2005英护本科药理学双语教学作业

2005 英护本科药理学双语教学作业Translation for English Nursing Department承德医学院药理教研室Department of PharmacologyChengde Medical CollegeJune 2007EditorWang Rui-TingAssociate professorAuthorsHaoXi-Jun郝希俊ProfessorTongJi-Ming佟继铭ProfessorShangYa-Zhen商亚珍ProfessorWangRui-Ting王瑞婷Associate professorMeiAi-Min梅爱敏Associate professorLiBao-Qun李宝群LecturerZuoYan-Zhen左彦珍AssistantYangYu-Jie杨宇杰Associate professorGuanLi-Hua关丽华AssistantCONCENTSChapter 1 Introduction . 1Chapter 2 Pharmacodynamics 2Chapter 3 Pharmacokinetics 3Chapter 4 Autonomic Pharmacology .4Chapter 5 Cholinoceptor-activating and AchE inhibitor.5Chapter 6 Organophosphates Anticholinesterase Intoxication 6Chapter 7 Anticholinergic Drugs (M antagonist) . 7Chapter 8 Adrenergic Drugs 8Chapter 9 Adrenoceptor Blocking Drugs .10Chapter 10 Sedative-Hypnotics .11Chapter 11 Antiepileptic Drugs .12Chapter 12 Antipsychotic Drugs .13Chapter 13 Analgesics .15Chapter 14 Antipyretic-Analgesia and Anti-inflammatory. 16Chapter 15 Renin- Angiotensin System.17Chapter 16 Anti- Arrhythmia Agents 1819Chapter 17 Diuretics and Osmotic DiureticsChapter 18 Anti-hypertensive Drugs 20Chapter 佃 Drugs for Congestive Heart Failure 21Chapter 20 Anti-Angina Pectoris Drugs 22Chapter 21 Drugs Acting on the Blood and Blood Forming Organ23Chapter 22 Histamine-Receptor Antagonist24Chapter 23 Drugs Acting on Respiratory System 25Chapter 24 Drugs Acting on Digestive Systetmtttt tt t 26Chapter 25 Adrenocortical Hormones .27 29Chapter 26 Agents Affecting the Thyroid Gland28Chapter 27 Antidiabetic drugsChapter 1 General Principles of Pharmacology- Introduction1 Pharmacology deals with the chemical and physical properties, action, mechanism of action, biotransformation , side effects, clinical uses and contraindications of drugs.2 Pharmacodynamicsis the study of the biochemical and physiological effects of drugs and their mechanism of action.3 Pharmacokinetics deals with the changes of drug concentration in the human body following administration.4 Drugs are substances used for the purposes of prevention, diagnosis and treatment of disease.Pharmacology biotransformation Pharmacodynamics Pharmacokinetics Physiology 病理学5 The basic medical knowledge, such as physiology, biochemistry, pathology, pathophysiology, microbiology, immunology and molecular biology are applied to elucidate the mechanisms of drugsaction , and to establish the theoretical basis of using drugs rationally in clinic. 药理学 生物转化 药效学 药代学 生理学 pathology Elucidate .阐明1Chapter 2 Pharmacodynamics1 Treatment can be classified into etiological and symptomatic treatment according to therapeutic effect.2 Adverse effect includes side effect, toxic effect, residual effect, withdrawal reaction, allergic reaction, idiocyncrasy.3 pharmacological effect can be classified into graded response and quantal response according to effect property.4 efficacy: the maximum effect of a drugs, it is related to intrinsic activity. Intrinsic activity is the ability of a drug to produce an effect.5 potency: refers to the different doses of two drugs that are needed to produce the same degree of effect. It is related to affinity. Affinity is the tendency of a drug to combine with the receptor.6.ED50:the dose at which 50% of the individuals exhibit the specified quantal effect.7 LD 50:the dose at which 50% of the animal exhibit death. Therapeutic index(TI)=LD 50/ED508 Agonist: is a drug that has high affinity to receptor and high intrinsic activity, produces a pharmacological effect when it combines with receptor.9 An antagonist binds to the receptor to inhibit the action of an agonist, but initiate no effect themselves. The inhibition can be overcome by increasing the concentration of the agonist, ultimately achieving the same maximal effect.10 receptor can be classified into four types: G protein-coupled receptor, ligand-gated ion channel, tyrosine-protein kinase receptor, intracellular receptor.11 Affinity: the tendency of a drug to form a combination with the receptors.12 intrinsic activity:its inherent ability to produce an effect.13 competitive antagonist: competitive antagonists compete with agonists in a reversible fashion for the same receptor site . When the antagonist is present, the log dose-responsecurve is shifted to the right but the maximal response of the agonist is unchangeble when increasing concentration of a agonist enoughly.etiological 病 因 的 symptomatic adverse 不利的 efficacy 效能residual 残 留的withdrawal 停药intrinsic 内 在的potency 效价强度affinity 亲和力agonist激动剂antagonist 拮抗剂tyrosine酪氨酸allergic 过敏的reversible l 可逆的2Chapter 3Pharmacokinetics1 Pathways that drugs transporting across membrane include passive diffusion, active transport, carrier-mediated facilitated diffusion, endocytosis .2 intracorporeal process of drug includes absorption, distribution, metabolism,excretion. Absorption is the process that drug enters blood from the administration site.3 first- pass elimination: following absorption from the gastrointestinal tract, drugs pass initially through