PALIPERIDONE

PALIPERIDONE
(pa-li'per-i-done)
Invega
Classifications: psychotherapeutic; antipsychotic, atypical;
Therapeutic: atypical antipsychotic
Prototype: Clozapine
Pregnancy Category: C

Availability

3 mg, 6 mg, and 9 mg extended release tablets

Action

Interferes with binding of dopamine to dopamine type 2 (D₂) receptors, serotonin (5-HT_2A) receptors, and alpha-adrenergic (alpha₁ and alpha₂) receptors.

Therapeutic Effect

Effective in controlling symptoms of schizophrenia as well as other psychotic symptoms.

Uses

Treatment of schizophrenia.

Contraindications

Hypersensitivity to paliperidone, isperidone; elderly with dementia-related psychosis; concurrent administration with drugs that produce QT_c 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.

Cautious Use

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

Schizophrenia
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)

Renal Impairment
Cl_cr50–79 mL/min: max 6 mg/d POCl_cr 10–49 mL/min: max 3 mg/d PO

Administration

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, headache, hypertonia, parkinsonism, somnolence, tremor. CV: Atrioventricular block, bundle branch block, ECG T-wave abnormalities, hypertension, orthostatic hypotension, QT_c prolongation, sinus arrhythmia, tachycardia. GI: Abdominal pain, dry mouth, dyspepsia, nausea, salivary hypersecretion. Metabolic: Increased insulin levels. Special Senses: Blurred vision.

Interactions

Drug: Enhanced CNS depression with alcohol 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.

Pharmacokinetics

Absorption: Bioavailability is 28%. Peak: 24 h. Distribution: 74% protein bound. Metabolism: In liver (26–41%). Elimination: Urine (major, 50–70% unchanged) and stool (minor). Half-Life: 23 h.

Nursing Implications

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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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