anticholinergic drug

抗胆碱能药物
  • 文章类型: Journal Article
    绿色和白色化学通过其无与伦比的潜力来提高可持续性和效率,对化学工业的革命性至关重要。在这项研究中,绿色和白色指标的九种可持续发展工具,包括绿色分析程序指数(GAPI),ComplexGAPI,分析绿色,样品制备的分析绿色度量,分析生态尺度(ESA)分析方法绿色度评分,高效液相色谱-环境评估工具(HPLC-EAT),分析方法体积强度,和蓝色适用性等级指数(BAGI),已开发用于评估环境友好性的创新和简单的平均定心比率光谱(MCR)和反相高效液相色谱(RP-HPLC)策略,用于同时分析和分离环戊酸酯(CYC)和C12和C14同系物在纯溶液和眼用溶液中苯扎氯铵(BNZ)。流动相,由缓冲液磷酸盐和乙腈(35:65,v/v)形成,调节至pH6.3,并使用215nm的UV检测。实验流速为2.0mLmin-1,分析柱为L11InertsilPh-3(150mm×4.6mm,5µm)。所有序列在25°C下在柱烘箱中运行。MCR方法有效地解决了药物的光谱重叠。CYC和BNZ在227.5和220.4nm处采用了这种方法,分别。作为HPLC分析的一部分,采用等度法,磷酸盐缓冲液和乙腈在35:65的流动相中。在所有药物的20-320µgmL-1和5-30µgmL-1范围内,HPLC和MCR方法的校准曲线之间的相关系数均大于0.999。该技术产生优异的初级回收率,从97.2%到100.5%不等。建议的方法已根据国际协调理事会准则得到验证。
    Green and white chemistry are vital to revolutionizing the chemical industry through their unparalleled potential to enhance sustainability and efficiency. In this study, nine sustainability tools of both green and white metrics, including green analytical procedure index (GAPI), ComplexGAPI, analytical greenness, analytical greenness metric for sample preparation, Analytical Eco-Scale (ESA), analytical method greenness score, high-performance liquid chromatography- environmental assessment tool (HPLC-EAT), analytical method volume intensity, and blue applicability grade index (BAGI), have been developed for appraising environmental friendliness for both innovative and straightforward mean centering of ratio spectra (MCR) and reversed-phase high-performance liquid chromatography (RP-HPLC) strategies utilized for concurrent analysis and separation of cyclopentolate (CYC) and C12 and C14 homologs of benzalkonium chloride (BNZ) in pure and ophthalmic solution. The mobile phase, formed of buffer phosphate and acetonitrile (35:65, v/v), was adjusted to pH 6.3, and 215-nm UV detection was used. The experimental flow rate was 2.0 mL min-1, and the analytical column was L11 Inertsil Ph-3 (150 mm × 4.6 mm, 5 µm). All sequences were run at 25°C in the column oven. The MCR approach effectively resolved the drug\'s spectral overlapping. CYC and BNZ employed this approach at 227.5 and 220.4 nm, respectively. As part of the HPLC analysis, an isocratic method was employed with phosphate buffer and acetonitrile in the mobile phase at 35:65. A correlation coefficient greater than 0.999 was observed between the calibration curves for the HPLC and MCR methods in the ranges of 20-320 µg mL-1 and 5-30 µg mL-1 for all drugs. The technique yields excellent primary recovery rates, ranging from 97.2% to 100.5%. The recommended approach has been validated according to International Council for Harmonization guidelines.
