a novel approach on pharmacokinetic / pharmacodynamic correlations of risperidone: understanding its safety and efficacy profiles
| Autor: | Dalia Simona Miron, Carol Davila, Victor Voicu, Andrei Medvedovici, Flavian Ştefan Rădulescu |
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| Rok vydání: | 2010 |
| Předmět: |
Drug
Risperidone Endocrine and Autonomic Systems business.industry medicine.drug_class Endocrinology Diabetes and Metabolism medicine.medical_treatment media_common.quotation_subject Atypical antipsychotic Pharmacology Endocrinology Pharmacokinetics Pharmacodynamics Medicine business Antipsychotic Active metabolite Molecular entity media_common medicine.drug |
| Zdroj: | Acta Endocrinologica (Bucharest). 6:265-285 |
| ISSN: | 1843-066X 1841-0987 |
| DOI: | 10.4183/aeb.2010.265 |
| Popis: | The pharmacokinetic characteristics of a compound as well as the immediate consequences of its physicochemical behavior during interactions with biological structures, represent the key issues for its pharmacodynamic profile, starting from the most fundamental global aspects (i.e. central and / or peripheral action) to the most detailed ones (i.e. molecular mechanism of action). Successive metabolic reactions lead to either bioactivation or bioinactivation of the molecular entity. A particular importance is currently assigned to several molecular physicochemical descriptors, for instance the polarity degree (mirroring the changes of partition coefficients and of the permeability of biological structures), and emphasizing on distribution and renal excretion rate. The active metabolite (9-hydroxy-risperidone) of the atypical antipsychotic agent risperidone has an increased polar character and, consequently, its pharmacokinetic profile is modified compared to the parent drug: especially the penetration through the bood brain barrier and the efflux pump mediated transport were considered. In this context, the kinetic characteristics and their correlation with the pharmacodynamic properties for the two active entities, as well as the consequences dealing with the antipsychotic efficacy, the safety and efficacy profiles can be anticipated. The present approach critically asseses the available data from literature corroborated with the personal findings over the last years. |
| Databáze: | OpenAIRE |
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