This study evaluates the relationship between weight loss, circulating inflammatory markers and lipids from 24 patients before and after 6 months of pharmacotherapy as a standard of care for anti-obesity treatment

开始日期2023-06-01

申办/合作机构

LSU Health Sciences Center

[+2]

ACTRN12619000391178 / Completed临床3期

A bioequivalence study of two pharmaceutical preparations of Amfepramone 75mg in healthy volunteers, to assessment the interchangeability of the pharmaceutical preparations

开始日期2017-02-03

申办/合作机构-

100 项与盐酸安非拉酮相关的临床结果

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100 项与盐酸安非拉酮相关的转化医学

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100 项与盐酸安非拉酮相关的专利（医药）

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341

项与盐酸安非拉酮相关的文献（医药）

2024-09-27·MEDICINE

Combination of diethylpropion with dietary intervention results in body weight and fat loss with preserved muscle mass in obese patients

Article

作者: Amalia, Fiki ; Nugraha, Gaga Irawan ; Ariyanto, Eko Fuji ; Ghozali, Mohammad ; Imadudda’wah, Fata ; Fatimah, Siti Nur

Combining pharmacotherapy with lifestyle intervention is recommended for obese class II patients who fail lifestyle therapy and for obese class I patients. Diethylpropion, an obesity medication, has been approved for use in Indonesia, which is an Asia-Pacific country. This retrospective study aimed to assess the short-term effects of diethylpropion on weight and fat loss in obese patients in Indonesia. Secondary data were collected from 142 patients’ medical records with a body mass index ≥ 25 kg/m2 who underwent short-term diethylpropion treatment for 84 days between January 2022 and November 2023 at the Kimia Farma Nutrition Clinic in Bandung, Indonesia. Blood pressure, body weight, height, waist circumference, and body composition were assessed at each follow-up visit to determine the fat and muscle mass. Patients were prescribed diethylpropion 25 mg 3 times daily every 2 weeks together with dietary intervention. Kruskal–Wallis test was used to analyze the changes in body weight, skeletal muscle, fat mass, and waist circumference after the diethylpropion therapy. Mann–Whitney test was used for the relation between age, sex, and body mass index with weight loss on the last day of follow-up. Simple linear regression analysis was also performed to identify the correlation between weight loss and therapy duration. This study showed body weight reduction of up to 9.5 ± 3 kg (10 ± 0.0%) (P = .008) on 84 days of treatment. Significant fat loss 11.5 ± 4.6 kg (20.5 ± 0.0%) (P = .005) was also reported in our study without significant loss of muscle mass ‐2.4 ± 4.6 kg (3.6 ± 1.3%) (P = .58). Waist circumference was insignificantly reduced by 5.6 ± 0.0 cm (4.9 ± 2.8%) (P = .21) after 84 days of diethylpropion therapy. This study revealed no significant changes in patient systolic and diastolic pressures despite showing mild increases after 70 days. The combination of diethylpropion and an appropriate diet resulted in weight loss accompanied by significant fat loss and preserved muscle mass without an increase in blood pressure during the 12-week treatment period.

2024-03-01·World journal of microbiology & biotechnology

Evaluation of stability of (1R,2 S)-(−)-2-methylamino-1-phenyl-1-propanol hydrochloride in plasma and urine samples-inoculated with Escherichia coli using high-performance liquid chromatography (HPLC)

Article

作者: Almaary, Khalid S ; Alobaidi, Ahmed S ; Khaled, Jamal M ; Kadaikunnan, Shine ; Alharbi, Naiyf S ; Al-Huwaymil, Rayan M

Abstract:

