常用免疫抑制剂人血中定量监测方法研究进展

免疫抑制剂在临床上主要用于治疗自身免疫性疾病和预防脏器移植排斥。免疫抑制剂的使用需要进行治疗药物监测,其检测结果通常作为临床医生调整用药剂量的重要依据之一。本文就目前临床常用的免疫抑制剂他克莫司、环孢素、霉酚酸酯、糖皮质激素及新型免疫抑制剂西罗莫司和依维莫司在人血中浓度的检测方法作一综述,以供参考。     

免疫抑制剂的应用分析与临床评价

目的：免疫抑制剂在器官移植和自身免疫系统疾病方面疗效显著。目前市场上免疫抑制剂种类繁多,作用机制多样。本文阐述免疫抑制剂的应用分析与临床评价。方法：采用国内、外文献综述方法。结果与结论：由3年数量份额上分析,销售数量和销售金额最多的排序前3位品种为霉酚酸酯、环孢素、他克莫司。而他克莫司有望成为器官移植的首选药物。     

器官移植术后他克莫司与三唑类抗真菌药的相互作用及影响因素研究进展

他克莫司作为一线免疫抑制剂,广泛用于器官移植术后自身排斥反应的防治。因他克莫司有治疗窗狭窄、个体差异大等特点,且为CYP450酶的底物,所以与其他药物联用时易发生药物-药物相互作用。三唑类抗真菌药是CYP450酶的抑制剂,与他克莫司联用会导致他克莫司血药浓度升高且毒性增加,临床使用期间应定期监测他克莫司血药浓度,以保障用药的安全性和有效性。现就他克莫司与三唑类抗真菌药之间的潜在相互作用及影响因素进行综述,为器官移植患者个体化使用他克莫司提供参考。     

《中国新药杂志》2005年第9单元继续教育试题

1 下列药物不属于免疫抑制剂的是_____。 A环抱菌素 B他克莫司 C西罗莫司 D胸腺肽 E硫唑嘌呤     

抗真菌抗生素和免疫抑制剂

微生物来源的具免疫抑制活性的抗真菌抗生素如环孢素、他克莫司(FK506)、雷帕霉素和霉酚酸已被开发为器官移植抗排斥药物和自身免疫性疾病的治疗药物.笔者介绍了这些药物的抗真菌和免疫抑制活性以及作用机制等,还介绍了一些从抗真菌抗生素中开发的和从微生物中分郭得到的具有抗真菌活性的新免疫抑制剂.抗真菌抗生素和免疫抑制剂之间似乎有存在着一定的关系,对发现新的抗真菌抗生素和免疫抑制剂具有一定的意义.     

中药、中药成分与常见食物对他克莫司血药浓度的影响

笔者通过查阅相关文献,对中药、中药成分或常见食物和他克莫司相互作用的情况进行归纳和分析,了解中药、中药成分或常见食物对免疫抑制剂他克莫司血药浓度的影响。发现他克莫司与临床使用的一些中药、中药成分或常见食物会发生不良药物相互作用,从而使药物血药浓度或免疫抑制作用发生改变。因此他克莫司与这些中药、中药成分或食物合用时,应密切关注他克莫司的血药浓度变化,以确保治疗的安全和有效。     

我国2004～2006年免疫抑制剂市场状况分析

目的:为临床合理、安全应用免疫抑制剂提供参考。方法:收集《全国医药经济信息网》中有关免疫抑制剂销售数量和销售金额的数据,并参考国内、外文献,进行对比分析。结果与结论:2004~2006年销售数量和销售金额最多排序列前3名的品种为霉酚酸酯、环孢霉素、他克莫司;而他克莫司有望成为器官移植的首选治疗药物。     

他克莫司免疫抑制方案改善儿童肝移植术后的研究进展

肝移植作为一种有效的治疗手段广泛地应用于儿童终末期肝病的治疗。为了预防可能发生的排斥反应,患儿需要长期服用免疫抑制剂。他克莫司是一种具有强效免疫抑制特性的大环内酯类药物,以他克莫司为主的免疫抑制方案可以减少排斥反应和激素抵抗型排斥反应的发生率。探讨了基因多态性、减少剂量或撤药、不同剂型之间转换以及免疫抑制剂短期、长期生存结果对儿童肝移植术后的影响,以期优化他克莫司的给药方案,为器官移植患儿的他克莫司药物监测和剂量调整提供参考。     

