Drug Design, Development and Therapy最新文献

{"title":"Recent Developments in Drug Design of Oral Synthetic Free Fatty Acid Receptor 1 Agonists.","authors":"Lei Liu, Qinghua Zhang, Yichuan Ma, Ling Lin, Wenli Liu, Aizhong Ding, Chunjian Wang, Shuiping Zhou, Jinyong Cai, Hai Tang","doi":"10.2147/DDDT.S487469","DOIUrl":"10.2147/DDDT.S487469","url":null,"abstract":"<p><p>Over the past two decades, synthetic FFAR1 agonists such as TAK-875 and TSL1806 have undergone meticulous design and extensive clinical trials. However, due to issues primarily related to hepatotoxicity, no FFAR1 agonist has yet received regulatory approval. Research into the sources of hepatotoxicity suggests that one potential cause lies in the molecular structure itself. These structures typically feature lipid-like carboxylic acid head groups, which tend to generate toxic metabolites. Strategies to mitigate these risks focus on optimizing chemical groups to reduce lipophilicity and prevent the formation of reactive metabolites. Recent studies have concentrated on developing low-molecular-weight compounds that more closely resemble natural products, with CPL207280 showing promising potential and liver safety, currently in Phase II clinical trials. Moreover, ongoing research continues to explore the potential applications of FFAR1 agonists in diabetes management, as well as in conditions such as non-alcoholic fatty liver disease (NAFLD) and cerebrovascular diseases. Utilizing advanced technologies such as artificial intelligence and computer-aided design, the development of compact molecules that mimic natural structures represents a hopeful direction for future research and development.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5961-5983"},"PeriodicalIF":4.7,"publicationDate":"2024-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11646431/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142827729","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":"Determination of Nemonoxacin in Small Volumes of Rat Plasma and Bile by a Novel HPLC-Fluorescence Assay and Its Application to Disposition and Biliary Excretion Kinetics.","authors":"Ruei-Lin Wu, Wei-Chun Wang, Ching-Ling Cheng, Cheng-Yuan Tsai, Chen-Hsi Chou","doi":"10.2147/DDDT.S476173","DOIUrl":"10.2147/DDDT.S476173","url":null,"abstract":"<p><strong>Background: </strong>Nemonoxacin is a novel non-fluorinated quinolone antibiotic for the treatment of community-acquired pneumonia. To investigate the pharmacokinetics (PK) of nemonoxacin, a simple and sensitive high-performance liquid chromatography assay (HPLC) was needed.</p><p><strong>Methods: </strong>An HPLC method with fluorescence (FL) detection was developed for the quantification of nemonoxacin in plasma and bile. Ultraviolet (UV) and FL characteristics were examined for the optimal detection conditions. Nemonoxacin and the internal standard gatifloxacin were extracted from plasma utilizing ethyl acetate-isopropanol (70/30, v/v). For bile sample preparation, direct dilution with the mobile phase buffer was used. Chromatographic separation was achieved on a C6-phenyl column (5 μm, 25 cm × 4.6 mm i.d.) at 30 °C with a flow rate of 1 mL/min. The mobile phase was composed of methanol and 50 mM potassium dihydrogen phosphate containing 0.5% (v/v) triethylamine (pH 7.5) (45/55 and 35/65 (v/v) for plasma and bile samples, respectively). FL was measured at an emission wavelength of 465 nm with excitation at 285 nm.</p><p><strong>Results: </strong>The calibration curves were linear with a lower limit of quantification of 5 and 100 ng/mL in a small volume of plasma (50 μL) and bile (10 μL). The intra- and inter-day precision was within 9.0% and the accuracy was within 7.6% deviation of the nominal concentration. Nemonoxacin was stable under various storage/handling conditions tested. The method was successfully employed to describe the plasma and biliary profiles of nemonoxacin in rats following a single intravenous dose of 1 mg/kg. Nemonoxacin displayed two-compartment disposition kinetics. The bile-to-plasma area under concentration-time curve ratio (AUC_bile/plasma) estimated was 50.7, indicating that nemonoxacin was actively secreted into bile.</p><p><strong>Conclusion: </strong>A validated method was developed and found to be specific, precise and accurate. The applicability of this proposed method was substantiated in pharmacokinetic studies in rats.