Abstract
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.
MeSH terms
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Antipsychotic Agents / administration & dosage
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Antipsychotic Agents / adverse effects
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Antipsychotic Agents / pharmacokinetics*
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Brain / drug effects
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Brain / metabolism
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Dose-Response Relationship, Drug
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Haloperidol / administration & dosage
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Haloperidol / adverse effects
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Haloperidol / pharmacokinetics
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Humans
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Isoxazoles / administration & dosage
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Isoxazoles / adverse effects
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Isoxazoles / pharmacokinetics*
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Metabolic Clearance Rate / physiology
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Piperidines / administration & dosage
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Piperidines / adverse effects
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Piperidines / pharmacokinetics*
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Receptors, Dopamine D2 / drug effects
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Receptors, Dopamine D2 / metabolism
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism
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Risperidone
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Schizophrenia / blood*
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Schizophrenia / drug therapy
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Schizophrenic Psychology*
Substances
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Antipsychotic Agents
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Isoxazoles
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Piperidines
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Receptors, Dopamine D2
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Receptors, Serotonin
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Haloperidol
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Risperidone