BMC Pharmacology & Toxicology最新文献

{"title":"Exploration of the optimal concentration of quercetin liposome nanoparticles for the treatment of liver damage.","authors":"Nana Yin, Jian Pang, Xiangyan Liu","doi":"10.1186/s40360-025-00951-x","DOIUrl":"10.1186/s40360-025-00951-x","url":null,"abstract":"<p><strong>Background: </strong>Hepatic injury is a common pathological process for a wide spectrum of liver diseases. Quercetin has been found to counteract this process by scavenging free radicals, but its therapeutic effect is limited due to poor water-solubility. Thus, the question of how to deliver quercetin to a target organ effectively with minimal side effects has remained a clinical challenge. Our previous research findings indicate that when quercetin is delivered in the form of liposomal nanoparticles, its targeting efficiency to the liver is significantly enhanced. Although quercetin liposomal nanoparticles have been shown to improve the therapeutic effect on liver damage compared to traditional quercetin treatment, the optimal dosage of liposomal quercetin still warrants further exploration. The aim of this study was therefore to ascertain whether there are differences in the therapeutic effects on liver damage at different dosages of quercetin liposomes and to determine the optimal dosage.</p><p><strong>Methods: </strong>62 rats modeled with liver injury were enrolled and distributed into 4 groups, where they were treated with quercetin liposome nanoparticles, blank liposome nanoparticles, simple quercetin, and normal saline accordingly. Serum samples were measured for liver function indicators, and tissue samples were analyzed by pathohistological examination. Statistical analysis was performed to quantify the difference between the experimental and control groups.</p><p><strong>Results: </strong>Both liver function and histopathological examinations demonstrated enhanced therapeutic effects as the concentration of quercetin liposome drugs increased. Moreover, compared to traditional quercetin treatments, liposomal quercetin nanoparticles of varying concentrations uniformly provide better liver protection, with the highest dose group showing the best therapeutic effect. In addition, low concentration carrier liposome nanoparticles also showed a certain protective effect on the liver damage in rats.</p><p><strong>Conclusion: </strong>Liposomal quercetin nanoparticles exhibit superior efficacy in liver protection and repair compared to pure quercetin, with the highest dose group showing the best therapeutic effect.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"112"},"PeriodicalIF":2.8,"publicationDate":"2025-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12117872/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144172112","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The assessment of the relationship between anticholinergic burden and short-term blood pressure variability.","authors":"Cevdet Furkan Köşker, Reşit Emre Alparğan, Muhammed Ali Coşkuner, Gökhan Köker, Bilgin Bahadır Başgöz","doi":"10.1186/s40360-025-00952-w","DOIUrl":"10.1186/s40360-025-00952-w","url":null,"abstract":"<p><strong>Background: </strong>This study aimed to investigate the relationship between short-term blood pressure variability (BPV) and anticholinergic burden (ACB) in adults with hypertension.</p><p><strong>Methods: </strong>This study included 238 hypertensive patients aged 50 and older who underwent ambulatory blood pressure monitoring. The medications used by the patients were recorded, and the ACB of each medication was calculated using the ACB Scale. The BPV was assessed based on 24-hour ambulatory blood pressure measurements using three methods: standard deviation (SD), coefficient of variation of the standard deviation (SD-CoV), and weighted standard deviation (wSD), with evaluations conducted for both day-time and night-time periods.</p><p><strong>Results: </strong>A total of 139 patients (58.40%) had no ACB score, 64 (26.89%) had an ACB score of 1, and 35 (14.71%) had an ACB score of 2 or higher. ACB scores were significantly higher among patients with heart disease, and ACB tended to increase with age. However, no statistically significant relationship was found between ACB and mean blood pressure, nocturnal blood pressure dips, or any parameters of short-term BPV including Sd, SD-CoV and wSD.