and efficacy not established
Administration
May take with or without food
Swallow tablet whole with liquids, do not chew, crush or divide
Drug Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Akathisia
Somnolence
Tachycardia
Hyperprolactinemia
Some others similar to placebo (eg, headache)
<10% (selected)
Cough
Dystonia
Extrapyramidal symptoms
Orthostatic hypotension
QT prolongation
Sialorrhea
Priapism
Weight gain
Constipation
Indigestion
Contraindications & Cautions
Black Box Warnings
Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature.
This drug is not approved for the treatment of patients with dementia-related psychosis.
Contraindications
Documented hypersensitivity to paliperidone or risperidone
Any condition or drugs that prolong QT interval
Severe preexisting GI stenosis
Cautions
Avoid overheating and dehydration
History of seizures
Hyperprolactinemia occurs and persists during chronic administration
Prolongs QT interval modestly
Potential risk of neuroleptic malignant syndrome
Risk of orthostatic hypotension
FDA Warning regarding off-label use for dementia in elderly
Leukopenia/neutropenia and agranulocytosis reported; possible risk factors for leukopenia/neutropenia include pre-existing low white blood cell count (WBC) and history of drug-induced leukopenia/neutropenia ( if history of clinically significant low WBC or drug-induced leukopenia/neutropenia, monitor complete blood count (CBC) frequently during first few months of therapy; discontinue drug at first sign of a clinically significant decline <1000/mm3 in WBC in absence of other causative factors and continue monitoring WBC until recovery)
Metabolic changes
- Atypical antipsychotic drugs have been associated with metabolic changes that may increase cardiovascular/cerebrovascular risk
- These metabolic changes include hyperglycemia, dyslipidemia, and body weight gain
- Increased risk of hyperglycemia and diabetes; in some cases, hyperglycemia concomitant with use of atypical antipsychotics has been associated with ketoacidosis, hyperosmolar coma, or death
- While all of the drugs in the class have been shown to produce some metabolic changes, each drug has its own specific risk profile
Pregnancy & Lactation
Pregnancy Category: C
Neonates exposed to antipsychotic drugs during the 3rd trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery
These complications vary in severity; in some cases, symptoms have been self-limited, while in other cases neonates have required intensive care unit support and prolonged hospitalization
Lactation: excreted in breast milk, do not nurse
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Half-Life, Elimination: (oral) 23 hr, (IM) 25-49 days
Peak Plasma Time: (oral) 24 hr, (IM) 13 days
Bioavailability: 28%
Protein Bound: 74%
Vd: 487 L
Metabolism: by CYP2D6 & CYP3A4
Excretion: feces (11%); urine (80%)
Mechanism of Action
Antagonist of dopamine D2 & serotonin Type 2 (5HT2A) receptors
Also alpha blocker & H1 blocker
Major metabolite of risperidone
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