他克莫司慢性肾毒性机制及其防治药物的研究进展

他克莫司（tacrolimus）作为常用的免疫抑制剂,广泛用于器官移植术后和多种自身免疫性疾病。但长期服用他克莫司可导致慢性肾毒性,引起器官存活率下降、死亡率升高等,极大影响临床结局。近年研究表明,氧化应激、细胞自噬、细胞凋亡、肾素-血管紧张素系统（renin-angiotensin-system,RAS）以及炎症介导他克莫司慢性肾毒性（tacrolimus-induced chronic nephrotoxicity,TICN）的发生发展。相应地,抗氧化剂、RAS抑制剂、钙离子通道阻滞剂及某些天然药物等对TICN显示出了一定的防治效果。基于此,该文综述了TICN的发生机制和防治药物的研究进展,以期为TAC的临床安全使用和未来研究提供参考。     

新型免疫抑剂他克莫司药物动力学研究进展

新型大环内酯类免疫抑制剂他克莫司,现已在器官移植中广泛用于抗排斥反应及自身免疫系统疾病的治疗,本文综述该药 的药物动力学进展,及各种因素对其药物动力学的影响、药物治疗窗及血药浓度监测方法,为临床合理用药提供参考。     

The new drug approvals of 1987, 1988, and 1989: trends in drug development

The new drug approvals of 1987, 1988, and 1989 were analyzed to determine whether there are any emerging trends in the US drug development and review processes. Sixty-four new drugs were approved by the FDA during this period, of which 55 met the Center for the Study of Drug Development's definition of a new chemical entity (NEC). For the 55 NCEs, the mean length of the investigational new drug application (IND) phase (IND filing to NDA submission) was 5.2 years, the new drug application (NDA) phase (NDA submission to approval) was 2.9 years, and the total phase (IND filing to NDA approval) was 8.1 years. Nine of the 55 NCEs were classified by the FDA as 1A (important therapeutic gain), 15 were classified as 1B (modest gain), 29 were classified as 1C (little or no gain), and 2 were classified as 1AA (drugs to treat AIDS and AIDS-related conditions); 10 drugs were granted orphan status. The mean NDA phase for 1A drugs was 2.4 years; 1B drugs, 2.9 years; 1C drugs, 3.1 years; 1AA drugs, 1.4 years; and orphan drugs, 2.5 years. Forty-four of the 55 NCEs (80%) were available in foreign markets before US approval was given, with a mean of 6.5 years of prior marketing. These data are consistent with figures for previous years and suggest little change in the rate of new drug development and review in the United States.     

抗真菌药的进展与临床应用评价

目的：缘于环境的污染、抗生素的滥用和致炎操作的侵袭,深部真菌感染已成为一个严重的公众问题,本文阐述对抗真菌感染药的进展与临床评价。方法：采用国内、外文献综述方法。结论与讨论：抗真菌药近年来进展迅猛,抗真菌活性较之传统药物有所增强,为对抗真菌感染的治疗提供了全新的效果,标志着一个新的里程的开始。     

网络药理学:药物发现的新思想

新药研发是医药产业发展的核心驱动力,也是社会发展的重要需求,但近年来,随着对药物研发要求的不断提高,新药研发正面临着巨大困难,单靶点高选择性的新药研发思想遇到了挑战,已经显示出发展的局限性。网络药理学是近年来在单靶点药物研究的基础上提出的新药发现新策略。本文围绕网络药理学的形成基础和目前研究现状,探讨网络药理学发展的方向和应用前景,同时分析网络药理学的局限性和存在的问题,并通过与传统中医药学理论和中药复方有效成分组学的思想相比较,探讨网络药理学在新药研发中的应用。     

Pediatric licensing status and the availability of suitable formulations for new medical entities approved in the United States between 1998 and 2002

The availability of new medical entities for children in the United States was examined at the time of marketing approval and 3 years later. New medical entities approved in the United States in each of the years 1998 to 2002 were identified using the Center for Drug Evaluation and Research Web site. Each Physicians' Desk Reference published in the years 1998 to 2005 was examined to determine formulations and licensing information. For the 133 new medical entities licensed to be marketed in the period 1998 to 2002, the number licensed for children increased from 5 (4%) to 39 (29%) in the 3 years after registration. After 3 years' marketing, 79 (59%) drugs were in formulations suitable for children, and 27 (20%) of the new medical entities were licensed and had a suitable formulation for children. Incentives to improve access for children to medicines should focus more on demonstration of improved access.     

