The pharmacology and formulation of paliperidone extended release.

Paliperidone, or 9-hydroxyrisperidone (Invega(®), Janssen, Antwerp, Belgium) is the major active metabolite of the atypical antipsychotic risperidone (Risperdal(®), Janssen). It possesses a similar, though not identical, receptor pharmacology to the parent molecule. There are additional differences in terms of its predominant renal metabolism, lower protein binding and decreased inhibition of P-glycoprotein leading to decreased potential for drug-drug interactions.

Sustained drug delivery optimizes long-term treatment of patients with schizophrenia.

Chronic disorders such as schizophrenia require long-term treatment programs in order to maintain patients at the lowest level of symptomatology, reduce the likelihood of psychotic relapse, and support achievement of remission and recovery. Evidence suggests that treatment with long-acting injectable antipsychotics reduces the impact of partial compliance and provides predictable release of medication, assuring continuous therapeutic coverage. Until recently, only conventional antipsychotic agents were available in long-acting formulations, thereby foregoing the advantages of the atypical class.

Practical application of pharmacotherapy with long-acting risperidone for patients with schizophrenia.

Objective: It is now generally accepted that the use of second-generation, or atypical, antipsychotics for schizophrenia represents an advance over conventional antipsychotic agents. However, adherence continues to be a problem, as with other medications for chronic disorders. Long-acting formulations of conventional antipsychotics partly address adherence problems, but their use is limited by tolerability issues.