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Hormonal and pharmacological manipulation of the circadian clock: recent developments and future strategies.

The mammalian circadian oscillator, located in the suprachiasmatic nuclei of the anterior hypothalamus, serves as the principal source of rh … potentially very large (Copinschi et al., 1995; Jamieson et al., 1998). For example, the effects of zolpidem vs. placebo on sleep, daytime alertness, and fatigue in travelers who complain of jet lag was co

Trazodone in the Management of Major Depression Among Elderly Patients with Dementia: A Narrative Review and Clinical Insights.

ObjectiveMajor depressive disorder (MDD) often co-occurs with dementia and other neurological disorders, and treatment with antidepressants can improve symptoms, quality of life, and survival in these patients. This narrative review provides an expert opinion about the role and effectiveness of trazodone in the treatment of older adults with MDD and cognitive impairment due to physical illnesses, such as dementia.ResultsBecause of its mechanism of action, trazodone can treat several depression symptoms often seen in people with dementia, including insomnia, agitation, anxiety, cognitive impair

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… Zopiclone use was associated with similar rates of injurious falls and major osteoporotic fractures and all-cause mortality compared with trazodone. 77 Interestingly, in a study of a total of 31,055 patients receiving maintenance hemodialysis, of whom 18,941 were zolpidem initiators (61%) and 12,114 … Zolpidem versus trazodone initiation and the risk of fall-related fractures among individuals receiving maintenance hemodialysis. Clin J Am Soc Nephrol . 2020;16(1):88–97. doi: 10.2215/CJN.10070620 79. Hwang T, Shah T, Sadeghi-Nejad H. A review of antipsychotics and priapism. …

Role of the alpha subunit in the modulation of GABA(A) receptors by anabolic androgenic steroids.

Neural transmission mediated by circuits expressing alpha2 subunit-containing gamma-aminobutyric acid type A (GABA(A)) receptors is critical for the expression of behaviors known to be altered by anabolic androgenic steroids (AAS). Here we show that micromolar concentrations of AAS, which reflect levels found in steroid abusers, induce positive modulation of currents from alpha2beta3 gamma2L recombinant receptors elicited by pulses of GABA that mimic synaptic conditions in a manner that is mechanistically distinct from modulation induced at alpha1beta3 gamma2L receptors. Specifically, at alpha

Sleep disturbances in a neuropathic pain-like condition in the mouse are associated with altered GABAergic transmission in the cingulate cortex.

Insomnia is a common problem for people with chronic pain. Cortical GABAergic neurons are part of the neurobiological substrate that underlies homeostatic sleep regulation. In the present study, we confirmed that sciatic nerve ligation caused thermal hyperalgesia and tactile allodynia in mice. In this experimental model for neuropathic pain, we found an increase in wakefulness and a decrease in non-rapid eye movement sleep under a neuropathic pain-like state. Under these conditions, membrane-bound GABA (γ-aminobutyric acid) transporters (GATs) on activated glial fibrillary acidic protein-posit

Non-benzodiazepine hypnotic use for sleep disturbance in people aged over 55 years living with dementia: a series of cohort studies.

BACKGROUND: Sleep disturbance affects around 60% of people living with dementia and can negatively affect their quality of life and that of their carers. Hypnotic Z-drugs (zolpidem, zopiclone and zaleplon) are commonly used to treat insomnia, but their safety and efficacy have not been evaluated for people living with dementia. OBJECTIVES: To estimate the benefits and harms of Z-drugs in people living with dementia with sleep disturbance. DESIGN: A series of observational cohort studies using existing data from (1) primary care linked to hospital admission data and (2) clinical cohort studie…

Identification of amino acid residues responsible for the alpha5 subunit binding selectivity of L-655,708, a benzodiazepine binding site ligand at the GABA(A) receptor.