The preservation of drug stability in biological evidence during the processes of collection and storage poses a substantial obstacle to the progress of forensic investigations. In conjunction with other constituents, the microorganisms present in the samples play a vital role in this investigation. The present investigation employed the high-performance liquid chromatography (HPLC) technique to assess the stability of (1R,2 S)-(–)-2-methylamino-1-phenyl-1-propanol hydrochloride in plasma and urine samples that were inoculated with Escherichia coli. These samples were subjected to storage conditions of 37 °C for 48 h and − 20 °C for a duration of 6 months. Minimal inhibitory concentration (MIC) and Minimal bactericidal concentration (MBC) of MPPH against E. coli were determined using microdilution method. The stability of MPPH in plasma and urine samples inoculated with E. coli was investigated using HPLC method. The results showed the MIC and MBC of MPPH were 87.5 ± 25 ppm and 175 ± 50 ppm, respectively. While MPPH remained stable in plasma for 48 h at 37 °C, it showed a notable decrease of about 11% in stability when stored in urine for the same period and temperature. From the beginning of the first month, a decrease in the stability of the compound appeared in all samples that were stored at − 20 °C, and the decrease reached 7% for plasma samples and about 11% for urine samples. The decrease in the stability reached its peak in the sixth month, reaching more than 30% and 70% of plasma and urine samples preserved at − 20 °C. This work concluded that E. coli can negatively affect the stability of MPPH in plasma and urine samples. This may lead to incorrect conclusions regarding the analysis of biological samples in criminal cases.

2023-03-01·Heliyon

Comparative antihyperglycemic, analgesic and anti-inflammatory potential of ethanolic aerial root extracts of Ceriops decandra and Ceriops tagal: Supported by molecular docking and ADMET analysis

Article

作者: Devnath, Hiron Saraj ; Mazumder, Kishor ; Golder, Mimi ; Sadhu, Samir Kumar ; Biswas, Biswajit

Ceriops decandra (Griff.) (CD) and Ceriops tagal (Perr.) (CT) are two mangrove plants of the Sundarbans distributed along the coastal areas of South Asia and South Pacific Africa. Traditionally, these plants are used to treat diabetes, pain, angina, hemorrhage, and ulcer. In this study, we investigated the antioxidative, antihyperglycemic, analgesic, and anti-inflammatory potential of the aerial roots of CD and CT. At first, the antioxidative potential of CD and CT ethanolic extracts were investigated qualitatively and quantitatively by 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical and hydrogen peroxide scavenging assays and by determining total antioxidant capacity. The total phenolic, flavonoid, tannin, and terpenoid contents of CD and CT were also estimated. The extracts' antihyperglycemic, analgesic, and anti-inflammatory potential were evaluated by oral glucose tolerance test, acetic acid-induced writhing test, and formaldehyde-induced paw-edema test, respectively. In vitro α-glucosidase and α-amylase enzyme inhibitory activities were also assessed. The CD and CT extracts were also analyzed using GCMS for the presence of phytochemicals. Then, molecular docking was carried out with α-glucosidase, α-amylase, cyclooxygenase-II (COX-II), 3-lipoxygenase (3-LOX) enzymes using the compounds found in GCMS analysis as well as the previously reported compounds from CD and CT. Finally, the pharmacokinetic and toxicological profiles of eight selected compounds were assessed with SwissADME and admetSAR server. In the antioxidative, antihyperglycemic, analgesic, and anti-inflammatory activity tests, CT extract showed a greater potential than CD extract. In addition, CT extract demonstrated higher α-glucosidase enzyme inhibitory activity in comparison to CD extract although CD extract exhibited better α-amylase enzyme inhibitory activity. Molecular docking studies revealed the presence of potentially bioactive compounds in both CD and CT. 2-(2-methylphenyl)-1-phenyl-(z)-1-propene of CD demonstrated good binding affinities for α-glucosidase, COX-II, and 3-LOX. In addition, 5S*,8S*,9S*,10R*,13S*)-18-hydroxy-16-nor-3-oxodolabr-4(18)-en-15-oic acid had high binding interactions for both α-glucosidase and α-amylase while 2',5,5'-tetramethyl-1,1'-biphenyl, 2-methyl-4-(3'-phenylpropyl)piperidine and decandrin C had high binding interactions for both COX-II and 3-LOX. Finally, 5S*,8S*,9S*,10R*,13S*)-18-hydroxy-16-nor-3-oxodolabr-4(18)-en-15-oic acid, decandrin C, 2-(2-methylphenyl)-1-phenyl-(z)-1-propene and 2-methyl-4-(3'-phenylpropyl)piperidine demonstrated better pharmacokinetic and toxicological properties in the ADMET analysis compared to the others. Hence it can be concluded that the present study supports the traditional usage of CD and CT for diabetes and pain and reveals the presence of bioactive phytochemicals in both.