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5947-5960"},"PeriodicalIF":4.7,"publicationDate":"2024-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11646372/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142827643","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":"Intraoperative Use of Sodium Bicarbonate Ringer's Solution Instead of Sodium Lactate Ringer's Solution to Reduce Endothelial Glycocalyx Degradation and Improve Postoperative Recovery During Cardiopulmonary Bypass Cardiac Surgery: A Single-Center Prospective Cohort Study.","authors":"Yujie Shi, Yuan Shi, Yujia Tao, Bingyan Xu, Xiaoming Wang, Yanhu Xie, Min Zhang","doi":"10.2147/DDDT.S501657","DOIUrl":"10.2147/DDDT.S501657","url":null,"abstract":"<p><strong>Objective: </strong>To investigate the effect of sodium bicarbonate Ringer's solution (BRS) on the degradation of endothelial glycocalyx components in patients undergoing cardiopulmonary bypass (CPB) during cardiac surgery, and to evaluate its impact on endothelial glycocalyx preservation and postoperative recovery.</p><p><strong>Patients and methods: </strong>A total of eight patients scheduled for elective CPB heart surgery were included and randomly divided into two groups: the sodium lactate Ringer's solution (LRS) group and the BRS group. ELISA was used to measure plasma concentrations of syndecan-1, matrix metalloproteinase-9 (MMP-9), matrix metalloproteinase-3 (MMP-3), IL-6, IL-8, TNF-α, and TGF-β at predefined time points: T0 (before induction of anesthesia), T3 (immediately after weaning from CPB), T5 and T6 (24 and 72 hours postoperatively). Serum creatinine concentrations were measured within 48 hours postoperatively. The incidence of postoperative delirium (POD) was assessed three days after surgery. Postoperative mechanical ventilation time, duration of stay in the intensive care unit and hospital stay were also documented.</p><p><strong>Results: </strong>The BRS group had significantly lower plasma concentrations of syndecan-1 at T3 (7.98 [7.43, 8.92] ng/mL vs 9.54 [8.4, 10.73] ng/mL, <i>P</i> < 0.001) and T5 (4.20 [3.31, 4.96] ng/mL vs 5.40 [3.95, 6.55] ng/mL, <i>P</i> = 0.001) in comparison with the LRS group (<i>P</i><0.01). Syndecan-1 levels in both groups were similar at T6 (3.18 [2.88, 3.5]ng/mL vs 3.12 [2.77, 3.45] ng/mL, <i>P</i> > 0.05). Additionally, MMP-9, MMP-3, IL-6 and IL-8 were significantly lower at T3 and T5 in the BRS group (<i>P</i><0.05 and <i>P</i><0.01, respectively). However, no significant differences were observed between the two groups in the incidence of acute kidney injury (AKI) or POD (<i>P</i> > 0.05).</p><p><strong>Conclusion: </strong>BRS has the potential to reduce glycocalyx degradation in patients undergoing heart valve surgery with CPB. However, both groups demonstrated similar post-postoperative clinical outcomes, including the rates of AKI and POD.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5881-5893"},"PeriodicalIF":4.7,"publicationDate":"2024-12-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11645961/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142827722","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":"Effect of Remimazolam vs Midazolam on Early Postoperative Cognitive Recovery in Elderly Patients Undergoing Dental Extraction: A Prospective Randomized Controlled Study.","authors":"Bing Liu, Peijuan Wang, Lirong Liang, Wei Zhu, Hui Zhang","doi":"10.2147/DDDT.S491223","DOIUrl":"10.2147/DDDT.S491223","url":null,"abstract":"<p><strong>Purpose: </strong>Elderly patients undergoing dental extraction are particularly susceptible to delayed cognitive recovery after sedation. This study aimed to compare the effects of remimazolam and midazolam on early postoperative cognitive recovery in elderly patients undergoing dental extraction.</p><p><strong>Patients and methods: </strong>This was a single-centre randomized controlled study with elderly patients scheduled for receiving dental extraction under sedation of remimazolam (Group R) or midazolam (Group M). The primary outcome was postoperative cognitive recovery, as measured by the Montreal cognitive assessment 5-minute (MoCA 5-minute) 30 min postoperatively (T₃₀). Secondary outcomes included MoCA 5-minute score 1 h postoperatively (T_1h), incidence of post-extraction bleeding, intraoperative adverse events, success rate of sedation, time to discharge, and complications.