Articles published on Sedative Effects
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- Research Article
- 10.13105/wjma.v14.i1.112793
- Mar 18, 2026
- World Journal of Meta-Analysis
- Amna Hassni + 13 more
BACKGROUND Dexmedetomidine (DEX) is a drug that is specifically an agonist for the alpha-2 adrenergic receptor, which has been explored for potential use in the provision of anesthesia during flexible bronchoscopy. Tactical mechanisms enable DEX to be able to provide sedation without marked respiratory depression hence aiding patients with poor respiratory reserve. AIM To investigate the safety and efficacy of DEX by examining heart rate, blood pressure, oxygen saturation, patient satisfaction and adverse effects. METHODS A meta-analysis following Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines was conducted across PubMed, Scopus, and the Cochrane Library. Randomized controlled trials comparing DEX with other sedatives (midazolam, remimazolam, propofol) during bronchoscopy were included. Primary outcomes were mean heart rate, mean oxygen saturation, and patient discomfort. Secondary outcomes included Ramsay Sedation Score, cough, pain and distress, ease of bronchoscopy, quality of sedation, composite scores, and adverse effects. A random-effects model was used for analysis. RESULTS Fourteen randomized controlled trials involving 1920 patients were finalized. Patients using DEX had a higher mean oxygen saturation throughout the procedure (P < 0.0003, I ² = 18%) and a decreased mean heart rate (P < 0.00001, I ² = 22%). Additionally, DEX significantly increased the incidence of bradycardia (P = 0.00001, I ² = 53%). The results show no difference in discomfort experienced by the patients when compared to the control groups. CONCLUSION Results show DEX to have a significant risk of bradycardia and hypotension. The effect on patient satisfaction was indeterminate; larger trials are required to confirm long-term safety and efficacy.
- Research Article
- 10.1177/87551225261426559
- Mar 10, 2026
- The Journal of pharmacy technology : jPT : official publication of the Association of Pharmacy Technicians
- Erin St Onge + 4 more
Objective: To review the efficacy, safety, and tolerability of a sublingual formulation of cyclobenzaprine for the treatment of fibromyalgia. Data Sources: A literature search was conducted through PubMed and DrugBank using the following terms: cyclobenzaprine, fibromyalgia, sublingual, Tonmya, and TNX-102 SL. Study Selection and Data Extraction: Articles describing the pharmacology, pharmacokinetics, efficacy, safety, and/or tolerability of sublingual cyclobenzaprine were included in this review. Data Synthesis: Cyclobenzaprine is a tricyclic antidepressant like agent which exhibits sedative and muscle relaxant effects in the treatment of fibromyalgia. Clinical trials have demonstrated improvements in daily pain scores compared with placebo. Common adverse events associated with this agent include oral hypoesthesia, oral paresthesia, and abnormal taste. Conclusions: Pharmacologic agents receive a weak recommendation for use in the treatment guidelines and include agents such as duloxetine, pregabalin, tramadol, amitriptyline, and a nonsublingual formulation of cyclobenzaprine. Tonmya, the newest agent approved for fibromyalgia, provides clinicians with an additional treatment option in a convenient dosage form for this potentially debilitating condition.
- Research Article
- 10.1007/s00210-026-05188-x
- Mar 9, 2026
- Naunyn-Schmiedeberg's archives of pharmacology
- Md Shadin + 7 more
Physcion (PHY), an anthraquinone derivative, has demonstrated various biological properties, including antioxidant and anti-inflammatory effects. This study aimed to evaluate the sedative activity of PHY in Swiss mice using in vivo and in silico approaches. The thiopental sodium (TS)-induced sleep model, fireplace test, and hole cross test were employed to assess sedation along with molecular docking studies. PHY significantly (p < 0.05) reduced sleep latency (17.29 ± 2.33min) and increased sleep duration (162.85 ± 8.38min) compared to controls at higher doses. It also significantly increased (p < 0.05) jump time and decreased the number of hole crosses. Co-administration of PHY with diazepam (DZP) enhanced sedation, while Co-administration with flumazenil (FLN) attenuated it, suggesting modulation of GABAA receptors. In silico molecular docking revealed a strong binding affinity (- 8.1 kcal/mol) of PHY with GABAA receptor subunits α1 and β2, comparable to DZP. Pharmacokinetic and toxicity predictions showed favorable profiles, supporting the potential of PHY as a sedative agent. Overall, PHY exhibited significant sedative effects likely mediated through the GABAergic pathway.