L-655,708 is a ligand for the benzodiazepine site of the gamma-aminobutyric acid type A (GABA(A)) receptor that exhibits a 100-fold higher affinity for alpha5-containing receptors compared with alpha1-containing receptors. Molecular biology approaches have been used to determine which residues in the alpha5 subunit are responsible for this selectivity. Two amino acids have been identified, alpha5Thr208 and alpha5Ile215, each of which individually confer approximately 10-fold binding selectivity for the ligand and which together account for the 100-fold higher affinity of this ligand at alpha5-

Alzheimer's Disease: Cellular and Pharmacological Aspects.

Alzheimer's disease was described more than 100 years ago and despite the fact that several molecules are being tested for its treatment, which are in phase III trials, the disease continues to progress. The main problem is that these molecules function properly in healthy neurons, while neuronal pathology includes plasma membrane disruption, malfunction of various organelles, and hyperphosphorylation of Tau and amyloid plaques. The main objective of this article is the discussion of a neuronal restoration therapy, where molecules designed for the treatment of Alzheimer's disease would probabl

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… . | [ 46 ] Zolpidem | In progress | Benzodiazepine analog. | [ 46 ] Suvorexant | In progress | Orexin receptor antagonist. | [ 46 ] Velcade | RER use is suggested | Proteosome inhibitor, could be used in RER stress. | [ 47 ] Carfilzomib | Suggested use RER | Proteosome inhibitor. | [ 48 ] VX-809 | Suggested … Molecules That Reduce the Symptoms of the Disease Various drugs that can reduce the symptoms of AD have been tested, including escitalopram (serotonin reuptake inhibitors), methylphenidate (central nervous system stimulant), nabilone (cannabinoid agonist), zolpidem (benzodiazepine analogue), and suvorexant …

[Benzodiazepines and schizophrenia, a review of the literature].

AIn this work, the authors have analysed the principal studies on the interest in the use of benzodiazepines in schizophrenia. The first dou … eems to be specific of small doses of lorazepam (<5 mg/day). It should be compared to the effect of zolpidem in the same conditions. This prescription should be limited to acute catatonia, with no effect on chronic catatonia. Benzodiazepines and neuroleptic side effects - The use of benzodiazepines to treat some side effects of neuroleptics such as akathes …

Prevalence, putative mechanisms, and current management of sleep problems during chemotherapy for cancer.

Sleep problems are highly prevalent in cancer patients undergoing chemotherapy. This article reviews existing evidence on etiology, associated symptoms, and management of sleep problems associated with chemotherapy treatment during cancer. It also discusses limitations and methodological issues of current research. The existing literature suggests that subjectively and objectively measured sleep problems are the highest during the chemotherapy phase of cancer treatments. A possibly involved mechanism reviewed here includes the rise in the circulating proinflammatory cytokines and the associate

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… The most commonly prescribed sleep aids were lorazepam (31.4%) and zolpidem (29.4%). This study also found that patients with preexisting psychiatric issues and sleep problems were more likely to request and take sleep aids from their provider. … The majority of sleep aids (46%) used by the patients were prescription sedatives/hypnotics (eg, zolpidem, lorazepam) followed by 24% of patients taking analgesics (eg, ibuprofen). 118 Altogether, these findings show that a significant minority of patients diagnosed with cancer use sleep aids. …

Critically timed ethanol exposure reduces GABAAR function on septal neurons developing in vivo but not in vitro.

Six-day 'binge' ethanol intoxication postnatal days (PD) 4-9 delays up-regulation of gamma-aminobutyric acid type A receptors (GABAARs) in developing rat septal neurons [Dev. Brain Res. 130 (2001) 25]. This distortion occurs during synaptogenesis and could contribute to cognitive dysfunction in fetal alcohol syndrome (FAS). Here, we asked two questions concerning requirements for vulnerability to GABAAR blunting by ethanol. First, we asked whether receptor blunting required PD 4-9 ethanol exposure in rat pups and found that just a brief 2-day exposure (PD 8-9) was as effective as all 6 days. H

Anti-fracture Efficacy of Monthly Risedronate Compared with That of Weekly Risedronate in Postmenopausal Korean Women with Osteoporosis: A Nationwide Cohort Study.