项与盐酸安非拉酮相关的新闻（医药）

2024-11-28

·国际糖尿病idiabetes

体重管理新纪元：减重治疗药物研发多波折，GLP-1RA周制剂提供新变革！

点击“蓝字”关注我们编者按：肥胖医学协会将肥胖定义为一种严重的、慢性的、进行性的、复发性的、可治疗的多因素神经行为疾病，其中体内脂肪增加促进脂肪组织功能障碍和异常脂肪组织的压迫，导致不良的代谢、生物学和社会心理健康等后果。肥胖患者面临着发病率和死亡率增加的问题，同时在执行日常任务（如爬楼梯）时也受到限制。肥胖与220多种并发症有关，例如2型糖尿病（T2DM）、代谢功能障碍相关脂肪性肝病（MASLD）和慢性肾脏病（CKD），这些并发症也限制了患者的能力，亟需药物治疗[1]。过去多年，减重治疗药物研发历经诸多波折，胰高糖素样肽-1受体激动剂（GLP-1RA）的减重适应证获批为肥胖治疗提供了新变革！本刊邀请解放军总医院第一医学中心臧丽教授对减重药物的研发历史进行回顾，一起来看看！臧丽教授解放军总医院第一医学中心内分泌科副主任医师副教授硕士生导师中华医学会糖尿病学分会青年委员会副主任委员中国医师协会内分泌代谢科分会青年委员会副主任委员北京医学会糖尿病学分会委员兼工作秘书解放军医学会内分泌学分会青年委员会秘书长国际糖尿病杂志青年编委《Diabetes Care 中文版》青年编委《Endocrine Reviews 中文版》青年编委肥胖症的药物治疗有着悠久而曲折的历史，早在19世纪末，西方就已出现用药物治疗肥胖的方法，如甲状腺激素类药物等。在随后100多年，线粒体解偶联剂、肾上腺素能药物等逐渐进入市场。但可惜好景不长，许多有前景的药物因各种问题而被陆续撤回（图1）[2-4]。图1. 目前FDA批准的减重药物预览究其根本，安全性是导致减重药物撤市的重要原因。其中，大多数药物（如西布曲明、芬氟拉明、右芬氟拉明、彩虹药丸）与心血管不良影响相关，而部分药物（如利莫那班）可能导致自杀风险增加，部分药物（如甲基苯丙胺）会导致药物依赖和滥用的可能性增加。此外，由于成瘾潜力或出现快速耐受，某些药物仅建议短期使用（芬特明、安非拉酮、盐酸卡汀）[2-4]。上市减重药物选择有限，研发面临多重挑战由于技术和社会原因，寻求抗肥胖药物一直极具挑战性。目前，经美国食品药品监督管理局（FDA）批准用于抗肥胖的药物有脂肪酶抑制剂的奥利司他、去甲肾上腺素（NE）激动剂/γ-氨基丁酸（GABA）激动剂和谷氨酸拮抗剂的芬特明/托吡酯组合、阿片受体拮抗剂/多巴胺（DA）和NE再摄取抑制剂的纳曲酮/安非他酮组合、GLP-1RA的利拉鲁肽和司美格鲁肽以及GIP/GLP-1双靶点激动剂的替尔泊肽（图2）[2-4]，而我国批准的药物仅有奥利司他、贝那鲁肽0.2 mg、司美格鲁肽2.4 mg、利拉鲁肽3.0 mg这4种药物[2-4]。图2. FDA批准的治疗肥胖症的药物及其作用部位其中，奥利司他作为脂肪酶抑制剂可通过抑制胃肠道和胰腺脂肪酶，从而阻断甘油三酯的水解并减少肠内皮对脂肪酸的吸收。研究发现，其通常会导致与食物一起消耗的大约1/3的脂肪酸不被吸收[2]。XENDOS研究发现，奥利司他组体重减轻为5.8 kg，服用奥利司他后不良反应主要为便秘、腹痛、腹泻、头晕、月经紊乱和皮疹等，长期应用可能导致脂溶性维生素如维生素D、维生素E、维生素K等缺乏[5]。 GLP-1RA占据主导地位，引领减重新变革实现体重正常化以及适当的耐受能力和安全性的长期药物治疗仍然是一个难以克服的挑战。然而，最近针对包括GLP-1RA在内的先进治疗候选药物的临床试验使大家相信，突破性的、基于药物的肥胖管理有可能实现。2014年，FDA批准利拉鲁肽3 mg用于治疗成人肥胖，成为首个用于体重管理的GLP-1RA[2-4]。今年，FDA批准司美格鲁肽2.4 mg用于初始体重指数（BMI）≥30 kg/m2（肥胖）或≥27 kg/m2至<30 kg/m2（超重）且存在至少1种体重相关合并症，如高血糖、高血压、血脂异常、阻塞性睡眠呼吸暂停或心血管疾病等患者，成为首个用于体重管理的GLP-1RA周制剂。