药理学英文作业及答案

1、 药理学作业 -周师兄General principles1. Which route of administration is most likely to subject a drug to a first-pass effect?a. Intravenousb. Inhalationalc. Orald. Sublingual (SL)e. Intramuscular2. Two drugs may act on the same tissue or organ through independent receptors, resulting in effects in opposite

2、 directions. This is known asa. Physiologic antagonismb. Chemical antagonismc. Competitive antagonismd. Irreversible antagonisme. Dispositional antagonism3. If a drug is repeatedly administered at dosing intervals that are equal to its elimination half-life, the number of doses required for the plas

3、ma concentration of the drug to reach the steady state isa. 2 to 3b. 4 to 5c. 6 to 7d. 8 to 9e. 10 or more 4. The pharmacokinetic value that most reliably reflects the amount of drug reaching the target tissue after oral administration is thea. Peak blood concentrationb. Time to peak blood conc

4、entrationc. Product of the Vd and the first-order rate constantd. Vde. Area under the blood concentration-time curve (AUC)5. Of the following, which is a phase II biotransformation reaction?a. Sulfoxide formationb. Nitro reductionc. Ester hydrolysisd. Sulfate conjugatione. Deamination 6. The gr

5、eater proportion of the dose of a drug administered orally will be absorbed in the small intestine. However, on the assumption that passive transport of the nonionized form of a drug determines its rate of absorption, which of the following compounds will be absorbed to the least extent in the stoma

6、ch?a. Ampicillin (pKa = 2.5)b. Aspirin (pKa= 3.0)c. Warfarin (pKa = 5.0)d. Phenobarbital (pKa = 7.4)e. Propranolol (pKa = 9.4) 7. Of the following characteristics, which is unlikely to be associated with the process of facilitated diffusion of drugs?a. The transport mechanism becomes saturated

7、at high drug concentrationsb. The process is selective for certain ionic or structural configurations of the drugc. If two compounds are transported by the same mechanism, one will competitively inhibit the transport of the otherd. The drug crosses the membrane against a concentration gradient and t

8、he process requires cellular energye. The transport process can be inhibited noncompetitively by substances that interfere with cellular metabolism 8. Which of the following is unlikely to be associated with oral drug administration of an enteric-coated dosage form?a Irritation to the gastric m

9、ucosa with nausea and vomitingb Destruction of the drug by gastric acid or digestive enzymesc. Unpleasant taste of the drugd. Formation of nonabsorbable drug-food complexese. Variability in absorption caused by fluctuations in gastric emptying time9. Which of the following is classified as belonging

10、 to the tyrosine kinase family of receptors?a. GABA -A receptorb. -adrenergic receptorc. Insulin receptord. Nicotinic II receptore. Hydrocortisone receptor2.Explanation of terms1、Bioavailability2、Hepatoenteral circulation3、Half-life time4、50% lethal dose5、Absorption6、Ateady state plasma concentratio

11、n7、Pharmacokinetics8、Pharmacodynamics9、adverse effect10、antagonist11、potency12、symptomatic treatment13、therapeutic index14、first-pass effect(elimination)15、enzyme inhibitor16、etiological treatment17、median effective dose18、side effects19、dose- effect relationship20、structure activity relationship21、

12、tolerance22、tachyphylaxis 1. Describe factors affecting absorption of drug.2. Describe receptor characters.3. Which is the most common process for drug transfer across cell membranes and point out its characteristics.4. List the characteristics of plasma protein binding of drugs. 5. What i

13、s the hepatic microsomal enzymes? List their main characteristics.6. What is the difference between the action and the effect of a drug?7. Use receptor-action theory to elucidate what is the difference between the competitive antagonist and the non-competitive antagonist. 1.c   