</p><p><strong>Conclusion: </strong>No significant association was found between ACB and short-term BPV. To the best of our knowledge, this is the first study to investigate this relationship, which may inspire further research.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"113"},"PeriodicalIF":2.8,"publicationDate":"2025-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12117873/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144172114","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ranolazine as a therapeutic agent for diabetic cardiomyopathy: reducing endoplasmic reticulum stress and inflammation in type 2 diabetic rat model.","authors":"Matin Mohyadini, Aghele Fahimi, S Zahra Bathaie, Hamid Yaghooti","doi":"10.1186/s40360-025-00945-9","DOIUrl":"10.1186/s40360-025-00945-9","url":null,"abstract":"<p><strong>Background: </strong>Diabetic cardiomyopathy (DCM) is a significant cardiovascular complication of diabetes, characterized by structural and functional heart muscle dysfunction. Oxidative stress, endoplasmic reticulum (ER) stress, and inflammation are pivotal in the pathogenesis of DCM. Ranolazine, primarily used for angina, has demonstrated potential cardioprotective effects. This study investigates the effects of ranolazine on oxidative stress, ER stress, and inflammation in the heart tissue of type 2 diabetic rats.</p><p><strong>Methods: </strong>Diabetes was induced in male Wistar rats using Nicotinamide (110 mg/kg) and Streptozotocin (60 mg/kg). The rats were then divided into control and diabetic groups, with further subdivision into ranolazine-treated and untreated subgroups. Ranolazine was administered via gavage for eight weeks. Various parameters, including body weight, heart weight, serum glucose, troponin-I levels, oxidative stress markers, ER stress markers, and inflammatory markers, were assessed.</p><p><strong>Results: </strong>Diabetic rats showed increased heart weight and decreased body weight over eight weeks. Ranolazine treatment improved body weight but didn't affect serum glucose levels. The treatment significantly lowered serum troponin-I and oxidative stress markers, increased superoxide dismutase (SOD) and glutathione (GSH) levels, and decreased malondialdehyde (MDA) concentrations. Additionally, ranolazine reduced the expression of stress-related genes (GRP78, XBP1, and NLRP3) and lowered serum IL1β levels.</p><p><strong>Conclusions: </strong>The results indicate that ranolazine protects against DCM by attenuating oxidative stress, ER stress, and inflammation. Its potential as a therapeutic agent for DCM warrants further investigation.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"111"},"PeriodicalIF":2.8,"publicationDate":"2025-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12117744/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144156884","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Safety evaluation of baloxavir marboxil: analysis and discussion utilizing real adverse events from the FAERS database.","authors":"Xiaolong Lai, Liuyin Jin, Yixia Zhou, Yang Li, Lindan Sheng, Guomin Xie, Jianjiang Fang","doi":"10.1186/s40360-025-00940-0","DOIUrl":"10.1186/s40360-025-00940-0","url":null,"abstract":"<p><strong>Background: </strong>As a novel anti-influenza agent, baloxavir marboxil lacks real-world safety data in large populations. Therefore, this study aimed to investigate adverse drug events (ADEs) associated with baloxavir marboxil by analyzing the Food and Drug Administration Adverse Event Reporting System (FAERS) database.</p><p><strong>Methods: </strong>Adverse event reports involving baloxavir marboxil were extracted from the FAERS database spanning the fourth quarter of 2018 to the third quarter of 2023. Demographic characteristics and reporter profiles were analyzed to characterize the exposed population. A disproportionality analysis was performed using four validated pharmacovigilance algorithms: reporting odds ratio (ROR), proportional reporting ratio (PRR), Bayesian Confidence Propagation Neural Network (BCPNN), and multi-item gamma Poisson shrinker (MGPS). These complementary approaches were employed to detect, prioritize, and validate potential safety signals.