Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders

  title={Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders},
  author={Atheir I. Abbas and Bryan L. Roth},
  journal={Expert Opinion on Pharmacotherapy},
  pages={3251 - 3259}
  • A. Abbas, B. Roth
  • Published 28 November 2008
  • Medicine, Psychology
  • Expert Opinion on Pharmacotherapy
Background: Pimavanserin tartrate is the first 5-HT2A inverse agonist to enter clinical trials as a treatment for L-dopa-induced psychosis in Parkinson's disease and for augmentation of low-dose risperidone treatment in schizophrenia. Pimavanserin is also being evaluated as a possible anti-insomnia drug. Objective: To discuss the potential of pimavanserin to fill multiple therapeutic needs. Methods: The problems with currently approved antipsychotics and sleep agents are explored to highlight… 
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    Journal of psychosocial nursing and mental health services
  • 2016
Based on its inverse agonist effect at 5HT2A receptors, pimavanserin may have potential for treating symptoms associated with the use of hallucinogen drugs and for treating akathisia associated with antipsychotic medications.
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Since the advent of chlorpromazine in the 1950s, D2 receptor antagonist activity has been synonymous with antipsychotic medications. This single mechanism of action may explain the similarities in
Role of 5-HT2A receptor antagonists in the treatment of insomnia
Overall, the polysomnography data strongly support an increase in slow-wave sleep and a decrease in waking after sleep onset following treatment with 5-HT2A receptor antagonists, although it has been more difficult to show subjective improvements in sleep with these agents.
Atypical antipsychotic agents were developed in response to problems with typical agents, including lack of efficacy in some patient s, lack of improvement in negative symptoms, and troublesome adverse effects, especially extrapyramidal symptoms (EPSs) and tardive dyskinesia (TD).
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A Comparative Review of New Antipsychotics
  • O. Blin
  • Psychology, Medicine
    Canadian journal of psychiatry. Revue canadienne de psychiatrie
  • 1999
A decision algorithm for comparing drugs used for psychotic disorders, based on biochemical profile, experimental pharmacology, postiron emission tomography (PET) scan results, and clinical efficacy on positive, negative, anxious, depressive, and cognitive symptoms is proposed.
H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs
It is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H1-histamine receptors, which are known to induce weight gain with chronic use.
Serotonin receptors represent highly favorable molecular targets for cognitive enhancement in schizophrenia and other disorders
Evidence is provided for and against the use of selective 5-HT receptor drugs as cognition enhancing agents for schizophrenia and other disorders, and it is likely that serotonergic drugs will soon be available as cognition enhances medications for disorders other than schizophrenia.
Placebo-controlled evaluation of four novel compounds for the treatment of schizophrenia and schizoaffective disorder.
The NK(3) and 5-HT(2A/2C) antagonists showed evidence of efficacy in the treatment of schizophrenia and schizoaffective disorder, and a smaller number of patients receiving placebo was permitted to test the efficacy of the four novel compounds.
PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain.
Administration of ACP-103 to healthy volunteers was found to be safe and well tolerated, and single oral doses were found to fully saturate 5-HT2A receptors in human brain as determined by PET.
Effectiveness of antipsychotic drugs in patients with chronic schizophrenia.
Olanzapine was the most effective in terms of the rates of discontinuation, and the efficacy of the conventional antipsychotic agent perphenazine appeared similar to that of quetiapine, risperidone, and ziprasidone.
The effects of clozapine, risperidone, and olanzapine on cognitive function in schizophrenia.
Atypical antipsychotic drugs as a group appear to be superior to typical neuroleptics with regard to cognitive function, however, available data suggest that these drugs produce significant differences in specific cognitive functions.
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For patients with schizophrenia who prospectively failed to improve with an atypical antipsychotic, clozapine was more effective than switching to another newer atypicals antipsychotics.
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The current pipeline of drugs for schizophrenia is discussed, outlining many of the strategies and targets currently under investigation for the development of new schizophrenia drugs and highlighting the importance of developing new paradigms for drug discovery in schizophrenia.