Drug Design, Development and Therapy最新文献

{"title":"Remimazolam Suppresses Oxidative Stress and Apoptosis in Cerebral Ischemia/Reperfusion Injury by Regulating AKT/GSK-3β/NRF2 Pathway.","authors":"Mei Duan, Ning Yu, Jia Liu, Yang Zhao, Jing Zhang, Siyi Song, Shilei Wang","doi":"10.2147/DDDT.S478692","DOIUrl":"https://doi.org/10.2147/DDDT.S478692","url":null,"abstract":"<p><strong>Introduction: </strong>The mechanism of remimazolam, a benzodiazepine that activates γ-aminobutyric acid a (GABAa) receptors, in cerebral ischemia/reperfusion (I/R) injury is not well understood. Therefore, we explored whether remimazolam activates protein kinase B (AKT)/glycogen synthase kinase-3β (GSK-3β)/nuclear factor erythroid 2-related factor 2 (NRF2) to attenuate brain I/R injury in transcerebral I/R-injured rats and transoxygenic glucose deprivation/reperfusion (OGD/R)-injured SY5Y cells.</p><p><strong>Material and methods: </strong>Remimazolam was added at the beginning of cell and rat reperfusion, and the PI3K/AKT inhibitor LY294002 was added to inhibit the AKT/GSK-3β/NRF2 pathway 24 h before cellular OGD/R treatment and 30 min before rat brain I/R treatment. The viability and apoptosis rate of SY5Y cells, neurological deficit score, cerebral infarction volume and morphological changes of rat brain cells as well as the protein expression of Bax, Bcl2, Caspase 3, Cleaved-Caspase 3 and the number of TdT-mediated dUTP Nick-End Labeling (TUNEL)-positive cells in the penumbral region were detected. Reactive oxygen species (ROS), malondialdehyde (MDA), superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), NRF2, heme oxygenase 1 (HO-1), AKT, P-AKT, GSK-3β, P-GSK-3β protein expression, and nuclear translocation of NRF2 were measured in cell and animal assays.</p><p><strong>Results: </strong>Reduced SY5Y cell viability and increased apoptosis caused by OGD/R injury, elevated neurological deficit scores and cerebral infarct volume induced by brain I/R injury in rats, cerebral cell injury, as well as elevated Bax, Cleaved-Caspase 3, decreased Bcl2, and increased number of TUNEL-positive cells in rat brain tissue were all moderated by remimazolam. Decreased GSH-Px, SOD and Elevated MDA, ROS induced by OGD/R-injured SY5Y cells and brain I/R-injured rats were moderated by remimazolam. Meanwhile, remimazolam increased NRF2, HO-1, P-AKT, P-GSK-3β, and the nuclear accumulation of NRF2. The PI3K/AKT inhibitor LY294002 reversed the role of remimazolam in brain I/R injury.</p><p><strong>Conclusion: </strong>This study demonstrates that remimazolam activates the AKT/GSK-3β/NRF2 pathway, thereby attenuating oxidative stress and apoptosis to protect against brain I/R injury.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"111-128"},"PeriodicalIF":4.7,"publicationDate":"2025-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11725640/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143055868","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Review of the Therapeutic Potential of Ginseng and Its Bioactive Components in Nonalcoholic Fatty Liver Disease.","authors":"Liyuan Hao, Shenghao Li, Caige Li, Zhiqin Zhang, Xiaoyu Hu, Huimin Yan","doi":"10.2147/DDDT.S500719","DOIUrl":"10.2147/DDDT.S500719","url":null,"abstract":"<p><p>Non-alcoholic fatty liver disease (NAFLD) is the major cause of chronic liver disease worldwide, with no universally recognized effective treatments currently available. In recent years, ginseng and its principal active components, such as ginsenosides, have shown potential protective effects in the treatment of these liver diseases. In NAFLD, studies have demonstrated that ginseng can improve hepatic lipid metabolism, reduce inflammatory responses, and inhibit oxidative stress and fibrosis, thereby attenuating the progression of NAFLD. Additionally, ginseng inhibits oxidative stress by scavenging free radicals and enhancing antioxidant enzyme activities, and it can impede fibrosis by interfering with the fibrotic signaling pathways. These combined effects contribute to attenuating the progression of NAFLD. These findings highlight the promise of ginseng as a potential therapeutic candidate for the treatment of NAFLD. However, despite the significant efficacy of ginseng in human NAFLD treatment, the number and quality of clinical studies remain limited, with a lack of large-scale, multicenter clinical trials to confirm these effects. Moreover, the pharmacokinetic properties of different ginsenosides, optimal therapeutic dosages, and the safety of long-term use require further investigation. This review summarizes the existing evidence on the mechanisms of action of ginseng and its active components in human NAFLD, assesses their potential as therapeutic options, and proposes future research directions to provide stronger scientific support for clinical application. Additionally, we performed a network pharmacology analysis of ginseng in relation to NAFLD to identify and investigate potential targets of ginseng in the treatment of NAFLD. This analysis aims to provide a theoretical foundation for the development of ginseng -based drugs for combating NAFLD.