2015年电大《药物化学》期末复习简答题考试资料小抄.doc

电大药物化学期末复习简答题考试资料小抄1、试写出下列药物在相应条件下的分解产物H+或OH-答：2-甲氨基-5氯-二苯酮 甘氨酸2.药物的杂质是指哪些物质？有哪些来源？为什么要制定药物中杂质的限度？答：药物的杂质是指在生产、贮藏过程中引进或产生的药物以外的其他化学物质，包括由于分子手性存在而产生的非治疗活性的光学异构体。来源有生产过程和贮藏过程。杂志的存在不仅影响药物的纯度，同时还会带来非治疗活性的副作用，必须加以控制，通常要规定药物的杂志限度3.麻醉药主要分为哪两大类？作用机制有何不同？答：麻醉药分为全麻药和局麻药，全麻药作用于中枢神经系统，局麻药作用于外周神经系统。4.局麻药是如何发展起来的?按化学结构可分为哪几类?答：局麻药是从古柯树叶中提取的可卡因进行结构改造改造而来，按化学结构可分为：1.芳酸脂类，2.酰胺类，3.氨基酮和氨基醚类5.盐酸普鲁卡因有哪些化学性质?与哪些结构特点有关?答：分子中含脂键，易被水解 含芳伯胺基，易被氧化变色，有重氮化-偶合反应具有叔胺结构，具有生物碱样性质6.巴比妥类药物有哪些化学性质?为什么苯巴比妥钠要做成粉针剂?答：具有弱酸性，可溶于氢氧化钠和碳酸钠溶液，生成苯巴比妥钠，其水溶液为碱性，与酸性药物或吸收空气中的CO2，可析出苯巴比妥沉淀本品为丙二酰脲衍生物，显丙二酰脲类药物的显色反应。本品钠盐溶液放置易分解，产生苯基丁酰脲沉淀失去活性。故配置成粉针剂7.如何用化学方法区别地西泮和奥沙西泮?说明其原理.答：将两种药品分别放入酸、碱中加热水解，地西泮分解产物没有芳伯氨基，奥沙西泮产物中含有芳伯胺基，对两者分解产物经重氮化后与-萘酚偶合，生成橙色沉淀者即为奥沙西泮。8.抗癫痫药物主要分为哪些结构类型?说明代表药物的作用特点.答：苯巴比妥（巴比妥类）用于癫痫大发作;苯妥因（乙内酰脲类）对癫痫大发作和精神运动型发作有效对小发作无效；三甲二酮（恶唑烷酮类）用于失神性小发作，对大发作无效；乙琥胺（丁二酰亚胺类）是癫痫小发作首选9.抗精神药物主要有哪些结构类型?各举一例药物.答：吩噻嗪类： 氯丙嗪 噻吨类：氯普噻吨 丁酰苯类 ：氟哌啶醇苯酰胺类： 舒必利 二苯并氮杂卓： 氯氮平10.抗抑郁药主要分为哪几类?各举一例药物.答：三环类 多赛平 单胺氧化酶抑制剂 异烟肼 5-H再摄取抑制剂 氟西汀11.利尿药有哪些结构类型？各举一例药物。.答：利尿药结构类型主要有：（1）磺酰胺类及苯并噻嗪类 如 氢氯噻嗪（2）苯氧乙酸类 依他尼酸 （3）甾类 螺内酯（4）其他类 甘露醇12.咖啡因在水中的溶解度很小，如何能增加其在水中的溶解度？.答：咖啡因可与有机酸或其碱金属盐，如苯甲酸钠、水杨酸钠、枸橼酸钠等形成复盐而增加水中溶解度。13.H1受体拮抗剂主要有哪些结构类型？个举一例药物。答：H1受体拮抗剂的结构类型主要有：（1）乙二胺类 ： 西替利嗪（2）氨基醚类： 盐酸苯海拉明（晕海宁） （3）丙胺类 ：马来酸氯苯那敏（扑尔敏）（4）三环类：异丙嗪（5）哌啶类 ： 阿司咪唑（息斯敏）14.苯海拉明的主要副反应是什么？为什么将其和8-氯茶碱成盐使用？答：苯海拉明的主要副反应是嗜睡和中枢抑制副作用。中枢兴奋药8-氯茶碱可以降低苯海拉明的不良反应 。15.从结构特点分析为什么麻黄碱的作用比肾上腺素弱，但作用较持久？答：该类药结构中苯环上羟基可显著地增强拟肾上腺素作用。肾上腺素具有儿茶酚结构，活性大，但不稳定，作用时间短暂。麻黄碱苯环上无羟基，作用减弱，作用时间延长。16.试比较阿托品，东莨菪碱，山莨菪碱及樟柳碱的化学结构的差异，并说明与生理活性大小的关系。答：四种药物化学结构非常相似，均是莨菪醇和莨菪酸所成的酯，所不成的只是有无6、7位氧桥、6位羟基或莨菪酸位羟基。氧桥的存在使分子的亲脂性增强，易透过血脑屏障，增强中枢作用。而6位羟基或莨菪酸位羟基的存在，使分子的亲水性增强，中枢作用减弱。东莨菪碱分子中有氧桥，中枢作用最强；樟柳碱虽也有氧桥，但其莨菪酸位还有羟基，综合影响的结果是中枢作用弱于阿托品；山莨菪碱6位多一羟基，作用最弱。东莨菪碱阿托品樟柳碱山莨菪碱17.为什么内源性的乙酰胆碱不能成为临床上的治疗药物？答：（1）乙酰胆碱对所有的胆碱能受体无选择性，导致产生副作用（2）乙酰胆碱为季铵化合物，不易通过生物膜，因而生物利用度低（3）乙酰胆碱的化学稳定性差，在体内易被酯酶水解而失活18.抗高血压药物可分为哪几大类？各举一例药物。答：（1）作用于中枢神经系统的药物 如甲基多巴 （2）神经节阻断药 美加明（3）作用于神经末梢的药物 利舍平（利血平）（4）血管紧张素转化酶抑制剂 卡托普利（5）肾上腺素受体拮抗剂 美托洛尔（6）作用于血管平滑机的药物 地巴唑（7）利尿药 氢氯噻嗪（8）钙拮抗剂 氨氯地平19.分别说明钙拮抗剂，-受体拮抗剂，ACE抑制剂及羟甲戊二酰辅酶A还原酶抑制剂的主要临床用途，各举一例药物。答：-受体拮抗剂：抗高血压或抗心绞痛或抗心律失常 钙拮抗剂：抗高血压或抗心绞痛或抗心律失常 ACE抑制剂：抗高血压或充血性心衰 磷酸二酯酶抑制剂 ：抗心力衰竭 20.试简述利舍平的不稳定性。答：在光和热的影响下，利舍平的3-H能发生差向异构化，生成无效的3-异利舍平。在光和氧的作用下发生氧化，生成3-去氢利舍平及3，5-二烯利舍平。21.为什么SMZ常和TMP组成复方制剂使用？答：磺胺甲噁唑（SMZ）可以抑制二氢叶酸合成酶，阻断细菌合成二氢叶酸，甲氧苄啶抑制二氢叶酸还原酶，阻断二氢叶酸还原成四氢叶酸，两者合用时，可使细菌体内的四氢叶酸的合成受到双重阻断，因而产生协同抗菌作用，作用增强，因此两者常合用。22.简述喹诺酮类药物的构效关系。答：通过对喹诺酮类药物的结构和生物活性的研究，可将其构效关系总结如下：（1） B环是抗菌作用的必需结构，变化小；而A环可作较大改变，可以是苯环，吡啶环，嘧啶环等。（2） 3位COOH和4位C=O是药效必不可少的部分，被其他取代基取代时活性消失。（3） 1位取代基对抗菌活性影响较大，可以为脂肪烃基和芳烃基。若为脂肪烃基，以乙基或与乙基体积相近的取代基为好；若为脂环烃基，以环丙基最好；若为芳烃基，可以是苯基或其他芳香基。