Antispasmodics

抗痉挛药
  • 文章类型: Journal Article
    功能性腹痛是一种中枢和外周致敏过程融合的疾病,导致超敏反应和异常性疼痛。鉴别诊断是用有机消化,肾,妇科,内分泌,或神经系统疾病。每个患者的治疗应该是个性化的。在使人衰弱的疼痛的情况下,可以启动具有不同作用机制的药物组合疗法,而在不太严重的情况下,建议根据临床反应逐步引入药物进行治疗.第一行包括一般生活方式建议和抗痉挛物质,像薄荷油,抗胆碱能/抗毒蕈碱,和钙通道拮抗剂.在二线治疗中,添加神经调节剂。最后,当这些措施失败时,三线治疗如加巴喷丁和非典型抗精神病药被考虑.如果有专门的治疗师可以治疗这些疾病,则应考虑进行心理干预。
    Functional abdominal pain is a disorder in which central and peripheral sensitization processes converge, leading to hypersensitivity and allodynia. Differential diagnosis is made with organic digestive, renal, gynecological, endocrine, or neurological diseases. Treatment should be individualized for each patient. In cases of debilitating pain, therapy combining drugs with different mechanisms of action can be initiated, while in less severe cases, therapy with a progressive introduction of drugs based on clinical response is advised. The first line includes general lifestyle advice and antispasmodic substances, like peppermint oil, anticholinergic/antimuscarinic, and calcium channels antagonists. In the second line of treatment, neuromodulating agents are added. Finally, when these measures fail, third-line treatments such as gabapentine and atypical antipsychotics are considered. Psychological interventions should be considered if specialized therapists are available to manage these disorders.
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  • 文章类型: Journal Article
    一个快速的,简单,准确,精确,和廉价的荧光协议已被提出用于分析磷酸二酯酶-IV抑制剂,即盐酸drotaverine。荧光协议基于通过在pH3.1(乙酸盐缓冲液)定量添加drotaverine来估计曙红Y荧光强度的降低。形成离子对复合物,这导致染料的荧光强度猝灭,而无需在534nm处预先提取(λex。339nm)。深入研究并优化了影响络合物生成的不同反应周边(drotaverine和曙红之间的离子对)。开发的荧光法方案能够在0.4至2.5µgmL-1的线性范围内定量估计drotaverine。在针对ICH指南的方法验证之后,它被用于测定其商业制剂中的drotaverine。通过与其他报道方法的比较,开发和验证的荧光协议是能够估计drotaverine在商业制备具有良好的准确性和优异的精度。
    A fast, simple, accurate, precise, and cheap fluorimetric protocol has been proposed for analysis of a phosphodiesterase-IV inhibitor, namely drotaverine hydrochloride. Fluorimetric protocol is based on estimating the decrease in the eosin Y fluorescence intensity by quantitative addition of drotaverine at pH 3.1 (acetate buffer). An ion pair complex is formed, which leads to quenching in the fluorescence intensity of the dye without need of prior extraction at 534 nm (λex. 339 nm). Different reaction perimeters which influence the production of complex (ion pair between drotaverine and eosin) were deeply investigated and optimized. The developed fluorimetric protocol is capable for quantitative estimation of drotaverine in linear range of 0.4 to 2.5 µg mL-1. After method validation in respect to ICH guidelines, it was applied to determine drotaverine in its commercial preparation. By comparing with other reported method, the developed and validated fluorimetric protocol is capable for estimation of drotaverine in commercial preparation with good accuracy and excellent precision.