- Research Article
- 10.1186/s44158-026-00370-2
- Mar 4, 2026
- Journal of anesthesia, analgesia and critical care
- Majid Sezavar + 5 more
The benefits of Dexmedetomidne in sedation of mechanically ventilated pediatric patients are still challenging. In this study, we compared the efficacy and safety of Dexmedetomidine versus Midazolam for achieving deep sedation in pediatric patients receiving mechanical ventilation. A randomized clinical trial was conducted across three affiliated hospitals during February 2023 until February 2024. Eligible mechanically ventilated children aged 1month to 18years were randomized 1:1 to receive either Dexmedetomidine (0.25-1 mcg/kg/h) or midazolam (1-4 mcg/kg/min) for sedation, alongside fentanyl analgesia. Sedation was assessed using the Ramsey Sedation Scale and target scores set on 5-6. Primary outcomes included success rates in achieving target sedation at the beginning of mechanical ventilation; secondary outcomes encompassed hemodynamic adverse effects (hypotension, bradycardia), follow-up assessment of sedation level of successful patients over the next 6h, mortality rate, mean arterial blood pressures and heart rates (HR) changes, mechanical ventilation and PICU stay duration. Among 130 eligible patients, 120 were analyzed after exclusions (60 per group). Demographic characteristics were similar between groups. The primary outcome revealed that Dexmedetomidine was less effective than Midazolam in achieving target sedation levels across all ages (p < 0.001). In infants under one year, there was no significant difference in sedation effectiveness between the two medications (P = 0.157). Notably, Dexmedetomidine patients required higher drug doses to maintain sedation over 6h, while Midazolam patients experienced fewer adjustments (p < 0.001). Hemodynamic complications were significantly less frequent in the Dexmedetomidine group (3.3% vs. 23.3% for hypotension; p < 0.01). However, the two groups did not differ in terms of MAP and HR changes (P = 0.255; P = 0.063). Mortality, mechanical ventilation duration and length of PICU stay were not different between two groups (P = 0.853; P = 0.076; P = 0.082). Dexmedetomidine is inferior to Midazolam for deep sedation during mechanical ventilation in children aged 1month to 18years. However, it can be effective in infants under one year of age. Dexmedetomidine presents a lower risk of hemodynamic side effects compared to Midazolam. IRCT20190522043672N3 on February 16, 2023.
- Research Article
- 10.1097/ajn.0000000000000264
- Mar 1, 2026
- The American journal of nursing
- Brian Peach + 4 more
Survivors of acute respiratory distress syndrome (ARDS) frequently report vivid memories of their hospitalization. These memories can cause intense physical and emotional reactions. The COVID-19 pandemic contributed to a dramatic increase in ARDS incidence, but few studies have explored the nature and triggers of memories in postpandemic ARDS survivors. This qualitative study aimed to analyze the vivid memories and explore the multisensory memory triggers of adult ARDS survivors who received mechanical ventilation in the ICU between 2020 and 2023, during the COVID-19 pandemic. An interpretative phenomenological design was used. Semistructured interviews were conducted in person or via videoconference. Participants were asked to describe their most vivid memory from their ICU stay and any visual, auditory, olfactory, and tactile triggers of ICU-related memories. Interview data were analyzed using thematic analysis. A total of 35 ARDS survivors were interviewed. Five major themes and 17 subthemes emerged from the data. Major themes included the following: altered reality "dreams" while under the effects of sedation, recalled experiences of death, loss of control, bedside interactions, and multisensory triggers reminding survivors of real ICU environmental exposures and events. Nearly half the participants (n = 16; 46%) reported dreams as their most vivid memory. The term dreams was used because it was often unclear whether the memories occurred while participants were asleep or in a delirious state. Most participants (n = 31; 89%) reported at least one sensory memory trigger, with visual and auditory triggers the most common. Triggers often prompted the recall of factual ICU-related memories. Understanding the content and triggers of memories experienced by ARDS survivors can help guide nursing care across the health care continuum and facilitate interventions geared toward prevention and recovery.
- Research Article
- 10.1016/j.neuro.2026.103408
- Mar 1, 2026
- Neurotoxicology
- Kalinka Kendra Mayeski + 7 more
Promethazine provokes behavioral alterations and disrupts redox homeostasis in planarians.