14、2c.    3b   4e   5d    6e    7d   8d   9c    1生物利用度：是药物活性成分从制剂释放吸收进入血液循环的程度和速度。2肝肠循环：指由肝脏排泄的药物，随胆汁进入肠道再吸收而重新经肝脏进入全身循环的过程。3半衰期：是指血浆消除t1/2,是指血浆药物浓度降低一半所需的时间。4半数致死量：表示在规定时间内，通过指定感染途径，使一定体重或年龄的某种动物半数死亡所需最

15、小细菌数或毒素量。5吸收：机体从环境中吸收营养物质到体内的过程。6稳定血药浓度：在给药间隔内消除的药量等于给药剂量，从而达到平衡是的血药浓度。7药物代谢动力学；主要是定量研究药物在生物体内的过程（吸收、分布、代谢和排泄），并运用数学原理和方法阐述药物在机体内的动态规律的一门学科。8药物效应动力学；主要研究药物对机体的作用、作用规律及作用机制，其内容包括药物与作用靶位之间相互作用所引起的生物化学、生理学和形态学变化，药物作用的全过程和分子机制。9不良反应；是指按正常用法、用量应用药物预防、诊断或治疗疾病过程中，发生与治疗目的无关的有害反应。10拮抗药；能与受体结合，具有较强的亲和力而无内在活性（

16、=0）的药物。11效价强度；用于作用性质相同的药物之间的等效计量的比较，是指能引起等效反应（一般采用50%效应量）的相对浓度或剂量。12对症治疗；用药物改善疾病症状。13治疗指数；通常将半数致死量（LD50）半数有效量（ED50）的比值称为治疗指数，用以表示药物的安全性。14首过效应；从胃肠道吸收入门静脉系统的药物在到达全身血循环前必先通过肝脏，如果肝脏对其代谢能力很强，或由胆汁排泄的量大，则使进入全身血循环的有效药物量明显减少，这种作用称为首过消除。15酶抑制剂；是一类可以结和酶并降低其活性的分子。16对因治疗；针对病因进行治疗。17半数有效量；在量反应中是指能引起50%最大反应强度的药物剂

17、量；在质反应中只引起50%实验动物出现阳性反应的药物剂量。18副反应；应用治疗量药物后出现的与治疗无关的反应。19量效关系；在一定的范围内，药物的效应与靶部位的浓度成正相关，而后者决定于用药剂量或血中药物浓度，定量地分析与阐明两者间的变化规律称为量效关系。20构效关系；药物的化学结构与药物效应的关系。21耐药性；是病原体或肿瘤细胞对反复应用的化学治疗药物的敏感性降低。也称抗药性。22快速耐受性；有些药物在短时间内重复给予而使机体反应减弱，最后虽然剂量加得很大也不能得到原来的反应。药物的此种现象称为药物的快速耐受或急性耐受，这种特性叫快速耐受性。1因素有；药物的理化性质、给药途径、制剂因素等。2

18、特性有；灵敏性、特异性、饱和性、可逆性、高亲和力等。3最常见的是简单扩散，特点有；不需要能量、不需要载体、无饱和现象、无竞争性抑制等。4特性有；饱和性、竞争性抑制、疾病对药物与血浆蛋白结合的影响。5肝微粒体酶即肝脏微粒体细胞色素p450酶系统，该系统主要酶为细胞色素p450，由于该酶能促进数百种药物的代谢，又称肝药酶。特性有；选择性低、变异性大。6区别为；药物作用是药物对机体组织发挥的原发作用，而药物效应是药物原发作用引起的机体器官组织能够被观察、记录、测定到的功能、代谢等的变化。7区别为；竞争性拮抗剂的效应给药被增加激动剂浓度所对抗，而非竞争性拮抗剂不行。竞争性拮抗剂可以提高ED50值，而非

19、竞争性拮抗剂不行。 Autonomic Nervous System 1.Compare the Pharmacology of physostigmine and neostigmine.2.Compare ocular effects of pilocarpine, physostigmine, atropine and phenylephrine.3.Compare the Pharmacology of Noradrenaline, adrenaline, and isoprenaline?4.List the indications and the contraindica