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  • 文章类型: Systematic Review
    这篇综述强调了巴氯芬和替扎尼定对老年社区居住成年人的不良反应。
    进行了文献检索,包括“不利影响”的搜索条件,\"\"巴氯芬,\"\"老年人,\"\"坠落,\"\"骨折,“和”替扎尼定。“如果研究描述了50岁及以上的社区居住成年人,他们接受口服巴氯芬或替扎尼定。联邦药物管理局不良事件报告系统(FAERS)数据被编制用于不良反应发生率。
    文献检索于2019年7月完成,并于2023年6月更新。由2名独立审阅者进行的审阅产生了15条记录。FAERS确定了486(巴氯芬)和305(替扎尼定)感兴趣的不良反应。
    两项评估老年人使用巴氯芬的回顾性队列研究显示,慢性肾病(7.2%vs0.1%)和终末期肾病(每日剂量20mg或更多;相对危险度[RR]19.8,95%CI=[14.0-28.0])患者的脑病住院率增加。其他文章为病例报告;10篇报道运动障碍,脑病或定向障碍,以及与巴氯芬有关的困倦,5篇文章报道了替扎尼定的心动过缓和/或低血压。FAERS公共仪表板显示,关注的不利影响的总体发生率分别为12.1%和28.7%,巴氯芬和替扎尼定的跌倒发生率分别为27.8%和29.2%,分别。巴氯芬和替扎尼定与老年人的不良反应有关。应该考虑替代代理人,但是,如有必要,提供者应从较低剂量开始并缓慢增加。
    这篇综述强调了在老年人中谨慎使用巴氯芬和替扎尼定的重要性。
    UNASSIGNED: This review highlights adverse effects of baclofen and tizanidine in older community-dwelling adults.
    UNASSIGNED: A literature search was conducted, including search terms of \"adverse effect,\" \"baclofen,\" \"elderly,\" \"falls,\" \"fractures,\" and \"tizanidine.\" Studies were included if they described community-dwelling adults aged 50 years and older who received oral baclofen or tizanidine. The Federal Drug Administration Adverse Event Reporting System (FAERS) data were compiled for adverse effect incidence.
    UNASSIGNED: The literature search was completed in July 2019 and updated in June 2023. Reviews performed by 2 independent reviewers yielded 15 records. FAERS identified 486 (baclofen) and 305 (tizanidine) adverse effects of interest.
    UNASSIGNED: Two retrospective cohort studies evaluating baclofen use in older adults showed increased hospitalizations for encephalopathy in chronic kidney disease (7.2% vs 0.1%) and end-stage renal disease (daily dose 20 mg or more; relative risk [RR] 19.8, 95% CI = [14.0-28.0]). Other articles were case reports; 10 articles reported dyskinesias, encephalopathy or disorientation, and drowsiness associated with baclofen, and 5 articles reported bradycardia and/or hypotension with tizanidine. The FAERS Public Dashboard revealed 12.1% and 28.7% overall incidence of adverse effects of interest, with a 27.8% and 29.2% incidence of falls for baclofen and tizanidine, respectively. Baclofen and tizanidine are associated with concerning adverse effects in older adults. Alternative agents should be considered, but, if necessary, providers should start at lower doses and increase slowly.
    UNASSIGNED: This review highlights the importance of using baclofen and tizanidine with caution in older adults.
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  • 文章类型: Journal Article
    胃肠道疼痛的治疗在许多肠-脑相互作用(DGBI)障碍的管理中仍然是重大挑战。药物和各种行为疗法是疼痛为主的DGBI如肠易激综合征的潜在治疗选择。功能性消化不良,功能性胃灼热,和中枢介导的腹痛综合征。在这篇杂志上发表的回顾性研究中,Luoetal.使用罗马基金会全球流行病学研究,从全球角度检查DGBI患者中处方止痛药的使用情况。这篇综述文章概述了各种药物疼痛管理药物的使用模式(阿片类药物,中枢神经调质,抗痉挛药,和其他外周作用剂)和非药物疗法在DGBI疼痛管理的临床实践建议中。
    Treatment of gastrointestinal pain remains a significant challenge in the management of many disorders of gut-brain interaction (DGBI). Pharmacologic agents and various behavioral therapies are among the potential therapeutic options for pain-predominant DGBI such as irritable bowel syndrome, functional dyspepsia, functional heartburn, and centrally mediated abdominal pain syndrome. In the retrospective study published in this journal, Luo et al. examine the use of prescription pain medications from a global perspective among patients with DGBI using the Rome Foundation Global Epidemiology Study. This review article provides an overview of usage patterns of various pharmacologic pain management agents (opioids, central neuromodulators, antispasmodics, and other peripherally acting agents) and non-pharmacologic therapies in the context of clinical practice recommendations on the management of DGBI pain.