- Research Article
- 10.1016/j.rvsc.2025.106019
- Mar 1, 2026
- Research in veterinary science
- Amanda L James + 5 more
Evaluation of the impact of acepromazine on tissue oxygenation in horses sedated with detomidine.
- Research Article
- 10.1016/j.ejmech.2025.118534
- Mar 1, 2026
- European journal of medicinal chemistry
- Xiaodi Zhang + 9 more
Rational design, synthesis and characterization of novel chimeric peptides containing the kappa-opioid agonists CR845 and dynorphin A-derived peptides.
- Research Article
- 10.1007/s00417-026-07174-8
- Feb 27, 2026
- Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie
- Kaori Morii + 4 more
WHAT IS KNOWN : •Low-concentration nitrous oxide (LCNO) has been used in dentistry and some ophthalmic procedures and is believed to reduce anxiety and discomfort. •Evidence for its sedative effect in cataract microsurgery has largely relied on subjective patient reports rather than objective monitoring. • This study provides objective evidence, using bispectral index (BIS) monitoring, that LCNO induces mild sedation during routine cataract microsurgery. •LCNO significantly reduced the BIS values during surgery without causing clinically relevant changes in the vital signs or adverse events, supporting its safety and practicality for outpatient cataract surgery.
- Research Article
- 10.3390/nano16050304
- Feb 27, 2026
- Nanomaterials (Basel, Switzerland)
- Fei Liu + 8 more
Linalyl acetate is a key bioactive component of essential oils with notable calming and sedative effects; however, its high volatility severely limits stability and practical application. Herein, bimodal mesoporous silica (BMMs) was employed as an efficient carrier to encapsulate linalyl acetate using liquid- and gas-phase loading strategies, enabling high loading capacity and sustained release. Under optimized gas-phase conditions (600 mg·mL-1, 85 °C, 2 h), a maximum loading capacity of 80.13% was achieved. The X-ray diffraction (XRD) and small-angle X-ray scattering (SAXS) patterns, scanning electron microscopy (SEM) images, N2 adsorption-desorption isotherms, Fourier transform infrared (FT-IR) spectra, and thermogravimetric (TG) performances confirmed the successful confinement of linalyl acetate within the bimodal mesoporous channels. Particularly, the SAXS patterns revealed the pronounced fractal characteristics, whereas the increased mass-fractal dimension (Dm) values indicated the enhanced structural compactness, and higher surface-fractal dimension (Ds) values reflected increased surface roughness upon loading. Release experiments conducted in an open environment demonstrated an excellent sustained-release performance, with only 22.41% of linalyl acetate released from BMMs over 30 days, compared with 94.41% for the free compound. Molecular dynamics simulations further elucidated that the interactions between linalyl acetate molecules and surface silanol groups dominated the adsorption process and governed diffusion within the mesoporous channels. These findings suggested that BMMs provide a robust platform for stabilizing volatile fragrance compounds and achieving long-term controlled release.
- Research Article
- 10.1136/emermed-2025-215690
- Feb 27, 2026
- Emergency medicine journal : EMJ
- Fredrick Smith + 3 more
Acute behavioural disturbance (ABD), formally known as excited delirium, is an under-recognised clinical picture often characterised by abnormal physiology and extreme agitation. The condition is potentially dangerous for both patients and practitioners, particularly in the prehospital setting. Our objective was to systematically review the evidence for management of ABD within the prehospital environment. A systematic literature search (PROSPERO CRD42023447238) of PubMed, Cochrane trials, Cochrane reviews, Embase, Web of Knowledge, Google Scholar and MEDLINE was performed from inception until February 2025. Any study that examined the management of ABD prehospitally was included. Randomised controlled trials, observational cohort studies and case series that were written in English were included. Methodological quality of included studies was interpreted using the ROBINS-I (Risk Of Bias In Non-randomised Studies - of Interventions) and GRADE (Grading of Recommendations Assessment, Development and Evaluation) approach. From 6091 studies, 42 were included; none were high quality and 6 were moderate quality. Ketamine demonstrated the most effective sedation (range 79-98% of all patients included achieving adequate sedation as defined in the studies), although doses and methods of administration varied significantly. Midazolam generally showed a higher number of side effects than other drugs studied. Droperidol was not found to have a higher mortality than others, and no effect was seen on the QT interval. Ketamine was found to be the most studied drug for treatment of ABD in the prehospital setting and is likely the most effective method of sedation at a dose of 5 mg/kg intramuscularly. Midazolam appears to have a higher risk of side effects, particularly respiratory-related, in comparison to other sedative agents. Conclusions are limited by the quality of evidence currently available and additional research is required to establish the most effective mode of administration and dose for this population group, as well as better definition of the presenting condition and outcome measures. CRD42023447238.