究其原因，GLP-1RA一方面可延缓胃排空和胃肠蠕动，增加机体饱腹感，降低摄食；同时增加能量消耗，促进内脏白色脂肪向棕色脂肪转化，随着棕色脂肪产热增加，增加能量耗损；另一方面，GLP-1RA可直接刺激阿黑皮素原（POMC）/可卡因苯丙胺调节转录物（CART）阳性神经元，并通过GABA信号间接抑制神经肽Y（NPY）和刺鼠相关肽（AgRP）阳性神经元的神经投射，从而抑制食欲，减少摄食量[2-4]。 STEP系列研究证实了司美格鲁肽2.4 mg每周一次皮下注射与安慰剂相比的疗效和安全性。其结果显示，司美格鲁肽2.4 mg组治疗68周后，显著降低体重达15%~17%（图3）[6-11]。图3. 司美格鲁肽2.4 mg显著降低体重司美格鲁肽2.4 mg的安全性也经过了验证，不良事件发生率与安慰剂组相仿，导致停药的不良事件发生率低，通常为轻中度、一过性的胃肠道反应，如恶心、腹泻、呕吐和便秘等，并随治疗时间延长而逐渐减轻或消失[6-11]。纳入STEP 1、2、3和5研究的事后分析发现，68周时，与安慰剂相比，司美格鲁肽2.4 mg治疗不仅不会增加出现抑郁或自杀意念/行为症状的风险，而且可能与抑郁症状的小幅减少相关。结语药物研发过程漫长而艰辛，许多药物因各种原因退市，不能成为临床用药。尽管如此，临床肥胖患者需求和巨大市场仍是持续进行抗肥胖药物研发的强大动力。随着GLP-1RA减重适应证的批准上市，肥胖治疗出现了新变革。相信未来随着新兴生物医学工程技术的发展以及个性化多分子药物的开发，肥胖治疗会更安全、更持久、更有效，不仅能更好地减轻体重，还能改善心脏代谢健康，为肥胖症的精准医疗开辟新径。注：不同剂量的司美格鲁肽注射液用于不同的适应证，本材料所提及的司美格鲁肽（2.4 mg）注射液的适应证均为适用于长期体重管理治疗的GLP-1RA周制剂。其具体适应证为：适用于在控制饮食和增加体力活动的基础上对成人患者的长期体重管理，初始体重指数（BMI）符合以下条件：≥30 kg/m2（肥胖），或≥27 kg/m2至<30 kg/m2（超重）且存在至少1种体重相关合并症，例如高血糖、高血压、血脂异常、阻塞性睡眠呼吸暂停或心血管疾病等。参考文献（上下滑动可查看） 1.Craig HC, et al. Obes Pillars. 2024 Aug 8; 12: 100123. 2.Pilitsi E, et al. Metabolism. 2019; 92: 170-192. 3.Müller TD, et al. Nat Rev Drug Discov. 2022; 21(3): 201-223. 4.Onakpoya IJ, et al. BMC Med. 2016; 14(1): 191. 5.Ludvik B, et al.Diabetes Care. 2004; 27(2): 436-440. 6.Wilding JPH, et al. N Engl J Med. 2021; 384(11): 989-1002. 7.Davies M, et al. Lancet. 2021; 397(10278): 971-984. 8.Wadden TA, et al. JAMA. 2021; 325(14): 1403-1413. 9.Rubino D, et al. JAMA. 2021; 325(14): 1414-1425. 10.Garvey WT, et al. Nat Med. 2022; 28(10): 2083-2091. 11.Kadowaki T, et al. Lancet Diabetes Endocrinol. 2022; 10(3): 193-206. 声明：本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。最新《国际糖尿病》读者专属微信交流群建好了，快快加入吧！扫描左边《国际糖尿病》小助手二维码（微信号：guojitnb），回复“国际糖尿病读者”，ta会尽快拉您入群滴！（来源：《国际糖尿病》编辑部）版权声明版权属《国际糖尿病》所有。欢迎个人转发分享。其他任何媒体、网站未经授权，禁止转载。