20、tions of propranolol?5. List the steps in the synthesis, storage, release and inactivation of acetylcholine。6. Describe the types and subtypes of adrenergic receptors, their locations, and physiologic response to activation. 1. The drug of choice for the treatment of anaphylactic shock is:(A) h

21、istamine (B) epinephrine (C) norepinephrine (D) isoproterenol(E) diphenhydramine 2. Phentolamine often causes an increase in heart rate and in the force of contraction by which of the following mechanisms:(A) Directly stimulating cardiac b1 receptors(B) Antagonizing the vagal tra

22、nsmitter(C) Releasing histamine from mast cells, which stimulates the heart(D) Blocking peripheral vasoconstriction, which produces reflex stimulation of the heart(E) Increasing the amount of calciumavailable to the heart 3、If a drugs half-life is 10h，when it is repeatedly administered at dosin

23、g intervals that are equal to its t1/2, the time of the drug to reach the steady state concentration is （）  A、20 to 30h         B、30 to 40h     C、40 to 50h    D、60h or more       4、 At

24、small dose, atropine effects on secretions are (   )A. sweat and salivary gland secretions are greatly reduced. B. intestinal gland secretions are greatly reduced.C. bronchial secretions are greatly reduced D. gastric acid secretion are greatly reduced 5、抢救心跳骤停的药物是：（    

25、; ）A、adrenaline      B、noradrenaline       C、isoprenaline    D、digoxin       6、The drug of choice for the treatment of allergic shock is(   )A、isoprenaline      B、Ad

26、renaline   C、Atropine     D、Noradrenaline  7、伴尿量减少的中毒性休克最好用（   ） A、isoprenaline   B、noradrenaline   C、adrenaline   D、 dopamine     1:毒扁豆碱作用与新斯的明相似，但无直接激动受体作用。其结构为叔胺类化合物，可进入中枢。眼内局部应用时，其作用类似于毛

27、果芸香碱，但较强而持久，表现为瞳孔缩小，眼内压下降。吸收后外周作用与新斯的明相似，表现为M、N胆碱受体激动作用，进人中枢后亦可抑制中枢 AChE活性而产生作用。中枢作用较强，可作为中药麻醉时的催醒药。现主要局部滴眼用于治疗青光眼，作用较毛果芸香碱强而持久，但刺激性大。2:毛果芸香碱、毒扁豆碱：缩瞳、降低眼内压、调节痉挛。阿托品、苯肾上腺素：扩瞳、升高眼内压、调节麻痹。毒扁豆碱。3肾上腺素是、受体激动药，药理作用变现为兴奋心血管系统、抑制支气管平滑肌和促进新陈代谢；而去甲肾上腺素是1、2受体激动剂，它对冠状血管产生舒张作用，对其它血管产生收缩作用，可使心率减慢，小剂量可使脉压加大，大剂量可使脉压

28、减小；异丙肾上腺素是1、2受体激动剂，可使心率加快，心收缩力增强，可使血管舒张，骨骼肌舒张，可松弛支气管平滑肌。4：适应症：高血压、心绞痛、心率失常；禁忌症：心功能不全、窦性心率过缓、房室传导延搁、支气管哮喘、肝功能不全。5:a生物合成：胆碱和乙酰辅酶A在胆碱乙酰化酶催化下，合成ACh。b释放：胞裂外排。c消除：被乙酰胆碱酯酶水解。6：1受体：主要分布于血管平滑肌、瞳孔开大肌、心脏和肝脏，激活后产生缩瞳、血管平滑肌收缩等；2受体：主要存在于去甲肾上腺能及胆碱能神经末梢的突触前膜，也存在于肝细胞、血小板、脂肪细胞、血管平滑肌上，激活后可产生血管平滑肌收缩等；1受体：主要分布于心脏、肾小球旁细胞，