BackgroundIntermittent dosing regimens for oral risedronate (once-monthly and once-weekly) were developed for patient convenience. While several studies have reported the anti-fracture efficacy of weekly dosing, few have assessed monthly dosing. The lower efficacy of monthly dosing has been previously suggested. The aim of this study was to compare the anti-fracture efficacy of monthly and weekly dosing.MethodsWe obtained information from the Korea National Health Insurance Service database from 2012 to 2017 of Korean women of ≥50 years of age who used weekly or monthly risedronate. We compare

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… Zolpidem use and risk of fractures: a systematic review and meta-analysis. Osteoporos Int. 2016;27:2935–44. doi: 10.1007/s00198-016-3605-8. 29. Kim DH, Lim H, Chang S, Kim JN, Roh YK, Choi MK. Association between body fat and bone mineral density in normal-weight middleaged Koreans. …

Increasing use of sodium nitrite in suicides-an emerging trend.

Sodium nitrite (NaNO2) is a compound with broad practical applications in food preservation, automotive maintenance, and animal control. Sodium nitrite is also potentially fatal when ingested, as it interferes with the ability of red blood cells to transport oxygen. While incidents of accidental consumption have been reported in the literature, case reports of sodium nitrite being used as a pharmacological suicide agent are becoming more frequent. Therefore, a study was undertaken to evaluate trends in sodium nitrite deaths in South Australia between 2000 and 2019. All cases of fatal sodium ni

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… located in desk drawer • Cylinders of nitrogen gas found under desk and in vehicle | • Early putrefactive changes • Blue-gray hypostasis • Brown discoloration of blood • Pulmonary edema and congestion • Urine dipstick positive for nitrite | • Alcohol (0.038%) • Metoclopramide (0.21) • Paracetamol (32) • Zolpidem …

Упорное использование опиоидов связано с более коротким выживанием миэломы.

Цель &quot; Превышение &quot; содержания опиоидов связана со значительным кризисом в области общественного здравоохранения, однако по-прежнему имеет решающее значение в качестве адъюнкт-процесса лечения во многих миеломах (ММ). Остаются вопросы о балансе между выгодами от продолжающегося использования опиоидов, особенно когда миэлома пациента находится в ремиссии. Этот ретроспективный обзор посвящен ассоциации хронического опиоида (COU) среди пациентов, преимущественно цветных. 174 В одном из городских медицинских центров были изучены пациенты, получившие аутологическую трансплантацию стволовы

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… Banerjee R, Lazar AA, Dunn L, Knoche J, Lo M, Arora S et al (2021) Benzodiazepine and zolpidem prescriptions during autologous stem cell transplantation. EJHaem 2(2):276–279 37. Del Fabbro E (2014) Assessment and management of chemical coping in patients with cancer. …

A randomized multicenter clinical trial to evaluate the efficacy of melatonin in the prophylaxis of SARS-CoV-2 infection in high-risk contacts (MeCOVID Trial): A structured summary of a study protocol for a randomised controlled trial.

OBJECTIVES: Primary objective: to evaluate the efficacy of melatonin as a prophylactic treatment on prevention of symptomatic SARS-CoV-2 inf … ption.Treatment with fluvoxamine.Treatment with benzodiazepines or benzodiazepine analogues such as zolpidem, zopiclone or zaleplon.Pregnancy.Breastfeeding.History of potentially immune derived diseases such as: lupus, Crohn's disease, ulcerative colitis, vasculitis or rheumatoid arthritis.Insulin-dependent diabetes mellitus.Known history of hypersensitivi …

:: 8th Европейский конгресс фармацевтики: выдержки из выступлений

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… Moreover, 24-h exposure to diazepam revealed sex-specific effects, with parallels to the human response to Zolpidem, an anti-insomnia medication. 8 Females exhibited pronounced anxiolytic effects and elevated GABA-A receptor expression in the telencephalon, aligning with human studies indicating slower … Questions and Answers: Risk of next-morning impairment after use of insomnia drugs; FDA requires lower recommended doses for certain drugs containing zolpidem (Ambien, Ambien CR, Edluar, and Zolpimist), https://www.fda.gov/drugs/drug-safety-and-availability/questions-and-answers-risk-next-morning-impairment-after-use-insomnia-drugs-fda-requires-lower …

Digital Life Coaching During Stem Cell Transplantation: Development and Usability Study.