2024-02-15

·梅斯医学

一年瘦100斤？普通人如何有效减肥...... | 值得收藏

近日，“贾玲在一年时间内减肥100斤”的话题引起了许多网友的热议。需要指出的是，减肥并不是一蹴而就的事情，科学减肥需要做到合理饮食，健康运动；此外，减肥一定要控制速度，千万不可过快，短期内极速减重并不适合大部分普通人。普通人如何做到科学减肥？本期，医学新视点结合《美国医学会杂志》（JAMA）最新发表的成人肥胖管理综述文章，总结了肥胖诊断和治疗最新临床证据和研究进展，以期为大家提供参考。截图来源：JAMA好好的，怎么突然就变胖了？肥胖本质上是长期能量不平衡，摄入量大于消耗量，再加上多种因素的影响（如遗传），难免不逐渐“变胖”。影响肥胖的因素较多，主要是遗传、环境、疾病、睡眠等。多数肥胖都与多基因突变有关，部分基因突变与体重指数（BMI）相关，而单一基因突变导致的肥胖则比较少见；工作场所、学校、家庭周边有众多餐饮店、社区活动场所有限等都可能造就“肥胖环境”；睡眠不足也可能导致肥胖。怎样算胖？目前定义肥胖最常用的指标是BMI，即体重（kg）/身高（m）的平方。根据WHO的定义：超重：BMI 25~29.99 kg/m21级肥胖：BMI 30~34.99 kg/m22级肥胖：BMI 35~39.99 kg/m23级肥胖：BMI ≥40 kg/m2换句话说，若您的体重指数（BMI）≥30 kg/m2，则意味着已经“肥胖”。需要说明的是，亚洲人群在BMI较低时就可能出现心脏代谢疾病，所以有专家和临床指南建议降低亚洲人群肥胖BMI的阈值。此外，仅使用BMI来定义一个人“胖不胖”，临床上对此也是有争议的，因为BMI并不能直接测量脂肪体积或是解释个体化差异，所以近年来学者们提出了在BMI基础上增加其他评估指标，以更好的判断个体是否肥胖，如腰围。根据现行指南建议，对于BMI在25~34.9 kg/m2的患者，应基于其腰围进行风险分层，其中男性为102 cm，女性为88 cm；埃德蒙顿肥胖分期系统根据独立于BMI的因素进行风险分层，风险程度评分越高，则全因死亡率风险增加；根据患者病史和查体结果，如激素异常（甲状腺功能减退、皮质醇增多症）、精神病（如暴食症）、医源性肥胖（如药物治疗）和遗传疾病（如阿黑皮素原缺乏症）等，筛查是否为继发性肥胖；评估体重相关的合并症情况，如非酒精性脂肪肝或阻塞性睡眠呼吸暂停综合征等，这对于后续患者的转诊和治疗非常重要。减肥前，先了解这两个问题以患者为中心的减肥策略患者应与临床医生共同商讨减肥策略。医生在与患者沟通病情时，应在获得患者同意后再开始讨论患者体重问题，且在交流过程中注意沟通措辞（如超重、BMI升高等）。5A’s模式有助于医患共同决策，即[Assess（评估）、建议（Advise）、达成共识（Agree）、帮助（Assist）、随访（Arrange）]，在医患沟通和随访的过程中，每个“A”都可能出现，而每次多个“A”或许都能增加患者的减肥动力（HR=1.31，95%CI=1.11~1.55）。设定合理的减肥目标研究显示，相比于不设定减肥目标的个体，设定个体减肥目标可增加12个月内至少减肥10%的患者比例。减肥目标的设定因人而异，需要综合考虑患者的喜好、身体成分、合并症等情况。减重5%：高血压患者舒张压和收缩压可分别降低3 mmHg和2 mmHg；减重5%~10%：糖尿病患者糖化血红蛋白（HbA1c）可降低0.6%~1.0%，高密度脂蛋白胆固醇升高2 mg/dl；减重10%~15%：可能需要同时改善其他情况，如处理脂肪肝变性、阻塞性呼吸睡眠暂停综合征等；减重15%以上：接受减重手术的患者，若减重超过15%，则与全因死亡率下降相关，生活质量显著改善。