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An Update on the Pharmacological Aspects of Vaccines and Antivirals for the Management of Monkeypox 猴痘疫苗和抗病毒药物的药理学研究进展
IF 0.2 Q4 Medicine Pub Date : 2022-12-01 DOI: 10.1177/0976500X231156733
Jerin James, P. A., K. P, J. Rani, S. V.
Monkeypox is a self-limiting zoonotic disease caused by the monkeypox virus belonging to the genus of orthopox viruses. Initially considered an ‘African disease’, this infection has crossed the boundaries to affect other continents and it has raised tremendous concerns among the general public as well as the medical fraternity all over the world, particularly because of the lack of specific vaccinations and drugs for the management of the illness. Epidemiological evaluation of the current infection has reported that it is mainly transmitted through sexual contact in bisexual men, mostly whites, and in those with pre-existing human immunodeficiency virus infection. The most common presentations were skin rash, anogenital lesions, or mucosal lesions along with systemic symptoms. It has been established that the vaccines and drugs approved for the management of smallpox could be used for the management of the current monkeypox outbreak. Vaccinia Immune Globulin (VIG) and vaccines like JYNNEOS and ACAM2000 and antiviral drugs like tecovirimat, cidofovir (CDV), and brincidofovir are being considered for those patients with serious diseases. It is imperative for physicians to understand the pharmacological aspects of these drugs for delivering better care to patients with monkeypox, which is eventually essential for the containment of this infection. This review covers updates on vaccines as well as drugs for the prevention and management of monkeypox.
猴痘是由猴痘病毒引起的一种自限性人畜共患疾病,属于正痘病毒属。最初被认为是一种“非洲疾病”,这种感染已经跨越国界影响到其他大陆,它引起了世界各地普通公众和医学界的极大担忧,特别是因为缺乏特定的疫苗接种和疾病管理药物。对当前感染的流行病学评估报告称,它主要通过双性恋男性(主要是白人)和已有人类免疫缺陷病毒感染者的性接触传播。最常见的表现是皮疹、肛门生殖器病变或粘膜病变以及全身症状。已经确定,批准用于管理天花的疫苗和药物可以用于管理当前的猴痘疫情。Vaccinia Immune Globulin(VIG)和JYNNEOS和ACAM2000等疫苗以及tecovirimat、cidofovir(CDV)和brincidovovir等抗病毒药物正在考虑用于那些患有严重疾病的患者。医生必须了解这些药物的药理学方面,以便为猴痘患者提供更好的护理,这最终对遏制这种感染至关重要。这篇综述涵盖了预防和管理猴痘的疫苗以及药物的最新情况。
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引用次数: 1
Self-assumed Neurologic Related Condition Deviated Metoclopramide-Induced Acute Dystonic of Oculogyric Crisis in a Woman of Childbearing Age: A Case Report 一例育龄妇女自我假设的神经系统相关疾病——胃复安诱发的急性眼功能不全危象:一例报告
IF 0.2 Q4 Medicine Pub Date : 2022-12-01 DOI: 10.1177/0976500X221142377
N. Ismail, A. Jha, K. Goh, L. Ming, Mohd Shahezwan Abd Wahab, N. Shah, Akshay Shah, Andi Hermansyah
A 26-year-old Malaysian woman (childbearing age) attended a private primary care clinic with a known case of gastroesophageal reflux disease (GERD) and complained of persistent nausea and a few episodes of vomiting. She had no known drug allergy, no surgical history, no hospitalization in the last two years, was a non-smoker, and no history of drug or alcohol abuse. The patient was prescribed Tab metoclopramide 10 mg TDS and Tab ranitidine 150 mg BD for five days. About 30 min after oral administration of both medicines, her eyes rolled involuntary upward, leading to lateral deviation of the eyes, and mouth jaws clenched as if “dislocated jaws.” The patient was immediately brought into an emergency department (ED) of a public tertiary care hospital. A drug challenge test was done which resulted in the withdrawal of metoclopramide. The accompanied sister later disclosed that the patient had taken metoclopramide and ranitidine from a private clinic earlier in the day. The patient self-assumed to have a sudden seizure, due to excessive hot weather and dehydration. A slow intravenous infusion of 50 mg/mL diphenhydramine hydrochloride in 0.9% w/v NaCl 100 mL was administered stat. Consequently, the symptoms vanished after approximately 30 min of the therapy, devoid of relapse. The patient was discharged from ED post 8 hours of monitoring with complete recovery. Physicians frequently prescribe metoclopramide to treat nausea and vomiting, which may cause adverse drug reaction of acute dystonic oculogyric crisis (OGC). Due to its unwanted and unpredictable extrapyramidal symptoms, metoclopramide should be prescribed and dispensed with caution. Thorough history taking at ED is imperative for correct early diagnosis and treatment, as metoclopramide-induced dystonic OGC has a high probability of confusion with other causes of dystonia such as conversion and seizures, encephalitis, tetanus, and hypercalcemic tetany.
