手性药物的药动学、药效学及不良反应

本文探讨手性药物的代谢动力学及药效学特征,阐明其药理活性和不良反应实质。结果表明有些手性药物在临床上的应用是有益的,有些则会造成不良后果。因此,通过对手性药物的深入研究,对临床合理应用手性药物具有重要的意义。     

谈谈老年患者的药物不良反应问题

随着人口老龄化程度逐步增加,对于老年患者如何合理用药,笔者就此做一简要分析.1 导致老年人ADR的因素1.1 老年人生理、生化功能的特点 老年人的脑细胞逐年减少、脑血流量下降,耗氧量降低,脑血管阻力增加;心肌收缩力减弱,心输出量降低,血压随着年龄增长而上升,反射性调节功能降低,易发生体位性低血压;肾小球滤过率、肾小管的排泄和重吸收能力相应下降,肾功能约为青年人的1/2;肝细胞与肝血流量减少,使肝的解毒能力下降;膀胱逼尿肌力通常下降     

谈谈老年患者的药物不良反应问题

随着人口老龄化程度逐步增加,对于老年患者如何合理用药,笔者就此做一简要分析。 1 导致老年人ADR的因素 1.1 老年人生理、生化功能的特点 老年人的脑细胞逐年减少、脑血流量下降,耗氧量降低,脑血管阻力增加;心肌收缩力减弱,心输出量降低,血压随着年龄增长而上升,反射性调节功能降低,易发生体位性低血压;肾小球滤过率、肾小管的排泄和重吸收能力相应下降,肾功能约为青年人的1/2;肝细胞与肝血流量减少,使肝的解毒能力下降;膀胱逼尿肌力通常下降。     

老年人心血管药物临床应用分析

目前,我国60岁以上老年人口已达2.22亿人,占总人口的16.1％.老年人心血管疾病增加,伴随基础疾病和合并用药的增多,导致药物不良反应(ADR)增多.故老年病人的合理用药是一个重要的问题.现从药物动力学、药效学、心血管药物相互作用及老年人易发生的不良反应,分析老年人临床合理用药.     

依据药动学和药效学参数合理使用抗菌药物

抗菌药物的药理学研究内容主要包括药代动力学(PK)与药效学(PD)。随着研究的不断深入,人们发现抗菌药物PK/PD参数与药物的临床疗效密切相关。依据抗菌药物对细菌作用的方式和PK/PD特性,将抗菌药物分为浓度依赖型抗菌药     

抗真菌药物的药动学和药效学研究进展

目的:介绍临床常用抗真菌药物的药动学和药效学研究进展,旨在为临床合理用药提供相关依据。方法:查阅国内、外相关文献,进行系统的阅读复习,并进行综合分析。结果:真菌感染发病复杂,诊断困难,预后较差,但是抗真菌药物研发的不断进步,为临床医生用药提供了更多选择,真菌感染的治疗和预后将逐步得到改善。结论:临床常用抗真菌药物的药动学和药效学研究,对于临床合理用药具有重要的指导意义。     

心血管系统药物的PK-PD模型研究进展

目的对心血管系统药物的药动学-药效学(PK-PD)模型研究进行回顾和展望。方法查阅文献资料,对相关内容进行总结。结果所得PK-PD模型以S-Emax模型居多。心血管系统药物的PK-PD模型日益呈现出精细化和复杂化的趋势。结论应用PK-PD模型对心血管系统药物的研究前景广阔,值得进一步推广。     

食物对心血管系统药物作用的影响

食物可通过错综复杂的机制影响药物的疗效和毒性,从而对病人产生有利或不利影响。对此作用进行研究具有非常重要的临床意义。本文就食物对心血管系统药物作用的影响加以综述。     

新型抗真菌药物caspofungin

caspofungin是新型葡聚糖合成酶抑制剂类抗真菌药物中第 1个上市的药物 ,它能有效抑制 β ( 1,3) D 葡聚糖的合成 ,从而干扰真菌细胞壁的合成。caspofungin在体内、外具有广泛的抗真菌活性 ,包括曲菌和念珠菌。多中心试验表明 ,caspofungin治疗难治性或不能耐受其他治疗的侵袭性曲菌感染病人的临床有效率为 4 0 .7%。 2个随机双盲试验表明 ,caspofungin能有效治疗咽或食道念珠菌感染。侵袭性曲菌病人对caspofungin的耐受性较好。本文综述了caspofungin的药效学、药动学特性、临床疗效和不良反应等。     