29、激活后可使心脏产生正性变化；2受体：主要分布于支气管平滑肌、骨骼肌、和肝脏，激活后可使支气管平滑肌舒张、骨骼肌舒张；3受体：主要分布于脂肪细胞、心脏，激活后可对脂肪的分解起调节作用。1：B    2：D   3：C   4：A   5：A   6：B    7：D Cardiovascular System Dry cough  is a common, annoying side effect to the use

30、 of which of the following drugs? （  ）A. Angiotensin-converting enzyme inhibitors    B.calcium channel-blockers C. - blockers  D. M- blockers22 Which of the following drug is the first choice for hypertensive crisis （ ）A. clonidine B. sodium nitroprusside

31、 C. -receptor blocker D .thiazides diuretics  33Adverse reaction of ACEI include all of the following EXCEPT A. hypotension   B. cough   C. hyperkaliemia   D. hypokaliemia 44Which of the following drugs is considered to be most effective in relieving and preventing

32、 ischemic episodes in patients with variant angina? （ ）A. propranolol B. diltiazem C. nifedipine D. verapamil 55A drug that decreases blood pressure by a CNS action is （ ）A. captopril B. Propranolol C. nitroprusside sodium D. Clonidine66.Which of the following

33、 is unlikely to occur with nitroglycerin? （  ）A. Decreased heart rate    B. Decreased end-diastolic blood pressure C. Decreased myocardial oxygen demand  D. Decreased preload and afterload 77Propranolol is a potent blocker of beta-adrenergic sympathetic activity. It has been

34、 found to be detrimental in patients with: （  ）A. bronchial asthma B. hypertension C. hyperthyroidism D. atrial fibrillation 88Which of following antihypertensive drug is AT1 antagonist:（  ）A. captopril   B. nifedipine C. losartan D. thiazides 99Vera

35、pamil exerts its effects through which of the following actions? （  ）A. Preventing entry of calcium through slow channels B. Enhancing potassium effluxC. Increasing sodium entry D.Antagonizing the opening of the fast sodium channel 10The drugs could be used for treatment of CHF (congestive

36、 heart failure) (  )a  digoxin  b hydrochlorothiazide   c captopril   d all of a, b and c  Questions1.What is the signs of cardiac glycosides intoxication and how to prevent or treatment?2.List the pharmacological actions and indications of the

37、cardiac glycosides.3.List the mechanism and indications of antiangina agents including nitroglycerin, propranolol and calcium channel blocker.4.Describe the pharmacological basis of treating angina pectoris in combination of nitroglycerin and propranolol.5. Classify the drugs for antihypertention an

38、d give examples.6.List the mechanism and indications of ACEI and lorsartan. 1.A   2.B  3.D  4.C  5.D  6.A  7.A  8.C  9.A  10.D  1:中毒症状有：胃肠道反应：厌食、恶心、呕吐、腹泻等；中枢神经系统：眩晕、头痛、疲倦、失眠、视觉障碍等；心脏反应：各种心律失常症状。防治：若出现症状，应及时减量或停用强心苷和排钾利尿药。快速型心律失常，应及时补钾，对重症快速

39、性心律失常，用苯妥英钠救治；利多卡因可用来治疗强心苷引起的严重室性心动过速和心室纤颤，对于房室传导阻隔、窦性心动过缓、窦性停博，可用阿托品经脉注射治疗。2：强心苷药理作用：正性肌力作用、减慢心率作用、对心脏的负性传导作用；适应症：慢性心功能不全：对心瓣膜病、先天性心脏病、动脉粥样硬化及高血压引起的心力衰竭效果良好，对伴有心房颤动或心室率过快者疗效最好；某些心率失常如：心房纤颤、心房普动、阵发性室上性心动过速。3：硝酸甘油的基本药理作用为松弛平滑肌，能降低心脏前后负荷，降低心肌耗氧量，改变冠脉血液分布，增加缺血区血液灌注；可用与缓解各种类型心绞痛症状或预防心绞痛的发作，如：心绞痛、急性心肌梗死、