一名26岁的马来西亚妇女(育龄)因已知的胃食管反流病(GERD)病例到一家私人初级保健诊所就诊,并抱怨持续恶心和几次呕吐。她没有已知的药物过敏,没有手术史,过去两年没有住院治疗,不吸烟,也没有吸毒或酗酒史。给患者开了10 mg甲氧氯普胺TDS和150 mg雷尼替丁BD,持续5天。口服这两种药物约30分钟后,她的眼睛不由自主地向上滚动,导致眼睛侧向偏斜,口颚紧闭,仿佛“下巴脱臼”。患者立即被送往公立三级护理医院的急诊科。药物激发试验导致胃复安停药。陪同的姐姐后来透露,患者当天早些时候从一家私人诊所服用了甲氧氯普胺和雷尼替丁。由于天气太热和脱水,患者自我认为突然发作。静滴50 mg/mL盐酸苯海拉明在0.9%w/v NaCl 100 mL中。因此,治疗约30分钟后症状消失,没有复发。患者在监护8小时后出院,完全康复。医生经常开胃复安来治疗恶心和呕吐,这可能会引起急性肌张力障碍性眼脊髓危象(OGC)的药物不良反应。由于甲氧氯普胺具有不必要且不可预测的锥体外系症状,因此应谨慎开药。全面的ED病史对于正确的早期诊断和治疗至关重要,因为甲氧氯普胺诱导的肌张力障碍OGC很可能与肌张力障碍的其他原因混淆,如转换和癫痫发作、脑炎、破伤风和高钙血症性破伤风。
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引用次数: 1
Australia’s Pharmacology Research: A Scientometric Assessment of High-Cited Papers During 2002–2021 澳大利亚药理学研究:2002-2021年高引用论文的科学评估
IF 0.2 Q4 Medicine Pub Date : 2022-12-01 DOI: 10.1177/0976500X231154967
K. Ahmed, B. Gupta, G. M. Mamdapur
Objectives To analyze Australia’s high-cited papers (HCPs) receiving ≥100 citations in pharmacology during 2002–2021 and examine the research characteristics, study performance of the top 30 leading participating organizations and authors, and identification of top 30 journals publishing in this area and sub-fields of their research. Materials and Methods Australia’s HCPs on pharmacology research from the top 30 most productive organizations were identified and extracted from the Scopus database from 2002 to 2021 on 21 September 2022 using a search strategy. Select bibliometric measures were utilized to evaluate the publication productivity of important players in this area. The network analysis was performed to evaluate the collaborative interactions amongst the countries, organizations, authors, and keywords. Results Of the 19,418 Australia’s publications (articles) in pharmacology from the top 30 most productive organizations during 2002–2022, only 685 (3.53%) were HCPs, which together received 1,14,623 citations, averaging 164.4 citations per paper (CPP) and the citations ranged from 100 to 1,230. Two papers had more than 1,000 citations and 16 papers had 500 citations. Of the 685 HCPs, 40.58% (278) and 11.39% (78) received external funding support and were international collaboratives. The most productive organizations were Monash University (n = 155), the University of Queensland (n = 111) and the University of Melbourne (n = 97). The most impactful organizations in terms of CPP and relative citation index (RCI) were James Cook University (203.22 and 1.21), Australian National University (196.67 and 1.18) and Queensland University of Technology (193.45 and 1.16). The most productive authors were J. Li (n = 24), C. J. H. Porter (n = 24) and R. L. Nation (n = 23) (Monash University, Melbourne); and the most impactful authors in terms of CPP were A. Christopoulos (Monash Institute of Pharmaceutical Sciences, Melbourne) (288.21), C.W. Pouton (Monash University, Melbourne) (241.50), and D.L. Peterson (University of Queensland, Brisbane) (225.58). The most productive journals were Antimicrobial Agents and Chemotherapy (n = 59), Environmental Pollution (n = 43) and Journal of Medicinal Chemistry (n = 42). The most impactful journals in terms of CPP were Nature Reviews Drug Discovery (371.8), Antiviral Research (286.86) and European Journal of Pharmaceutical Sciences (253.0). The most important keywords with their frequency of appearances were Animal Experiments (108), Metabolism (76), Drug Effects (67), Animal Models (65), Protein Expression (64), Anti-Bacterial Agents (62), Drug Delivery Systems (54), Drug Formulation (44), Signal Transduction (42), and so on. Conclusion There is an urgent need to increase national funding and expand international collaboration in priority areas, which will help to increase and diversify research output and improve research impact.