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  • 文章类型: Journal Article
    Globally, the prevalence of self-medication among young people has increased exponentially. Due to the basic knowledge and easy access to medicines, undergraduate students at health science colleges are likely to self-medicate. This research was undertaken to assess self-medication prevalence and its contributing factors among female undergraduate students in health science colleges at Majmaah University, Saudi Arabia.
    A descriptive, cross-sectional study involving 214 female students from the Majmaah University in Saudi Arabia\'s health science colleges-Medical: (82, 38.31%) and Applied Medical Science College (132, 61.68%)-was conducted. A self-administered questionnaire with sociodemographic information, drugs used, and reasons for self-medication was used for the survey. Non-probability sampling techniques were used to recruit participants.
    Of the 214 female participants, 173, 80.84 % (medical: 82, 38.31% and applied medical science: 132, 61.68%) confirmed that they were on self-medication. The majority of participants (42.1%) were between the ages of 20 and 21.5 years (mean ± SD: 20.81 ± 1.4). The main reasons for self-medication were quick relief from the illness (77.5%) followed by saving time (76.3%), minor illnesses (71.1%), self-confidence (56.7%), and laziness (56.7%). The use of leftover drugs at home was common among applied medical science students (39.9%). The main indication for self-medication included menstrual problems (82.7 %), headache (79.8%), fever (72.8%), pain (71.1%), and stress (35.3%). The most common drugs used included antipyretic and analgesics (84.4%), antispasmodics (78.9%), antibiotics (76.9%), antacids (68.2%), multivitamins, and dietary supplements (66.5%). On the contrary, the least used drugs were antidepressants, anxiolytics, and sedatives (3.5, 5.8, and 7.5 %, respectively). Family members were the main source of information for self-medication (67.1%), followed by self-acquired knowledge (64.7%), social media (55.5%), and least were friends (31.2%). For adverse effects of the medication, the majority of them consulted the physician (85%) followed by consulting the pharmacist (56.7%) and switched to other drugs or decreased drug dosage. Quick relief, saving time, and minor illness were the main reasons for self-medication among health science college students. It is recommended to conduct awareness programs, workshops, and seminars to educate on the benefits and adverse effects of self-medication.
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  • 文章类型: Journal Article
    肠易激综合征(IBS)是一种功能性胃肠病,具有复杂的发病机制和多方面的治疗方法,旨在缓解临床症状,提高患者的生活质量。它的治疗包括饮食改变和各种药物组的药物,如止泻药,抗胆碱能药,血清素受体拮抗剂,靶向氯离子通道,等。本文重点介绍了一些甲贝维林前体作为潜在的解痉挛药的合成和生物学评估。
    方法:进行旨在预测化合物的药效学特征的模拟分析。基于这些预测,建立了化合物的离体生物电活性(BEA)和免疫组织化学作用。对化合物进行了彻底的生物学评估,以评估其体外抗微生物和细胞毒性活性。
    结果:所有新合成的化合物都具有类似药物的性质,其中3-甲基-1-苯基丁烷-2-胺3由于Ca2通道调节而显示出BEA的显着变化,Ca2+内流调制,以及随后平滑肌细胞反应的变化。免疫组织化学研究显示与获得的BEA数据具有良好的相关性,将胺3定义为前导结构。对于所有测试的化合物,没有观察到对人类恶性白血病细胞系(LAMA-84,K-562)的细胞毒性。
    结论:根据实验结果,我们概述了3-甲基-1-苯基丁-2-胺3作为口服活性长期治疗IBS的潜在有效选择。
    Irritable bowel syndrome (IBS) is a functional gastroenterological disorder with complex pathogenesis and multifaceted therapy approaches, aimed at alleviating clinical symptoms and improving the life quality of patients. Its treatment includes dietary changes and drugs from various pharmacological groups such as antidiarrheals, anticholinergics, serotonin receptor antagonists, targeting chloride ion channels, etc. The present article is focused on the synthesis and biological evaluation of some mebeverine precursors as potential antispasmodics.