皮肤科局部用药新载体的研究进展

近年来,随着皮肤病发病率的增加,传统剂型在治疗皮肤病中存在的药物稳定性差、透皮效率和皮肤保留量低等问题也逐渐凸显出来,因此需要药学人员研究、开发皮肤科局部用药的新载体。本文通过对近几年相关文献的查阅、分析、归纳和总结,综述了当前皮肤科局部用药新型载体的种类、特点及应用。     

The treatment of Helicobacter pylori infection: the changing picture of a still unresolved problem

More than 20 years from the discovery of Helicobacter pylori there is still a need to eradicate the bacterium. The efficacy of the current preferred first-line therapy--the triple regimen--has progressively decreased over the last 5 - 6 years, paralleling the progressive increase in the prevalence of resistant bacterial strains. Similarly, the quadruple therapy has progressively lost its importance as rescue therapy in some countries where bismuth is no longer available. A large number of studies investigating new combinations of drugs, new antibiotics and new regimens have been published in recent years. The most promising regimens--sequential therapy and triple therapy with lovofloxacin--have progressively gained importance but still need further confirmation of their efficacy before they can replace the old protocols in the everyday treatment of H. pylori infection.     

Trends in drug development: the 1985-86 new drug approvals

New drug approvals in 1985 and 1986 were analyzed to determine whether any new trends have emerged in the US drug development process. Fifty-three new drugs (including three biologic products) were approved during this period; 46 met the Center for the Study of Drug Development's definition of a new chemical entity (NCE). More than 70% of the 46 approvals were granted in the fourth quarter, 50% in December alone. Four were FDA classified as 1A (important therapeutic gain), 24 as 1B (modest gain), and 16 as 1C (little or no gain); two biologics were not classified. Nine drugs were given orphan status. For the 37 non-orphan drugs, the duration of the "development phase" (IND filing to NDA submission) was 5.6 years; the "review phase" (NDA submission to approval) was 2.6 years; and the "total time" (IND filing to NDA approval) was 8.2 years. Review phase for the four 1A drugs was 2.4 years; for the 24 1B drugs, 2.6 years; for the 16 1C drugs, 2.8 years; and for the nine orphan drugs, 2.7 years. Of the 46 drugs, 33 (71.7%) were available in foreign markets prior to US approval with a mean of 5.5 years of prior marketing. Although the total of 46 NCE approvals in 1985 and 1986 represents a two-year high, there has been a dramatic shift towards fourth quarter approvals. Lengths of the development and FDA review phases are in keeping with those values for previous years.     

制药工业展望

简要评述了世界制药工业２０年取得突破的新药，在开发中的具有 新作用机制的药物，药理滨革命性进展以及新药研究开在采用的新研究手段，在此基础上对世界医药市场与制药工业作了展望。     

Bruker Daltonics: leading the way from basic research to mass-spectrometry-based clinical applications

For several years, Bruker Daltonics has been committed to the development of new applications of mass spectrometry in clinical research, which have the potential to become next-generation diagnostic procedures. After introducing the CLINPROTtrade mark product a couple of years ago, for biofluid analysis in the search of predictive peptide biomarkers indicating certain disease conditions, Bruker Daltonics recently expanded their portfolio with the MALDI BioTypertrade mark and the MALDI Molecular Imagertrade mark to enter new markets, such as the identification of microorganisms and molecular imaging. This article focuses on the current activities and future perspectives of these new clinical research solutions.     

全军新药研究的现状,趋势及对策

本文着重论述了近几年来全军新药研究的现状、趋势，新药研究报批中存在的问题及其对策以及新药研究、开发、转化为生产力的六个环节。