选择合理的减肥治疗方案减肥方案整体可分为5大类：行为干预、营养干预、体力活动、药物治疗和减肥手术。行为干预行为干预措施包括：团体、个体或基于现代技术的生活方式改变、教育、同伴支持、辅导、自我监测、认知重建和目标设定。中高强度的干预措施通常可减重5%~10%，约2.39~2.86 kg，频繁称体重也有助于减重和维持减重效果。需要注意的是，由于代谢适应性和激素变化导致的患者依从性降低，通常减肥6个月左右会到达平台期。营养干预建议减少每日热量摄入，来达到减重目的，通常每天应制造500~750 kcal的热量差。减少热量摄入和维持减重效果的具体策略包含：控制、减少或拒绝超加工食品（如含糖饮料）的摄入，增加水果和蔬菜的摄入量；根据个体偏好、代谢风险和长期坚持的可能性，来选择适合自己的饮食方案。额外的饮食计划也可以与减少热量策略相结合，如得舒（DASH）饮食。相比于日常饮食，每天用高蛋白奶昔或能量棒代替1~2顿日常饮食有助于减重（差异-1.44 kg，95%CI=-2.48 kg~-0.39 kg）。不过，虽然有部分证据表明，极低热量饮食不仅可减肥还能改善心血管疾病风险，但现行临床指南实践并不支持这些策略，若真要采用该策略，需要营养师的参与介入。体力活动体力活动通常不作为单独的减重方式，但体力活动有助于维持体重和心脏代谢健康。中等强度的有氧运动（定义为最大心率的50%~70%）与内脏脂肪减少和适度的体重减轻（平均减重2~3 kg）有关。抗阻训练（肌肉强化）有助于减肥过程中保持瘦/无脂肪质量。临床指南建议：所有患者每周应采取150~300分钟的中等强度或75~150分钟的剧烈体力活动，以及每周2~3次抗阻训练。鼓励不要久坐，可以每小时起来活动2分钟，也可以佩戴智能电子设备，提醒每天多活动，如果每天多走1800步，就可能减重0.5~1.5 kg。药物治疗肥胖治疗药物取得了重要进展。对于采取生活方式干预后不能有效减重的患者，指南建议：肥胖/超重以及有体重相关并发症的非妊娠患者，应考虑开始使用减重药物。一旦开始药物治疗，临床医生应考虑到减肥药的双重益处，如糖尿病患者使用胰高糖素样肽-1（GLP-1）受体激动剂，可在改善血糖水平的同时达到减重的目的。同时，临床医生也应告知患者即使使用减肥药，也需要与改变生活方式相结合才能达到和维持良好体重，减肥药有可能需要终身使用，因为停药后体重反弹是常见情况。不建议使用减肥补充剂，如某些绿茶提取物。1）GLP-1受体激动剂（司美格鲁肽或利拉鲁肽）2014年，美国FDA批准皮下注射的利拉鲁肽可用于治疗肥胖，但需要每日用药；2021年，皮下注射的司美格鲁肽被美国FDA批准用于治疗肥胖。口服减肥药也日渐得到患者和医生的广泛关注，发表于《柳叶刀》（The Lancet）的OASIS 1试验结果显示，每日一次50 mg司美格鲁肽口服治疗可使超重或肥胖成人（未伴有2型糖尿病）体重大幅度下降（治疗68周平均下降15.1%）。2）TirzepatideTirzepatide是一款新型降糖药，属于葡萄糖依赖性促胰岛素多肽（GIP）和胰GLP-1受体双重激动剂，每周一次皮下注射给药。发表于《新英格兰医学杂志》（NEJM）的研究显示，每周一次tirzepatide（15 mg）皮下注射给药，持续72周治疗后肥胖成人患者的体重减轻程度达到极其显著的20.9%（基于疗效评估减重达23.6kg），而体重减轻≥5%的患者占比达到了91%！此外，36.2%接受tirzepatide（15 mg）治疗的患者达到了预设体重减轻≥25%的探索性终点。