药品不良反应监测工作的策略研究

为了进一步推动我国药品不良反应监测工作的开展,本文采用比较研究的方法,对中美两国在药品不良反应监测工作上的差异进行了探讨,在此基础上找出并分析我国在开展药品不良反应监测工作过程中存在的问题,最后提出我国有效开展药品不良反应监测工作的一般策略。     

Ocular adverse drug reactions

Drug-induced ocular side effects are described according to recent reports from the literature, the National Registry of Drug-Induced Ocular Side Effects, the World Health Organization (WHO) and the FDA. Adverse events are categorised as certain, probable/likely, possible, unlikely, conditional/unclassified and unassessable/unclassifiable where indicated. Ocular side effects of clinical importance are highlighted with guidelines for recognition, reporting and treatment of adverse drug reactions (ADRs). The current and future status of pharmacovigilance in ocular toxicology is addressed.     

EUDRAGENE: European collaboration to establish a case-control DNA collection for studying the genetic basis of adverse drug reactions

Type B adverse drug reactions (ADRs) are often serious, limit the usefulness of drugs that are otherwise effective, and increase the risks of drug development as they often lead to postmarketing withdrawal. There is evidence that susceptibility to at least some Type B ADRs is under strong genetic influence. Identifying genes in which variation influences susceptibility has obvious practical value for genetic testing and might also make it easier to screen molecules likely to cause ADRs at an early stage of the drug development process. Research in this area is hampered by the lack of a resource in which to study genetic determinants of susceptibility to Type B ADRs. As serious Type B ADRs are rare, case-control designs are the most frequently-used approach. The EUDRAGENE collaboration seeks to develop a resource using an international collaboration. This will provide a basis for adverse drug susceptibility genome association-wide studies using tag single nucleotide polymorphisms, or a direct approach using putative functional polymorphisms.     

Mechanistic basis of adverse drug reactions: the perils of inappropriate dose schedules

Adverse drug reactions (ADRs) have long been recognised as a significant cause of morbidity and mortality. They account for a substantial number of clinical consultations, hospital admissions and extended duration of in-patient stay as well as mortality. By far the most common ADRs are the concentration-dependent pharmacological reactions, the majority of which ought to be preventable. As a result of high concentrations of the parent drug and/or its metabolite(s), there is an augmentation of primary pharmacological activity and/or appearance of new and undesirable secondary pharmacological activity. Typically, these high concentrations result from administration of high doses in an attempt to maximise efficacy and/or modulation of the pharmacokinetics of a drug by either genetic or non-genetic factors. High plasma concentrations of parent drug may result from inherited impairment or drug-induced inhibition of its pharmacokinetic disposition. Conversely, inherited overcapacity or drug-induced induction of the metabolism of a drug may result in low concentrations of parent drug and frequently, rapid accumulation of its metabolites. Environmental, dietary and phytochemical factors may also influence the activity of drug metabolising enzymes. As with inherited polymorphisms of acetylation and cytochrome P450-based drug metabolising enzymes, polymorphisms of other conjugation reactions, such as glucuronidation, increasingly appear to be associated with drug toxicity. Diseases of organs involved in elimination of a drug also alter its pharmacokinetics, plasma concentration and, therefore, the profile of its concentration-dependent ADRs. Inherited mutations, concurrently administered drugs or presence of certain diseases may also alter the sensitivity of some pharmacological targets, accounting for a substantial number of ADRs and interactions. When there is enhanced pharmacodynamic sensitivity, plasma drug concentrations that are apparently within the normal 'non-toxic' range give rise to ADRs. Recent advances have also provided important insights into the wider scope of drug-drug interactions. Interactions that occur at P-glycoproteins, drug transporters and efflux pumps, at various transmembrane interfaces such as the gastrointestinal wall, renal tubules, hepatobiliary border and blood-brain barrier, are beginning to explain many non-metabolic interactions. These alter the systemic exposure to drugs and have so far, begun to explain unexpected neurotoxicity and hepatotoxicity. The function of these transporters is also genetically modulated. These advances, together with continued increased awareness and education of prescribers and pharmacists, offer great opportunities for substantially minimising concentration-related ADRs.     

Immunology of adverse drug reactions

Adverse reactions to drugs often include an immunologic response. An understanding of immunologic mechanisms is useful in understanding the clinical manifestations of drug allergy. Predisposing factors to the development of allergic reactions to drugs include host factors as well as drug factors. Immune response relates to what we know about the components of the immune system as well as their differentiation and maturation processes. Immunologic reactions are often classified as Type I, Type II, Type III or Type IV, and these reaction types often correlate with clinical manifestations. For each reaction type the mechanism, drugs implicated, clinical manifestations, and treatment can be described.