Pharmacological profile of risperidone.

The pharmacodynamics and pharmacokinetics of risperidone, an important atypical antipsychotic drug with potent serotonin-5-HT2 and dopamine-D2 receptor blocking effects, are presented. The pharmacology of atypical versus typical antipsychotic drugs is discussed in the contest of a pathophysiological conceptualization for schizophrenia which incorporates a parkinsonian model with an important role for serotonin and excitatory amino acid neurotransmission. In the normal therapeutic dose range, risperidone displays dose-linear pharmacokinetics in humans and reaches steady-state within 24 hours. Risperidone metabolism yields a active metabolite, 9-OH-risperidone, that has a similar pharmacological profile to the patient compound and therefore contributes to the clinical efficacy of the drug.