BACKGROUND: For patients with multiple myeloma receiving high-dose chemotherapy followed by autologous stem cell transplantation (SCT), acute life disruptions and symptom burden may lead to worsened quality of life (QOL) and increased emotional distress. Digital life coaching (DLC), whereby trained coaches deliver personalized well-being-related support via phone calls and SMS text messaging, has been shown to improve QOL among SCT survivors. However, DLC has not been investigated during the acute peri-SCT period, which is generally characterized by symptomatic exacerbations and 2-week hospita

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… Benzodiazepine and zolpidem prescriptions during autologous stem cell transplantation. eJHaem. 2021 Feb 06;2(2):276–279. doi: 10.1002/jha2.148. 21. Mishkin AD, Shapiro PA, Reshef R, Lopez-Pintado S, Mapara MY. …

Marine Natural Products, Multitarget Therapy and Repurposed Agents in Alzheimer's Disease.

Alzheimer's disease (AD) is a multifactorial disease characterized by the presence of amyloid plaques, neurofibrillary tangles, and nerve cell death that affects, mainly, older people. After decades of investigation, the search for an efficacious treatment for AD remains and several strategies can be and are being employed in this journey. In this review, four of the most promising strategies, alongside with its most promising agents under investigation or development are highlighted. Marine natural products (MNP) are a source of unique chemical structures with useful biological activities for

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… Eight agents target neuropsychiatric symptoms such as agitation, apathy, and sleep disorders (AVP-786, AXS-05, brexpiprazole, escitalopram, methylphenidate, mirtazapine, nabilone, and zolpidem) and three agents are being studied as symptomatic cognitive enhancers ( Ginkgo biloba , guanfacine, octohydroaminoacridine …

15th Конгресс Европейской ассоциации клинической фармакологии и терапии (ЕАКПТ)

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Is Systemic Immunosuppression a Risk Factor for Oral Cancer? A Systematic Review and Meta-Analysis.

Even if the relationship between immunosuppression and increased incidence of systemic cancers is well known, there is less awareness about the risk of developing oral cancer in immunosuppressed patients. The aim of this review was to evaluate the association between immunosuppression and the development of oral cancer. Two authors independently and, in duplicate, conducted a systematic literature review of international journals and electronic databases (MEDLINE via OVID, Scopus, and Web of Science) from their inception to 28 April 2023. The assessment of risk of bias and overall quality of e

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… Relationship of zolpidem and cancer risk: A Taiwanese population-based cohort study Mayo Clin. Proc. 2012 87 430 436 10.1016/j.mayocp.2012.02.012 22560522 PMC3498427 158. Tandle A.T. Sanghvi V. Saranath D. Determination of p53 genotypes in oral cancer patients from India Br. J. …

Impact of physical exercise in cancer survivors during and after antineoplastic treatments.

Cancer patients experience symptoms and adverse effects of treatments that may last even after the end of treatments. Exercise is a safe, non-pharmacological and cost-effective therapy that can provide several health benefits in cancer patient and survivors, reducing cancer symptoms and cancer treatment side effects. The purpose of this review is to describe how the physical exercise is capable to reduce cancer symptoms and cancer treatment side effects. We realized a pragmatic classification of symptoms, dividing them into physical, psychological and psycho-physical aspects. For each symptom

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… Pharmacologic strategies include hypnotics (both benzodiazepine and non-benzodiazepine such as zopiclone and zolpidem), antidepressants, antihistamines and melatonin. …