3）Phentermine-Topiramate/Naltrexone-Bupropion/奥利司他/Gelesis1002012年，美国FDA批准联合Phentermine-Topiramate用于治疗肥胖，Phentermine-Topiramate的具体减肥机制尚不明确，普遍认为可降低食欲但不能减少热量摄入。Naltrexone-Bupropion在2014年被美国FDA批准用于治疗肥胖。Phentermine-Topiramate和Naltrexone-Bupropion均未在中国未获批。奥利司他在1999年被美国FDA批准用于治疗肥胖，可平均减重2.8%~4.8%，已在中国获批。2019年，Gelesis100被美国FDA批准用于治疗肥胖，相关临床试验结果显示，Gelesis100治疗6个月后，59%接受治疗的患者体重至少减轻5%，27%接受治疗的的患者体重减轻10%以上。4）部分短期用药和可能增重的药物此外，美国FDA还批准了部分短期使用的减重药，分别是phentermine、diethylpropion、benzphetamine和phendimetrazine，可在短期内使用（12周）。除了减重药物外，部分药物也可能与体重增加有关，如降糖药（格列本脲、胰岛素等）、抗抑郁药（阿米替林、米氮平等）、抗精神病药（奥氮平、富马酸喹硫平等）、抗癫痫药（加巴喷丁、卡马西平等）、β受体阻滞剂、甾体类避孕药、皮质类固醇和抗逆转录病毒等。使用这些药物时临床医生应告知患者体重增加的风险，建议患者监测体重变化情况。手术治疗目前，美国FDA批准了2种内窥镜减重手术：内镜下胃内气囊置入术和内镜袖状胃成形术。胃内气囊会占据胃部空间，延迟胃排空，增加饱腹感。研究显示，对于BMI在30~40 kg/m2的患者，通过生活干预和胃内气囊置入术后，体重减轻了10.2%。袖状胃成形术是通过减少胃的体积来达到减重目的。研究显示，相比于单纯改变生活方式，改变生活方式联合袖状胃成形术的患者治疗52周后，体重减轻了13.6%。最近指南建议：对于BMI≥35 kg/m2和30~34.9 kg/m2且伴有体重相关合并症的患者，应考虑采取代谢减重手术。目前主流的代谢减重手术为胃旁路术和袖状胃切除术。减肥是长期“事业”，关注随访很重要减重后的随访很重要，理想情况下应每4~6周随访一次，以及时发现和解决可能存在的药物不良反应和并发症。手术的随访需要与外科医生沟通确认。减重成功后，如何维持健康的体重，体重不反弹，不复发并不是一件容易的事情，必要时需要持续的临床干预。根据纵向观察性研究，减重成功后仍能维持健康体重的人群通常采用以下策略：1）定期体力活动（通常每周＞200分钟）；2）定期自我称体重；3）减少热量的饮食模式。考虑到相比于单纯生活方式干预，药物治疗在维持减肥效果方面更佳，部分临床指南支持长期使用减肥药。因此，与其他慢性疾病相似，减重也可能需要终身监测。参考资料[1] Elmaleh-Sachs A, Schwartz JL, Bramante CT, et al. Obesity Management in Adults: A Review. JAMA. 2023 Nov 28;330(20):2000-2015. doi: 10.1001/jama.2023.19897. PMID: 38015216.来源 | 医学新视点编辑 | 阿拉斯加宝版权说明：梅斯医学（MedSci）是国内领先的医学科研与学术服务平台，致力于医疗质量的改进，为临床实践提供智慧、精准的决策支持，让医生与患者受益。欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。点击下方「阅读原文」立刻下载梅斯医学APP！