（4） 5位取代基以氨基为最好。（5） 6，7，8位的取代基变化范围较大。6，8位分别或同时引入氟原子，抗菌活性增大，7位引入五元或六元杂环，抗菌活性明显增强，以哌嗪基为最好。23.试写出青霉素在酸，碱，-内酰胺酶作用下的分解产物。答：在稀酸条件下，生成青霉二酸；在强酸并加热条件下生成青霉胺和青霉醛酸。碱性或-内酰胺酶条件下生成青霉酸、青霉酰胺和青霉酸酯。24.什么是烷化剂？主要包括哪些结构类型？答：烷化剂是在体内能形成缺电子的活泼中间体或其他具有活泼的亲电性基团的化合物，进而与细胞中的生物大分子中含有丰富电子的基团发生共价结合，使其丧失活性或使DNA分子发生断裂，导致肿瘤细胞死亡，抗肿瘤活性强。烷化剂按化学结构可分为：氮芥类、乙撑亚胺类、甲磺酸酯及多元醇类、亚硝基脲类。25.氮芥类药物的结构是由哪两部分组成？各自发挥什么作用？答：烷基化部分和载体部分。烷基化部分（即通式中的双-氯乙胺基，也称氮芥基）是抗肿瘤活性的功能基团；载体部分主要影响药物在体内的吸收、分布等药代动力学性质，通过选择不同的载体，可以达到提高药物选择性和疗效、降低毒性的目的。26.试从环磷酰胺在正常组织及肿瘤组织中代谢产物的不同说明为什么其毒性比其他氮芥类药物小。答：环磷酰胺是利用前药化原理设计出来的药物。由于氮原子上连有吸电子的磷酰基，降低了氮原子的亲核性，因此在体外对肿瘤细胞无效。进入体内后，由于正常组织和肿瘤组织中所含的酶的不同，导致代谢产物不同，在正常组织中的代谢产物是无毒的4-酮基环磷酰胺和羧基化合物 ，而肿瘤组织中缺乏正常组织所具有的酶，代谢途径不同，经逆Michael加成反应生成丙烯醛和磷酰氮芥，后者经非酶水解生成去甲氮芥，这三个代谢产物都是较强的烷化剂。因此环磷酰胺对正常组织的影响较小，其毒性比其它氮芥类药物小。27.抗代谢肿瘤药物主要分为哪几类？各举一例药物。答：嘧啶拮抗物 阿糖胞苷 嘌呤拮抗物 巯嘌呤 叶酸拮抗物 甲氨蝶呤28.试举出五例抗肿瘤天然药物。答：博莱霉素、丝裂霉素C、阿霉素、喜树碱、长春新碱29.如何用化学方法区别炔雌醇和地塞米松？试以反应式表示。答：炔雌醇中存在乙炔基 地塞米松存在-羟基酮结构，其甲醇溶液与碱性酒石酸铜共热，生成氧化亚铜的橙红色沉淀。反应式见书P23830.糖皮质激素有哪些临床用途。答：糖皮质激素具有调节糖、脂肪、和蛋白质的生物合成和代谢的作用，还具有抑制免疫应答、抗炎、抗毒、抗休克作用。31.分别什么维生素A,D,E,K,B1,B2,B6及维生素C的临床用途。答：维生素A临床上主要用于因维生素A缺乏引起的夜盲症、角膜软化、皮肤干燥、粗糙及粘膜抗感染能力低下等症的治疗；还用于妊娠、哺乳期妇女和婴儿等的适量补充。维生素D临床上主要用于因维生素D缺乏引起的佝偻病或软骨病、婴儿手足搐搦症、老年性骨质疏松症等的治疗和预防。维生素E临床上主要用于习惯性流产、不孕症及更年期障碍、进行性肌营养不良、间歇性跛行及动脉粥样硬化等的防治。维生素K临床上主要用于凝血酶原过低症、新生婴儿出血症等的防治。维生素B1临床上主要用于因维生素B1缺乏引起的脚气病及消化不良等疾病的治疗。维生素B2临床上主要用于因维生素B2缺乏引起的各种粘膜和皮肤炎症，如口角炎、唇炎、舌炎等。维生素B6临床上主要用于治疗因放射治疗引起的恶心、妊娠呕吐、异烟肼等药物引起的周围神经炎、白细胞减少症、座疮脂溶性湿疹等。维生素C临床上主要用于坏血病的预防与治疗，及肝硬化急性肝炎和砷、汞、铅、苯等慢性中毒时的肝脏损害急慢性传染病等的辅助治疗。32.药物与受体的结合有哪几种方式？答：化学的方式通过共价键结合形成不可逆复合物。物理的方式通过离子键、氢键、离子偶极、范德华力和疏水性等形成可逆的复合物。33.药物的手性构型对药物的活性产生哪些影响？答：（1）对映体具有等同的药理活性和强度。（2）对映体产生相同的药理活性，但强弱不同。（3）对映体中一个有活性，一个没有活性。（4）对映异构体之间产生相反的活性。（5）对映异构体之间产生不同类型的药理活性。34.为什么青霉素G钠盐(或钾盐)须做成粉针剂？答：青霉素钠盐或钾盐水溶液的碱性较强，-内酰胺环会开环，生成青霉酸，失去抗菌活性。因此青霉素的钠盐或钾盐必须做成粉针剂，使用前新鲜配制。35.简述非甾体抗炎药的作用机理？答：非甾体抗炎药有解热镇痛、抗炎作用，但以抗炎作用为主，临床上侧重于风湿性、类风湿性关节炎、红斑狼疮等症的治疗。目前临床使用的大部分非甾体抗炎药是通过抑制花生四烯酸环氧酶的活性，阻断前列腺素的生物合成而发挥抗炎抗风湿作用。36.为什么阿司匹林及扑热息痛在保存过程中颜色会加深？答：阿司匹林在空气中较稳定，遇湿气即缓缓水解生成水杨酸和乙酸，遇碱和加热水解更快。其成品中由于原料残存或储存时保管不当，可能含有过多水杨酸杂质，该杂质不仅对人体有毒性，而且较易氧化成一系列醌式有色物质，因此颜色逐渐变为淡黄、红棕甚至黑色。扑热息痛在空气中稳定，水溶液的稳定性与Ph值有关，在pH值=6时最为稳定，半衰期为21.8年（25），在酸性及碱性条件下稳定性较差，水解产物为对氨基酚，可进一步发生氧化降解生成醌亚胺类化合物，颜色逐渐变成粉红色、棕色、最后成黑色，故制剂及保存要注意。37.简述拟肾上腺素药物的构效关系？答：主要有以下几点：(1) 必须具有苯乙胺的基本结构。(2) 苯环上羟基可显著地增强拟肾上腺素作用，而3，4-二羟基化合物比4-羟基化合物的活性大。(3) 多数拟肾上腺素药在氨基的 位具有羟基（多巴胺、多巴酚丁胺例外），此羟基的存在对活性有显著影响，一般R构型光学异构体具有较大活性。(4) 侧链氨基被非极性烷基取代时，基团的大小与受体的选择性有密切关系，在一定范围内，取代基愈大，对 受体的选择性愈大，对 受体的亲和力就愈小。(5) 侧链氨基的碳原子上引入甲基，则由于甲基的位阻效应，阻碍单胺氧化酶（MAO）对氨基的氧化代谢脱氨从而使药物的作用时间延长。38.什么是代谢拮抗？举例说明代谢拮抗原理在药物设计中的应用。答：所谓代谢拮抗就是设计与生物体内基本代谢物的结构有某种程度相似的化合物，使之竞争性地和特定的酶相作用，干扰基本代谢物的被利用，从而干扰生物大分子的合成；或以伪代谢物的身份掺入生物大分子的合成中，形成伪生物大分子，导致致死合成，从而影响细胞的生长。