</p><p><strong>Results: </strong>106 patients (53 in each group) were eligible for the study. At T₃₀, MoCA 5-minute score was 25 (IQR 23.5, 27) in Group R, significantly higher than that of 23 (IQR 21, 25) in Group M (P < 0.001). This difference persisted at T_1h [27 (IQR 26, 28) vs 26 (IQR 25, 27), P = 0.003]. Group R also exhibited better hemostasis, with a lower post-extraction bleeding rate at T₁ (5.67% vs 33.96%, χ² = 13.36, P < 0.001). Group R showed significantly shorter times to peak sedation after the first dose of medication, awake time, and time to discharge compared to Group M (P < 0.001, P < 0.001, P < 0.001).</p><p><strong>Conclusion: </strong>Remimazolam sedation significantly improves early postoperative cognitive recovery, leading to expedited hemostasis and a shorter discharge time.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5895-5904"},"PeriodicalIF":4.7,"publicationDate":"2024-12-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11639880/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142827716","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":"Clinical Utility of Various Formulations of Calcipotriene and Betamethasone Dipropionate for the Treatment of Plaque Psoriasis in Patients Aged 12 Years or Older.","authors":"Kamila Kędra, Adam Reich","doi":"10.2147/DDDT.S240867","DOIUrl":"10.2147/DDDT.S240867","url":null,"abstract":"<p><p>Plaque-type psoriasis is a chronic immune-mediated inflammatory skin disease of uncertain etiology, significantly impacting patient well-being. This chronic condition not only contributes to stigmatization and mental health challenges but also poses an independent risk for cardiovascular and other comorbid diseases. Affecting approximately 60 million people globally, psoriasis manifests primarily as mild-to-moderate disease in about 80% of cases, where topical therapy is pivotal. The most commonly used topical antipsoriatic therapy involves a combination of vitamin D3 analog (calcipotriene - Cal) and a synthetic potent corticosteroid (betamethasone dipropionate - BD). Various formulations of Cal/BD, including ointment, gel (topical suspension), and aerosol foam, have been approved by the US Food and Drug Administration (FDA). The cream based on the PAD (Polyaphron Dispersion) technology is another formulation of this combination drug, expanding the therapeutic options for patients with psoriasis. This article summarizes the most relevant published studies concerning the efficacy and safety of different calcipotriol and betamethasone formulations treating of plaque-type psoriasis in patients aged 12 or older.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5827-5839"},"PeriodicalIF":4.7,"publicationDate":"2024-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11636291/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142817181","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":"Safety, Tolerability and Pharmacokinetics of Intravenous Sodium Taurodeoxycholate, HY209, a GPCR19 Agonist Inhibiting Inflammasomal Activation.","authors":"Woo Kyung Chung, Inseung Jeon, In-Jin Jang, Seung-Yong Seong, Seon Ae Han, Kyung-Sang Yu","doi":"10.2147/DDDT.S438507","DOIUrl":"10.2147/DDDT.S438507","url":null,"abstract":"<p><strong>Background: </strong>HY209 is a synthesized sodium taurodeoxycholate (TDCA) that is expected to serve as a novel treatment for sepsis by inhibiting the inflammasomal activation that suppresses the production of pro-inflammatory cytokines. This study aimed to assess the safety, tolerability and pharmacokinetics (PKs) of HY209 after intravenous administration in healthy subjects.</p><p><strong>Methods: </strong>A dose-block randomized, double-blind, placebo-controlled, single ascending dose study was conducted. Eight subjects in each dose group were randomized to receive an intravenous administration of HY209 (0.1, 0.2, 0.4, 0.8 and 1.6 mg/kg) or a placebo at a 3:1 ratio. Safety and tolerability variables including adverse events (AEs) and vital signs were monitored. For the PK analysis, serial blood samples were collected for 72 hours at baseline and up to 24 hours post-dose. A power model was used to evaluate the dose-proportionality of HY209. Given that TDCA is an endogenous compound, time-matched baseline differences in plasma concentrations were analyzed.