目的分析2002-2021年澳大利亚药理学领域被引频次≥100次的高被引论文(HCPs),考察前30名主要参与机构和作者的研究特点、研究表现以及该领域及其子领域前30名期刊的发表情况。材料与方法采用检索策略,于2022年9月21日从Scopus数据库中确定并提取2002年至2021年澳大利亚前30名最具生产力组织的药理学研究HCPs。采用文献计量学方法评价该领域重要参与者的出版效率。进行网络分析以评估国家、组织、作者和关键词之间的协作互动。结果2002-2022年,澳大利亚前30大科研机构发表的19418篇药理学论文(文章)中,只有685篇(3.53%)是hcp,共被引用114623次,平均每篇论文(CPP)被引用164.4次,被引用次数在100 ~ 1230次之间。2篇论文被引用1000次以上,16篇论文被引用500次以上。在685家HCPs中,40.58%(278家)和11.39%(78家)获得了外部资金支持,并且是国际合作机构。生产力最高的组织是莫纳什大学(n = 155)、昆士兰大学(n = 111)和墨尔本大学(n = 97)。在CPP和相对引文指数(RCI)方面,影响力最大的机构分别是詹姆斯库克大学(203.22和1.21)、澳大利亚国立大学(196.67和1.18)和昆士兰理工大学(193.45和1.16)。最高产的作者是J. Li (n = 24)、C. J. H. Porter (n = 24)和R. L. Nation (n = 23)(墨尔本莫纳什大学);CPP影响最大的作者为A. Christopoulos(墨尔本莫纳什药物科学研究所)(288.21)、C.W. Pouton(墨尔本莫纳什大学)(241.50)和D.L. Peterson(布里斯班昆士兰大学)(225.58)。发表最多的期刊是《抗菌药物与化疗》(n = 59)、《环境污染》(n = 43)和《药物化学》(n = 42)。CPP影响最大的期刊是Nature Reviews Drug Discovery(371.8)、抗病毒研究(286.86)和European Journal of Pharmaceutical Sciences(253.0)。出现频率最高的关键词是动物实验(108)、代谢(76)、药物作用(67)、动物模型(65)、蛋白质表达(64)、抗菌药物(62)、药物传递系统(54)、药物制剂(44)、信号转导(42)等。迫切需要增加国家资助,扩大重点领域的国际合作,这将有助于增加和多样化研究产出,提高研究影响力。
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引用次数: 0
A Deep Insight into the Correlation Between Gut Dysbiosis and Alzheimer’s Amyloidopathy 肠道营养不良与阿尔茨海默病淀粉样变性相关性的深入研究
IF 0.2 Q4 Medicine Pub Date : 2022-12-01 DOI: 10.1177/0976500X221150310
S. Kondaveeti, Dithu Thekkekkara, Lakshmi Narayanan T, S. Manjula, Y. M. Tausif, Amrita Babu, S. Meheronnisha
Recent research has shown a strong correlation between gut dysbiosis and Alzheimer’s disease (AD). The purpose of this review is to investigate the relationship between gut dysbiosis, immune system activation, and the onset of AD and to examine current breakthroughs in microbiota-targeted AD therapeutics. A review of scientific literature was conducted to assess the correlation between gut dysbiosis and AD and the various factors associated. Gut dysbiosis produces an increase in harmful substances, such as bacterial amyloids, which makes the gut barrier and blood-brain barrier more permeable. This leads to the stimulation of immunological responses and an increase in cytokines such as interleukin-1β (IL-1β). As a result, gut dysbiosis accelerates the progression of AD. The review highlights the connection between gut dysbiosis and AD and the potential for microbiota-targeted therapies in AD treatment. Pictorial Abstract
最近的研究表明,肠道生态失调与阿尔茨海默病(AD)之间存在着强烈的相关性。这篇综述的目的是研究肠道微生态失调、免疫系统激活和AD发病之间的关系,并考察微生物群靶向AD治疗的最新突破。对科学文献进行了综述,以评估肠道微生态失调与AD之间的相关性以及各种相关因素。肠道微生态失调会增加有害物质,如细菌淀粉样蛋白,使肠道屏障和血脑屏障更具渗透性。这导致免疫反应的刺激和细胞因子如白细胞介素-1β(IL-1β)的增加。因此,肠道生态失调加速了AD的进展。这篇综述强调了肠道生态失调与AD之间的联系,以及微生物群靶向治疗AD的潜力。图片摘要
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引用次数: 0
Antimicrobial Resistance, Phenotypic Characteristics, and Biofilm Production in Citrobacter freundii Isolates Obtained from Urinary Tract Infections 从尿路感染中分离的弗氏柠檬酸杆菌的抗微生物药物耐药性、表型特征和生物膜生成
IF 0.2 Q4 Medicine Pub Date : 2022-12-01 DOI: 10.1177/0976500X221147747
P. Shinu
