重视药品的二次开发

由于全新药物的开发费用、开发难度的上升，世界各国药物开发研究人员将药物开发重点转移到产品的二次开发，如拓展老药的新用途、开发新剂型等，以期获得新的有效治疗药物。     

143例药品不良反应报告分析

目的 分析本院药物不良反应(ADR)发生的原因及规律,促进临床安全合理用药.方法 对本院2011年143例ADR报告从患者性别年龄、给药途径、药品品种等方面进行回顾性统计分析.结果 ADR发生率以60岁以上年龄组(25.87％)、静脉给药组(88.81％)及中药制剂组(37.06％)最高,ADR累及器官/系统以皮肤及其附件损害最常见(40.12％).结论 医院应加强ADR的宣传培训工作,增强医护人员对ADR的认识,规范ADR报表的填报,为临床安全合理用药提供参考资料.     

不可随意给药物"改头换面"

张女士50刚出头,听朋友说女性40岁以后缺钙比较严重,容易发生骨质疏松症,继而会出现弯腰驼背,既不利于健康,又影响体型.为防止这种情况的出现,她经别人推荐,到药店买回乐力胶囊服用.服了几天,她觉得胶囊太大,难吞下,于是,她便把胶囊拔开,倒出里边的药粒用水送服.     

药品不良反应14例分析

药品不良反应(ADR)监测,是医院安全有效,合理用药,提高医疗质量的一个重要手段。为全面了解我院ADR发生情况和探讨ADR发生的易感因素,现将我院2002年6月～2003年12月收集到的14例药品不良反应,加以简要分析。1资料来源与方法1.1病例资料:我院2002年6月～2003年12月门诊和住院的药品不良反应14例(门诊3例,住院11例)。14例ADR中,11例为住院患者,占同期住院患者总数1.63 % ,3例为门诊患者占同期门诊人次0.1 %。男8例、女6例,年龄13～62岁、60岁以上者1例,平均年龄30岁,以16～41岁的青壮年居多共11例。有既往过敏史6例。1.2方法:将14例ADR…     

浅谈口服药品服药时间

药物口服是临床最常用的给药途径之一,安全、方便、经济,口服给药的时间有空腹服用、餐前服用、餐后服用、清晨服用、睡前服用等几种类型。药物的服药时间是根据药物的药效学、药动学的不同及药物与食物的关系等多种因素决定的。掌握正确的服药时间是保证药物治疗效果的要素之一,为了规范调剂工作中的发药交待环节,笔者对指导患者服药的说明书进行调查分析。     

药物剂型及给药途径的合理应用分析

目的：对不同药物剂型及给药途径的合理应用进行分析讨论。方法：通过对相关文献资料的查阅,综合分析不同药物剂型及给药途径的影响,进而探讨合理给药的途径。结果：不同剂型及给药途径,对临床适应症的选择、药物的血药浓度、达峰时间、患者的顺应性有着不同的影响。结论：应根据产品的剂型特点及使用途径,结合患者的实际情况,选择合适的药物剂型和给药途径。     

510例抗感染药品不良反应报告分析

抗感染药是目前临床应用最广泛的一类药品,对其开展药品不良反应(ADR)调查,是提高医疗质量,规范用药行为,促进合理用药的重要环节.为了解这类药品ADR发生情况,探讨发生因素,现对江苏省2002年1月～12月收集的ADR报告表进行回顾性分析和讨论.     

影响药物临床疗效的因素浅析

药物防治疾病的疗效受多方面因素的制约。如病人的年龄、性别、病理状态、个体差异、遗传因素和精神因素等。药物的剂量和剂型、给药途径、给药时间和次数．以及反复用药、合并用药等均可影响药物的作用。     

某区妇幼保健院345例药品不良反应报告的相关因素分析

目的:分析妇幼保健院药品不良反应报告的相关因素,为安全用药提供参考。方法:选择2014年4月—2016年4月间上报的345例药品不良反应报告,采用回顾性分析法,分析引起药品不良反应患者年龄以及涉及的药物类别、给药途径、累及器官等因素。结果:345例药品不良反应报告中,年龄段在18~40岁患者占41.45%显著高于其他年龄段患者;药物类别中抗感染药物占36.52%显著高于其他类别药物;心血管系统药物、神经系统药物构成比分别占13.91%和10.14%,仅次于抗感染药物;给药途径中,静脉滴注占55.65%显著高于其他给药途径;口服给药占26.38%仅次于静脉滴注;累及消化系统占56.52%显著高于其他脏器和系统,累及心血管系统占24.93%仅次于消化系统。结论:对药品不良反应报告予以全面分析,医院药品不良反应的发生存在一定规律与特征,可为临床合理用药提供有效指导,从而提高治疗安全性。     

