药英整理的重.doc

Unit 5 Lead compounds Words: lead compound[not intended to be used as a clinical agent临床药物,is a starting point], agonist[激动剂], antagonist[拮抗剂], chemical modification, high-throughput screening(HTS)[高通量药物筛选 ], target[靶点] Knowledge points(选择 判断) How to understand “lead compound is the starting point from which a clinically(临床的) useful compound can be developed?”先导化合物是发展研发临床有效化合物的起点。 The tests to detect a lead compound can reveal effects on different levels. 检测先导化合物测试可以揭示在不同水平的影响. 【A physiological（生理学的） effect, a cellular（细胞学的） effect, a molecular（分子的） effect.】 Agonist is used as a lead compound to design a receptor（受体）antagonist. Example, histamine is used as a lead compound to develop cimetidine. Strategies in the search for new lead compound. Systematic screening a chemical library(inadequate diversity缺乏多样性, low hit rates低阳性率, poor bioavailability生物利用度差or toxicity profiles毒性反应); structure modification(start with known active principles有效组份,a better specific activity profile选择性更专一)；serendipity(意外新发现, 机缘凑巧);rational drug design(合理药物设计) Unit 11 Words: indication适应症, contraindication禁忌症, active ingredient有效成分, inactive ingredient, brand name商品名, generic name通用名称, chemical name, primary, secondary, arthritis关节炎, osteoarthritis骨关节炎, pediatrics儿科学, Knowledge points: different sections in package insert [包括药物的化学结构，药理和毒理作用（pharmacological and toxicological action），临床适应症和禁忌症（clinical indications and contraindications），注意事项(precautions),报告的不良反应（reported adverse reactions），用量建议，现有剂型（available dosage form）] The tragedy of sulfanilamide【磺胺的悲剧：它是第一种磺胺类的抗菌剂药物，但是它是以甘二醇为稀释剂的，是一种抗冻剂的化学类似物，100多个人，其中有很多是小孩子，在服药后死亡。此后美国食品与药物管理局（FDA）制定相关法律，严管严查，没收掺假药物，挑选专家团队对于older drugs的药品说明书进行修订。 What is off-label use（the practice of prescribing pharmaceuticals for an unapproved indication or in an unapproved age group, unapproved dose or unapproved form of administration.） What is orphaning clause and why do a lot of medicines carry such an orphaning clause孤儿条款（not to be used in children?, since c