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  • 文章类型: Randomized Controlled Trial
    飞行模拟器在机组人员培训中起着至关重要的作用。偶尔,晕动病的症状,定义为模拟器疾病,在这些会议期间发展。晕动病的预防方法已经被彻底调查,然而,只有少数研究检查了模拟疾病的预防性治疗。这项研究的目的是研究东pol碱(抗胆碱能药)与桂利嗪(抗组胺药)预防直升机模拟器疾病的功效。在这项研究中,使用了经过验证的模拟器疾病问卷(SSQ)评分来确定模拟器疾病症状的严重程度。计算初步SSQ分数和每次排序后的SSQ分数。每个参与者都被给予东pol碱,在每个训练日的第一次训练前,以双盲随机方式服用桂利嗪或安慰剂。41名直升机飞行员参加了审判。平均年龄为30.5±7.1。在服用桂利嗪两小时后,SSQ值从初步SSQ问卷的平均值73.30显著提高到平均值30.92(p=0.012,95%CI[8.071,76.703])。在缓解模拟器疾病症状方面,东莨菪碱的效果不如桂利嗪和安慰剂。这项研究是第一个比较东pol碱与cinnarizine预防模拟器疾病的研究。根据这项研究的结果,我们建议使用桂利嗪而不是东pol碱预防模拟器疾病。本文受版权保护。保留所有权利。
    Flight simulators have an essential role in aircrew training. Occasionally, symptoms of motion sickness, defined as simulator sickness, develop during these sessions. Preventive methods for motion sickness have been investigated thoroughly; however, only a few studies have examined preventive treatments for simulator sickness. The aim of this study was to examine the efficacy of scopolamine (an anticholinergic drug) compared with cinnarizine (an antihistaminic drug) for helicopter simulator sickness prevention. A validated simulator sickness questionnaire (SSQ) score was used to determine the severity of simulator sickness symptoms in this study. Preliminary SSQ scores and SSQ scores after each sortie were calculated. Each participant was given scopolamine, cinnarizine, or a placebo in a double-blind randomized manner before the first sortie of each training day. Forty-one helicopter pilots participated in the trial. The average age was 30.5 ± 7.1 years. SSQ values significantly improved from an average of 73.30 in the preliminary SSQ questionnaire to an average of 30.92 after 2 hours following the administration of cinnarizine (P = .012, 95%CI 8.071-76.703). Scopolamine was found to be less effective than both cinnarizine and the placebo in the alleviation of simulator sickness symptoms. This study is the first to compare scopolamine with cinnarizine for simulator sickness prevention. Based on the results of this study, we recommend the use of cinnarizine over scopolamine for simulator sickness prevention.
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  • 文章类型: Journal Article
    过敏性鼻炎(AR)是一种以打喷嚏、鼻痒为主要症状的鼻黏膜疾病。尽管AR治疗继续改善,仍然缺乏有效的药物。关于抗胆碱能药物能否有效和安全地缓解AR症状和减轻鼻黏膜炎症仍存在争议。这里,我们合成了101BHG-D01,这是一种新型的抗胆碱能药物,主要靶向M3受体,可以减少其他抗胆碱能药物对心脏的不良反应.我们评估了101BHG-D01对AR的影响,并研究了抗胆碱能治疗AR的潜在分子机制。我们发现101BHG-D01有效缓解AR症状,炎症细胞浸润减少,炎症因子(IL-4、IL-5、IL-13等)的表达减弱。)在各种AR动物模型中。此外,101BHG-D01减少了IgE攻击的大鼠腹膜间皮素(RPMC)中肥大细胞的活化和组胺的释放。此外,101BHG-D01降低MUC5AC在IL-13攻击的大鼠鼻上皮细胞(RNECs)和人鼻上皮细胞(HNEPCs)中的表达。此外,IL-13刺激显著增加JAK1和STAT6磷酸化,被101BHG-D01抑制。我们证明了101BHG-D01减少鼻粘膜的粘液分泌和炎症细胞浸润,这可能是通过减少JAK1-STAT6信号通路的激活而发生的,表明101BHG-D01是AR的有效且安全的抗胆碱能疗法。
    Allergic rhinitis (AR) is a nasal mucosal disease with sneezing and nasal itching as the main symptoms. Although AR treatment continues to improve, there remains a lack of effective drugs. There are still controversies regarding whether anticholinergic drugs can effectively and safely relieve the symptoms of AR and reduce inflammation in the nasal mucosa. Here, we synthesized 101BHG-D01, which is a novel anticholinergic drug that mainly targets the M3 receptor and may reduce the adverse effects of other anticholinergic drugs on the heart. We evaluated the effects of 101BHG-D01 on AR and investigated the potential molecular mechanism of anticholinergic therapy for AR. We found that 101BHG-D01 effectively alleviated AR symptoms, reduced the infiltration of inflammatory cells and attenuated the expression of inflammatory factors (IL-4, IL-5, IL-13, etc.) in various AR animal models. In addition, 101BHG-D01 reduced the activation of mast cells and the release of histamine from rat peritoneal mesothelial cells (RPMCs) challenged by IgE. Moreover, 101BHG-D01 reduced the expression of MUC5AC in IL-13-challenged rat nasal epithelial cells (RNECs) and human nasal epithelial cells (HNEpCs). Furthermore, IL-13 stimulation significantly increased JAK1 and STAT6 phosphorylation, which was suppressed by 101BHG-D01. We demonstrated that 101BHG-D01 reduced mucus secretion and inflammatory cell infiltration in the nasal mucosa, which may occur through a reduction in activation of the JAK1-STAT6 signaling pathway, indicating that 101BHG-D01 is a potent and safe anticholinergic therapy for AR.