</p><p><strong>Results: </strong>A total of 39 subjects completed the study. All AEs were mild, and no serious AEs were observed. There was no significant correlation between the frequency of AEs and the administered dose. A circadian pattern was observed in the plasma TDCA concentration at baseline. After infusion, the plasma TDCA was rapidly eliminated; the plasma TDCA concentration at one hour after the end of infusion showed no significant differences from the baseline. The baseline-adjusted maximum plasma concentration of TDCA demonstrated dose-proportionality in a HY209 range of 0.1-1.6 mg/kg.</p><p><strong>Conclusion: </strong>A single intravenous administration of HY209 was well tolerated and its systemic exposure showed dose-proportionality in a dose range between 0.1 and 1.6 mg/kg.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5853-5861"},"PeriodicalIF":4.7,"publicationDate":"2024-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11636299/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142817173","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":"The Latest Progress in the Application of Telitacicept in Autoimmune Diseases.","authors":"Baocheng Liu, Yaqi Zhao, Dongxia Liu, Xinya Li, Zhenzhen Ma, Qingrui Yang","doi":"10.2147/DDDT.S493923","DOIUrl":"10.2147/DDDT.S493923","url":null,"abstract":"<p><strong>Introduction: </strong>Humoral immunity plays a key role in the pathogenesis of autoimmune diseases, and B-lymphocyte activating factor (BAFF) and a proliferation-inducing ligand (APRIL) are essential for the maintenance of B-lymphocyte reservoirs and humoral immunity. In March 2021, telitacicept, the world's first dual target three-channel biologic, was approved in China for the treatment of SLE and is currently in clinical trials exploring multiple indications for other autoimmune diseases.</p><p><strong>Areas covered: </strong>This article summarizes the mechanism of action, pharmacokinetics, and clinical efficacy of telitacicept for the treatment of multiple autoimmune diseases.</p><p><strong>Expert opinion: </strong>So far, the efficacy and safety of telitacicept in autoimmune diseases have been fully demonstrated in clinical practice. There are still many unresolved issues regarding the timing of initiation and discontinuation, still needs to be evaluated in future studies.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5811-5825"},"PeriodicalIF":4.7,"publicationDate":"2024-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11633291/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142812512","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 [Letter].","authors":"Linxuan Wu, Jian Hu, Peng Yao","doi":"10.2147/DDDT.S509093","DOIUrl":"10.2147/DDDT.S509093","url":null,"abstract":"","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5793-5794"},"PeriodicalIF":4.7,"publicationDate":"2024-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11633288/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142812507","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":"Effect of Intravenous Lidocaine Infusion on Propofol Dose and Perioperative Pain During Moderate Sedation-Analgesia for Hysteroscopy: A Randomized Controlled Trial.","authors":"Fan Yang, Jie Wang, Huiwen Zhang, Yonghai Zhang, Wanji Yang, Ran Gao, Jingfang Yu, Xuexin Chen, Hanxiang Ma","doi":"10.2147/DDDT.S484486","DOIUrl":"10.2147/DDDT.S484486","url":null,"abstract":"<p><strong>Purpose: </strong>In China, the majority of hysteroscopic procedures require moderate sedation and analgesia. The efficacy of intravenous lidocaine in reducing the need for sedatives and alleviating perioperative pain during hysteroscopy remains equivocal. This study aims to determine whether the intravenous administration of lidocaine can reduce the required dose of propofol and enhance perioperative pain management.</p><p><strong>Patients and methods: </strong>We conducted a prospective, single-center, double-blind randomized controlled trial involving patients with ASA I-II undergoing hysteroscopy. Forty patients were randomly assigned in a 1:1 ratio to either receive an intravenous bolus dose of 1.5 mg/kg lidocaine, followed by a continuous intravenous infusion at 4 mg/kg/h until the conclusion of the procedure, or an equivalent volume of normal saline. Propofol was then titrated to maintain a MOAA/S score of ≤ 2.