例如：尿嘧啶是体内正常的嘧啶碱基，其掺入肿瘤组织的速度比其它嘧啶快，利用生物电子等排原理，以氟原子代替尿嘧啶5位上的氢原子，得到氟尿嘧啶。由于氟尿嘧啶和尿嘧啶的化学结构非常相似，在代谢过程中能在分子水平代替正常代谢物尿嘧啶，抑制了胸腺嘧啶合成酶，从而干扰了DNA的合成，导致肿瘤细胞死亡。请您删除一下内容，O(_)O谢谢！2015年中央电大期末复习考试小抄大全，电大期末考试必备小抄，电大考试必过小抄Shanghais Suzhou Creek has witnessed much of the citys history. Zhou Wenting travels this storied body of water and finds its most fascinating spots. Some lucky cities can boast a great body of water, like London with the river Thames and Paris with the river Seine. Shanghai is privileged enough to have two great bodies of water: Huangpu River and Suzhou Creek.Huangpu River became famous when colonists established clusters of grand buildings on its banks on what became known as the bund. Today, the bund overlooks the breathtaking skyline of Lujiazui financial district. Shanghais other body of water, however, Suzhou Creek, has been somewhat overshadowed. Suzhou Creek links the inland cities of Jiangsu province with Shanghai. When the British colonists, who arrived in the city after it was opened as a commercial port in 1843 found they could reach Suzhou, Jiangsu province, via the creek, they named it Suzhou Creek. Thanks to its location, a large amount of cargo and travelers were transported via the creek before rail links were established. But after a century of being utilized as a waterway to transport goods and labor, the creek grew dark and smelly. Industrial factories were established along the banks. In the 1990s it became a key task of the city government to clean the creek. Suzhou Creek, which snakes 17 km from the iconic Waibaidu Bridge downtown to the outer ring road in west Shanghai, maps the changing periods of the citys history, including the imprints of the concessions, the beginning of industrialization and the improvement in peoples living conditions. Where the Bund began In-between the shopping street of East Nanjing Road and the Bund, are a cluster of streets that give me the illusion that I am no longer in modern Shanghai. The streets are narrow and old and criss-cross each other. Any old residential house may turn out to be a former office of the British, constructed in the 1880s. Pawnshops and hardware stores that are hard to find elsewhere, are plentiful here. This area, at the confluence of Huangpu River and Suzhou Creek, is called the Bund Origin. Countless tour buses stop at the site every day and visitors from around the world get off to see this place, the starting point of the concessions in the city. It all started in 1872, when the former British Consulate General was constructed and the Bund began its transformation into an