药理学英文作业及答案.docx

1、药理学英文作业及答案 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 i

2、n opposite 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 fo

3、r the plasma concentration of the drug to reach the steady state isa. 2 to 3b. 4 to 5c. 6 to 7d. 8 to 9e. 10 or more4. 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

4、concentrationc. 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. Deamination6. The grea

5、ter 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 stomach

6、?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 at high

7、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 the proce

8、ss requires cellular energye. The transport process can be inhibited noncompetitively by substances that interfere with cellular metabolism8. Which of the following is unlikely to be associated with oral drug administration of an enteric-coated dosage form?a Irritation to the gastric mucosa with nau

9、sea 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 to the tyrosi

10、ne 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 concentration7、Pharmacokin

11、etics8、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、tolerance22、ta

12、chyphylaxis1. 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 is the hepatic microsomal e

13、nzymes? 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 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

14、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

15、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（=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

16、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

17、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

18、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，而非竞争性拮抗剂不行。 Autonomic Nervous System1.Compare the Pharmacology of physostigmine and neostigmine.2.Compare ocular effects of pilocarpine, physostigmine, atropine and phenyle

19、phrine.3.Compare the Pharmacology of Noradrenaline, adrenaline, and isoprenaline?4.List the indications and the contraindications 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 lo

20、cations, and physiologic response to activation.1. The drug of choice for the treatment of anaphylactic shock is:(A) histamine(B) epinephrine(C) norepinephrine(D) isoproterenol(E) diphenhydramine2. Phentolamine often causes an increase in heart rate and in the force of contraction by which of the fo

21、llowing mechanisms:(A) Directly stimulating cardiac b1 receptors(B) Antagonizing the vagal transmitter(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 calciumavailab

22、le to the heart3、If a drugs half-life is 10h，when it is repeatedly administered at dosing 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 40hC、40 to 50h D、60h or more 4、 At small dose, atropine effects on secretions are ( )

23、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 reduced5、抢救心跳骤停的药物是：（ ）A、adrenaline B、noradrenaline C、isoprenaline D、digoxin 6、The drug of choice for the t

24、reatment of allergic shock is( )A、isoprenaline B、Adrenaline C、Atropine D、Noradrenaline7、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

25、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

26、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，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

27、肪的分解起调节作用。1：B 2：D 3：C 4：A 5：A 6：B7：D Cardiovascular SystemDry cough is acommon, annoying side effect to the use of which of the following drugs? （ ）A. Angiotensin-converting enzyme inhibitors B.calcium channel-blockersC. - blockersD. M- blockers22 Which of the following drug is the first choice for

28、hypertensive crisis （）A. clonidineB. sodium nitroprusside 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

29、 and preventing ischemic episodes in patients with variant angina? （）A. propranololB. diltiazemC. nifedipineD. verapamil 55A drug that decreases blood pressure by a CNS action is （）A. captoprilB. PropranololC. nitroprusside sodiumD. Clonidine66.Which of the following is unlikely to occur with nitrog

30、lycerin? （ ）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 found to be detrimental in patients with: （ ）A. bronchial asth

31、maB. hypertensionC. hyperthyroidismD. atrial fibrillation 88Which of following antihypertensive drug is AT1 antagonist:（ ）A. captopril B. nifedipineC.losartanD. thiazides 99Verapamil 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 channel10The drugs could be used for treatment of CHF (congestive heart failure) ( )a digoxin bhydrochlorothiazide ccaptopril dall of a