Muscle relaxant

肌肉松弛剂
  • 文章类型: Journal Article
    尽管是相同治疗类别的药物(苯二氮卓类药物),他们每个人都表现出不同的行动。通常可以看出,布罗马西泮,氯硝西泮,and,阿普唑仑用于治疗焦虑症,恐慌症,和恐惧症.另一方面,咪达唑仑,替马西泮,氟拉西泮,和Nitrazepam用于治疗失眠和劳拉西泮被认为是具有抗惊厥作用的药物。由于作用机制是相同的,与蛋白质的结合模式应该有一些差异,这些差异会导致它们对身体的影响不同。对市场上可用的苯二氮卓类药物与GABAA受体的结合模式的深度筛选将有利于找出负责显示任何特定作用的负责氨基酸。这一揭示将有助于设计在体内具有最高有益效果和最低毒性的新分子。计算机模拟方法提供了关于结合模式的初始理解水平,进行体外和体内实验将更具体地宣称新设计药物的益处。
    Despite of being the drugs of the same therapeutic class (Benzodiazepines), each of them shows different actions prominently. It is commonly seen that Bromazepam, Clonazepam, and, Alprazolam are prescribed for the treatment of anxiety disorders, panic disorders, and phobias. On the other hand, Midazolam, Temazepam, Flurazepam, and Nitrazepam are indicated for the treatment of insomnia and Lorazepam is considered as a drug having anticonvulsant effects. As the mechanism of action is the same, there should be some differences in the binding patterns with the proteins that create differences in their impacts on the body. A deep screening of the binding patterns of the available Benzodiazepines in the market to the GABAA receptor will be beneficial to find out the responsible amino acids for being accountable for showing any specific action. This reveal will help design new molecules with the highest beneficial effect and lowest toxicity in the body. The in silico method provides the initial level of understanding regarding the binding patterns, performing in vitro and in vivo experiments will be more specific to claim the benefits of newly designed drugs.
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  • 文章类型: Journal Article
    当地的保健医生已经使用本港榕树来治疗疼痛,炎症,风湿病,和其他健康问题。
    在这项研究中,粗提物和不同的馏分,与分离的F.benghalensis化合物一起检查了它们作为肌肉松弛剂的作用,镇痛药,和镇静剂。
    对提取物和分离的化合物1进行肌肉松弛剂筛选,镇痛药,和镇静行动。乙酸介导的扭体模型用于镇痛评估,肌肉松弛潜力通过牵引和倾斜计划测试进行量化,并应用野外试验观察镇静效果。
    以各种剂量测试提取物/级分(25、50和100mg/kg)和分离的化合物(2.5、5、10和20mg/kg)。在乙酸介导的扭体模型中,观察到对carpachromene(64.44%)的明显减少(p<0.001),随后是乙酸乙酯(60.67%)和甲醇(58.42%)级分。对分离的化合物(71.09%)观察到明显的(p<0.001)肌肉松弛活性,随后是乙酸乙酯(66.98%)和甲醇(67.10%)级分。关于镇静作用,对分离的化合物(71.09%)有显著作用,随后是乙酸乙酯(66.98%)和甲醇(67.10%)级分。此外,使用分子对接探索分离化合物的结合模式。分子对接研究表明,分离的化合物对COX2和GABA具有良好的结合亲和力。我们分离的化合物可能对COX2和GABA受体具有抑制活性。
    无花果的提取物和分离的化合物可用作镇痛药,肌肉松弛剂,和镇静剂。然而,详细的分子和功能分析对于确定它们作为肌肉松弛剂的功能至关重要,镇痛药,和镇静剂。
    UNASSIGNED: Ficus benghalensis has been used by local health care practitioners to treat pain, inflammation, rheumatism, and other health issues.
    UNASSIGNED: In this study, the crude extract and diverse fractions, along with the isolated compound of F. benghalensis were examined for their roles as muscle relaxants, analgesics, and sedatives.
    UNASSIGNED: The extract and isolated compound 1 were screened for muscle-relaxant, analgesic, and sedative actions. The acetic acid-mediated writhing model was utilized for analgesic assessment, the muscle relaxant potential was quantified through traction and inclined plan tests, and the open field test was applied for sedative effects.