- Research Article
- 10.1038/s41390-026-04814-x
- Feb 26, 2026
- Pediatric research
- Athanasios Chamzas + 3 more
Therapeutic hypothermia (TH) is the standard of care for neonates with hypoxic-ischemic encephalopathy (HIE), but effective sedation remains a challenge. Opioids are widely used but are associated with respiratory depression, delayed enteral feeding, and neurodevelopmental concerns. This study assessed the efficacy, safety, and dose-response profile of dexmedetomidine as an alternative sedative. In this single-center retrospective cohort study, 163 neonates with HIE receiving TH between 2018 and 2024 were evaluated. Outcomes were compared between those receiving dexmedetomidine-based sedation (n = 61) versus opioid-only sedation (n = 102). Primary outcomes included cumulative opioid dose, sedation adequacy (NPASS), bradycardia <80 bpm incidence, and respiratory support needs. Dexmedetomidine was associated with 50% lower cumulative opioid exposure (46 vs. 95 μg/kg, p < 0.001), fewer rescue doses (3.3 vs. 5.0), shorter time to full enteral feeding (6 vs. 7 days, p < 0.001), and reduced mechanical ventilation (8.5% vs. 17%, p = 0.14). Sedation scores and hemodynamics were comparable. Bradycardia occurred in 41% of dexmedetomidine-treated neonates, leading to discontinuation in 30%. Dose-response analysis suggested efficacy plateaued above 0.5 μg/kg/hr, with increasing bradycardia risk. Dexmedetomidine was effective and generally well tolerated during TH. Infusion rates between 0.25 and 0.5 μg/kg/hr may optimize the balance of efficacy and safety. Dexmedetomidine use during therapeutic hypothermia in neonates with HIE reduced opioid exposure by 50% while maintaining sedation efficacy. Associated with earlier achievement of full enteral feeding and lower rates of mechanical ventilation compared with opioid-only sedation. Dose-response analysis identified an infusion range (0.25-0.5 μg/kg/hr) balancing sedation efficacy with bradycardia risk. Findings support dexmedetomidine as a viable first-line sedative during therapeutic hypothermia and inform safer dosing strategies.
- Research Article
- 10.3390/molecules31040752
- Feb 23, 2026
- Molecules (Basel, Switzerland)
- Kai Cheng + 12 more
The Acronicta major larva is a toxic agricultural pest that poses severe ecological management challenges. This study presents a sustainable strategy to valorize this hazardous biological waste into functional nanotherapeutics for insomnia by leveraging its unique intrinsic chemical composition. Carbon dots derived from Acronicta major larva (AM-CDs) were synthesized via one-step pyrolysis, which facilitated the natural molecular pre-assembly of N,S-codoping. Their physicochemical properties and cytotoxicity were evaluated using a series of characterizations and the CCK-8 assay. The sedative and hypnotic effects were assessed in mice with PCPA-induced insomnia through hot plate, Open Field and pentobarbital-induced sleep tests, and their potential mechanism was explored via neurotransmitter detection. The thermal process effectively eliminated intrinsic toxicity while retaining bioactivity via in situ heteroatom doping. AM-CDs exhibited favorable biocompatibility and significant sedative-hypnotic activity, reducing anxiety-related agitation without motor impairment. Mechanistically, AM-CDs effectively restored the GABA/5-HT/glutamate axis. Unlike direct central receptor binding, our findings suggest that this therapeutic effect is likely mediated through a systemic or peripheral regulatory pathway. This study demonstrates the conversion of toxic pests into safe and intrinsically bioactive nanomaterials, providing a dual solution for ecological pest management and novel neuroactive agent development, and validating the "Waste-to-Wealth" concept in biomedicine.