</p><p><strong>Results: </strong>Analysis of 8,824,675 ADE reports from the FAERS database identified 1,654 cases (0.19%) associated with baloxavir marboxil. Pediatric patients (< 18 years) exhibited the highest ADE reporting rate. Geospatial analysis revealed marked clustering, with 98.97% of reports originating from the United States (63.2%) and Japan (35.77%). We detected 47 significant safety signals spanning 27 System Organ Classes (SOCs), including established reactions such as pneumonia (n = 90) and vomiting (n = 77). Novel signals emerging from the analysis comprised hemorrhagic diathesis (n = 3), rhabdomyolysis (n = 25), hepatic dysfunction (n = 13), and cardiorespiratory arrest (n = 7). Notably, bleeding-related events (e.g., ischemic colitis, IC025 = 5.03) and neurological complications (e.g., febrile delirium, IC025 = 9.12) demonstrated statistically significant associations.</p><p><strong>Conclusion: </strong>This pharmacovigilance study identifies previously undercharacterized safety signals associated with baloxavir marboxil, including hemorrhagic complications, liver dysfunction, rhabdomyolysis, and life-threatening cardiorespiratory events. Pediatric populations and patients on anticoagulants may require heightened monitoring. While these findings provide critical pharmacovigilance insights, our study is inherently constrained by the spontaneous reporting system, which introduces potential underreporting, reporting biases, and confounding factors. Future research could employ more rigorous prospective study designs, integrating clinical trials and epidemiological studies, to more accurately assess the safety risks of baloxavir marboxil.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"110"},"PeriodicalIF":2.8,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12107739/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144149108","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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 probiotics on prognosis in patients with hepatectomy: a systematic review and meta-analysis of randomized controlled trial.","authors":"Qinghu Jiang, Hua Zou, Furui Zhong, Jian Ma","doi":"10.1186/s40360-025-00944-w","DOIUrl":"10.1186/s40360-025-00944-w","url":null,"abstract":"<p><strong>Objective: </strong>To investigate the effect of perioperative probiotics on prognosis in patients with hepatectomy.</p><p><strong>Method: </strong>By conducting a computer-based search of electronic databases to collect randomized controlled trials (RCTs) on the use of probiotics in the perioperative period for patients undergoing liver resection. Two researchers independently screened the literature, extracted data, assessed bias risk, and performed a meta-analysis using RevMan 5.4 software.</p><p><strong>Result: </strong>A total of 988 patients were enrolled across 14 studies. The results of the meta-analysis revealed that the probiotics group had lower rates of postoperative infectious complications (OR = 0.49; 95%CI 0.49 to 0.60; P < 0.01), serum endotoxin levels (SMD= -0.69; 95%CI -1.27 to -0.11; P = 0.02), white blood cell counts (SMD= -0.37; 95%CI -0.67 to -0.061.47; P = 0.02), hospital stays (SMD= -0.85; 95%CI -1.53 to -0.18; P = 0.01), and first postoperative exhaust times (SMD= -0.85; 95%CI -1.53 to -0.18; P = 0.01) compared to the control group. No significant differences in liver function indices (alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBiL) and international normalized ratio (INR)) or postoperative inflammatory markers (C-reactive protein (CRP), procalcitonin, interleukin-6 (IL-6)) were found between the two groups (all P > 0.05).</p><p><strong>Conclusions: </strong>Probiotics used perioperatively can lower postoperative infection risk and shorten hospital stays for hepatectomy patients, but they do not appear to aid in liver function restoration or inflammation reduction.</p><p><strong>Clinical trial number: </strong>Not applicable.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"109"},"PeriodicalIF":2.8,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12105156/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144149106","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Medication errors in malaria management in children: insights from pharmacovigilance data in the Democratic Republic of Congo.","authors":"Mireille Ngale Amba, Erick Kamangu Ntambwe, Aline Engo Biongo, Nsengi Ntamabyaliro, Gauthier Mesia Kahunu, Joseph Bodi Mabiala, Celestin Nsibu Ndosimao, Gaston Tona Lutete, Ghada Miremont-Salamé, Annie Fourrier-Réglat","doi":"10.1186/s40360-025-00941-z","DOIUrl":"10.1186/s40360-025-00941-z","url":null,"abstract":"<p><strong>Introduction: </strong>Since 2012, DRC adopted WHO recommendations for the malaria treatment with artemisinin-based drugs. Medication errors are defined as \"a failure in the treatment process that results in, or has the potential to result in, harm to the patient\". Medication errors are a major public health problem and one of the leading causes of death in the United States. The impact of medical errors can have severe consequences on children due to physiological features of children.