    UNASSIGNED: The extract/fractions (25, 50, and 100 mg/kg) and isolated compounds (2.5, 5, 10, and 20 mg/kg) were tested at various doses. A profound (p< 0.001) reduce in the acetic acid-mediated writhing model was observed against carpachromene (64.44%), followed by ethyl acetate (60.67%) and methanol (58.42%) fractions. A marked (p< 0.001) muscle relaxant activity was noticed against the isolated compound (71.09%), followed by ethyl acetate (66.98%) and methanol (67.10%) fractions. Regarding the sedative effect, a significant action was noted against the isolated compound (71.09%), followed by ethyl acetate (66.98%) and methanol (67.10%) fractions. Furthermore, the binding modes of the isolated compounds were explored using molecular docking. The molecular docking study revealed that the isolated compound possessed good binding affinity for COX2 and GABA. Our isolated compound may possess inhibitory activity against COX2 and GABA receptors.
    UNASSIGNED: The extract and isolated compounds of Ficus benghalensis can be used as analgesics, muscle relaxants, and sedatives. However, detailed molecular and functional analyses are essential to ascertain their function as muscle relaxants, analgesics, and sedatives.
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  • 文章类型: Journal Article
    黄连木在传统医学中被广泛使用。本研究旨在分离和评价黄连粗提物中3'4'78-四羟基-3-甲氧基黄酮的治疗效果。
    该研究利用柱色谱法进行分离。评估植物提取物及其分离的化合物的体内镇痛(热板模型),抗炎(角叉菜胶诱导的爪水肿),镇静剂(露天模型),和肌肉放松性能(倾斜平面和牵引试验)。
    在热诱导镇痛模型中,提取物(25,50和100mg/kg)和分离的化合物(2.5,5,10和15mg/kg)在较高剂量下观察到显著的镇痛效果.给药120分钟后,提取物(100mg/kg)显着延长了潜伏期(21.98秒)。分离的化合物在30分钟后延长了潜伏期(20.03秒),保持显著长达120分钟,延迟时间为24.11秒。抗炎作用显示在治疗的第5小时后,炎性反应减少50.23%(提取物)和67.09%(化合物)。两个样本都显示出显著的镇静作用,与阴性对照(180.99线)相比,提取物阻碍了54.11线的移动。与阴性对照相比,分离的化合物将交叉线的数目减少至15.23±SEM。两个样品也是显著的肌肉松弛剂。对接研究表明,该化合物的治疗效果是由于抑制COX和伤害性途径。
    从黄连木中分离的化合物具有显着的镇痛作用,抗炎,镇静剂,和肌肉放松的特性,通过抑制COX和伤害性途径具有潜在的治疗应用。
    UNASSIGNED: Pistacia chinensis is extensively employed in traditional medicine. This study aimed to isolate and evaluate the therapeutic effects of 3\'4\'78-tetrahydroxy-3-methoxyflavone from P. chinensis crude extract.
    UNASSIGNED: The study utilized column chromatography for isolation. The plant extract and its isolated compound were assessed for in vivo analgesic (hot plate model), anti-inflammatory (carrageenan-induced paw edema), sedative (open field model), and muscle relaxing properties (inclined plane and traction test).
    UNASSIGNED: In the thermal-induced analgesic model, a significant analgesic effect was observed for the extract (25, 50, and 100 mg/kg) and the isolated compound (2.5, 5, 10, and 15 mg/kg) at higher doses. The extract (100 mg/kg) significantly prolonged latency time (21.98 seconds) after 120 minutes of administration. The isolated compound elevated the latency time (20.03 seconds) after 30 minutes, remaining significant up to 120 minutes with a latency time of 24.11 seconds. The anti-inflammatory effect showed a reduction in inflammatory reactions by 50.23% (extract) and 67.09% (compound) after the fifth hour of treatment. Both samples demonstrated significant sedative effects, with the extract hindering movement by 54.11 lines crossed compared to the negative control (180.99 lines). The isolated compound reduced the number of lines crossed to 15.23±SEM compared to the negative control. Both samples were also significant muscle relaxants. Docking studies indicated that the compound\'s therapeutic effect is due to inhibiting COX and nociceptive pathways.
