scholarly journals Atypical antipsychotic Lumateperone Beyond Schizophrenia: Seeking clarity in a time of Uncertainty

2022 ◽  
Author(s):  
Wael MY Mohamed

Lumateperone (ITI-007) is a serotonin 5HT2A tosylate salt with high affinity for dopamine D2 and D1 receptors and the serotonin transporter. It is unusual in that it controls serotonin, dopamine, and glutamate neurotransmission concurrently, all of which have been implicated in severe mental illness. Consider it a multi-targeted ligand and multifunctional modulator of the serotoninergic system with possible precognitive, antipsychotic, antidepressant, and anxiolytic properties. While lumateperone has been explored as a new agent for schizophrenia therapy, it also provides a unique therapeutic option for a range of other psychiatric and neurological diseases, including behavioural signs of dementia or Alzheimer's disease, sleep problems, and bipolar depression. Additionally, it had a better safety profile than placebo, with no significant extrapyramidal side effects, hyperprolactinemia, or changes in cardiometabolic or endocrine characteristics. Additional study is needed to validate and analyse lumateperone's effectiveness, as well as to identify prospective therapeutic targets. This article gives a comprehensive overview of the most notable results and potential future applications of this chemical in personalised medicine, particularly for neurodegenerative diseases.

2020 ◽  
Vol 19 (4) ◽  
pp. 243-247
Author(s):  
Marianna Mazza ◽  
Giuseppe Marano ◽  
Gianandrea Traversi ◽  
Gabriele Sani ◽  
Luigi Janiri

: Lumateperone (ITI-007) is a tosylate salt with binding affinities to receptors implicated in the therapeutic actions of antipsychotic medications, including the serotonin 5HT2A receptors, dopamine D2 and D1 receptors and the serotonin transporter. It has a unique mechanism of action because it simultaneously modulates serotonin, dopamine, and glutamate neurotransmission, implicated in serious mental illness. It can be considered a multi-target-directed ligand and a multifunctional modulator of serotoninergic system with possible precognitive, antipsychotic, antidepressant and anxiolytic properties. Lumateperone has been investigated as a novel agent for the treatment of schizophrenia, but it represents a new potential option for other psychiatric and neurological diseases, such as behavioural symptoms of dementia or Alzheimer’s disease, sleep disturbances, bipolar depression. Besides, it has demonstrated a favourable safety profile without significant extrapyramidal side effects, hyperprolactinemia or changes in cardiometabolic or endocrine factors versus placebo. Additional studies are warranted to confirm and examine the benefit of lumateperone and possible therapeutic targets. This paper is a comprehensive and thorough summary of the most important findings and potential future role of this particular compound in personalized treatments.


2018 ◽  
Vol 17 (10) ◽  
pp. 723-727 ◽  
Author(s):  
Marianna Mazza ◽  
Giuseppe Marano ◽  
Gianandrea Traversi ◽  
Valentina Carocci ◽  
Benedetta Romano ◽  
...  

Background & Objective: Cariprazine is a piprazine derivative approved by the FDA in 2015 for the treatment of schizophrenia and bipolar manic or mixed episodes in adults. High affinity for D3 dopamine receptors and observed actions on 5HT1A, 5HT2A and alpha 1B receptors differentiate it pharmacologically from other antipsychotics. This review is a comprehensive and thorough summary of the most important findings on cariprazine use in bipolar mania and depression. Pharmacokinetics, pharmacogenetics, tolerability and safety adverse effects are discussed in this paper. Results & Conclusion: Moreover, the results from pivotal clinical trials are presented. Cariprazine represents an additional option for clinicians to treat patients with bipolar disorder. It shows a unique pharmacological profile and has demonstrated in randomized clinical trials efficacy and general tolerability compared to placebo in bipolar mania and seem to be a promising therapeutic option for bipolar depression.


