[A new atypical antipsychotic with partial dopamine agonist effect (aripiprazole)].
Aripiprazole act as a partial agonist on the D2 receptors in contrast to the other antipsychotic agents which exert a pure antagonist action. In the autoreceptors with large receptor reserve aripiprazole shows primarily agonistic action, while postsynaptically its antagonistic action becomes predominant. In addition aripiprazole is an antagonist at the 5-HT2A, receptor and a partial agonist on the 5-HT1 receptor. On the basis of these receptor actions it is suggested that aripiprazole works as a stabilizer of both the dopaminergic and serotoninergic systems. Probably due to this dual stabilizing effect aripiprazole ameliorates positive and negative as well as anxiety and cognitive symptoms. Especially the very rare extrapyramidal symptoms, prolactine level elevation, QT-interval lengthening and absence of severe body weight increase and metabolic disturbances are noteworthy, which all seriously impair the health condition, the quality of life and the therapy adherence of the patients. Due to the very low affinity of aripiprazole to the H1 and muscarinic receptors aripiprazole practically does not lead to increase of body weight. The significant clinical efficacy coupled with good tolerability assures high level clinical effectiveness for aripiprazole in the broad clinical practice.
Kerpel-Fronius
Sándor
S
Semmelweis Egyetem, Farmakológiai és Farmakoterápiai Intézet, Budapest.
Lóránt
Miklós
M
D014150:Antipsychotic Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use*; D000068180:Aripiprazole; D018849:Controlled Clinical Trials as Topic; D018491:Dopamine Agonists / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use*; D019317:Evidence-Based Medicine; D006801:Humans; D015201:Meta-Analysis as Topic; D024821:Metabolic Syndrome / Q000139:chemically induced / Q000517:prevention & control; D010879:Piperazines / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use*; D015363:Quinolones / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use*; D058825:Serotonin 5-HT1 Receptor Agonists; D058830:Serotonin 5-HT2 Receptor Antagonists
D014150:Antipsychotic Agents; D018491:Dopamine Agonists; D010879:Piperazines; D015363:Quinolones; D058825:Serotonin 5-HT1 Receptor Agonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D000068180:Aripiprazole