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"83-96"},"PeriodicalIF":4.7,"publicationDate":"2025-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11725245/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142969999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"RET Inhibitor SPP86 Triggers Apoptosis and Activates the DNA Damage Response Through the Suppression of Autophagy and the PI3K/AKT Signaling Pathway in Melanoma Cells.","authors":"Yuli Zhang, Haidong Liu, Kun Wang, Juan Zheng, Hong Luan, Ming Xin","doi":"10.2147/DDDT.S473390","DOIUrl":"10.2147/DDDT.S473390","url":null,"abstract":"<p><strong>Background: </strong>Melanoma is a highly lethal form of skin cancer, and effective treatment remains a significant challenge. SPP86 is a novel potential therapeutic drug. Nonetheless, the specific influence of SPP86 on autophagy, particularly its mechanisms in the context of DNA damage and apoptosis in human melanoma cells, remains inadequately understood. Thus, this study aims to explore the effects of SPP86 on autophagy and to elucidate its association with cell proliferation, apoptosis, and DNA damage in melanoma cells.</p><p><strong>Methods: </strong>This study assessed the anti-tumor effects of SPP86 on cell viability, colony formation, apoptosis, and DNA damage in two melanoma cell lines, A375 and A2058. Concurrently, the underlying mechanisms, including the PI3K/AKT signaling pathway and autophagy modulation, were also elucidated.</p><p><strong>Results: </strong>The study demonstrated that SPP86 exerts anti-tumor effects in melanoma cells through multiple mechanisms: it induces apoptosis, causes DNA damage, inhibits cell proliferation, and suppresses the PI3K/AKT signaling pathway. Importantly, the inhibition of autophagy appears to be a critical component of SPP86' s mode of action, with the modulation of autophagic processes influencing the cytotoxicity against melanoma cells.</p><p><strong>Conclusion: </strong>These promising findings suggest that SPP86 is a potential drug candidate for the treatment of melanoma, warranting further research and development.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"67-82"},"PeriodicalIF":4.7,"publicationDate":"2025-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11724630/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142970003","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Potential Cardiovascular Risks Associated with Naltrexone-Bupropion Treatment in Overweight Patients [Response to Letter].","authors":"Young Sang Lyu, Hongyup Ahn, Sangmo Hong, Cheol-Young Park","doi":"10.2147/DDDT.S512114","DOIUrl":"10.2147/DDDT.S512114","url":null,"abstract":"","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"65-66"},"PeriodicalIF":4.7,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11721147/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142970000","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Scutellarein Inhibits Osteosarcoma Growth by Targeting the TLR4/TRAF6/NF-κB Pathway.","authors":"Yingxu Shi, Yu Tang, Zhiwei Sun, Ping Sui, Yiming Shao, Zhonghao Wang, Jian Zhang, Ming Gao","doi":"10.2147/DDDT.S489092","DOIUrl":"https://doi.org/10.2147/DDDT.S489092","url":null,"abstract":"<p><strong>Purpose: </strong>Osteosarcoma (OS) is the most common malignant tumor associated with poor patient outcomes and a limited availability of therapeutic agents. Scutellarein (SCU) is a monomeric flavone bioactive compound with potent anti-cancer activity. However, the effects and mechanisms of SCU on the growth of OS remain unknown.</p><p><strong>Methods: </strong>The Cell Counting Kit-8, colony formation assay and 5-ethynyl-2'-deoxyuridine (EdU) incorporation assays were used to analyze cell proliferation ability in vitro. TLR4/TRAF6/NF-κB signaling transduction was investigated by RNA sequencing analysis, quantitative real-time polymerase chain reaction, Western blotting, NF-κB luciferase reporter assay, immunofluorescent staining, and immunoprecipitation. Molecular docking and cellular thermal shift assay were employed to confirm the binding interaction between SCU and TLR4. The effects of SCU and TLR4 overexpression on OS growth were analyzed using a xenograft tumor model and immunohistochemical staining.