- Research Article
- 10.3390/healthcare14040517
- Feb 18, 2026
- Healthcare (Basel, Switzerland)
- Lyuboslav Katov + 8 more
Higher body mass index (BMI) is associated with a greater burden of cardiometabolic comorbidities that may potentially increase the risk of sedation-related complications. However, the impact of BMI on sedation safety during complex electrophysiological procedures (CEPs) remains uncertain. In this study conducted at Ulm University Heart Center, patients undergoing CEPs were stratified into three BMI groups: normal weight, overweight, and obesity. Primary and secondary endpoints were analyzed using univariable and multivariable logistic regression analyses. The primary composite endpoint (PCE) was the occurrence of sedation-related complications, defined as oxygen saturation below 90% combined with abnormal peripheral venous blood gas results-specifically, a venous carbon dioxide level exceeding 70 mmHg, an increase of more than 30% from baseline, or a pH drop below 7.25. Secondary endpoints included sedative and opioid requirements as well as occurrence of individual components of the PCE. A total of 726 patients were included, with 299 (42.3%) being female. The study population comprised 236 patients (32.5%) of normal weight, 265 (36.5%) overweight, and 225 (31.0%) obese. Patients with higher BMI presented with a greater burden of comorbidities and lower baseline oxygen saturation at the start of the procedure. While absolute sedative and opioid doses remained stable or even increased with BMI, relative doses (mg/kg) were higher in normal-weight patients. No significant differences were observed between BMI groups for either the primary or secondary endpoints. Female sex emerged as an independent predictor of adverse sedation events, with a higher incidence of reaching the PCE (p = 0.046, OR 1.411). BMI alone was not associated with an increased risk of sedation-related complications during CEPs. Despite higher absolute drug requirements and a greater comorbidity burden in overweight and obese patients, procedural safety was comparable across all BMI categories. These findings emphasize that individualized sedation protocols, embedded within standardized monitoring frameworks, are essential to ensure safe and effective sedation in diverse patient populations.
- Research Article
- 10.64898/2026.02.16.705777
- Feb 16, 2026
- bioRxiv : the preprint server for biology
- Erbo Dong + 3 more
Prenatal stress (PNS) is a well-established risk factor for neuropsychiatric vulnerability, yet its sex-specific behavioral consequences remain incompletely defined. Because males and females follow distinct neurodevelopmental trajectories, clarifying how early-life stress differentially shapes behavior is essential for developing targeted interventions. However, few preclinical studies directly compare male and female offspring within the same experimental framework, limiting the ability to identify true sex-dependent effects. Using a validated mouse model of gestational restraint stress, we conducted a comprehensive, within-study assessment of sex-dependent behavioral outcomes in adult offspring. Behavioral domains included locomotor activity, anxiety-like behavior, sociability, fear learning and extinction, recognition memory, and alcohol-related responses (ethanol preference and behavioral sensitivity), all measured using identical paradigms across sexes. PNS broadly disrupted behavior and cognition in both sexes, increasing locomotor activity and anxiety-like behavior, impairing fear extinction and recognition memory, and altering behavioral sensitivity to ethanol's sedative effects. Direct comparison revealed distinct sex-dependent vulnerabilities: males showed reduced social interaction, whereas females exhibited numerically greater impairment in fear extinction and a significantly stronger ethanol preference. Baseline fear responses, total fluid intake, and sucrose consumption were unaffected. Prenatal stress programs neurobehavioral trajectories in a sex-dependent manner, conferring vulnerability to anxiety-related behavior, cognitive disruption, and alcohol use. By directly comparing males and females within the same experimental design, this study provides one of the most integrated evaluations of sex-specific PNS outcomes to date and offers a robust framework for investigating the biological mechanisms underlying divergent pathways to stress-related psychopathology.