    METHODS: In silico analysis aimed at predicting the pharmacodynamic profile of the compounds was performed. Based on these predictions, ex vivo bioelectrical activity (BEA) and immunohistochemical effects of the compounds were established. A thorough biological evaluation of the compounds was conducted assessing their in vitro antimicrobial and cytotoxic activity.
    RESULTS: All the newly synthesized compounds exerted drug-like properties, whereby 3-methyl-1-phenylbutan-2-amine 3 showed a significant change in BEA due to Ca2+ channel regulation, Ca2+ influx modulation, and a subsequent change in smooth muscle cell response. The immunohistochemical studies showed a good correlation with the obtained data on the BEA, defining amine 3 as a leader structure. No cytotoxicity to human malignant leukemic cell lines (LAMA-84, K-562) was observed for all tested compounds.
    CONCLUSIONS: Based on the experimental results, we outlined 3-methyl-1-phenylbutan-2-amine 3 as a potential effective choice for orally active long-term therapy of IBS.
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  • 文章类型: Journal Article
    UNASSIGNED:作为术前用药组成部分的抗痉挛药是否有助于通过食管胃十二指肠镜检查(EGDS)筛查来检测病变尚不清楚。我们的主要目的是调查这种可能性。
    UNASSIGNED:这项回顾性研究中的队列包括2015年10月至2020年9月在日本和歌山红十字会医学中心接受EGDS筛查的连续无症状个体。调查的病变包括食管鳞状细胞癌或腺癌,胃腺瘤或腺癌,十二指肠腺瘤或腺癌。
    UNASSIGNED:在31484名参与者中的72名(0.23%)中检测到目标病变,18260人和13224人接受和未接受术前抗菌药物,分别。这些组的病灶检出率分别为0.21%(38/18260)和0.26%(34/13224),分别为(P=0.40)。多因素logistic回归分析显示,抗痉挛药的给药与目标病变的检出率之间无相关性[P=0.24,赔率比(95%CI):1.46(0.78-2.75)]。
    未经授权:防痉挛药,超过一半的研究队列中使用了这些药物,没有提高靶向病变的检出率。
    UNASSIGNED: Whether administration of antispasmodics as a component of premedication contributes to detection of lesions by screening esophagogastroduodenoscopy (EGDS) remains unclear. Our primary aim was to investigate this possibility.
    UNASSIGNED: The cohort in this retrospective study comprised consecutive asymptomatic individuals who had undergone screening EGDS as part of a health check-up at the Japanese Red Cross Wakayama Medical Center from October 2015 to September 2020. The investigated lesions comprised esophageal squamous cell carcinoma or adenocarcinoma, gastric adenoma or adenocarcinoma, and duodenal adenoma or adenocarcinoma.
    UNASSIGNED: Targeted lesions were detected in 72 of 31 484 participants (0.23%), 18 260 and 13 224 of whom had received and not received pre-procedure antispasmodics, respectively. The rates of detection of lesions in these groups were 0.21% (38/18260) and 0.26% (34/13224), respectively (P = 0.40). Multivariate logistic regression analysis showed no association between administration of antispasmodics and rates of detection of targeted lesions [P = 0.24, Odds ratio (95% CI): 1.46 (0.78-2.75)].
    UNASSIGNED: Antispasmodics, which were administered to more than half of the study cohort, did not improve the rate of detection of targeted lesions.