the financial street of the East. Now the site of the former consulate is called “No 1 Waitanyuan”, which translates to “the Bund Origin”, to honor its beginnings. The entire complex of this historical site comprises of five buildings, the former British Consulate General, the official residence of the consul, the former Union Church, the church apartments and the former Shanghai Rowing Club. The size of the courtyard is equivalent to that of four standard soccer fields. The building of the former consulate is a two-storey masonry building on an H-shaped plan in typical English renaissancestyle. The building is designed with a five-arch verandah on the ground floor with a raised terrace facing the garden, while the facade features an entry portico beneath a colonnaded loggia. It has been turned into a caf where dinner and afternoonteaare available. Visitors can choose to sit indoors or outdoors to enjoy the magnificent gardens with nearly 30 ancient trees.Yuanmingyuan Road behind the complex is also a historical site. The road has been revamped as a pedestrian shopping street and high-end brands have seized the best spots. Altogether, 14 old buildings, including those used for offices and residences constructed during 1920s and 1930s, remain. Today, it is a popular location for commercialfashionphoto shoots. New Tianan Church, or Union Church, stands at the intersection of Yuanmingyuan Road and Suzhou Creek. The church, designed in the style of the English countryside, has a capacity of 500 people. It was very popular during the concession period but was converted into factory offices after 1949. The church we see today is a replica, the original burned down in 2007. There used to be an outdoor swimming pool, the first of its kind in Shanghai, beside the church but has been filled-in and is now a small garden. Bridge of romance There is perhaps no other place thats more representative of Shanghai than this bridge, which appears in quite a lot ofmovies about the city. Dozens of couples visit every day to pose for their pre-wedding photos on the bridge where Suzhou Creek begins and interconnects with Huangpu River. This is Waibaidu Bridge, or the Garden Bridge. The soon-to-be-wed couples pose in splendid attire on the bridge, leaning against the railing or sitting on the wooden floor. Some even risk walking into the middle of the road to get the perfect shot.Colorful lights illuminate the bridge throughout the night, making it a picturesque place for pre-wedding portraits and lovers to meet. Constructed in 1873 and designed by a British company, the 106-meter-long