Objective To evaluate the link between phenotypic traits, antimicrobial resistance, and biofilm-producing capacity of urinary isolates of Citrobacter freundii (C. freundii). Methods Both pan-antibiotic-susceptible and -resistant C. freundii isolates (n = 120) obtained from laboratory-confirmed urinary tract infections were analyzed for their link between antimicrobial resistance, phenotypic characteristics, and biofilm production. Results Of the total C. freundii isolates (n = 120), 30% (37/120) of them formed large colonies. Among the total large colonies produced (n = 37), they were present in 21.62%, 10.81%, 13.5%, 16.2%, 21.62%, and 16.21% in the control group, CIP-group, FOS-group, COT-group, Gent-group, and ESBL groups, respectively. Compared to the pan-susceptible isolates, the occurrence of large-sized-colony-forming strains was relatively reduced in most of the drug-resistant groups. The overall distribution of mucoid colonies produced (n = 54) includes 9.25%, 18.51%, 16.66%, 18.51%, 20.3%, and 16.66% in the control group, CIP-group, FOS-group, COT-group, Gent-group, and ESBL groups, respectively. Of the total isolates that produced biofilm (n = 51), 11.76% of isolates showed biofilm formation in the control group. Alternatively, the rate was found to be 15.68%, 11.76%, 25.49%, 19.6%, and 15.68% in the CIP-group, FOS-group, SXT-group, Gen-group, and ESBL-groups, respectively. Conclusion This study correlates the association between phenotypic characteristics, antimicrobial resistance, and biofilm production, the three main characteristics of C. freundii.
目的评价弗氏柠檬酸杆菌(C.freundii)尿液分离株的表型特征、耐药性和生物膜产生能力之间的关系。方法分析从实验室确诊的尿路感染中获得的泛抗生素敏感和耐药性弗氏梭菌分离株(n=120)的耐药性、表型特征和生物膜产生之间的联系。结果在120株弗氏梭菌分离株中,有30%(37/120)形成大菌落。在产生的总大菌落(n=37)中,对照组、CIP组、FOS组、COT组、Gent组和ESBL组中,它们分别占21.62%、10.81%、13.5%、16.2%、21.62%和16.21%。与泛感分离株相比,在大多数耐药组中,大规模集落形成菌株的发生相对减少。产生的粘液菌落的总体分布(n=54)在对照组、CIP组、FOS组、COT组、Gent组和ESBL组中分别为9.25%、18.51%、16.66%、18.51%和20.3%。在产生生物膜的总分离株中(n=51),对照组11.76%的分离株显示生物膜形成。另外,CIP组、FOS组、SXT组、Gen组和ESBL组的发病率分别为15.68%、11.76%、25.49%、19.6%和15.68%。结论本研究将弗氏梭菌的表型特征、耐药性和生物膜产生这三个主要特征联系起来。
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引用次数: 1
Neuroprotective Effects of P-Coumaric Acid on Haloperidol-Induced Catalepsy Through Ameliorating Oxidative Stress and Brain Dopamine Level 对香豆酸通过改善氧化应激和脑多巴胺水平对氟哌啶醇诱导的猝睡的神经保护作用
IF 0.2 Q4 Medicine Pub Date : 2022-12-01 DOI: 10.1177/0976500X221150837
Afsar S. Pathan, P. Jain, V. Kumawat, Ujwal N. Katolkar, S. Surana
Objective To evaluate the effect of p-coumaric acid (p-CA) on haloperidol-induced catalepsy in Swiss albino male mice. Methods To induce catalepsy, haloperidol (1 mg/kg i.p.) was administered for 21 consecutive days. p-CA (50, 75, and 100 mg/kg, PO) was administered 30 min before haloperidol injection for 21 consecutive days. For catalepsy, locomotor activity and motor coordination scores were recorded on the 17, 14, and 21 days of drug treatment, while the gait analysis score was recorded on day 21. After behavioral testing, animals were sacrificed, and various