- The emergence of new antidepressants for clinical use: Agomelatine paradox versus other novel agents. [Review]
- IRIBRO Rep 2019; 6:95-110
- This study was designed with the rational aim of discussing the emerging antidepressant agents that are likely to bring positive landmark, tremendous improvement and significant impact to the managem…
This study was designed with the rational aim of discussing the emerging antidepressant agents that are likely to bring positive landmark, tremendous improvement and significant impact to the management of patients with depression disorders. It also elaborates on the Agomelatine paradox vis-a-vis the other novel antidepressant agents. The emerging antidepressants are: selective monoamine oxidase inhibitors (MAOIs) such as bifemelane, pirlindole, toloxatone, selegiline, rasagiline and safinamide; serotonin-norepinephrine reuptake inhibitors (SNRIs) such as ansofaxine, nefopam and levomilnacipran; norepinephrine reuptake inhibitors (NRIs) such as Reboxetine, viloxazine, teniloxazine (also known as sulfoxazine or sufoxazine), and atomoxetine; Vilazodone (a serotonin 5-HT1A autoreceptor partial agonist with serotonin reuptake inhibition [SPARI]); Vortioxetine (a serotonin receptors antagonist with serotonin reuptake inhibition [SARI]); atypical antipsychotics such as olanzapine, quetiapine, risperidone, lurasidone, aripiprazole and brexpiprazole; N-methyl-d-aspartate (NMDA)-glutamatergic neurotransmission system blockers such as ketamine, CP-101,606 (traxoprodil), GLYX-13 (rapastinel), NRX-1074 (Apimostinel) and Riluzole. While Agomelatine (a melatonergic MT 1 and MT 2 receptors agonist and a selective serotonergic 5-HT 2B and 5-HT 2C receptors antagonist [MASSA]) remains a paradoxical agent that doesn't fit into any of the currently available classes of antidepressant agents and its pharmacological properties also deemed it unfit and inappropriate to be classified into another separate novel class of antidepressants contrary to the reports published in previous reference literatures. Lastly, this review remarkably advocates for the incorporation of the atypical antipsychotics and NMDA-glutamatergic ionoceptor blockers as new member classes of the antidepressant agents because of their clinically significant roles in the management of depression disorders.
- Early antipsychotic exposure affects NMDA and GABAA receptor binding in the brains of juvenile rats. [Journal Article]
- PRPsychiatry Res 2019; 273:739-745
- Antipsychotics were developed to treat schizophrenia in adults; however they have been increasingly prescribed in children and adolescents. The NMDA and GABAA receptors are involved in neurodevelopme…
Antipsychotics were developed to treat schizophrenia in adults; however they have been increasingly prescribed in children and adolescents. The NMDA and GABAA receptors are involved in neurodevelopment and the pathophysiology of various mental disorders in children and adolescents. Male and female juvenile rats were treated orally with risperidone (0.3 mg/kg, 3 times/day), aripiprazole (1 mg/kg), olanzapine (1 mg/kg) or vehicle (control), starting from postnatal day (PD) 23 (±1 day) for 3 weeks (corresponding to the childhood-adolescent period in humans). Quantitative autoradiography was used to detect the binding density of [3H]MK-801 (an NMDA receptor antagonist) and [3H]muscimol (a selective GABAA receptor agonist). Aripiprazole elevated the [3H]MK801 binding levels in the NAcC of male rats, and the NAcS and CPu of female rats. Risperidone increased [3H]MK801 levels in the CPu of female rats, and the NAcS of male rats. Aripiprazole upregulated [3H]muscimol binding levels in the CPu and NAcC of male rats, while it elevated the [3H]muscimol levels in the PFC of female rats, compared to controls. These results suggest that early treatment with these antipsychotics modulates NMDA and GABAA neurotransmission in juveniles, which may play a role in their clinical efficacy in the control of mental disorders in children and adolescents.
- The Difference of Fasting Blood Sugar of Male Patients with Schizophrenia Treated with Flexible Dose between Aripiprazole and Risperidone in Medan, Indonesia. [Journal Article]
- OAOpen Access Maced J Med Sci 2019 May 15; 7(9):1446-1451
- CONCLUSIONS: This research revealed that based on the equivalence of risperidone and aripiprazole dosage given to the male patients with schizophrenia, the treatment using risperidone can significantly increase the fasting blood sugar level compared to the aripiprazole treatment in week 8.
- Comparative effectiveness of second generation long-acting injectable antipsychotics based on nationwide database research in Hungary. [Journal Article]
- PlosPLoS One 2019; 14(6):e0218071
- CONCLUSIONS: Our results indicate the superiority of second generation long-acting antipsychotics with regard to rates of treatment discontinuation and periods of persistence to the assigned medication.