40、慢性心力衰竭及用于控制血压。普萘洛尔可以降低心肌耗氧量、改善心肌缺血区供血，可用于治疗心绞痛及心肌梗死。4.因为这2种药物可以取长补短，硝酸甘油的优点是：降低心室壁张力、心室容积及心室压力，缺点是：升高心率和心肌收缩力；普萘洛尔的优点是：降低心率及心肌收缩力，缺点是：心室容积增大。5：1肾素-血管紧张素系统抑制药：ACEI：卡托普利；AT1受体阻断药;氯沙坦；2Ca+通道阻滞药：硝苯地平；3：利尿药：氢氯噻嗪；4交感神经抑制药：中枢性降压药：可乐定；神经节阻断药：美加明；去甲肾上腺素能神经末梢阻断药：利血平；肾上腺素首体阻断药：哌唑嗪、普萘洛尔及拉贝罗尔；5血管扩张药：直接扩血管药：硝普钠；钾

41、通道开放药：二氮嗪。6：作用机制：抑制循环及局部组织的ACE、减少缓激肽的降解、抑制交感神经递质的释放、自由基清除作用，可用于治疗高血压、慢性心功能衰竭、治疗急性心肌梗死与预防心脑血管意外、治疗糖尿病性肾病及其他肾病；氯沙坦对AT1受体有选择性阻断作用，可用于高血压的治疗。Central Nervous System The use of morphine is contraindicated in(A) myocardial infarction   (B) acute pulmonary edema   (C) simple diarrhe

42、a(D) kidney colic            (E) bronchial asthma 2. Effects of phenothiazines include all the following EXCEPT(A) orthostatic hypotension, constipation, and urinary retention(B) Parkinson-like syndrome (C) hypoprolactinemia 

43、  (D) antiemesis(E) control of psychotic behavior 3. Akathisia, Parkinson-like syndrome, galactorrhea, and amenorrhea are side effects of perphenazine, caused bya. Blockade of muscarinic receptorsb. Blockade of -adrenergic receptorsc. Blockade of dopamine receptorsd. Supersensitivity of do

44、pamine receptorse. Stimulation of nicotinic receptors4. The pharmacologic effects of morphine include all EXCEPT:a. behavioral changesb. miosisc. respiratory depressiond. diarrheae. postural hypotension Questions1.What is the mechanism of central actions of benzodiazepines?2.How do chlorpromazi

45、ne compare with aspirin in reducing hyperthermia?3.How do pethidine compare with aspirin in analgesic actions?4.What is the site and mechanism of antipsychotic actions of chlorpromazine?5.List the CNS actions and main adverse reactions of chlorpromazine?6.List the CNS actions, mechanism and indicati

46、ons of morphine.7.How dose aspirin influence blood clotting?8.What is the relationship between dose and pharmacology of aspirin?9.What is the untoward effects of aspirin and how to prevent it?10. Describe how barbiturates affect CNS function and the differences between barbiturates and benzodiazepin

47、es. 1:E  2:C  3:C  4:D    1:苯二氮卓类作用机制为：它通过增加GABA控制的Cl-通道的开放频率，使得神经细胞超极化，产生突触后抑制效应，从而加强对突触的抑制作用。2：阿司匹林的降温作用是因为它抑制了下丘脑COX，阻断了PGE2合成，使体温调节中枢的体温调定点恢复正常，与环境温度无关，只对发热病人有影响；而氯丙嗪降温作用是因为它抑制了下丘脑体温调节中枢，使体温调节失灵，与环境温度有关，它也可降低正常人的体温。3：哌替啶的镇痛作用是它可以激动阿片受体，从而镇痛作用；而阿司匹林是通过抑制外周病变部位的C