</p><p><strong>Results: </strong>SCU was found to significantly inhibit OS cell proliferation, and RNA sequencing analysis suggested that the NF-κB pathway is closely associated with this process. Further studies revealed that SCU inhibited the canonical NF-κB pathway through its binding with TLR4, which disrupted the interaction of TLR4 and TRAF6. Moreover, SCU also repressed NF-κB signal transduction by inhibiting TLR4 expression. Furthermore, SCU was revealed to suppress OS cell proliferation by targeting TLR4 in vitro and in vivo.</p><p><strong>Conclusion: </strong>SCU exhibited a dual impact by inhibiting TLR4 expression and disrupting TLR4-TRAF6 interaction, resulting in NF-κB inactivation, thereby blocking OS growth.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"51-64"},"PeriodicalIF":4.7,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11720808/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143055874","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluating Avacopan in the Treatment of ANCA-Associated Vasculitis: Design, Development and Positioning of Therapy.","authors":"Jolijn R van Leeuwen, Luca Quartuccio, Juliana Bordignon Draibe, Iva Gunnarson, Ben Sprangers, Y K Onno Teng","doi":"10.2147/DDDT.S341842","DOIUrl":"https://doi.org/10.2147/DDDT.S341842","url":null,"abstract":"<p><p>Recently, avacopan has been approved for the treatment of ANCA-associated vasculitis (AAV). Avacopan is an inhibitor of the C5a-receptor, which plays an important role in chemotaxis and the amplification loop of inflammation in AAV. In the most recent, international guidelines avacopan is recommended as steroid-sparing agents for the management of AAV. Here, we review the clinical trials that have led to demonstrate that avacopan is an effective treatment option in the management of AAV, where it can significantly reduce the cumulative dosage of glucocorticoids (GC). Despite the new guideline recommendations, clear guidance on how to employ avacopan in real-world clinical practice is lacking. We therefore also address in this review the data and clinical experience with avacopan obtained from real-world evidence. Combining preclinical studies, clinical trials, and real-world evidence helps to provide a better position of avacopan for the management of AAV in routine clinical practice, taking advantage of the GC-sparing effects of avacopan as a possible solution for the current challenge of reducing GC-toxicity in AAV patients. Furthermore, we delineate current knowledge gaps and future research areas that need to be addressed.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"23-37"},"PeriodicalIF":4.7,"publicationDate":"2025-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11717651/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143055867","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Efficacy and Safety of Ciprofol for Anesthesia in Painless Colonoscopy with Varying Body Mass Indices Patients: A Prospective, Single-Center, Observational Study.","authors":"Yaqi Li, Mailong Yuan, Ping Zhang, Tao Zhou, Mingsheng Zhang, Jinhui Xu","doi":"10.2147/DDDT.S496783","DOIUrl":"https://doi.org/10.2147/DDDT.S496783","url":null,"abstract":"<p><strong>Background: </strong>Ciprofol, a novel intravenous anesthetic derived from propofol, exhibits high lipophilicity. Its pharmacokinetics and pharmacodynamics may vary across different body mass indices (BMI) categories, but data on its optimal dosing as well as its safety and efficacy during colonoscopy anesthesia in varying BMI groups are lacking.</p><p><strong>Objective: </strong>To evaluate the efficacy and safety of ciprofol during anesthesia for painless colonoscopy in patients with varying BMI, and to explore the correlation between BMI and induction dose.</p><p><strong>Methods: </strong>The BMI classification standard used in this study followed the criteria used in China. This prospective, single-center, observational study enrolled two hundred patients and they were divided into three groups with BMI: Group A (18.5-23.9 kg/m²), Group B (24-27.9 kg/m²), and Group C (28-39.9 kg/m²). Ciprofol was administered slowly (3 seconds per milliliter) until MOAA/S ≤1. Induction dose, additional ciprofol use, procedure duration, recovery time, vital signs, and adverse events were recorded.</p><p><strong>Results: </strong>The total induction dose was higher in Groups B and C than in Group A, with Group C receiving the highest dose (P<0.001). Dose per kilogram of TBW was lower in Groups B and C (P<0.001), while corrected body weight (CBW)-based dosing showed no significant difference between groups (P=0.287). There were no significant differences in procedure duration, recovery time, or adverse events among groups.