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  • 文章类型: Case Reports
    抗胆碱能药物,比如Biperiden,苯托品,还有苯海拉明,在1980年代和1990年代用于抗精神病药恶性综合征(NMS)。然而,自2000年以来,它们未被推荐用于NMS的药物治疗,因为它们可以通过抑制出汗来防止体温降低。然而,抗胆碱能药物是否真的加重NMS仍不清楚.这项研究强调了抗胆碱能药物的有用性,作为目前NMS的药物治疗不再引起人们的注意。我使用抗胆碱能药物治疗了四名NMS患者。两名患者单独接受了Biperiden治疗,另外两名患者接受了Biperiden和其他药物的联合治疗,包括丹曲林,金刚烷胺,或者地西泮.肌内注射biperiden改善肌肉僵硬,震颤,吞咽困难,和运动障碍默症。精神科医生熟悉抗胆碱能药物,因为它们用于抗精神病药物诱导的静坐不能和帕金森病。我的研究表明抗胆碱能药物,特别是可注射的配方,可以是NMS的治疗选择。
    Anticholinergic drugs, such as biperiden, benztropine, and diphenhydramine, were used for neuroleptic malignant syndrome (NMS) in the 1980s and 1990s. However, they have not been recommended for pharmacotherapy in NMS since 2000, as they may prevent a decrease in body temperature by suppressing sweating. However, whether anticholinergic drugs actually exacerbate NMS remains unclear. This study highlights the usefulness of anticholinergic drugs, which are no longer attracting attention as current pharmacological treatments for NMS. I treated four NMS patients using anticholinergic drugs. Two patients were treated with biperiden alone, and the other two patients were treated with a combination of biperiden and other drugs, including dantrolene, amantadine, or diazepam. Intramuscular injection of biperiden improved muscle rigidity, tremors, dysphagia, and akinetic mutism. Psychiatrists are familiar with anticholinergic drugs as they are used for antipsychotic-induced akathisia and Parkinsonism. My study suggests that anticholinergic drugs, especially injectable formulations, can be a therapeutic option for NMS.
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  • 文章类型: Journal Article
    盐酸戊乙奎醚(PHC)已被用作抗胆碱能药物,用于治疗急性有机磷农药中毒(AOPP)。这项荟萃分析的目的是探讨PHC在AOPP中使用抗胆碱能药物方面是否优于阿托品。
    我们搜索了Scopus,Embase,科克伦,PubMed,ProQuest,奥维德,WebofScience,中国科技期刊数据库(VIP),独秀,中国生物医学文献(CBM),万方,和中国国家知识基础设施(CNKI),从成立到2022年3月。在纳入所有合格的随机对照试验(RCTs)后,我们进行了质量评估,数据提取,和统计分析。使用风险比率(RR)进行统计,加权平均差(WMD),和标准平均差(SMD)。
    我们的荟萃分析包括来自中国242家不同医院的240项研究的20797名受试者。与阿托品组相比,PHC组死亡率下降(RR=0.20,95%置信区间[CI]:0.16-0.25,P<0.001),住院时间(WMD=-3.89,95%CI:-4.37至-3.41,P<0.001),并发症总发生率(RR=0.35,95%CI:0.28-0.43,P<0.001),不良反应总发生率(RR=0.19,95%CI:0.17-0.22,P<0.001),总症状消失时间(SMD=-2.13,95%CI:-2.35至-1.90,P<0.001),胆碱酯酶活性恢复到正常值50-60%的时间(SMD=-1.87,95%CI:-2.03至-1.70,P<0.001),昏迷时间(WMD=-5.57,95%CI:-7.20至-3.95,P<0.001),机械通气时间(WMD=-2.16,95%CI:-2.79~-1.53,P<0.001)。
    作为AOPP中的抗胆碱能药物,PHC与阿托品相比具有若干优势。
    UNASSIGNED: Penehyclidine hydrochloride (PHC) has been used for many years as an anticholinergic drug for the treatment of acute organophosphorus pesticide poisoning (AOPP). The purpose of this meta-analysis was to explore whether PHC has advantages over atropine in the use of anticholinergic drugs in AOPP.