</p><p><strong>Objectives: </strong>To identify, describe, and propose actionable strategies to address medication errors during malaria treatment in children with adverse effects in the DRC.</p><p><strong>Methods: </strong>This is a cross-sectional study of the ADR reports of children (< 18 years old) in the DRC recorded in VigiBase^®, the WHO pharmacovigilance database, from 2010 to February 2018. Five treatment process criteria (choice of treatment, dosage, duration, timing and route of administration) were selected to identify medication errors.</p><p><strong>Results: </strong>Medication errors accounted for 65,9% of the 851 cases retrieved from VigiBase^®. Children aged 2-11 years represented 55.2% of the study population. The choice of treatment, duration and dosage were the main prescription criteria for deviations.</p><p><strong>Discussion: </strong>The availability of alternative formulations, self-medication and inadequate dosage forms are factors contributing to medication errors. The information available in VigiBase^® did not allow us to evaluate the overall process of malaria management. Pharmacovigilance must be consolidated to raise awareness among consumers and providers and to ensure more effective monitoring.</p><p><strong>Conclusion: </strong>Non-compliance with national guidelines for the management of malaria is important in DRC. Our study amply demonstrates the need to strengthen the four pillars of the WHO's third global challenge, \"Medication without harm\", to reduce medication errors. This study advocates a significant mobilisation of resources for the training of health professionals and the strengthening of pharmacovigilance. Field studies on the management of malaria in children should be conducted to quantify drug errors.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"108"},"PeriodicalIF":2.8,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12100975/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144126286","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Safety, pharmacokinetics, preliminary efficacy, pharmacodynamics, and immunogenicity of QX002N, an anti-IL-17A monoclonal antibody, after short-term treatment of active ankylosing spondylitis.","authors":"Min Wu, Qianqian Li, Min Fang, Hong Zhang, Yanhua Ding","doi":"10.1186/s40360-025-00885-4","DOIUrl":"10.1186/s40360-025-00885-4","url":null,"abstract":"<p><strong>Background: </strong>To investigate the safety, pharmacokinetics, preliminary efficacy, pharmacodynamics, and immunogenicity of QX002N, an interleukin-17 A monoclonal antibody, in Chinese patients with active ankylosing spondylitis (AS).</p><p><strong>Methods: </strong>In this phase 1b, double-blind, placebo-controlled, multiple ascending dose study, eligible patients with active AS were randomized into three dose (40, 80, or 160 mg) cohorts, with a 4:1 ratio in each cohort to subcutaneously receive either QX002N or a placebo once every 2 weeks with six doses in total. All patients were followed for 14 weeks (98 days) after the last dose. The primary endpoints were the safety and pharmacokinetics of QX002N, and the secondary endpoints included its preliminary efficacy, pharmacodynamics, and immunogenicity.</p><p><strong>Results: </strong>Thirty patients (n = 10 in each cohort) were included, with 24 receiving QX002N and 6 receiving a placebo. A total of 85 adverse drug reactions, predominantly Grade 1-2, were identified in 20 out of 24 patients (83.3%) who took QX002N. The exposure to QX002N increased proportionally with the dose escalating from 40 mg to 160 mg. Patients taking 160 mg QX002N achieved higher response rates (ASAS20: 87.6% at Week 8 [Day 56]); ASAS40: 50.0% at Week 12 [Day 78]), than those taking 40-mg or 80-mg QX002N. An increase in interleukin-17 A and a decrease in interleukin-6 levels in the serum, with decreases in the erythrocyte sedimentation rate and high-sensitivity C-reactive protein levels, were observed. Anti-drug antibodies were detected in only one of 24 patients taking QX002N.