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  • 文章类型: Systematic Review
    背景:在中国,针灸已被广泛用于治疗肠易激综合征(IBS)。一些随机对照试验(RCTs)已经证明了它们的有效性,但它很少与一线解痉挛药进行比较以验证其有效性。因此,我们使用调整后的间接治疗比较荟萃分析,比较了针刺与解痉挛治疗IBS的疗效.方法:Embase,OVIDMedline,从开始到2022年3月14日,搜索了Cochrane中央对照试验登记册数据库,没有语言限制。纳入了将抗痉挛药或针灸与安慰剂或抗痉挛药之一进行比较的随机对照试验。感兴趣的主要结果是腹痛的改善。次要结果是整体IBS症状和不良事件的缓解。随机效应模型被用来汇集数据。效应大小通过标准化平均差(SMD)或相对比率来测量,并按P评分对针灸和不同止痉挛药的有效性进行排序。结果:纳入35个RCT(n=5,190)。分析表明,西美托,drotaverine,针灸,和pinarverium在缓解腹痛方面优于安慰剂;cimetropium(SMD,-3.00[95CI,-4.47至-1.53],P分数=0.99)排名最有效。在成对比较中,在缓解腹痛方面,针灸治疗效果优于除西咪嗪和屈他维林外的大多数解痉挛药,尽管组间差异在统计学上无统计学意义。在整体IBS症状缓解的连续结果分析中,结果表明,pinaverium更有效(SMD,1.72[95CI,0.53至2.92],P评分=0.90)比安慰剂。曲美布汀和针灸比安慰剂有更大的改善,但组间无显著差异。在成对比较中,针灸比匹维胺更有效(SMD,-1.11[95CI,-1.94至-0.28])缓解整体IBS症状。在分析不良事件时,针灸的不良事件发生率低于大多数其他解痉挛药。结论:西梅,drotaverine,和针灸在改善腹痛方面都优于安慰剂。在缓解全球IBS症状方面,针灸优于匹维胺,和针灸的不良事件比大多数抗痉挛药更低。
    Background: Acupuncture has been extensively applied to manage irritable bowel syndrome (IBS) in clinical practice in China. Some randomized controlled trials (RCTs) have demonstrated their efficacy, but it has rarely been compared with first-line antispasmodics to verify their effectiveness. Therefore, we compare acupuncture with antispasmodics in the treatment of IBS by using an adjusted indirect treatment comparison meta-analysis. Methods: Embase, OVID Medline, and the Cochrane Central Register of Controlled Trials databases were searched from inception to 14 March 2022, with no language restrictions. RCTs comparing antispasmodics or acupuncture with placebo or one of the antispasmodics were enrolled. The primary outcome of interest was the improvement of abdominal pain. And the secondary outcomes of interest were the relief of global IBS symptoms and adverse events. The random-effects model was utilized to pool data. The effect size was measured by standardized mean difference (SMD) or relative ratio, and the effectiveness of acupuncture and different antispasmodics were ranked by P-scores. Results: Thirty-five RCTs (n = 5,190) were included. The analysis showed that cimetropium, drotaverine, acupuncture, and pinarverium were superior over placebo in relieving abdominal pain; cimetropium (SMD, -3.00 [95%CI, -4.47 to -1.53], P-score = 0.99) ranked the most effective. In pairwise comparisons, acupuncture had a greater improvement than most antispasmodics except cimetropium and drotaverine in relieving abdominal pain, although the between-group difference was statistically insignificant. In the analysis of continuous outcome in the relief of global IBS symptoms, the result showed that pinaverium was more effective (SMD, 1.72 [95%CI, 0.53 to 2.92], P-score = 0.90) than placebo. Trimebutine and acupuncture had greater improvements than placebo, but no significant difference was shown between groups. In pairwise comparisons, acupuncture was more effective than pinaverium (SMD, -1.11 [95%CI, -1.94 to -0.28]) in relieving global IBS symptoms. In the analysis of adverse events, acupuncture had a lower adverse event rate than most of the other antispasmodics. Conclusion: Cimetropium, drotaverine, and acupuncture were all better than placebo in improving abdominal pain. Acupuncture was preferred over pinaverium in relieving global IBS symptoms, and acupuncture had lower adverse events than most antispasmodics.