    UNASSIGNED: We searched Scopus, Embase, Cochrane, PubMed, ProQuest, Ovid, Web of Science, China Science and Technology Journal Database (VIP), Duxiu, Chinese Biomedical literature (CBM), WanFang, and Chinese National Knowledge Infrastructure (CNKI), from inception to March 2022. After all qualified randomized controlled trials (RCTs) were included, we conducted quality evaluation, data extraction, and statistical analysis. Statistics using risk ratios (RR), weighted mean difference (WMD), and standard mean difference (SMD).
    UNASSIGNED: Our meta-analysis included 20,797 subjects from 240 studies across 242 different hospitals in China. Compared with the atropine group, the PHC group showed decreased mortality rate (RR=0.20, 95% confidence intervals [CI]: 0.16-0.25, P <0.001), hospitalization time (WMD=-3.89, 95% CI: -4.37 to -3.41, P <0.001), overall incidence rate of complications (RR=0.35, 95% CI: 0.28-0.43, P <0.001), overall incidence of adverse reactions (RR=0.19, 95% CI: 0.17-0.22, P <0.001), total symptom disappearance time (SMD=-2.13, 95% CI: -2.35 to -1.90, P <0.001), time for cholinesterase activity to return to normal value 50-60% (SMD=-1.87, 95% CI: -2.03 to -1.70, P <0.001), coma time (WMD=-5.57, 95% CI: -7.20 to -3.95, P <0.001), and mechanical ventilation time (WMD=-2.16, 95% CI: -2.79 to -1.53, P <0.001).
    UNASSIGNED: PHC has several advantages over atropine as an anticholinergic drug in AOPP.
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  • 文章类型: Journal Article
    In this work, Atropine as the anticholinergic drug was measured using the environmentally friendly sensor. In this regard, Self-cultivated Spirulina platensis with electroless silver was employed as a powder amplifier in carbon paste electrode modification. Also, 1-Hexyl-3 methylimidazolium Hexafluorophosphate (HMIM PF6) ion liquid as a conductor binder was used in the suggested electrode construction. Atropine determination was investigated by voltammetry methods. According to voltammograms, the electrochemical behavior of atropine depends on pH, and pH 10.0 was used as the optimal condition. Moreover, the diffusion control process for the electro-oxidation of atropine was verified by the scan rate study, so the diffusion coefficient (D∼ 3.0136×10-4cm2/sec) value was computed from the chronoamperometry study. Furthermore, responses of the fabricated sensor were linear in the concentration range from 0.01 to 800 μM, and the lowest detection limit of the Atropine determination was obtained at 5 nM. Moreover, the stability, reproducibility, and selectivity factors of the suggested sensor were confirmed by the results. Finally, the recovery percentages for atropine sulfate ampoule (94.48-101.58), and water (98.01-101.3) approve of the applicability of the proposed sensor to Atropine determination in real samples.
