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CHRISTIAN DOLDER, PHARM.D., BCPs, is Associate Professor, School of Pharmacy, Wingate University, Wingate, NC, and Clinical Pharmacist, NorthEast Medical Center, Concord, NC. MICHAEL NELSON, B.S.PHARM., PH.D., is Associate Professor; and ZACHARIAH DEYO is Pharm.D. candidate, School of Pharmacy, Wingate University.

Address correspondence to Dr. Dolder at the School of Pharmacy, Wingate University, Campus Box 3087, Wingate, NC 28174 (cdolder{at}wingate.edu).

Purpose. The efficacy, safety, pharmacology, pharmacokinetics, drug–drug interactions, and administration of paliperidone for schizophrenia are reviewed. Summary. Paliperidone is a benzisoxazole derivative and the principal active metabolite of risperidone. Representative of most oxidative metabolites, paliperidone is less lipophilic than risperidone. Like other atypical antipsychotics, paliperidone has a greater affinity for serotonin type 2A- receptor blockade relative to dopamine type 2-receptor blockade. Paliperidone’s advanced-generation osmotic release delivery system allows for the avoidance of dosage adjustment when initiating therapy and may decrease the frequency of antido-paminergic effects that would occur with an immediate-release formulation. The pharmacologic actions of paliperidone are similar to other high potency atypical antipsychotics. The receptor-binding profile of paliperidone most closely resembles that of risperidone and ziprasidone. Paliperidone differs from risperidone and most other antipsychotics by its relatively low extent of enzymatic metabolism. A limited number of investigations have demonstrated the ability of paliperidone to produce significant improvements in psychopathology, functioning, and relapse in patients with schizophrenia when compared with placebo. Paliperidone appears to have a similar adverse-effect profile compared to risperidone, except for an increased rate of hyperprolactinemia. The recommended dose of paliperidone for the treatment of adults with schizophrenia is 6 mg every morning. Conclusion. Paliperidone does not offer any clear advantage over other atypical antipsychotics with a similar receptor-binding profile, such as risperidone and ziprasidone. Nevertheless, a few investigations have demonstrated the ability of paliperidone to produce significant improvements in psychopathology, functioning, and relapse when compared with placebo. Based on limited studies, the frequency of adverse effects, except for hyperprolactinemia, appears to favor paliperidone over risperidone. Index terms: Antipsychotic agents; Dosage; Drug administration; Drug interactions; Mechanism of action; Paliperidone; Pharmacokinetics; Schizophrenia; Sustained action medications; Toxicity

 

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