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  • 文章类型: Practice Guideline
    肠易激综合征(IBS)是一种常见的功能性胃肠病,与严重的疾病负担有关。该美国胃肠病学协会指南旨在支持从业人员决定使用药物治疗IBS伴主要腹泻(IBS-D),并且是对先前技术审查和指南的更新。
    建议评估的分级,开发和评估框架用于评估证据并提出建议。技术审查小组根据临床医生和患者的重要性对临床问题和结果进行了优先排序,并对以下药物进行了证据审查:利福昔明,Alosetron,洛哌丁胺,三环抗抑郁药,选择性5-羟色胺再摄取抑制剂,和抗痉挛药.指南小组审查了证据,并使用证据到决定框架来制定建议。
    专家组就IBS-D患者管理的8项建议达成一致小组对伊洛沙多林提出了有条件的建议,利福昔明,Alosetron,(中等确定性),洛哌丁胺(非常低的确定性),三环抗抑郁药,和解剖学(低确定性)。小组对使用选择性5-羟色胺再摄取抑制剂提出了有条件的建议(确定性低)。
    Irritable bowel syndrome (IBS) is a common functional gastrointestinal disorder associated with significant disease burden. This American Gastroenterological Association Guideline is intended to support practitioners in decisions about the use of medications for the pharmacological management of IBS with predominant diarrhea (IBS-D) and is an update of a prior technical review and guideline.
    The Grading of Recommendations Assessment, Development and Evaluation framework was used to assess evidence and make recommendations. The technical review panel prioritized clinical questions and outcomes according to their importance for clinicians and patients and conducted an evidence review of the following agents: eluxadoline, rifaximin, alosetron, loperamide, tricyclic antidepressants, selective serotonin reuptake inhibitors, and antispasmodics. The guideline panel reviewed the evidence and used the Evidence-to-Decision Framework to develop recommendations.
    The panel agreed on 8 recommendations for the management of patients with IBS-D. The panel made conditional recommendations for eluxadoline, rifaximin, alosetron, (moderate certainty), loperamide (very low certainty), tricyclic antidepressants, and anstispasmodics (low certainty). The panel made a conditional recommendation against the use of selective serotonin reuptake inhibitors (low certainty).
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  • 文章类型: Journal Article
    在波兰,drotaverine是最常购买的抗痉挛药,然而,关于其使用的现实世界数据却很少。我们评估了使用drotaverine的患者的情况,我们调查了全科医生(GP)的处方模式。在这个横截面中,基于问卷的研究,我们询问购买drotaverine的患者使用它的原因,它的感知功效,满意的治疗,和医生咨询。我们还向全科医生询问了drotaverine在实践中的状况。在650名招募的患者中,74%的人使用drotaverine治疗疼痛,67%的抽筋,19%为腹部不适。大约83%的患者在没有医生建议的情况下购买了drotaverine。在医生的建议下使用它的患者更常见的是女性,年长的,受教育程度较低。对于所有症状,第一次给药后平均严重程度评分下降~5分(0-10分)。98%的患者对drotaverine感到满意。在210名全科医生中,处方drotaverine的百分比是:肠易激综合征的42%,89%为胆石症,60%作为泌尿系感染的支持治疗,89%为肾结石,75%为月经疼痛。全科医生认为drotaverine更有用,有效,并且比其他药物更能耐受腹痛或痉挛。Drotaverine显着降低了服用的所有症状的严重程度,它被认为是有效和可以容忍的。
    In Poland, drotaverine is the most frequently purchased antispasmodic, yet there is a paucity of real-world data on its use. We evaluated the profiles of patients who used drotaverine, and we investigated prescription patterns among general practitioners (GPs). In this cross-sectional, questionnaire-based study, we asked patients who purchased drotaverine about their reasons for using it, its perceived efficacy, satisfaction with treatment, and physician consultation. We also asked GPs about the status of drotaverine in their practice. Among 650 recruited patients, 74% used drotaverine for pain, 67% for cramps, and 19% for abdominal discomfort. Approximately 83% of patients purchased drotaverine without a physician\'s advice. Patients who used it after a physician\'s advice were more frequently female, older, and less educated. For all symptoms, mean severity scores decreased by ~5 points (0-10 scale) after the first dose. Ninety-eight percent of patients were satisfied with drotaverine. Among 210 GPs, the percentages prescribing drotaverine were: 42% for irritable bowel syndrome, 89% for cholelithiasis, 60% as supportive therapy for urinary infections, 89% for nephrolithiasis, and 75% for menstruation pain. The GPs perceived drotaverine as more useful, effective, and tolerable than other drugs for abdominal pain or cramps. Drotaverine significantly reduced the severity of all symptoms for which it was taken, and it was perceived as effective and tolerable.
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