- Research Article
- 10.3760/cma.j.cn112140-20250922-00865
- Feb 12, 2026
- Zhonghua er ke za zhi = Chinese journal of pediatrics
- F Fang + 7 more
Objective: To characterize current practices and awareness regarding analgesia and sedation management among healthcare providers in pediatric intensive care unit (PICU) across China, and to explore the implementation status of related strategies. Methods: A two phase nationwide cross sectional questionnaire study (2018 and 2022 ) was conducted, involving 53 and 52 hospitals respectively across 22 provinces, 4 municipalities, and 5 autonomous regions. The study assessed the status and awareness of analgesia and sedation management. The questionnaire comprised 3 sections: demographic data (7 items), awareness level assessment (8 items), and implementation status (18 items). The differences were analyzed using the chi-square test or Fisher's exact probability test. Results: A total of 265 and 528 questionnaires were collected in 2018 and 2022,respectively. Analgesia and sedation practices were universally implemented across all participating PICU. In 2022, awareness of the organ-protective effects of analgesia and sedation, as well as recognition of delirium and withdrawal syndrome, was significantly higher than in 2018 (both P<0.001). The Facial Pain Scale was the most commonly used pain assessment tool, with utilization rates of 86.8% (46/53) in 2018 and 80.8% (42/52) in 2022. For sedation assessment, the Ramsay Sedation Scale ranked as the most prevalent tool, used in 85.0% (45/53) and 75.0% (39/52) hospitals in 2018 and 2022, respectively. The Comfort Behavior Scale (COMFORT) was used in 10 hospitals (18.9%) in 2018 and 18 hospitals (34.6%) in 2022, while its revised version (COMFORT-B) was used in 10 hospitals in both years (18.9% in 2018 and 19.2% in 2022), indicating limited clinical adoption. The most frequently administered analgesic was fentanyl, accounting for 40.0% (106/265) in 2018 and 22.5% (119/528) in 2022. The most common sedative was midazolam, accounting for 70.9% (188/265) and 37.9% (200/528) of use in 2018 and 2022, respectively. In 2022, the application rates of remifentanil and dexmedetomidine were both higher than those in 2018 (18.0% (95/528) vs. 5.7% (15/265), 22.3% (118/528) vs. 6.8% (18/265), χ2=22.46, 30.05, both P<0.001). The combination of fentanyl and midazolam remained the most frequently used analgesic-sedative regimen, accounting for 45.3% (120/265) in 2018 and 22.3% (118/528) in 2022, respectively. Conclusions: PICU clinicans, awareness of the organ-protective effects of analgesia and sedation, as well as the identification of withdrawal syndrome and delirium, has been significantly enhanced. The clinical utilization rate of remifentanil and dexmedetomidine has also increased notably in 2022. Moving forward, further standardization of analgesia and sedation protocols is imperative to optimize the quality of sedation-analgesia care in the PICU.
- Research Article
- 10.29296/25877313-2026-02-03
- Feb 12, 2026
- Problems of Biological Medical and Pharmaceutical Chemistry
- I Markin + 6 more
The increased interest in drugs containing substances derived from medicinal plant raw materials is a consequence of the search for new ways and methods of obtaining medicinal substances with fewer side effects compared to substances created synthetically. The composition of the skumpia tannic extract contains a large number of biologically active substances (BAS), where the leading place is occupied by flavonoids, phenolic carboxylic acids, glycosides, anthocyanins and terpenes. The analysis of domestic and foreign publications on the use of kozhevennaya scumpia as a source of valuable BAS for the needs of pharmaceutical and perfumery and cosmetics industries is presented. The analysis revealed that the substances con-tained in it are valuable, such as quercetin, kaempferol, which have anti-inflammatory effects, rutoside, which has angioprotective effects, rutin, which has antioxidant properties, hyperoside, which has antidepressant, sedative and anxiolytic effects, ferullic acid, which has cardioprotective, anti-arrhythmic effects. Russia has sufficient reserves of raw skumpia tannery to cover the needs of pharmaceutical production. As a result of a review of current scientific sources, it can be concluded that skumpia leatherworm has a rich chemical composition and is a promising medicinal plant for the production of BAS by industrial pharmacy in order to manufacture phytopreparations with wound-healing, antifungal, choleretic, immunomodulatory, sedative, antioxidant, cardioprotective and antitumor effects
- Research Article
- 10.3390/ph19020307
- Feb 12, 2026
- Pharmaceuticals (Basel, Switzerland)
- Jinyoung Park + 6 more
Background/Objectives: γ-Aminobutyric acid aminotransferase (GABA-AT) is a key enzyme responsible for GABA catabolism and represents a validated therapeutic target for epilepsy. Although existing GABA-AT inhibitors such as vigabatrin are clinically effective, their long-term use is limited by safety concerns, highlighting the need for alternative inhibitors with improved profiles. In this study, we employed an integrated natural product-oriented discovery strategy to identify novel GABA-AT inhibitors from plant-derived compounds. Methods: A library of 1006 plant-derived compounds collected from seven medicinal plants traditionally associated with sedative or anxiolytic effects was subjected to primary virtual screening using GNINA. Top-ranked candidates were further refined through secondary precision docking using aglycone forms to account for biologically relevant metabolic conversion. Detailed interaction analyses and molecular dynamics simulations were performed to assess binding stability and energetic favorability. Results: Based on computational prioritization, quercetin, salvianolic acid A, and scutellarein were selected for experimental validation. Cell-based GABA-AT activity assays in HepG2 cells demonstrated that quercetin and salvianolic acid A significantly inhibited intracellular GABA-AT activity, exhibiting comparable or greater efficacy than vigabatrin, while scutellarein showed moderate inhibition. The observed cellular inhibitory effects were consistent with predicted binding modes and dynamic stability observed in in silico analyses. Conclusions: Collectively, this study highlights the utility of an aglycone-focused, structure-based screening strategy for natural product drug discovery and identifies plant-derived aglycones as promising GABA-AT inhibitor candidates for further pharmacological development.
