Paliperidone

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Information about Paliperidone

Paliperidone is a second generation (atypical) antipsychotic agent that is available in both oral and long acting parenteral forms and is used in the treatment of schizophrenia.

Liver safety of Paliperidone

Paliperidone is associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent acute liver injury.

Mechanism of action of Paliperidone

Paliperidone (pal" ee per' i done) is a second generation antipsychotic agent which appears to act as a dopamine type 2 (D2) and serotonin (5-HT)-2A receptor antagonist and is similar in structure and mechanism of action to risperidone. Indeed, paliperidone is the primary active metabolite of risperidone, its chemical name being 9-hydroxyrisperidone. Several randomized controlled trials have shown that oral paliperidone improves symptoms of schizophrenia and is comparable in effect to risperidone and ziprasidone.

FDA approval information for Paliperidone

Oral formulations of paliperidone were approved for use in the United States in 2006 as treatment for schizophrenia and schizoaffective disorder, as extended release tablets of 1.5, 3, 6 and 9 mg under the brand name Invega. Subsequently, parenteral formulations of paliperidone palmitate were developed that could be administered every one or three months. These palmitate formulations are given intramuscularly in varying doses and are available under the brand names Invega Sustenna and Invega Trinzia.

Side effects of Paliperidone

Common side effects of paliperidone include dizziness, dry mouth, somnolence, fatigue, nasal congestion, anxiety, restlessness and weight gain.

Paliperidone therapy is also associated with postural hypotension and prolongation of the QTc interval. The intramuscular formulations also can cause local injection site and hypersensitivity reactions. Rare, but potential severe adverse reactions (mentioned in most antipsychotic and antidepressant product labels) include tardive dyskinesia, major neurologic events, neuroleptic malignant syndrome, orthostatic hypotension, seizures and neutropenia.

Antipsychotic agents

First Generation

Second Generation (Atypicals)


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