药物剂型及给药途径的临床合理应用性

目的探讨不同药物剂型和不同的给予途径的临床合理应用性。方法通过对临床不同药物剂型和不同给予途径产生的不同药效的分析,以探讨合理的给药途径。结果目前临床上的药物剂型主要包括注射剂、片剂、胶囊剂、颗粒剂、栓剂、软膏剂以及气雾剂等;给药的途径主要包括静脉注射、注射用药、口服给药以及舌下给药;同一药物给予不同的剂型治疗所发挥出的临床疗效存在显著的差异性。结论由于药物剂型复杂,并涉及到多种方面的内容,药效也会随着药物剂型的不同和给药途径的不同而改变,因此在临床应用中应用遵循用药原则,以提高疗效。     

第二代三唑类抗真菌药物的研究进展

侵袭性真菌病的发病率和病死率逐年上升,新型抗真菌药物的研究和开发也越来越受到重视,尤其是三唑类抗真菌药物。本文综述国内外近期关于第二代三唑类抗真菌药物的研究进展,以期为未来临床真菌病的治疗及新药研发提供新的思路。     

A review on the impact of P-glycoprotein on the penetration of drugs into the brain. Focus on psychotropic drugs.

In recent years there has been increasing focus on the role of the drug transporter P-glycoprotein (P-gp) with regard to drug penetration into the brain. Studies using mice devoid of functional P-gp have revealed that P-gp at the blood-brain barrier (BBB) can exert a profound effect on the ability of some drugs to enter the brain, e.g. cardiovascular drugs (digoxin, quinidine), opioids (morphine, loperamide, methadone), HIV protease inhibitors, the new generation of antihistamines, and some antidepressants and antipsychotics. Among the latter group, risperidone is strongly influenced having about 10 times higher cerebral concentration in P-gp knock-out mice than in control mice. Taking into account that polytherapy is commonplace in psychiatry, theoretically there is a risk of drug-drug interactions with regard to P-gp at the BBB. Here we review the evidence for a role of P-gp with regard to psychoactive drugs from in vitro studies and experiments in knock-out mice devoid of functional P-gp. Moreover, the evidence for significant drug-drug interactions involving psychotropic drugs in rodents is considered. Clinical observations suggesting a role for P-gp in relation to drug-drug interactions at the BBB are sparse, and a definite conclusion awaits further studies. Also, the possible clinical relevance of P-gp genetic polymorphisms is questionable, and more investigations are needed on this subject.     

Medical drugs from humus matter: Focus on mumie

In this review, we focus on the medicinal drugs from humus matter such as peat, sapropel, and mumie. The most clinically available medicines, containing peat and sapropel extracts, are Torfot, Tolpa Peat Preparation (TPP), Peloidodistillate, Humisol, Peloidin, FiBS, and Eplir. Much attention in the review is concentrated on mumie composition, its pharmacological properties, and new pharmacological drugs with mumie (Shilagen, Abana, Cystone, Diabecon 400, EveCare, Geriforte, Lukol, Pilex, Rumalava, Tentex forte, Nefrotec, Adrenotone, Siotone, La‐Tone Gold, Andro‐Surge, Solanova Libidoplex). It was concluded that therapeutic properties of crude extracts from peat, sapropel, and mumie have similarity to the ones of fulvic and humic acids. They are antibacterial, antitoxic, antiradical, antiulcerogenic, antiarthritic, immunomodulatory, and antiinflammatory properties. Possible directions for better development of new drugs from humus matter are discussed. Drug Dev. Res. 57:140–159, 2002. © 2002 Wiley‐Liss, Inc.     

Focus on new drugs in development against human cytomegalovirus

The limitations of current therapies for human cytomegalovirus (HCMV) coupled with the continued impact of HCMV disease in the immunocompromised host are the driving force for the development of new drugs against HCMV. This review predominantly focuses on new non-DNA polymerase inhibitors of HCMV replication. Drugs such as tomeglovir (BAY-384766), 2-bromo-5,6-dichloro-1beta-D-ribofuranosyl benzimidazole (BDCRB) and GW-275175X act as inhibitors of the terminase complex that is involved in cleavage and packaging of the unit length DNA into the capsids. Although the viral protein kinase UL97 has been exploited as an activator of ganciclovir and its prodrug valganciclovir, a new inhibitor maribavir (benzamidavir) has been shown to be a highly potent inhibitor of this enzyme. Many of these compounds have undergone successful phase I clinical trials. There are other compounds which have been identified through drug-screening but are at the earlier stages of development.     

