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Plasma antipsychotic concentration and receptor occupancy, with special focus on risperidone long-ac

Plasma antipsychotic concentration and receptor occupancy, with special focus on risperidone long-ac

  1. NeuroChi
    Abstract Although effective plasma concentration ranges have been established for some
    antipsychotics, conventional and atypical, there is considerable inter-patient pharmacokinetic
    variation. Positron-emission tomography (PET) can be used to estimate D2-like receptor
    occupancy in the brain needed for an antipsychotic effect and the level above which
    extrapyramidal side effects (EPS) develop. For conventional antipsychotics, the window
    occupancy is approximately 70—80%. For the atypical antipsychotic risperidone, the antipsychotic
    effect starts at approximately 60% occupancy, with occupancy above 80% leading to EPS.
    The new formulation, risperidone long-acting injectable (RLAI), comprises risperidone in a
    biodegradable polymer. It is effective long-term at doses of 25 or 50 mg injected i.m. every 2
    weeks. The constant and slow release of the long-acting formulation leads to less fluctuation in
    plasma levels and to a D2-like receptor occupancy which is below the threshold for EPS.
    D 2005 Elsevier B.V. and ECNP. All rights reserved.
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