</p><p><strong>Conclusions: </strong>Subcutaneous administration of QX002N demonstrates a favorable safety profile, with linear pharmacokinetic characteristics. Promising clinical responses in pharmacodynamics and preliminary efficacy have been observed. Immunogenicity does not appear to be a concern.</p><p><strong>Trial registration: </strong>This study was registered with Chinadrugtrials.org.cn (CTR20201277), the data of registration was in 20 Jul, 2020.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"107"},"PeriodicalIF":2.8,"publicationDate":"2025-05-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12090559/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144101256","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Immunomodulatory effects of detoxification agents on dendritic cell populations in methamphetamine addiction.","authors":"Ghasem Mosayebi, Seyed Mohammad Moazzeni, Hadiseh Farahani, Hassan Solhi, Mohammad Rafiei, Ali Ghazavi","doi":"10.1186/s40360-025-00943-x","DOIUrl":"10.1186/s40360-025-00943-x","url":null,"abstract":"<p><strong>Background and aim: </strong>Drug abuse can impact the function of immune cells, leading to a compromised immune system response. This study aimed to investigate the immunomodulatory effects of Methamphetamine and its detoxification agents on peripheral blood dendritic cells.</p><p><strong>Methods: </strong>A total of 60 participants were enrolled, including 30 individuals with Methamphetamine addiction and 30 matched healthy controls. Participants were assessed at three time points: at the beginning of detoxification, at the end of detoxification, and one-month post-detoxification. Flow cytometry was employed to analyze dendritic cell subsets (CD11c + myeloid dendritic cells and CD123 + plasmacytoid dendritic cells) and surface marker expression (HLA-DR, CD11c, CD123).</p><p><strong>Results: </strong>The percentages of both CD11c + and CD123 + dendritic cells in peripheral blood were significantly lower in Methamphetamine addicts compared to the control group. Detoxification with Risperidone corrected this reduction, while the combination of Risperidone and Methylphenidate failed to produce any change in the percentage of dendritic cells. The expression of HLA-DR, CD11c, and CD123 markers was downregulated in the dendritic cells of Methamphetamine addicts. Treatment with Risperidone restored these markers, whereas the combination therapy further exacerbated the downregulation of these markers.</p><p><strong>Conclusion: </strong>The findings suggest that detoxification with Risperidone may help ameliorate the immunological disorders associated with Methamphetamine use.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"106"},"PeriodicalIF":2.8,"publicationDate":"2025-05-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12087069/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144101339","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A study on the pharmacokinetic bioequivalence of oral tablet formulations of riluzole among healthy volunteers utilizing HPLC-MS/MS.","authors":"Fei Yu, Rui Wang, Keli Wang, BoYang Lin, Xuan Zhou, Linghong Chen, Li Ma, Zheng Liao, Wanggang Zhang","doi":"10.1186/s40360-025-00931-1","DOIUrl":"10.1186/s40360-025-00931-1","url":null,"abstract":"<p><strong>Introduction: </strong>This randomized, open-label, two period, two treatment, fasting bioequivalence trial was conducted to demonstrate the bioequivalence between riluzole tablets manufactured by Jiangsu Enhua Pharmaceutical Co., Ltd. and the reference preparations from Sanofi Winthrop Industry (certified by Sanofi Mature IP) in healthy individuals.</p><p><strong>Objective: </strong>The study aimed to compare the pharmacokinetic parameters and evaluate the bioequivalence of both preparations when taken on an empty stomach. Additionally, the safety profile of both preparations was assessed in the study population.</p><p><strong>Methods: </strong>Seventy-two subjects participated in the trial and received riluzole tablets once per dosing cycle while fasting. They were randomLy assigned to either a 50-mg test or reference formulation, with a 7-day washout period between cycles. Venous blood samples (4 mL) were collected 22 times from each subject, starting before dosing (0 h) and ending 48 h after. Plasma riluzole concentrations were measured using liquid chromatography tandem mass spectrometry. This clinical trial has been officially registered in the Chinese Clinical Trial Register (accessible at http://www.chinadrugtrials.org.cn/index.htmL ) with the registration number CTR20230637 on March 02, 2023.