2020 ◽  
Vol 10 ◽  
pp. 204512532097379
Author(s):  
Danielle Hett ◽  
Steven Marwaha

Bipolar disorder (BD) is a debilitating mood disorder marked by manic, hypomanic and/or mixed or depressive episodes. It affects approximately 1–2% of the population and is linked to high rates of suicide, functional impairment and poorer quality of life. Presently, treatment options for BD are limited. There is a strong evidence base for pharmacological (e.g., lithium) and psychological (e.g., psychoeducation) treatments; however, both of these pose challenges for treatment outcomes (e.g., non-response, side-effects, limited access). Repetitive transcranial magnetic stimulation (rTMS), a non-invasive brain stimulation technique, is a recommended treatment for unipolar depression, but it is unclear whether rTMS is an effective, safe and well tolerated treatment in people with BD. This article reviews the extant literature on the use of rTMS to treat BD across different mood states. We found 34 studies in total ( N = 611 patients), with most assessing bipolar depression ( n = 26), versus bipolar mania ( n = 5), mixed state bipolar ( n = 2) or those not in a current affective episode ( n = 1). Across all studies, there appears to be a detectable signal of efficacy for rTMS treatment, as most studies report that rTMS treatment reduced bipolar symptoms. Importantly, within the randomised controlled trial (RCT) study designs, most reported that rTMS was not superior to sham in the treatment of bipolar depression. However, these RCTs are based on small samples ( NBD ⩽ 52). Reported side effects of rTMS in BD include headache, dizziness and sleep problems. Ten studies ( N = 14 patients) reported cases of affective switching; however, no clear pattern of potential risk factors for affective switching emerged. Future adequately powered, sham-controlled trials are needed to establish the ideal rTMS treatment parameters to help better determine the efficacy of rTMS for the treatment of BD.


2012 ◽  
Vol 30 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Eric Prommer

Olanzapine is an atypical antipsychotic agent of the thienobenzodiazepine class. Olanzapine blocks multiple neurotransmitter receptors, including dopaminergic (D1, D2, D3, and D4), serotonergic (5-hydroxytryptamine 2A [5-HT2A], 5-HT2C, 5-HT3, and 5-HT6), adrenergic (α1), histaminic (H1), and muscarinic (M1, M2, M3, and M4) receptors. Olanzapine has a high affinity for the 5HT2A receptor, which is up to 5 times greater than the dopamine receptor, resulting in less propensity to the development of extrapyramidal side effects. The affinity of olanzapine for multiple receptors has lead to the identification of olanzapine as an important agent in the treatment of delirium, nausea, and vomiting. Olanzapine has been demonstrated to have opioid-sparing properties. Olanzapine is principally metabolized by glucuronidation, with a smaller metabolic contribution from the cytochrome oxidase system. Adverse effects of olanzapine include somnolence, postural hypotension, constipation, dizziness, restlessness, and weight gain. The purpose of this article is to outline the pharmacodynamics, pharmacology, and evidence for the use of olanzapine in palliative care.


2015 ◽  
Vol 54 (3-4) ◽  
pp. 148-161 ◽  
Author(s):  
Attila Szijártó ◽  
András Fülöp

Background: Major liver resection is the only therapeutic option for patients with malignant liver tumors. However, extended hepatectomy often leads to postoperative liver failure, mainly due to insufficient amounts of the remnant liver. Recently, selective portal vein occlusion (PVO) has been introduced to increase the remnant liver volume. This novel surgical technique initiated a progressive development in liver surgery, resulting in a significant increment in potential candidates for curative liver resection. Summary: The theoretical basis for this great advancement is formed by an understanding of the mechanisms of PVO-induced liver regeneration, mainly obtained from animal studies. The aim of this review is to give a comprehensive overview of the relevant animal models of PVO and to discuss the main characteristics of triggered liver regeneration, including the induced hemodynamic, morphological and functional alterations as well as the underlying molecular mechanisms, which might be of interest in both the laboratory and the clinic. Key Messages: Although basic research revealed the main characteristics of PVO-triggered liver regeneration within the last decades, several important issues regarding the regenerative process remain uncertain. To answer these open questions, additional well-designed animal experiments are needed in the future, which allow further refinement of this surgical technique.