    UNASSIGNED: The isolated compound from Pistacia chinensis exhibits significant analgesic, anti-inflammatory, sedative, and muscle relaxing properties, with potential therapeutic applications by inhibiting COX and nociceptive pathways.
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  • 文章类型: Journal Article
    引言镁因其减少罗库溴铵的起效时间而同时延长其作用持续时间的能力而被认可。这项研究旨在评估镁预处理在快速顺序插管患者中使用两种不同剂量的罗库溴铵减少起效时间的功效。材料和方法这项随机前瞻性双盲临床研究涉及50名美国麻醉医师协会(ASA)I/II的患者,术前没有困难插管的指征,在全身麻醉下进行择期手术。将患者分为两组:A组在插管前15分钟接受60mg/kg的镁和1.2mg/kg的罗库溴铵,B组接受60mg/kg镁,然后接受0.6mg/kg罗库溴铵。两组在给药后最后一次抽搐消失时对插管条件进行评估和分级。考虑到插管的方便性,声带位置,以及对气管导管插入的反应。同时,在插管前记录血流动力学变化,插管后一分钟五分钟.结果与具有镁预处理的1.2mg/kg的罗库溴铵相比,具有0.6mg/kg的罗库溴铵的插管条件是相当的或同样良好的。结论镁预处理可增强罗库溴铵的神经肌肉阻滞作用,减少其发病时间,而没有临床上明显延长阻滞持续时间。
    Introduction Magnesium is recognized for its ability to reduce the onset time of rocuronium while simultaneously extending its duration of action. This study aims to assess the efficacy of magnesium pre-treatment in decreasing the onset time with two different doses of rocuronium in patients undergoing rapid sequence intubation. Materials and methods This randomized prospective double-blind clinical study involved 50 patients classified as American Society Of Anesthesiologists (ASA) I/II, with no preoperative indications of difficult intubation, undergoing elective surgery under general anesthesia. The patients were divided into two groups: group A received 60 mg/kg of magnesium 15 minutes before intubation with 1.2 mg/kg of rocuronium, and group B received 60 mg/kg of magnesium before 0.6 mg/kg of rocuronium. Intubating conditions were assessed and graded at loss of last twitch after administration in both groups, considering ease of intubation, vocal cord position, and response to the insertion of the tracheal tube. Simultaneously, hemodynamic variations were recorded just before intubation, at one minute and five minutes post-intubation. Results Intubating conditions with 0.6 mg/kg of rocuronium were comparable or equally good compared to 1.2 mg/kg of rocuronium with magnesium pre-treatment. Conclusions Magnesium pre-treatment enhances the neuromuscular blocking effect of rocuronium, reducing its onset time without clinically significant prolongation of the duration of the block.
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  • 文章类型: Journal Article
    手术时化疗和放疗后的患者可能会出现不同的全身性问题,这可能会使麻醉管理复杂化。肌肉松弛剂和化学治疗剂之间可能发生一些相互作用。
    本文旨在介绍在接受化疗和放疗的癌症患者中使用肌肉松弛剂的方法。
    我们的工作基于现有文献和作者的经验。
    根据我们的观察和对医学文献的全面检查,在接受化疗和放疗的个体中使用肌肉松弛剂时,建议谨慎行事。化疗和放疗后,所有肌肉松弛剂的行为都会有所不同,出于这个原因,从业者应该熟悉他们选择的肌肉松弛剂的药效学和药代动力学。
    UNASSIGNED: Patients after chemotherapy and radiotherapy while being operated can suffer from different systemic problems, which may complicate the anesthetic management. Some interactions between muscle relaxants and chemotherapeutics can occur.
    UNASSIGNED: This article aims to present the use of muscle relaxants in cancer patients who have undergone chemotherapy and radiotherapy.
    UNASSIGNED: Our work is based on the available literature and the authors\' experience.