</p><p><strong>Results: </strong>The results showed that the geometric mean ratios of key pharmacokinetic parameters-including the area under the plasma concentration-time curve from time zero to the last nonzero concentration (AUC_0 - t) (102.21%; confidence interval [CI], 96.85-107.86%), AUC from time zero to infinity (AUC_0-∞) (102.03%; CI, 96.86-107.47%), and the peak plasma concentration (C_max) (107.47%; CI, 95.03-121.54%)-all fell within the bioequivalence acceptance range of 80-125%. Importantly, no serious adverse events were reported, and no subjects withdrew due to adverse events, indicating good tolerability of both formulations among the healthy Chinese volunteers.</p><p><strong>Conclusion: </strong>These findings establish the bioequivalence of the 50-mg test preparation of oral riluzole tablets with the reference listed drug.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"105"},"PeriodicalIF":2.8,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12079988/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144075936","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Prevalence and clinical significance of potential drug-drug interactions of antimicrobials in Intensive Care Unit patients: a retrospective study.","authors":"Shanshan Xu, Zhihui Song, Jie Bai, Jiawei Wang","doi":"10.1186/s40360-025-00925-z","DOIUrl":"https://doi.org/10.1186/s40360-025-00925-z","url":null,"abstract":"<p><strong>Background: </strong>Antimicrobials are frequently prescribed in Intensive Care Units (ICUs), where drug-drug interactions (DDIs) with other medications may exacerbate clinical outcomes. Limited evidence exists on the prevalence and clinical impact of these interactions.</p><p><strong>Objective: </strong>To estimate the prevalence of potential DDIs (pDDIs) between antimicrobials and other drugs in ICU patients using two electronic DDIs databases, identify the actual DDIs and the most frequently implicated antimicrobials, and determine the risk factors associated with actual DDIs.</p><p><strong>Methods: </strong>We conducted a retrospective study on patients admitted to intensive care units from January to December 2023. Micromedex and Lexi-Interact were used to identify pDDIs and their severities. Furthermore, we used the Drug Interaction Probability Scale (DIPS) criteria to identify actual DDIs.</p><p><strong>Results: </strong>Among 2,154 patients, 2,163 pDDIs (108 unique pairs) were identified in 461 patients, and 2.87% (62 pDDIs in 46 patients) were classified as actual DDIs. The antimicrobials most likely to cause pDDIs included quinolones, triazole antifungals, and linezolid. Antimicrobial-drug pairs with a higher incidence of severe pDDIs included linezolid-dopamine/metoclopramide (hypertension), voriconazole-budesonide for inhalation (increased serum concentration of budesonide), and levofloxacin-amiodarone (QT prolongation). The antimicrobial-drug pairs with a higher occurrence of actual DDIs included linezolid-dopamine/dobutamine (hypertension), fluconazole-amiodarone/ritonavir (QT prolongation), and cefoperazone/vancomycin-furosemide (nephrotoxicity). Moderate agreement existed between the two databases for pDDIs detection (Cohen's kappa = 0.546), but severity ratings diverged. Multivariable analysis identified the number of drugs per patient (OR = 1.178, p < 0.001), the number of antimicrobials per patient (OR = 1.146, p < 0.038), and the length of stay in the ICU (OR = 1.093, p < 0.038) as significant risk factors.</p><p><strong>Conclusions: </strong>High pDDI rates involving antimicrobials were observed in ICU patients, though actual DDIs were infrequent. Notable severe risk pairs warrant vigilant monitoring, especially with a higher occurrence of actual DDIs. Discrepancies in DDI databases emphasize the need for multi-tool validation to optimize medication safety.</p>","PeriodicalId":9023,"journal":{"name":"BMC Pharmacology & Toxicology","volume":"26 1","pages":"104"},"PeriodicalIF":2.8,"publicationDate":"2025-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12076841/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144075951","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}