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  • 文章类型: Journal Article
    6-11岁未控制哮喘的儿童接受低剂量吸入性皮质类固醇(ICS)治疗,并逐步增加ICS剂量和/或增加维持治疗。如有必要。本研究的目的是评估噻托溴铵在重度和轻度症状哮喘患儿中的疗效和安全性。本前瞻性队列研究包括144名重度和轻度哮喘儿童(年龄,6-11年),根据哮喘控制问卷-采访员-管理,接受ICS(布地奈德)和≥1个月的控制剂治疗组合治疗≥1个月,评分≥1.5。除了具有≥1个控制器治疗的ICS之外,儿童接受5µg每日1次噻托溴铵(治疗组;n=72)或未接受噻托溴铵(对照组;n=72).与对照组相比,治疗组在噻托溴铵给药后3小时从基线开始1秒变化的最大用力呼气容积显着改善(384±31vs.248±28ml;P<0.0001)。1秒内的最大用力呼气容积(224±28vs.140±31ml;P<0.0001)和25-75%用力肺活量时的用力呼气流量(389±36vs.116±27ml/sec;P<0.0001)显示用噻托溴铵治疗后的显著改善。波谷强迫肺活量有显著差异(153±29vs.139±30毫升/秒;P<0.0001),平均每周抢救治疗使用量(0.29±0.08vs.0.36±0.09;P<0.0001),平均每周峰值呼气流量测量值(4.12±3.56vs.7.46±3.29l/min;P<0.0001)和平均每周无症状时间(0.19±0.04vs.两组之间的0.16±0.04天;P<0.0001)。两组患儿均能耐受任何不良反应。在患有严重和轻度症状哮喘的儿童(6-11岁)中,噻托溴铵5µg/天作为ICS的附加治疗,并采用≥1个控制治疗,被发现是有效且安全的(证据水平2;技术疗效阶段4)。
    Children aged 6-11 years with uncontrolled asthma are treated with low-dose inhaled corticosteroid (ICS) with stepwise increase in ICS dosage and/or add-on maintenance treatment, as necessary. The objective of the present study was to evaluate the efficacy and safety of tiotropium add-on treatment in children with severe and mild symptomatic asthma. The present prospective cohort study included 144 children with severe and mild asthma (age, 6-11 years) who received ICS (budesonide) with ≥1 controller treatment combination therapies for ≥1 month and score ≥1.5 based on Asthma Control Questionnaire-Interviewer-Administered. In addition to ICS with ≥1 controller treatment, children received 5 µg once-daily tiotropium (treatment group; n=72) or did not receive tiotropium (control group; n=72). The peak forced expiratory volume in 1-sec change from the baseline 3 h post-administration of tiotropium was significantly improved in the treatment group compared with the control group (384±31 vs. 248±28 ml; P<0.0001). The trough forced expiratory volume in 1-sec (224±28 vs. 140±31 ml; P<0.0001) and forced expiratory flow at 25-75% of forced vital capacity (389±36 vs. 116±27 ml/sec; P<0.0001) showed significant improvement following treatment with tiotropium. Significant differences were noted for trough forced vital capacity (153±29 vs. 139±30 ml/sec; P<0.0001), mean weekly rescue treatment usage (0.29±0.08 vs. 0.36±0.09; P<0.0001), mean weekly peak expiratory flow measurement (4.12±3.56 vs. 7.46±3.29 l/min; P<0.0001) and mean weekly symptom-free time (0.19±0.04 vs. 0.16±0.04 days; P<0.0001) between both cohorts. Children of both groups tolerated any adverse effects. Tiotropium 5 µg administered once/day as an add-on treatment to ICS with ≥1 controller treatments in children (6-11 years of age) with severe and mild symptomatic asthma was found to be efficacious and safe (level of evidence 2; technical efficacy stage 4).