    UNASSIGNED: Based on our observations and a thorough examination of the medical literature, it is advisable to exercise significant caution when employing muscle relaxants in individuals undergoing chemotherapy and radiotherapy. All muscle relaxants can behave differently after chemotherapy and radiotherapy, and for this reason, practitioners should familiarize themselves with the pharmacodynamics and pharmacokinetics of their chosen muscle relaxant.
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  • 文章类型: Letter
    暂无摘要。
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  • 文章类型: Journal Article
    目的:评估了腹部周围神经阻滞(PNB)和神经肌肉阻滞深度的组合对手术视野的影响。
    方法:38例接受机器人辅助腹腔镜前列腺癌根治术(RARP)的患者随机分为两组:PNB组(中度神经肌肉阻滞[4个1-3个抽搐]腹部PNB)和非PNB组(深度神经肌肉阻滞[强直后0-2次抽搐]无腹部PNB)。主要结果是腹腔压力从8mmHg增加到12mmHg时,通过脐口和腹膜之间的距离(Δ距离)变化来评估腹腔松弛深度的变化。次要结果是CO2的使用增加气腹压力和手术期间手术评分(SRS)的主观差异。
    结果:非PNB组和PNB组之间的Δ距离和8至12mmHg的CO2使用量没有显着差异(1.34±0.65vs.1.28±0.61厘米,p=0.763和3.64±1.68vs.4.34±1.44L,分别为p=0.180)。SRS也没有显著差异。压力从6mmHg增加到8mmHg的Δ距离值的比较,非PNB组和PNB组之间的6至10mmHg和6至12mmHg也没有显示组间差异,尽管压力增量存在显著的组内差异(p<0.001)。
    结论:我们的研究结果表明,腹部PNB的中度神经肌肉阻滞维持了RARP的足够手术空间,与深层神经肌肉阻滞所获得的空间没有显着差异。
    OBJECTIVE: The impact of the combination of abdominal peripheral nerve block (PNB) and the depth of neuromuscular blockade on the surgical field were assessed.
    METHODS: Thirty-eight patients undergoing elective robot-assisted laparoscopic radical prostatectomy (RARP) were randomized into two groups: a PNB group (moderate neuromuscular block [train-of-four 1-3 twitches] with abdominal PNB) and a non-PNB group (deep neuromuscular block [post-tetanic count 0-2 twitches] without abdominal PNB). The primary outcome was the change in the depth of the abdominal cavity relaxation assessed by the change in the distance (Δdistance) between the umbilicus port and peritoneum upon pneumoperitoneal pressure increase from 8 to 12 mmHg. The secondary outcomes were the CO2 usage for the pneumoperitoneal pressure increase and the subjective differences in the Surgical Rating Score (SRS) during surgery.
    RESULTS: The Δdistance and the CO2 usage from 8 to 12 mmHg did not differ significantly between the non-PNB and PNB groups (1.34 ± 0.65 vs. 1.28 ± 0.61 cm, p = 0.763 and 3.64 ± 1.68 vs. 4.34 ± 1.44 L, p = 0.180, respectively). There was also no significant difference in SRS. Comparisons of the Δdistance values for pressure increases from 6 to 8 mmHg, 6 to 10 mmHg and 6 to 12 mmHg between the non-PNB and PNB groups also showed no between-group differences, despite significant intra-group differences (p < 0.001) by pressure increment.
    CONCLUSIONS: Our findings indicate that moderate neuromuscular block with abdominal PNB maintained an adequate surgical space for RARP, with no significant difference from the space achieved by deep neuromuscular block.
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  • 文章类型: Journal Article
    在检查面罩通气后施用神经肌肉阻滞药物(NMBDs)的传统做法受到反复挑战。这项研究比较了在气道正常的患者中使用NMBD前后面罩通气的效率。测量的次要结果是面罩通气和气管插管条件的等级。
    经过道德批准,计划在全身麻醉下进行择期手术的18~65岁年龄组患者(n=120)被随机分为两组.第1组在检查面罩通气之前接受了NMBD。第2组在检查面罩通气后接受NMBD。肺部通风180秒,记录呼气潮气量(Vte)作为主要结局.使用汉斯对面罩通气的分级来对面罩通气进行分级。根据插管条件评估插管的难易程度(喉镜检查的难易程度,声带运动,和肢体运动)。采用SPSS20.0软件进行统计分析。
    对于总共180秒的面罩通风,第1组呼吸暂停后测量的平均值(标准偏差)Vte明显高于第2组[471.9(63.3)vs434.8(77.0)mL/次呼吸,P=0.004]。所有患者的插管条件都很好或很好。
    施用NMBDs导致更大的面罩Vte和更短的插管时间。
    UNASSIGNED: The traditional practice of administrating neuromuscular blocking drugs (NMBDs) after checking face mask ventilation is challenged repeatedly. This study compared the efficiency of face mask ventilation before and after administrating an NMBD in a patient with a normal airway. The secondary outcome measured was the grade of mask ventilation and tracheal intubating conditions.