biochemical and histopathology tests of the brain were conducted. Dopamine, malondialdehyde, reduced glutathione (GSH), superoxide dismutase (SOD), and catalase activity were examined in the brain. Results Chronic administration of haloperidol significantly increased catalepsy in mice. It also produced hypolocomotion, motor coordination, and gait disturbance in mice. p-CA significantly inhibited haloperidol-induced catalepsy. Haloperidol significantly increased malondialdehyde levels in the brain. While dopamine levels in the brain dropped along with GSH, SOD, and catalase activity levels, which also had an impact on the histology of the brain. p-CA significantly reduced haloperidol-induced increases in brain oxidative stress, dopamine levels in the brain, and brain histology in mice. Discussion p-CA significantly reduced haloperidol-induced catalepsy, possibly through reducing oxidative stress and increasing brain dopamine levels. It can be a good candidate drug for extrapyramidal symptoms in Parkinson’s disease and adjuvant therapy with antipsychotic drugs.
目的探讨对香豆酸(p-CA)对氟哌啶醇致瑞士白化雄性小鼠猝厥的作用。方法给药氟哌啶醇(1 mg/kg ig)连续21 d致麻痹。p-CA(50、75和100 mg/kg, PO)在氟哌啶醇注射前30分钟给予,连续21天。对于猝死,在药物治疗的第17、14和21天记录运动活动和运动协调评分,在第21天记录步态分析评分。行为试验结束后,处死动物,进行脑生化、组织病理学等各项检测。检测脑内多巴胺、丙二醛、还原型谷胱甘肽(GSH)、超氧化物歧化酶(SOD)和过氧化氢酶活性。结果长期给药氟哌啶醇可显著增加小鼠的猝倒性。它还在小鼠中产生运动减退、运动协调和步态障碍。p-CA显著抑制氟哌啶醇诱导的猝倒。氟哌啶醇显著增加了大脑中的丙二醛水平。而大脑中的多巴胺水平随着GSH、SOD和过氧化氢酶活性水平的下降而下降,这也对大脑的组织学产生了影响。p-CA显著降低了氟哌啶醇引起的小鼠脑氧化应激、大脑多巴胺水平和脑组织组织学的增加。p-CA可能通过减少氧化应激和增加脑多巴胺水平显著降低氟哌啶醇诱导的猝倒。它可以作为帕金森病锥体外系症状的良好候选药物和抗精神病药物的辅助治疗。
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引用次数: 1
Transgenic Rodent Models in Toxicological and Environmental Research: Future Perspectives 毒理学和环境研究中的转基因啮齿动物模型:未来展望
IF 0.2 Q4 Medicine Pub Date : 2022-09-01 DOI: 10.1177/0976500X221135691
P. Christapher, Thanapakiam Ganeson, SUMITHA, S. Parasuraman
The coexistence of humans and animals has existed for centuries. Over the past decade, animal research has played a critical role in drug development and discovery. More and more diverse animals, including transgenic animals, are used in basic research than in applied research. Transgenic animals are generated using molecular genetic techniques to add functional genes, alter gene products, delete genes, insert reporter genes into regulatory sequences, replace or repair genes, and make changes in gene expression. These genetically engineered animals are unique tools for studying a wide range of biomedical issues, allowing the exhibition of specific genetic alterations in various biological systems. Over the past two decades, transgenic animal models have played a critical role in improving our understanding of gene regulation and function in biological systems and human disease. This review article aims to highlight the role of transgenic animals in pharmacological, toxicological, and environmental research. The review accounts for various types of transgenic animals and their appropriateness in multiple types of studies.