</p><p><strong>Conclusion: </strong>Ciprofol is safe and effective for colonoscopy anesthesia across BMI groups, offering stable hemodynamics without prolonging recovery or increasing adverse events. CBW is a reliable dosing metric for overweight and obese patients.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"1-9"},"PeriodicalIF":4.7,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11707850/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143055865","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacokinetics and Bioequivalence of Two Fixed-Dose Combination Tablets of Valsartan/Amlodipine (80/5 Mg) in Healthy Chinese Subjects.","authors":"Mengli Tian, Jinlong Huang, Yingrong Chen, Qiuyue Jin, Hong Jiang, Cunyuan Shi, Jue Mei, Min Xu, Xiang Yu, Shuixin Yang","doi":"10.2147/DDDT.S485851","DOIUrl":"10.2147/DDDT.S485851","url":null,"abstract":"<p><strong>Purpose: </strong>The study aimed to investigate the pharmacokinetics and bioequivalence of coformulations of valsartan and amlodipine in healthy Chinese subjects under both fasting and fed conditions.</p><p><strong>Methods: </strong>The research was conducted under both fasting and fed studies and employed a single-center, randomized, open-label, single-dose, three-period design with partial-repeat and crossover elements. A total of 71 healthy Chinese adult participants were included under fasting (n = 36) and fed (n = 35) conditions. The subjects were orally administered valsartan/amlodipine tablets (80/5 mg) per cycle either as the test (T) or reference (R) formulation. The washout period was 14 days. Plasma concentrations of valsartan and amlodipine were determined using ultrahigh-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS), and the noncompartmental analysis method was used for estimating the pharmacokinetic parameters.</p><p><strong>Results: </strong>Under fasting conditions, the within-subject standard deviations (S_wr) of maximum plasma concentration (C_max), area under the concentration-time curve from time 0 to the time of the last-measurable plasma concentration (AUC_0-t), and area under the concentration-time curve from time 0 extrapolated to infinity (AUC_0-∞) for valsartan were calculated to be ≥0.294 and evaluated by the reference-scaled average bioequivalence (RSABE) method. The point estimates of the geometric mean ratios (GMRs) of C_max, AUC_0-t, and AUC_0-∞ for valsartan were 1.0805, 1.0991, and 1.1015 respectively, and the critical bounds were all less than 0. The S_wr of C_max, AUC_0-t, and AUC_0-∞ for amlodipine were all <0.294, and the 90% confidence intervals (CIs) of the GMRs fell within the bioequivalence range, as evaluated by the average bioequivalence (ABE) method. Under the fed condition, the S_wr of C_max, AUC_0-t, and AUC_0-∞ were all <0.294 for both valsartan and amlodipine; the ABE method was therefore employed for the evaluation of bioequivalence, and the 90% CIs of the GMRs fell within the bioequivalence range. All the observed adverse events were mild and transient.</p><p><strong>Conclusion: </strong>The two formulations of valsartan/amlodipine (80/5 mg) tablets were bioequivalent and safe.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"11-22"},"PeriodicalIF":4.7,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11705982/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142946443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"EC₅₀ and EC₉₅ of Remifentanil for Inhibiting Bronchoscopy Responses in Elderly Patients During Fiberoptic Bronchoscopy Under Ciprofol Sedation: An Up-and-Down Sequential Allocation Trial.","authors":"Hongmeng Lan, Susu Liu, Yeqing Liao, Bing Xu, Yuliu Lin, Xiaoshan Wu, Qiuling Chen, Huihe Chen, Xuehai Guan","doi":"10.2147/DDDT.S490907","DOIUrl":"https://doi.org/10.2147/DDDT.S490907","url":null,"abstract":"<p><strong>Background: </strong>Opioids are used to suppress cough during fiberoptic bronchoscopy (FOB). However, evidence regarding the optimal dose of remifentanil during FOB under ciprofol sedation is limited. This study aimed to investigate the effective concentration (EC) of remifentanil required to suppress bronchoscopy responses during FOB under ciprofol sedation in elderly patients.</p><p><strong>Materials and methods: </strong>Elderly patients aged 60 to 90 years with American Society of Anesthesiologists (ASA) physical status I-III, scheduled for FOB, were enrolled. Patients were assigned to either the male or the female group. Remifentanil was administered intravenously prior to ciprofol administration. The endpoints included responses to FOB, such as vocal cords movement, coughing, and body movement. The EC₅₀ and EC₉₅ values of remifentanil required to alleviate the responses to FOB were calculated using Dixon's up-and-down method for both male and female groups. Probit analysis was used to generate a dose-response curve.