bridge was the first-ever major bridge in Shanghai. In 1856, the first large wooden bridge, Wells Bridge, was built over Suzhou Creek but the bridge toll led to complaints from citizens. So 17 years later, another wooden bridge, which did not require tolls, was built. People called it Waibaidu, which means “going across for free”. The bridge was renovated as a steel truss structure in 1907. Because nearly 40 bridges have now been built over Suzhou Creek, the bridge is no longer a traffic artery but is more of an observation deck for tourists. It is a tradition in Shanghai for a grandmother to walk across a bridge with their grandchild when he or she reaches one month. This represents that the newborn has overcome all the twists and turns and its journey will be safe and smooth throughout his or her life. Waibaidu Bridge is always the best option because its the icon of Shanghai. The picture of my daughter when she was a baby held by her grandmother was also taken here. Its like a family tradition, says Wang Xuefen, a Shanghai native who has a newborn grandson. Changning Riverside There is a 5-km stretch of waterfront by Suzhou Creek in Changning district on Changning Road from the intersection of Hami Road to Jiangsu Road. It has become a popular place to take a walk and sunbathe on the lawn. There is an overpass at the intersection of Changning Road and Gubei Road for people to enjoy the view of the creek and a 3-km plastic runway on both sides of Changning Road, which attracts people of all ages, Chinese and expat. Jogging on the two sides gives a different feeling because the north side is next to the creek, and the south side is adjacent to the residential highrises, which is like jogging in the jungle, says Xiao Xu, a 27-year-old woman who lives nearby. The riverside used to be completely different. Dozens of textile mills, chemical plants and machine manufacturing factories were set up along the creek in the 1920s. They brought industrialization but also pollution. From the 1930s the creek could no longer be used as a source for tap water, and no living fish or shrimp could be found. Suzhou Creek in my memory is dark and smelly. I used to go to the riverbank to watch the sewage disposal running out from the chemical plants when I was a little girl. We didnt know it was pollution. We thought it was a red waterfall, says Huang Qi, a 57-year-old Shanghai resident. So the residential houses along the creek were unpopular, and only migrants with low incomes would live in that area, she says. However, things have changed. The plants were closed and turned int