人类和动物的共存已经存在了几个世纪。在过去的十年里,动物研究在药物开发和发现中发挥了关键作用。越来越多的多样性动物,包括转基因动物,被用于基础研究,而不是应用研究。转基因动物是利用分子遗传学技术产生的,可以添加功能基因、改变基因产物、删除基因、将报告基因插入调控序列、替换或修复基因以及改变基因表达。这些基因工程动物是研究广泛生物医学问题的独特工具,可以展示各种生物系统中的特定基因改变。在过去的二十年里,转基因动物模型在提高我们对生物系统和人类疾病中基因调控和功能的理解方面发挥了关键作用。这篇综述文章旨在强调转基因动物在药理学、毒理学和环境研究中的作用。该综述说明了各种类型的转基因动物及其在多种类型研究中的适用性。
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引用次数: 0
Progress Update on the Epidemiology of COVID-19 Variants and the Assessment Status of Developed Vaccines 新冠肺炎变异株流行病学及疫苗研制评价进展
IF 0.2 Q4 Medicine Pub Date : 2022-09-01 DOI: 10.1177/0976500X221138393
K. Venugopala
Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has spread rapidly and diffused to more than 180 countries at varying severities. This pandemic has accounted for increased mortality and morbidity in developed as well as developing nations. The WHO has announced that there is a persistent need for the evaluation of the COVID-19 vaccine effectiveness (VE) against major outcomes, which include severe diseases, symptomatic COVID-19, and mortalities related to COVID-19. Therefore, mass vaccination programs using vaccines of high effectiveness are among the strategies that have been used by governments worldwide to impede the COVID-19 pandemic transmission. In this regard, massive efforts were made by governments, scientists, biomedical researchers, and healthcare professionals leading to the successful development of various vaccines to bring this pandemic under control. This editorial aims to shed light on the epidemiological status of COVID-19 variants, namely, Delta, Omicron, and Deltacron variants as well as discuss the effectiveness of the currently available COVID-19 vaccines.
严重急性呼吸系统综合征冠状病毒2型已迅速传播,并以不同的严重程度扩散到180多个国家。这一流行病导致发达国家和发展中国家的死亡率和发病率增加。世界卫生组织宣布,持续需要评估新冠肺炎疫苗对主要结果的有效性,包括严重疾病、有症状的新冠肺炎和与新冠肺炎相关的死亡。因此,使用高效疫苗的大规模疫苗接种计划是世界各国政府用于阻止新冠肺炎大流行传播的策略之一。在这方面,政府、科学家、生物医学研究人员和医疗保健专业人员做出了巨大努力,成功开发了各种疫苗,以控制这一流行病。这篇社论旨在阐明新冠肺炎变异株,即德尔塔变异株、奥密克戎变异株和德尔塔克隆变异株的流行病学状况,并讨论目前可用的新冠肺炎疫苗的有效性。
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引用次数: 0
Tapinarof: A Felicitous Discovery in Psoriasis Treatment Tapinaraf:银屑病治疗中的一个惊人发现
IF 0.2 Q4 Medicine Pub Date : 2022-09-01 DOI: 10.1177/0976500X221130851
Indumathi Prabath, S. Subramanian, J. Rani
Tapinarof is a novel topical formulation approved recently, in May 2022, by the United States Food and Drug Administration to treat plaque psoriasis. Existing topical therapies for psoriasis are limited by systemic and local adverse effects, medication cost and repeated administration, thus significantly hampering the compliance of patients to therapy. These limitations can be resolved by tapinarof owing to its better efficacy and favourable safety profile in psoriasis management. Tapinarof was developed with a unique mechanism targeting the aryl hydrocarbon receptor (AhR) involved in inflammation and modulation of skin barrier integrity in inflammatory dermatological disorders such as psoriasis and atopic dermatitis. The efficacy and safety outcomes of tapinarof in psoriasis were justified through the two pivotal clinical trials, namely, PSOARING 1 and PSOARING 2. The common adverse effects observed with tapinarof are folliculitis, contact dermatitis and headache. The literature search was conducted for efficacy and safety of tapinarof in the electronic databases of PubMed and Cochrane using a combination of keywords such as tapinarof, psoriasis and AhR. This review will delineate the molecular mechanisms underlying the action of tapinarof and also summarise the trial data supporting the claim that tapinarof is replacing the existing standard of care in psoriasis management.