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  • 文章类型: Journal Article
    预期寿命的增加还伴随着治疗慢性病的药物使用的增加。多药与药物相关的问题有关,例如抗胆碱能负担的增加。老年人更容易受到中枢神经系统抗胆碱能作用的影响,反过来,可能与认知障碍有关。在本文中,我们开发了一个更新的抗胆碱能负担量表,CRIDECO抗胆碱能负荷量表(CALS)通过系统回顾文献,并与目前最常用的抗胆碱能负荷量表(ACB)进行比较.我们的新量表包括217种具有抗胆碱能特性的不同药物,比ACB多129。鉴于抗胆碱能药物对认知能力的影响,然后,我们使用这两种量表来研究西班牙成年受试者的抗胆碱能负荷与认知功能障碍之间的关系。在我们的人口中,当通过新的CALS测量时,我们观察到认知障碍与抗胆碱能负荷之间的关联,但不是在应用ACB时。使用更全面和升级的量表将可以更好地区分与使用抗胆碱能药物治疗认知障碍相关的风险。CALS可以帮助提高临床医生对使用药物相关问题的认识,或它们的组合,具有很大的抗胆碱能作用,并为每位患者推广更好的个性化药理学方法。
    The increase in life expectancy has also been accompanied by an increase in the use of medication to treat chronic diseases. Polypharmacy is associated with medication-related problems such as the increase in the anticholinergic burden. Older people are more susceptible to anticholinergic effects on the central nervous system and this, in turn, may be related to cognitive impairment. In this paper, we develop an updated anticholinergic burden scale, the CRIDECO Anticholinergic Load Scale (CALS) via a systematic review of the literature and compare it with the currently most used Anticholinergic Burden Scale (ACB). Our new scale includes 217 different drugs with anticholinergic properties, 129 more than the ACB. Given the effect that anticholinergic medications have on cognitive performance, we then used both scales to investigate the relationship between anticholinergic burden and cognitive impairment in adult Spanish subjects with subjective memory complaint. In our population, we observed an association between cognitive impairment and the anticholinergic burden when measured by the new CALS, but not when the ACB was applied. The use of a more comprehensive and upgraded scale will allow better discrimination of the risk associated with the use of anticholinergic medications on cognitive impairment. CALS can help raise awareness among clinicians of the problems associated with the use of medications, or combinations of them, with large anticholinergic effect, and promote a better personalized pharmacological approach for each patient.
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  • 文章类型: Journal Article
    Dementia is one of the greatest global challenges for public health; however, the relationship between anticholinergic drugs and dementia remains unclear. The aim of the present study was to perform a systematic review and meta-analysis of the predictive roles of anticholinergic drugs in dementia risk. After pooling fourteen longitudinal and case-control studies with a total of 1,564,181 subjects, anticholinergic drug use was associated with an increased risk of all-cause dementia and Alzheimer\'s disease. Both low and high anticholinergic drug burdens were associated with dementia. Moreover, there was a dose-dependent relationship between anticholinergic drugs and risk of dementia. With respect to the categories of anticholinergic drugs, antiparkinson, urological drugs, and antidepressants increased the risk for dementia; however, cardiovascular and gastrointestinal drugs played potentially protective roles. These findings underscore the importance of anticholinergic drugs as a potential modifiable risk factor for dementia and provide treatment priorities to optimize dementia prevention.
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  • 文章类型: Journal Article
    UNASSIGNED: Recent investigations showed that anticholinergic drugs could use for the management of storage symptoms after transurethral resection of the prostate (TURP). The use of intravesical botulinum toxin-A (BTX-A) for the management of overactive bladder is rapidly increasing. In this research, we assess the efficacy of BTX-A vs solifenacin in men suffering from bladder outlet obstruction-over active bladder (BOO-OAB) managed with TURP.
    UNASSIGNED: In this case-control study, 50 men with BOO-OAB randomized into two groups. The control group (A) underwent TURP and subsequently managed by solifenacin 5 mg daily, and the case group (B) underwent TURP and BTX-A injection in the bladder wall in the same session. Treatment success was the primary outcome and defined as post-injection improvement in the storage score of the International Prostate Symptom Score (IPSS) from baseline.
    UNASSIGNED: The IPSS, post-void residual volume, frequency, incomplete emptying, nocturia and urgency subscores considerably ameliorated after 12 weeks and 36 weeks for both groups, but it was more significant in the case arm. The quality of life (QoL) scores significantly improved after the treatments in both groups. Intervention group showed significant reductions regarding urgency incontinence compared with the solifenacin group at 12th and 36th weeks.
    UNASSIGNED: BTX-A is an effective and well-tolerated treatment in patients with benign prostatic hyperplasia (BPH) who are candidates of TURP and simultaneously suffer from OAB symptoms.
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