48、OX，使PGs合成减少而减轻疼痛。4：作用部位大脑的中脑-边缘系统和中脑-皮质系统，作用机制为氯丙嗪可以阻断这2个系统的D2样受体。5.中枢神经系统作用有：抗精神病作用、镇吐作用、对体温调节作用、加强中枢抑制药作用；主要不良反应有嗜睡、困倦、无力等中枢抑制作用，还有视力模糊、心动过速、口干、便秘等阿托品样作用，还有药源性帕金森综合症、静坐不能、急性肌张力障碍、迟发性运动障碍、过敏反应等。6：中枢神经系统作用为镇痛和镇静、抑制呼吸、镇咳、催吐、缩瞳、对体温的影响等；机制为通过激动阿片受体；适应症为剧烈疼痛、心源性哮喘、腹泻等。7：小剂量阿司匹林可以不可逆地抑制血小板的COX，由于成熟血小板不再合

49、成新的COX，所以受小屋影响的血小板永久性地丧失了合成TXA2的能力，而TXA2是诱发血小板聚集和血栓形成的重要内源性物质。8：小剂量阿司匹林可以不可逆地抑制血小板的COX，所以受小屋影响的血小板永久性地丧失了合成TXA2的能力，这是阿司匹林抗血栓形成机制；而大剂量也同时血管内皮细胞合成PGI2，从而促进血小板和血栓形成。9：胃肠道反应：应餐后服用、出血及凝血障碍：使用维生素K预防及手术前一周停用阿司匹林、水杨酸反应：一旦出现立即停药，加服或静脉滴注碳酸氢钠、瑞夷综合症：病毒感染时慎用阿司匹林、阿司匹林哮喘：用肾上腺素可部分对抗。10：巴比妥类药物对中枢神经作用为:它可以激动GABAA受体，增

50、加Cl-内流的时间，而苯二氮卓类作用机制为：它通过增加GABA控制的Cl-通道的开放频率，使得神经细胞超极化，产生突触后抑制效应，从而加强对突触的抑制作用。 Glucocorticoids 1.Glucocorticoids can be used for relief of the severe inflammatory symptoms caused by severe septic diseases. In that case, glucocorticoids must be used with        . 2.

51、List the mechanism and indications of glycocorticoids.3.To a patient suffered from Addisons disease, how and why a doctor use the glycocorticoids. 4.List the effects of glycocorticoids on blood cell components.1.足量有效抗菌药物。2。作用机制：这类药物大部分效应系糖皮质激素受体介导的基因效应，即与细胞内GR结合，通过启动基因转录或抑制基因转录，促进合成某些特异性蛋白质，或抑制某些特异性

52、蛋白质的合成，从而产生药理效应。适应证：严重感染或预防炎症后遗症、自身免疫病、器官移植排异反应、过敏性疾病、抗休克治疗、替代疗法、局部应用、血液病。3.因为病人患有这一疾病，肾上腺皮质功能减退，导致糖皮质激素分泌不足，故需要糖皮质激素来治疗，这是一种替代疗法。补充可维持正常神力功能的生理剂量的糖皮质激素即可。4.糖皮质激素可以降低外周血单核细胞、淋巴细胞、嗜酸性和嗜碱性粒细胞，可使红细胞和血红蛋白含量增加。大剂量可使血小板和纤维蛋白原增加、中性粒细胞数增多。 Chemotherapy The most active aminoglycoside against Mycobacteri

53、um tuberculosis is（  ）A. Streptomycin B. Amikacin   C. Neomycin   D. Kanamycin   2 The use of chloramphenicol may result in（  ）A. Bone marrow stimulation B. Phototoxicity C. Aplastic anemia D. Staining of teeth    3characteri

54、stics of the third-generation cephalosporins EXCEPT （ ）A .broad-spectrum of activity   B .easy permeation the blood-brain barrier C. activity to gram-positivegram-negative D. little renal toxicity    4 An inhibitor of DNA-dependent RNA polymerase, useful in tuberculosis

55、, is （ ）A. isoniazid    B. streptomycin   C. rifampin.   D. penicillin.    5Ototoxicity is a rare but serious manifestation of A. hydrochlorothiazide B. ethacrynic acid C. spironolactone D. triamterene    6Adverse effects resultin