    UNASSIGNED: After ethical approval, patients (n = 120) in the age group of 18-65 years scheduled for elective surgery under general anaesthesia were randomly assigned into two groups. Group 1 received an NMBD before checking face mask ventilation. Group 2 received an NMBD after checking face mask ventilation. Lungs were ventilated for 180 s, during which expiratory tidal volume (Vte) was recorded as the primary outcome. Hans\'s grading for face mask ventilation was used to grade mask ventilation. The ease of intubation was assessed based on intubating conditions (ease of laryngoscopy, vocal cord movement, and limb movement). SPSS 20.0 software was used for statistical analysis.
    UNASSIGNED: For a total of 180 seconds of mask ventilation, the mean (standard deviation) Vte measured after apnoea was significantly higher in Group 1 versus Group 2 [471.9 (63.3) vs 434.8 (77.0) mL/breath, P = 0.004]. The intubating condition was either excellent or good in all patients.
    UNASSIGNED: The administration of NMBDs resulted in a larger mask Vte and shorter intubation time.
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  • 文章类型: Randomized Controlled Trial
    高体脂百分比患者的药效学可能与肥胖患者相似。这项随机对照临床试验观察了罗库溴铵对不同体脂百分比(PBFs)患者的影响。本研究纳入了在上海市总医院进行全身麻醉下择期泌尿外科或盆腔手术的54例患者;纳入了51例患者进行数据分析。PBF正常(<25%)的患者根据总体重(N-TBW,对照组)。PBF较高(≥25%)的患者根据总体重(H-TBW)计算单剂量的罗库溴铵。PBF和罗库溴铵较高的患者根据无脂质量(H-FFM)给药。一组四个(TOF)-观察加速度描记器用于测量罗库溴铵的作用。H-TBW(91.9±28.8s)的起效时间明显短于N-TBW和H-FFM(p=0.003)。H-TBW的临床持续时间和药理持续时间明显长于其他组(p=0.000和0.000);三组的TOF比值0.25-0.9时间差异有统计学意义(p=0.005)。三组间恢复时间(p=0.103)和恢复指数(p=0.159)差异无统计学意义。基于FFM的罗库溴铵对高PBF患者的影响与正常患者相似。基于TBW计算的单剂量罗库溴铵可能会缩短起效时间,延长临床和药理持续时间,并延长恢复时间。
    The pharmacodynamics in patients with high body fat percentage might be similar to those in obese patients. This randomised controlled clinical trial observed the effects of rocuronium in patients with different percent body fats (PBFs). Fifty-four patients who underwent elective urological or pelvic surgery under general anaesthesia at Shanghai General Hospital were included in the present study; 51 patients were included for data analysis. Patients with normal PBF (<25%) were given a single dose of rocuronium calculated based on total body weight (N-TBW, control group). Patients with a higher PBF (≥25%) were given a single dose of rocuronium calculated based on total body weight (H-TBW). Patients with higher PBF and rocuronium were dosed based on fat-free mass (H-FFM). A train of four (TOF)-Watch acceleromyography monitor was used to measure the effects of the rocuronium. H-TBW (91.9 ± 28.8 s) had significantly shorter onset time than N-TBW and H-FFM (p = 0.003). H-TBW had significantly longer clinical duration time and pharmacological duration time than the other groups (p = 0.000 and 0.000, respectively); the TOF ratio0.25-0.9 time was significantly different among the three groups (p = 0.005). There were no significant differences in the recovery time (p = 0.103) or recovery index (p = 0.159) among the three groups. The effects of rocuronium dosed based on FFM in patients with high PBFs are similar to those in normal patients. A single dose of rocuronium calculated based on TBW might shorten the onset time, prolong the clinical and pharmacological duration times, and prolong the recovery time.