- Model-Guided Antipsychotic Dose Reduction in Schizophrenia: A Pilot, Single-Blind Randomized Controlled Trial. [Journal Article]
- JCJ Clin Psychopharmacol 2019 Jun 10
- CONCLUSIONS: Although our model-guided dose reduction strategy was found to be comparable with no-dose change in terms of dropout rates, safety issues have to be further examined.
- The protective effect of resveratrol against risperidone-induced liver damage through an action on FAS gene expression. [Journal Article]
- GPGen Physiol Biophys 2019; 38(3):215-225
- The purpose of the study is to examine the protective effect of resveratrol on the fatty acid synthase gene expression against the side-effects of risperidone in an experimental model in rat liver. I…
The purpose of the study is to examine the protective effect of resveratrol on the fatty acid synthase gene expression against the side-effects of risperidone in an experimental model in rat liver. In this study, thirty-five female Spraque-Dawley rats were divided into five groups (n = 7): Control, RIS (2 mg/kg risperidone daily), RSV1 (2 mg/kg risperidone + 20 mg/kg resveratrol), RSV2 (2 mg/kg risperidone + 40 mg/kg resveratrol), and RSV3 group (2 mg/kg risperidone + 80 mg/kg resveratrol). On treatment day 15, liver tissue was taken for analysis. The resveratrol treatment significantly reduced weight gain as opposed to the risperidone administration. Moreover, the fatty acid synthase gene expression level increased significantly in RSV1 group (p = 0.011). In addition, resveratrol enhanced the total antioxidant status, high-density lipoprotein cholesterol levels and decreased alanine aminotransferase, aspartate aminotransferase, total cholesterol, gamma glutamyl transpeptidase, low density lipoprotein cholesterol, oxidative stress index, triglycerides, and total oxidant status levels significantly (p < 0.05). In conclusion, this study revealed that treatment with resveratrol might protect liver tissue against the side--effects of risperidone over fatty acid synthase gene expression. Resveratrol could be an effective course of therapy for enhancing therapeutic efficacy.
- Antipsychotic use is inversely associated with gastric cancer risk: A nationwide population-based nested case-control study. [Journal Article]
- CMCancer Med 2019 Jun 10
- CONCLUSIONS: Antipsychotic use was inversely associated with gastric cancer risk, and dose-dependent effects against gastric cancer were also seen with several individual antipsychotic compounds.
- Effect of minor manufacturing changes on stability of compositionally equivalent PLGA microspheres. [Journal Article]
- IJInt J Pharm 2019 Jun 07; 566:532-540
- The physicochemical properties and drug release characteristics of Q1/Q2 equivalent microspheres are sensitive to minor manufacturing changes, which may alter their stability under different storage-…
The physicochemical properties and drug release characteristics of Q1/Q2 equivalent microspheres are sensitive to minor manufacturing changes, which may alter their stability under different storage-conditions. This may be undesirable due to the presence of a substantial amount of drug in microsphere products. Hence, the objective of the present work was to investigate the impact of minor manufacturing changes on the stability of Q1/Q2 equivalent microspheres under various storage conditions. Two Q1/Q2 equivalent risperidone microsphere formulations prepared with minor manufacturing changes (solvent system etc.) showed differences in their physicochemical properties (size, morphology, porosity etc.), drug release characteristics and hence, storage stability. Overall, both formulations were stable under long-term storage conditions (4 °C/ambient humidity). However, under the intermediate storage conditions (25 °C/ambient humidity), only formulation 1 was stable while formulation 2 showed significant polymer degradation, particle aggregation and alteration in the drug release characteristics. Lastly, under accelerated storage conditions (40 °C/ambient humidity vs 75% RH), the extent of polymer degradation, morphological changes and alteration of drug release characteristics of formulation 2 was significantly higher compared to that of formulation 1. Thus, minor manufacturing changes have the potential to significantly alter the storage stability and, hence, the quality and performance of complex drug products such as microspheres.
- Correlation of hair risperidone concentration and serum level among patients with schizophrenia. [Journal Article]
- GPGen Psychiatr 2019; 32(1):e100042
- CONCLUSIONS: The correlation analysis showed that the concentration of RSP in hair was statistically significant with the serum RSP concentration. In this study, we provided some experimental basis for hair as a new biomaterial to monitor the therapeutic drug concentration.
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- Potentially inappropriate prescribing in people with dementia: an Australian population-based study. [Journal Article]
- IJInt J Geriatr Psychiatry 2019 Jun 07
- CONCLUSIONS: PIP was more common in people dispensed medicines for dementia than comparisons. These results highlight the need for effective interventions to optimise prescribing in people with dementia.