- Research Article
- 10.4274/tjar.2025.252107
- Feb 9, 2026
- Turkish Journal of Anaesthesiology and Reanimation
- Nesibe Sena Bayburt + 3 more
Procedural sedation management in geriatric patients undergoing cystoscopy requires careful monitoring due to age-related physiological changes and increased sensitivity to anaesthetic agents. Although both target-controlled infusion (TCI) and conventional total intravenous anaesthesia (TIVA) techniques with propofol are commonly used methods for sedation, their comparative effectiveness and safety in this population remain subjects of ongoing investigation. This study aims to compare the effectiveness of the two techniques in terms of time to induction, recovery time, hemodynamic stability, airway intervention requirements, and propofol consumption. This prospective, randomized study enrolled 60 male patients aged 65 years and older who were scheduled to undergo elective cystoscopy. Participants were randomly assigned to either the TCI group (n = 30) or the TIVA group (n = 30). The two groups were compared in terms of induction time, recovery time, hemodynamic parameters, airway interventions, and total propofol consumption. Compared with the TCI group, the TIVA group presented significantly shorter induction-to-surgery initiation and recovery times (P=0.009 and P=0.016, respectively). However, systolic blood pressure was more stable in the TCI group compared to the TIVA group (P=0.014). Propofol consumption per unit time was greater in the TIVA group (P=0.048), although total propofol usage did not differ significantly. Airway intervention was more common in the TIVA group, particularly in the early phase; however, this difference was not significant. Both TCI and TIVA are effective sedation techniques for geriatric cystoscopy. While TIVA provides faster induction and recovery, TCI offers better hemodynamic stability and may reduce propofol requirements. Further studies are recommended to confirm these findings in broader patient populations.
- Research Article
- 10.3390/ani16040537
- Feb 9, 2026
- Animals : an open access journal from MDPI
- Jingjing Wang + 4 more
Ocimum basilicum essential oil (OBEO) is an effective anesthetic and sedative for large yellow croaker (Larimichthys crocea) during live transport. This study aimed to assess the impact of OBEO on various physiological and biochemical parameters during live transport, thereby enhancing animal welfare and survival. Fish were exposed to 0 and 5 mg/L OBEO for 72 h during transport. Blood and liver samples were collected every 12 h after transport to evaluate blood biochemistry, tissue damage, oxidative stress-related and inflammation-related gene expression, intestinal microbiota, and liver metabolomics. The results demonstrated that the OBEO treatment significantly reduced serum cortisol levels and heat shock protein 70 (p < 0.05) while increasing the activity of liver antioxidant enzymes in large yellow croakers. Furthermore, compared to the control group, the expression of genes related to oxidative stress and inflammation was upregulated (p < 0.05), thereby enhancing the antioxidant and anti-inflammatory capacities of the fish. Microscopic examination of gill tissues revealed that OBEO alleviated morphological damage. Additionally, OBEO treatment altered the composition of intestinal microbiota, which contributed to the regulation of inflammatory responses. Moreover, liver metabolomics analysis identified key metabolic pathways, including arachidonic acid metabolism, steroid hormone biosynthesis, and amino acid metabolism, which could mitigate liver damage and enhance antioxidant and immune functions. In conclusion, OBEO effectively reduces transport stress in large yellow croakers through physiological, molecular, and metabolic mechanisms, providing a promising strategy to improve animal welfare and survival rate during live transport.