肿瘤靶向药物不良反应的药学服务关注点

随着分子生物学技术的发展,越来越多的靶向药物被成功研发并上市。靶向药物具有靶向性强、不良反应相对较低等优点,能够对肿瘤细胞内异常的信号通路靶点特异性杀伤,进而抑制肿瘤的发生发展。但靶向药物的不良反应仍是无法回避的问题。同时,该类药品往往价格昂贵,如何合理使用,使其发挥应有的作用是药师应关注的问题。本文详述了靶向药物的分类以及上市情况,总结了靶向药物常见的不良反应及防治,以期为靶向药物的药学监护提供客观依据。     

Focus on new antiviral drugs for AIDS and smallpox treatments

More than 400 papers on medicinal chemistry were presented at the 231st National Meeting of the American Chemical Society in Atlanta, Georgia, U.S.A., March 26-30, 2006. A major focus was a large number of papers on new AIDS drug therapies being developed. The rapid development of HIV viral mutations is one reason expensive highly active antiretroviral therapy multidrug treatments are preferred. This increasing resistance of HIV to current drugs is spurring new drug development. In addition, concerns about bioterrorism have awakened interest in drug treatments for a viral disease once thought to be extinct, smallpox. This report will focus on these areas of research.     

New antiepileptic drugs that are second generation to existing antiepileptic drugs

In the last decade, 10 new antiepileptic drugs (AEDs) have been introduced that offer appreciable advantages in terms of their favourable pharmacokinetics, improved tolerability and lower potential for drug interactions. However, despite the large therapeutic range of old and new AEDs, approximately 30% of the patients with epilepsy are still not seizure free and, consequently, there is a substantial need to develop new AEDs. The new AEDs currently in development can be divided into two categories: drugs with completely new chemical structures such as lacosamide (formally harkoseride), retigabine, rufinamide and talampanel; and drugs that are derivatives or analogues of existing AEDs that can be regarded as second-generation or follow-up compounds of established AEDs. This article focuses on the second category and thus critically reviews the following second-generation compounds: eslicarbazepine acetate or BIA-2-093 and 10-hydroxy carbazepine (carbamazepine derivatives); valrocemide and NPS 1776 (isovaleramide; valproic acid derivatives); pregabalin and XP13512 (gabapentin derivatives); brivaracetam (ucb 34714) and seletracetam (ucb 44212; levetiracetam derivatives); and fluorofelbamate (a felbamate derivative). In addition, a series of valproic acid derivatives that are currently in preclinical stage has also been evaluated because some lead compounds of this series have a promising potential to become new antiepileptics and CNS drugs. For any of these follow-up compounds to become a successful second generation to an existing AED, it has to be more potent, safer and possess favourable pharmacokinetics, including low potential for pharmacokinetic and pharmacodynamic drug interactions.     

The METEOR study: frequency of metabolic disorders in patients with schizophrenia. Focus on first and second generation and level of risk of antipsychotic drugs

The objective of this crosssectional study was to estimate the prevalence of metabolic disorders and hypertension in patients with schizophrenia and to compare prevalence between patients treated with first-generation (FGA) and second-generation (SGA) antipsychotic drugs. The study included 2270 adults with schizophrenia. Patients were assigned to an FGA or SGA stratum on the basis of current treatment. Data were collected on sociodemographic, lifestyle and clinical variables. Blood pressure, waist and hip circumference, blood glucose, triglycerides and cholesterol were measured. The primary evaluation criterion was the prevalence of a glycaemic disorder. Secondary criteria were the prevalence of dyslipidaemia, obesity, hypertension and metabolic syndrome. A propensity score was used to control imbalance between strata. The prevalence of glycaemic disorders was 31.1% (FGA) and 27.6% (SGA). No between-strata difference in prevalence was observed for glycaemic disorders, dyslipidaemia or metabolic syndrome. The prevalence of hypertension was higher (P=0.033) in the FGA group. The proportion of women (but not men) who were overweight or obese was higher in the SGA group (P=0.035), as was the proportion reporting weight gain of more than 5 kg (P<0.001). In an exploratory unadjusted post-hoc analysis, significantly higher frequencies of dysglycaemia (28.5 vs. 22.0%; P=0.006), low HDL cholesterol (35.3 vs. 29.7%; P=0.023) and metabolic syndrome (36.7 vs. 30.7%; P=0.021) were observed in patients taking SGAs considered to carry high metabolic risk compared with those taking low-risk agents. In conclusion, metabolic disorders are prevalent in patients with schizophrenia treated with antipsychotics and are under-diagnosed and under-treated.