</p><p><strong>Results: </strong>Thirty-nine patients (19 males and 20 females) were enrolled. The EC₅₀ values (plasma concentration) of remifentanil for blunting FOB responses under ciprofol sedation were 3.25 (2.75 to 3.26) ng/mL and 2.25 (1.75 to 2.25) ng/mL in males and females, respectively (<i>p</i> = 0.0023). Probit analysis indicated that the EC₅₀ of remifentanil required to suppress responses to FOB under ciprofol sedation was 3.102 [95% confidence interval (CI):2.694 to 3.749] ng/mL and 2.052 [95% CI: 1.345 to 2.750] ng/mL in males and females, respectively. The EC₉₅ of remifentanil required to suppress responses to FOB under ciprofol sedation was 3.741 [95% CI: 3.366 to 7.699] ng/mL and 2.943 [95% CI: 2.456 to 9.533] ng/mL in males and females, respectively.</p><p><strong>Conclusion: </strong>The results indicate differences between males and females in the EC₅₀ and EC₉₅ of remifentanil needed to suppress responses to FOB under ciprofol sedation while preserving spontaneous breathing in elderly patients.</p><p><strong>Trial registration: </strong>The study was registered with chictr.org.cn (ChiCTR2300077720; 17 ^th November 2023).</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"6487-6497"},"PeriodicalIF":4.7,"publicationDate":"2024-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11699851/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142930907","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comparison of Remimazolam-Flumazenil and Propofol on Psychomotor Function and Emergence Following General Anesthesia in Surgical Abortion: A Randomized Controlled Trial.","authors":"Jinye Gu, Yang Liu, Xiaoyan Lin, Lei Fu, Jianbo Liu, Bona Sun, Xiaoyu Li, Bo Lu","doi":"10.2147/DDDT.S486892","DOIUrl":"https://doi.org/10.2147/DDDT.S486892","url":null,"abstract":"<p><strong>Objective: </strong> This study aims to compare the recovery profiles of remimazolam combined with flumazenil against those of propofol in patients undergoing painless surgical abortion, focusing on psychomotor function and emergence. Rapid recovery and restoration of psychomotor function are critical for enhancing patient safety and satisfaction in outpatient procedures like surgical abortion.</p><p><strong>Methods: </strong>A total of 110 patients scheduled for surgical abortion were randomly assigned to either the remimazolam group (Group R) or the propofol group (Group P) in a 1:1 ratio. Both groups received intravenous sufentanil for induction, followed by either remimazolam or propofol. Psychomotor function was assessed using the Digit Symbol Substitution Test (DSST) and Trieger Dot Test (TDT) at 30, 60, and 90 minutes post-anesthesia. Emergence parameters, including time to first eye opening and first verbal response, were recorded. Adverse events and hemodynamic parameters were also monitored.</p><p><strong>Results: </strong>The DSST scores at 30, 60, and 90 minutes post-anesthesia were similar between the Remimazolam group and the Propofol group (<i>F</i>=50.61, <i>P</i>>0.05, <i>η</i>²=0.0051). The TDT results were also comparable between the groups at all time points (<i>F</i>=0.12, 0.11 and 0.30, all <i>P</i>>0.05, <i>η²</i>=0.0002, 0.0003 and 0.0008). At 30 or 60 minutes post-anesthesia, DSST scores or TDT performance were significantly worse compared to preoperative baseline in both groups, indicating reduced psychomotor function (<i>P</i><0.05). The Remimazolam group showed significantly shorter times to first eye opening (54.48±3.45 s vs 99.22±11.78 s, <i>P</i>=0.0014, <i>Cohen's d</i>=5.15) and to obey verbal commands (61.85±3.78 s vs 131.1±12.79 s, <i>P</i><0.0001, <i>Cohen's d</i>=7.34) compared to the Propofol group.The incidence of injection pain and respiratory depression was significantly lower in the remimazolam group (<i>P</i><0.05), while hiccups were more common. Hemodynamic stability was maintained in both groups, with no significant differences in blood pressure or oxygen saturation (<i>P</i>>0.05).</p><p><strong>Conclusion: </strong> Remimazolam combined with flumazenil provides faster emergence and comparable psychomotor function to propofol in patients undergoing painless surgical abortion. This combination offers a promising anesthetic profile for procedures requiring quick recovery and minimal postoperative complications.</p><p><strong>Trial registration: </strong>ChiCTR2300075375, date of registration: 03/09/2023.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"6447-6457"},"PeriodicalIF":4.7,"publicationDate":"2024-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11697650/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142930897","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}