Classifications: psychotherapeutic; antipsychotic, atypical; Therapeutic: atypical antipsychotic
Pregnancy Category: C
3 mg, 6 mg, and 9 mg extended release tablets
Interferes with binding of dopamine to dopamine type 2 (D2) receptors, serotonin (5-HT2A) receptors, and alpha-adrenergic (alpha1 and alpha2) receptors.
Effective in controlling symptoms of schizophrenia as well as other psychotic symptoms.
Treatment of schizophrenia.
Hypersensitivity to paliperidone, isperidone; elderly with dementia-related psychosis; concurrent administration with drugs
that produce QTc prolongation including Class IA or Class III antiarrhythmic medications, antipsychotic medications, and antibiotics that
prolong the QT interval; hyperglycemia, ketoacidosis; GI narrowing (pathologic or iatrogenic); children <18 y.
History of cerebrovascular events; hypovolemia, dehydration, concurrent administration of antihypertensives; cardiovascular
disease; renal impairment; older adults; history of hypotension; CNS pathology; systemic infection; diabetes mellitus, obesity,
family history of diabetes mellitus; history of seizures; Parkinson disease; disorders that may lead to aspiration pneumonia
(e.g., severe Alzheimer's dementia); potential for suicidality.
Route & Dosage
Adult: PO Initially 6 mg/d; may adjust up/down in 3 mg increments; at least 5 d intervals needed for dosage increments (max: 12 mg/d)
Clcr 5079 mL/min: max 6 mg/d POClcr 1049 mL/min: max 3 mg/d PO
- Extended release tablets must be swallowed whole. They should not be chewed or crushed.
- Give in the morning with or without food.
- Store at 15°30° C (59°86° F). Protect from moisture.
Adverse Effects (≥1%)Body as a Whole:
Back pain, cough, pain in extremity, pyrexia. CNS: Akathisia, anxiety,
asthenia, dizziness, dystonia, extrapyramidal disorder, fatigue
hypertonia, parkinsonism, somnolence,
Atrioventricular block, bundle branch block, ECG T-wave abnormalities, hypertension, orthostatic hypotension, QTc
prolongation, sinus arrhythmia, tachycardia. GI:
Abdominal pain, dry mouth, dyspepsia, nausea, salivary hypersecretion. Metabolic:
Increased insulin levels. Special Senses:
Enhanced CNS depression
or cns depressants
. Paliperidone may enhance the effects of antihypertensive agents
. Paliperidone can diminish the effects of dopamine agonists (levodopa, bromocriptine, cabergoline, pergolide, pramipexole, ropinirole). Food:
High fat/high caloric meal increases paliperidone levels.
Bioavailability is 28%. Peak:
24 h. Distribution:
74% protein bound. Metabolism:
In liver (2641%). Elimination:
Urine (major, 5070% unchanged) and stool (minor). Half-Life:
Assessment & Drug Effects
- Baseline ECG recommended to rule out congenital, long-QT syndrome.
- Prior to initiating therapy, hypokalemia and hypomagnesemia should be corrected.
- Monitor CV status and monitor BP especially in those prone to hypotension.
- Reassess patients periodically and maintain on the lowest effective drug dose.
- Monitor closely neurological status of older adults.
- Supervise closely those with suicidal ideation.
- Monitor closely those at risk for seizures.
- Assess degree of cognitive and motor impairment, and assess for environmental hazards.
- Lab tests: Baseline and periodic serum electrolytes; periodic blood glucose, and complete blood counts.
- Monitor diabetics for loss of glycemic control.
Patient & Family Education
- Exercise caution with hazardous activities until response to drug is known.
- Carefully monitor blood glucose levels if diabetic.
- Do not engage in potentially hazardous activities until the response to drug is known.
- Be aware of the risk of orthostatic hypotension.
- The shell of the tablet may be eliminated whole, but this does not mean the drug was not absorbed.
- Monitor for signs and symptoms of suicidal ideation.
- Be aware of the possibility of seizure activity.