Tapinarof是一种新型外用制剂,最近于2022年5月被美国食品和药物管理局批准用于治疗斑块型银屑病。现有的银屑病局部治疗受到系统和局部不良反应、药物成本和重复给药的限制,从而严重阻碍了患者对治疗的依从性。这些局限性可以通过Tapinaraf解决,因为它在银屑病治疗中具有更好的疗效和良好的安全性。Tapinarof具有一种独特的机制,靶向参与炎症和调节炎症性皮肤病(如银屑病和特应性皮炎)中皮肤屏障完整性的芳烃受体(AhR)。Tapinaraf治疗银屑病的疗效和安全性结果是通过两项关键的临床试验证明的,即PSOARING1和PSOARING2。Tapinaraf常见的不良反应有毛囊炎、接触性皮炎和头痛。在PubMed和Cochrane的电子数据库中,使用Tapinaraf、银屑病和AhR等关键词的组合,对Tapinarav的疗效和安全性进行了文献检索。这篇综述将描述Tapinaraf作用的分子机制,并总结支持Tapinarav正在取代银屑病治疗中现有护理标准的试验数据。
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引用次数: 1
A Review on the Pharmacological Importance of PDE5 and Its Inhibition to Manage Biomedical Conditions PDE5的药理意义及其对生物医学疾病的抑制作用综述
IF 0.2 Q4 Medicine Pub Date : 2022-09-01 DOI: 10.1177/0976500X221129008
Queen Saikia, A. Hazarika, Ritu Mishra
Phosphodiesterase type 5 (PDE5) is a cyclic GMP (cGMP) specific protein. It hydrolyzes the phosphodiesterase linkage and catalyzes the conversion of cGMP to 5’ GMP, which controls different physiological activities of the body. PDE5 is associated with biomedical conditions like neurological disorders, pulmonary arterial hypertension, cardiomyopathy, cancer, erectile dysfunction, and lower urinary tract syndrome. Inhibition of PDE5 has now been proven pharmaceutically effective in a variety of therapeutic conditions. Avanafil, tadalafil, sildenafil, and vardenafil are the most commonly used PDE5 inhibitors (PDE5i) today which are often used for the management of erectile dysfunction, lower urinary tract syndromes, malignancy, and pulmonary arterial hypertension. However, these synthetic PDE5i come with a slew of negative effects. Some of the most common side effects include mild headaches, flushing, dyspepsia, altered color vision, back discomfort, priapism, melanoma, hypotension and dizziness, non-arteritic anterior ischemic optic neuropathy (NAION), and hearing loss. In light of the potential negative effects of this class of medications, there is a lot of room for new, selective PDE5 inhibitors to be discovered. We have found 25 plant botanical compounds effectively inhibiting PDE5 which might be useful in treating a variety of disorders with minimal or no adverse effects.
磷酸二酯酶5 (PDE5)是一种环GMP (cGMP)特异性蛋白。它水解磷酸二酯酶链,催化cGMP转化为5′GMP,控制机体的各种生理活动。PDE5与神经系统疾病、肺动脉高压、心肌病、癌症、勃起功能障碍和下尿路综合征等生物医学疾病有关。抑制PDE5现已被证明在多种治疗条件下具有药学上的有效性。阿那非、他达拉非、西地那非和伐地那非是目前最常用的PDE5抑制剂(PDE5i),常用于治疗勃起功能障碍、下尿路综合征、恶性肿瘤和肺动脉高压。然而,这些合成的PDE5i带来了一系列的负面影响。一些最常见的副作用包括轻度头痛、潮红、消化不良、色觉改变、背部不适、阴茎勃起、黑色素瘤、低血压和头晕、非动脉性前缺血性视神经病变(NAION)和听力损失。鉴于这类药物的潜在负面影响,有很大的空间来发现新的,选择性PDE5抑制剂。我们已经发现了25种有效抑制PDE5的植物化合物,这些化合物可能对治疗各种疾病有用,而且副作用很小或没有副作用。
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引用次数: 2
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Journal of Pharmacology & Pharmacotherapeutics
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