临床研究

2022-11-11

·ema

EMA confirms recommendation to withdraw marketing authorisations for amfepramone medicines

On 27 October 2022, EMA’s safety committee ( PRAC ) confirmed its recommendation to withdraw the marketing authorisations for amfepramone obesity medicines. This follows a re-examination of its previous recommendation of June 2022, which was requested by the companies that market these medicines. The recommendation follows a review which found that measures to restrict the use of these medicines for safety reasons have not been sufficiently effective. It found that the medicines were being used for longer than the recommended maximum period of 3 months, thereby potentially increasing the risk of serious side effects such as pulmonary arterial hypertension (high blood pressure in the lungs) and dependency. The medicines were also being used in patients with a history of heart disease or psychiatric disorders, increasing their risk of heart and psychiatric problems. In addition, there was evidence of use during pregnancy, which could pose risks to the unborn baby. The review considered all available information relating to these concerns, including data from two studies on the use of amfepramone medicines in Germany and in Denmark. In addition, the PRAC received advice from a group of experts, comprising endocrinologists, cardiologists and a patient representative. The PRAC considered introducing further measures to minimise the risk of side effects but could not identify any that would be sufficiently effective. The PRAC therefore concluded that the benefits of amfepramone medicines do not outweigh their risks and recommended that the medicines be removed from the market in the EU. The CMDh agreed with the PRAC recommendation and adopted its position by majority on 10 November 2022. Information for patients EMA is recommending that amfepramone obesity medicines should no longer be available because they are not always used as recommended. Inappropriate use can cause serious side effects, such as increased blood pressure in the arteries of the lungs, heart disease, dependency, psychiatric problems and harm to the unborn baby. In addition, the benefits of using these medicines in the treatment of obesity are considered limited. Other obesity treatment options are available. Contact your doctor to discuss which treatment would be suitable for you. If you have other questions or concerns about amfepramone medicines, speak to your doctor or pharmacist. Information for healthcare professionals EMA is recommending the withdrawal of the EU marketing authorisations for amfepramone medicines for the treatment of obesity. A review of available data has found that amfepramone medicines continue to be used outside the current risk minimisation measures included in the product information . Inappropriate use may increase the risk of serious adverse effects, including cardiovascular disease, pulmonary arterial hypertension, dependency and psychiatric disorders, as well as harmful effects if used during pregnancy. A review of available data also indicates that the efficacy of amfepramone in the treatment of obesity is limited. Healthcare professionals should advise patients about other treatment options. A direct healthcare professional communication (DHPC) will be sent in due course to healthcare professionals prescribing or dispensing the medicine and published on a dedicated page on the EMA website. More about the medicine Amfepramone is a sympathomimetic, which means that it acts in the brain and causes effects that are similar to those of adrenaline. Such medicines reduce a feeling of hunger. Amfepramone medicines are currently authorised in Denmark, Germany and Romania as treatment for patients with obesity (body mass index of at least 30kg/m 2 ) in whom other weight-reduction methods have not worked on their own. Amfepramone medicines were authorised to be used for 4 to 6 weeks and no longer than 3 months. Within the EU, amfepramone medicines are available under the following trade names: Amfepramon‑Hormosan 25 mg Weichkapseln, Amfepramon‑Hormosan 60 mg Retardkapseln, Regenon, Tenuate Retard 75 mg retardtablette and Regenon 25 mg capsule moi. More about the procedure The review of amfepramone medicines has been initiated at the request of the Romanian medicines agency (NAMMDR), under Article 31 of Directive 2001/83/EC . The review has been carried out by the Pharmacovigilance Risk Assessment Committee ( PRAC ), the Committee responsible for the evaluation of safety issues for human medicines, which has made a set of recommendations. Following a re-examination requested by the marketing authorisation holders , the PRAC subsequently confirmed its conclusions for amfepramone-containing medicines. Because these medicines are all authorised at national level, the PRAC recommendations were sent to the CMDh , which has adopted a position. The CMDh is a body representing EU Member States as well as Iceland, Liechtenstein and Norway. It is responsible for ensuring harmonised safety standards for medicines authorised via national procedures across the EU. As the CMDh position was adopted by majority vote, it will now be sent to the European Commission, which will issue a final legally binding decision applicable in all EU Member States. This review follows previous reviews on the benefits and risks of appetite-suppressing medicines (including amfepramone) in 1996 and 1999.

上市批准

100 项与盐酸安非拉酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	盐酸安非拉酮	A08AA03	DB00937

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
肥胖	美国	Nostrum Laboratories, Inc.	1960-11-17

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


SFN2013	N/A	-	-	Diethylpropion 20 mg/kg	糧膚餘衊鏇齋淵鬱齋鹹(簾襯淵製構窪構蓋願夢) = stronger at high doses 衊鑰構選構餘夢簾蓋憲 (觸齋襯繭獵鹹鹹夢積衊 ) 更多	-	2013-11-10