More than half a century ago, Delay and colleagues have discovered, quite accidentally, that antihistamine (chlorpromazine) relieves psychotic symptoms. This discovery prompted further investigation through a series of performed experiments aimed to elucidate the antipsychotic mechanism of action. Initial results have shown that antipsychotic drugs in experimental animals lead to "neuroleptic effect" (indifference). However, not until the end of 1960s, it becomes clear that all previously known antipsychotics block dopamine receptors, particularly postsynaptic D2 receptors. The next three decades marked the development and application of these so-called classic neuroleptics in the treatment of psychotic patients. During the nineteen nineties, as a result of ongoing efforts to achieve greater efficiency and reduce the scope of side effects, novel antipsychotics were synthesized (second generation antipsychotics--SGA). As a result the notion of serotonin-dopamine antagonist (SDA) was formulated. According to one of the hypothesis, "new", so called atypical antipsychotic drugs strongly block the serotonin (5-HT2), and weakly block the dopamine (D2) receptors. Yet, there is still a debate as to the molecular basis of atypicality, whether it is in dopaminergic and serotonergic antagonism of neurotransmission or it lays exclusively in the modulation of dopaminergic system and dissociation rate at the level of D2 receptors in specific brain regions. Although the synthesis and use of antipsychotics in clinical practice have radically changed not only the basic approach to the patient, but also the quality of life of millions of people, the question remains whether this is just "old wine in new glasses".
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Pak J Pharm Sci
January 2025
Department of Psychiatry, the Fifth People's Hospital of Luoyang, Luoyang City, Henan Province.
To explore the effect of lithium carbonate combined with olanzapine on glucose and lipid metabolism, as well as gender differences in treating bipolar disorder (BD). 110 BD patients admitted to the Fifth People's Hospital of Luoyang from February 2022 to January 2024 were retrospectively included in the study. Patients were categorized into two groups based on treatment: The single group (lithium carbonate, n = 50) and the coalition group (lithium carbonate + olanzapine, n=60).
View Article and Find Full Text PDFPak J Pharm Sci
January 2025
Department of Psychiatry, Wenzhou Seventh People's Hospital, Wenzhou, China.
The objective of this study was to evaluate the therapeutic effects of Chiglitazar combined with Rosa roxburghii Tratt (RRT) in inpatients diagnosed with psychiatric disorders and antipsychotic-induced metabolic syndrome (MetS).100 cases were included and divided into the Siglitazar group (n=50) and the Siglitazar + RRT group (n=50) Anthropometric measurements, lipid and glucose metabolism indicators, inflammatory markers and PANSS scores were assessed at baseline, 8 weeks and 12 weeks post-treatment. Both treatment groups exhibited significant reductions in waist circumference and improvements in lipid profiles and glucose metabolism indicators over the 12-week study period.
View Article and Find Full Text PDFJ Affect Disord
January 2025
Department of Medicine, University of British Columbia, 2194 Health Sciences Mall, Vancouver, British Columbia V6T 1Z3, Canada. Electronic address:
Quetiapine, an atypical antipsychotic widely prescribed for conditions such as schizophrenia, bipolar disorder, and major depressive disorder, has been associated with a potential risk of pancreatitis. This study aimed to quantify the association between quetiapine use and the occurrence of pancreatitis using data from the FDA Adverse Events Reporting System. Disproportionality analyses were conducted to evaluate the frequency of pancreatitis reports linked to quetiapine compared to other drugs in the FAERS database.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
January 2025
University Clinic for Psychiatry and Psychotherapy, Brandenburg Medical School Immanuel Klinik Rüdersdorf, Seebad 82/83, Rüdersdorf bei Berlin, 15562, Rüdersdorf, Germany.
Sexual dysfunctions (SD) are common and debilitating side effects of antipsychotics. The current study analyzes the occurrence of antipsychotic-related SD using data from the US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). FAERS was queried for sexual dysfunction adverse events (encoded by 35 different MedDRA preferred terms) secondary to amisulpride, aripiprazole, chlorprothixene, clozapine, haloperidol, loxapine, olanzapine, pipamperone, quetiapine, risperidone, and ziprasidone from 2000 to 2023.
View Article and Find Full Text PDFJ Comput Chem
January 2025
Centre for Inflammation, Centenary Institute and University of Technology Sydney, Faculty of Science, School of Life Sciences, Sydney, New South Wales, Australia.
Phosphodiesterase 5 (PDE5) inhibitors have shown great potential in treating Alzheimer's disease by improving memory and cognitive function. In this study, we evaluated fluspirilene, a drug commonly used to treat schizophrenia, as a potential PDE5 inhibitor using computational methods. Molecular docking revealed that fluspirilene binds strongly to PDE5, supported by hydrophobic and aromatic interactions.
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