2020 ◽  
Vol 13 (10) ◽  
pp. 326
Author(s):  
Marek Krzystanek ◽  
Artur Pałasz

Bipolar disorder is a chronic and remitting mental illness. Antidepressants are not effective in treating acute bipolar depression, and antipsychotic drugs used in the treatment of bipolar depression cause frequent side effects. This situation justifies the search for new drugs as well as the repurposing of drugs used in other indications. In an open and naturalistic serious case study, 4 patients diagnosed with bipolar I disorder, chronically treated with a mood stabilizer, in whom at least two antidepressants were ineffective in the depressive phase, were treated with amantadine. The woman received 100 mg/day and 3 men received the target dose of 200 mg/day. All patients treated with amantadine improved their depressive symptoms after 1 week of treatment. None of them experienced side effects or manic switch. To reduce the risk of a manic switch, the treatment with amantadine was discontinued 2 weeks after the improvement of depressive symptoms, and no recurrence of depressive symptoms was observed. Amantadine may be a further therapeutic option for the treatment of acute bipolar depression. The drug in this indication may act quickly and be well tolerated. Confirmation of the antidepressant efficacy of amantadine in this indication requires replication of the results and conducting clinical trials.


2019 ◽  
Vol 25 (10) ◽  
pp. 1402-1411 ◽  
Author(s):  
Giampaolo Brichetto ◽  
Ludovico Pedullà ◽  
Jessica Podda ◽  
Andrea Tacchino

Wearable sensors are designed to be worn on the body or embedded into portable devices (e.g. smartphones and smartwatches), allowing continuous patient-based monitoring, objective outcomes measuring, and feedback delivering on daily-life activities. Within the medicine domain, there has been a rapid increase in the development, testing, and use of wearable technologies especially in the context of neurological diseases. Although wearables represent promising tools also in multiple sclerosis (MS), the research on their application in MS is still ongoing, and further studies are required to assess their reliability and accuracy to monitor body functions and disability in people with MS (pwMS). Here, we provided a comprehensive overview of the opportunities, potential challenges, and limitations of the wearable technology use in MS. In particular, we classified previous findings within this field into macro-categories, considered crucial for disease management: assessment, monitoring, intervention, advice, and education. Given the increasing pivotal role played by wearables, current literature suggests that for pwMS, the time is right to shift from a center-based traditional therapeutic paradigm toward a personalized patient-based disease self-management. On this way, we present two ongoing initiatives aimed at implementing a continuous monitoring of pwMS and, consequently, providing timely and appropriate care interventions.


2021 ◽  
Author(s):  
Mina Kelleni

In this communication we demonstrate the development of a novel neurological compound of combined valproic acid and topiramate (TopVal) which might offer a potential therapeutic option for epilepsy, refractory epilepsy as well as other neurological diseases currently managed by either drug. A lower administered dose might help to achieve a higher safety profile when enrolled for randomized clinical trials against either drug.


2018 ◽  
Vol 29 (6) ◽  
pp. 600-605
Author(s):  
Elena A Mermeklieva

Aims: The aim of this study is to evaluate pattern visual evoked potentials as an objective electrophysiological method and to create reference values for Bulgarian population. Methods and Materials: Standardized four-channel equipment ‘Neuro-MEP 4’ produced by ‘Neurosoft’ Company was used. A group of 47 healthy individuals (94 eyes) was studied. The stimulation was monocular, with a contrast-reversing pattern from black to white and vice versa. The investigation was performed with a three-channel recording with equipment adjustments according to the latest published ISCEV standard for pattern visual evoked potentials (2016). Based on a comprehensive overview of the available literature, a protocol of stimulating, amplifying and recording the obtained potentials has been created. The values of pattern visual evoked potential wave components, P50, N75, P100, N145 and P200, were measured. Results: Based on a created protocol, latency and amplitudes of the individual wave components of pattern visual evoked potentials were obtained. The results were statistically processed to create reference values of all pattern visual evoked potentials components, which are used as reference of the laboratory for the Bulgarian population. Conclusion: Pattern visual evoked potentials are objective electrophysiological method which is used to diagnose and monitor numerous ophthalmological and neurological diseases as well as for objective study of visual acuity and visual field in children and aggravation. The creation of pattern visual evoked potentials reference values for the Bulgarian population and its implementation in clinical practice are of particular importance for studying the visual analyser function.


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