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  • 文章类型: Journal Article
    背景:由于药物的不良镇静作用,美国老年人口服肌肉松弛剂处方的增长令人担忧。巴氯芬是与脑病相关的γ-氨基丁酸激动剂肌肉松弛剂。我们对老年人口服巴氯芬与其他肌肉松弛剂(替扎尼定或环苯扎林)相关的跌倒和骨折风险进行了表征。
    方法:我们设计了一个新用户,使用GeisingerHealth的三级卫生系统数据进行主动比较研究,宾夕法尼亚州(2005年1月至2018年12月)。新接受巴氯芬治疗的老年人(年龄≥65岁),替扎尼定,或环苯扎林被包括在内。使用基于倾向评分的治疗加权逆概率(IPTW)来平衡58个基线特征的治疗组。使用精细灰色竞争风险回归来估计跌倒和骨折的风险。
    结果:研究队列由2205名新的巴氯芬使用者组成,1103个新的替扎尼定用户,和9708个新的环苯扎林使用者。在100天的中位随访中,与替扎尼定相比,巴氯芬与更高的跌倒风险相关(IPTW发病率,108.4vs.61.9/1000人年;次级分布危险比[SHR],1.68[95%CI,1.20-2.36])。与巴氯芬相关的跌倒风险与环苯扎林相当(SHR,1.17[95%CI,0.93-1.47]),中位随访时间为106天。使用巴氯芬与替扎尼定治疗的患者的骨折风险相似(SHR,0.85[95%CI,0.63-1.14])或环苯扎林(SHR,0.85[95%CI,0.67-1.07])。
    结论:与巴氯芬相关的跌倒风险大于替扎尼定,但不能与老年人的环苯扎林相比。老年巴氯芬使用者的骨折风险相当,替扎尼定,和环苯扎林。我们的发现可能会在处方口服肌肉松弛剂的日益常见的临床遭遇中提供风险收益考虑。
    The growth of oral muscle relaxant prescriptions among older adults in the United States is concerning due to the drugs\' adverse sedative effects. Baclofen is a gamma-aminobutyric acid agonist muscle relaxant that is associated with encephalopathy. We characterized the risk of fall and fracture associated with oral baclofen against other muscle relaxants (tizanidine or cyclobenzaprine) in older adults.
    We designed a new-user, active-comparator study using tertiary health system data from Geisinger Health, Pennsylvania (January 2005 through December 2018). Older adults (aged ≥65 years) newly treated with baclofen, tizanidine, or cyclobenzaprine were included. Propensity score-based inverse probability of treatment weighting (IPTW) was used to balance the treatment groups on 58 baseline characteristics. Fine-Gray competing risk regression was used to estimate the risk of fall and fracture.
    The study cohort comprised of 2205 new baclofen users, 1103 new tizanidine users, and 9708 new cyclobenzaprine users. During a median follow-up of 100 days, baclofen was associated with a higher risk of fall compared to tizanidine (IPTW incidence rate, 108.4 vs. 61.9 per 1000 person-years; subdistribution hazard ratio [SHR], 1.68 [95% CI, 1.20-2.36]). The risk of fall associated with baclofen was comparable to cyclobenzaprine (SHR, 1.17 [95% CI, 0.93-1.47]) with a median follow-up of 106 days. The risk of fracture was similar among patients treated with baclofen versus tizanidine (SHR, 0.85 [95% CI, 0.63-1.14]) or cyclobenzaprine (SHR, 0.85 [95% CI, 0.67-1.07]).
    The risk of fall associated with baclofen was greater than tizanidine, but not compared to cyclobenzaprine in older adults. The risk of fracture was comparable among the older users of baclofen, tizanidine, and cyclobenzaprine. Our findings may inform risk-benefit considerations in the increasingly common clinical encounters where oral muscle relaxants are prescribed.
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