</p><p><strong>Results: </strong>Compared with the control group, the lidocaine group showed a 13.8% decrease in the total dose of propofol (140.0[120.0, 155.0] mg vs 162.5[140.0, 197.5] mg), which was statistically significant (<i>P</i> = 0.014). The induction dose of propofol was 1.37 (1.29, 1.56) mg/kg in the lidocaine group and 1.61 (1.48, 1.94) mg/kg in the control group, respectively (<i>P</i> = 0.001). However, no significant differences were observed between the groups regarding the supplemental dose of propofol (<i>P</i> = 0.062), the number of involuntary movements during hysteroscopy (<i>P</i> = 0.384), or postoperative pain scores (T0: <i>P</i> = 0.628; T1: <i>P</i> = 0.886; T2: <i>P</i> = 0.711). Additionally, the incidence of intraoperative hypoxia (<i>P</i> = 1.000) and fatigue scores (T0: <i>P</i> = 0.878; T1: <i>P</i> = 0.401; T2: <i>P</i> = 0.056) between the two groups were not statistically significant.</p><p><strong>Conclusion: </strong>Intravenous lidocaine reduces the dose requirements of propofol during the induction phase of anesthesia. However, it does not have a significant influence on alleviating intraoperative and postoperative pain during hysteroscopic procedures.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5873-5880"},"PeriodicalIF":4.7,"publicationDate":"2024-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11633289/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142812297","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":"Effect of Pretreatment with a Small Dose of Esketamine on Myoclonus Induced by Etomidate: A Randomized Controlled Trial.","authors":"Liangliang Gao, Xinyu Lu, Aiping Tan, Jiaying Liufu, Yidan Xu, Lei Wei","doi":"10.2147/DDDT.S495130","DOIUrl":"10.2147/DDDT.S495130","url":null,"abstract":"<p><strong>Background: </strong>Etomidate has been observed to precipitate myoclonus in patients undergoing induction of general anaesthesia. This study was designed to investigate the effect of pretreatment with a small dose of esketamine on the incidence of myoclonus induced by etomidate.</p><p><strong>Methods: </strong>One hundred adult patients, who were scheduled to undergo selective operations with general anesthesia, were randomly divided into two groups, with one group receiving esketamine (Group E) and the other receiving normal saline (Group C). The group receiving esketamine (Group E) was administered an injection of 0.15 mg/kg of esketamine, while the control group (Group C) was given an equivalent volume of normal saline two minutes before the administration of 0.3 mg/kg of etomidate. The primary objective was to determine the incidence of etomidate-induced myoclonus. Secondary endpoints included the severity of etomidate-induced myoclonus and changes in haemodynamic variables at various time intervals. Additionally, the incidence of adverse effects such as dizziness, bradycardia, hypotension and hallucination were recorded from the administration of esketamine or normal saline to the injection of etomidate.</p><p><strong>Results: </strong>The incidence of myoclonus was significantly lower in Group E (20%) than in Group C (62%). Compared with the control group, the esketamine group also experienced a reduction in the moderate and severe of myoclonus. However, there was no statistically significant difference between the two groups for mild etomidate-induced myoclonus. The haemodynamic data (mean arterial pressure and heart rate) showed no statistically significant differences between two groups at the three time points. The incidence of dizziness, bradycardia, hypotension and hallucination was similar in both groups.</p><p><strong>Conclusion: </strong>Pretreatment with 0.15 mg/kg esketamine prior to anaesthesia induction with etomidate was observed to markedly reduce the incidence and severity of myoclonus, while having no effect on mild etomidate-induced myoclonus and maintaining a stable haemodynamic status.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"18 ","pages":"5773-5779"},"PeriodicalIF":4.7,"publicationDate":"2024-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11633297/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142812505","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}