the hepatic circulation. Some drugs are metabolized so extensively in the gut wall or liver before they reach the systemic circulation.4 bioavailability: it is defined as the fraction of unchanged drug reaching the systemic circulation following administration by any route, it is related to the area under the plasma concentration-time curve.5 drug metabolism invo Ives two kinds of biochemical reacti ons known as phase I and phase n reacti ons. Phase I react ion con sists of oxidatio n, reduct ion or hydrolysis. Phase n react ion invo Ives conjugatio n, acetylati on and methylati on.6 enzyme inducer and enzyme inhibitor7 first order kinetics: constant fraction of drug is eliminated per unit time.Zero order kinetics: same quantity of drug is eliminated per unit time.8 half life: the time taken for the concentration of drug to fall to half of the initial value.9 Apparent volume of distribution: a hypothetical volume of body fluid that would be required to dissolve the total amount of drug at the same concentration as that found in the blood.10 steady state: may be defined as a time of no net change in the amount of drug when rate of input equals rate of output.11 clearance :is defined as the volume of plasma which would have to lose all the drug it contains per unit time.endocytosisintracorporeal体内的oxidation 氧化reduction 还原hydrolysis 水解conjugation 结合acetylation乙酰化methylation 甲基化hepatic 肝的3Chapter 4 Autonomic Pharmacology1 cholinergic fibers include :(1) all (parasympathetic and sympathetic) preganglionic efferent autonomic fibers and somatic motor fibers to skeletal muscle.(2) all parasympathetic postganglionic fibers(3) a few sympathetic postganglionic fibers, the fibers innervate to sweat gland and skeletal muscle vascular dilating nerves(4) the nerve innervate to adrenal medulla2 adrenergic fibers: most of the sympathetic postganglionic fibers3 coupling mechanism of receptor-effectB receptor combines with G, Gs, activates AC, cAMP activates protein kinase which activates phosphoslation.a 2 receptor combines with G and inhibits AC activity , decreases cAMP.a 1 receptor couples with GP, activates PLC.4 M effectHeart:rate J cardiac contractility J conduction JBlood vessel: dilatio n, blood pressure/Eye: pupil constriction, intraocular pressureJ ciliary muscle constrictionSalivary gland: secretionViscera: bron chi con stricti on, gastr oin testi nal moveme nt T5 adrenergic effectHeart:B 1 rateT contractility T conductionT BpTBlood vessel:Coronary: a 1, a 2 constriction, B 2 dilationMuscleB 2 dilationVeins:a 1, a 2 constriction, B 2 dilationViscera: bronchi B 2 dilationEye: a 1 pupil dilatation , autonomic自主的Cholinergic 骨骼的Preganglionic 节 前 的 传出的parasympathetic 副 交 感 的 神经支配intraocular 眼 内 的睫状的salivaryi 唾液viscera 脏gastrointestinal 胃肠的skeletal efferent innervate ciliary 内4Chapter 5 Cholinoceptor-activating andCholinesterase -Inhibiting Drugs1 M-cholinoceptor agonists pilocarpinepharmacological effects:Eye: miosis, papillary constrictor muscledecrease intraocular pressurecyclospasm(spasm of accommodation), contraction of ciliary muscleGlands：increase secretion of sweat gland and salivary glandUses: glaucoma, iritis(prevent iris to lens)2 cholinesterase inhibitorscholinesterases divides into acetylcholinesterase(AchE) and pseudocholinesterose. The former is highly concentrated at neuromuscular junction, the later is present primarily in plasma and liver. Cholinesterase inhibitor will express M and N-cholinergic effects.3 Neostigmine(reversible)pharmacologic effects: cholinesterase inhibitor effect and direct activating N2 receptor clinical use: myasthenia gravispostoperative ileus and urinary retention: neostigmine excites GI tract smooth muscle and bladder detrusorparoxysmal supraventricular tachycardia: decrease heart rate.Overdosage of muscle relaxants: tubocurarine, but prohibit to use for succinylcholine intoxication.Side effects: nausea, vomiting, abdominal pain, tachycardia, fibrillation of muscle fibers, cholinergic crisis.Contraindications: mechanical intestinal obstruction, urinary obstruction, bronchialasthmamiosis 瞳 孔 缩 小 papillary 乳突的glaucoma 青 光 眼 iritis ciliary睫状的myasthenia gravis ileus 肠梗阻 哮喘 retention 渚留supraventricular 室上性 tubocurarine Contraindications 禁忌症 succinylcholine obstruction paroxysmal urinary detrusor tachycardia梗阻阵发性cyclospasm 调 节 痉 挛 虹 膜炎 重症肌无力 尿液的 asthma 逼尿肌 心动过速 筒 箭 毒 碱琥珀酰胆碱的 pilocarpine 毛 果芸 香碱Chapter 6 OrganophosphatesAnticholinesterase Intoxication and Cholinesterase Reactivators1 mechanism of intoxication: organophosphates combine with cholinesterase to form complex, then “aged”phosphorylated cholinesterase.2 acute intoxicationM signs and symptoms: miosis, salivation, increase bronchial secretion, sweating, bronchoconstriction, vomiting, diarrhea, bradycardia, hypotention.N actions: involuntary twitchings3 treatment of acute intoxication: atropine antagonize M symptoms. Cholinesterase re-activator(pyraloxime methoiodide, PAM; prelidoxime chloride, PAM-CL) is capable of regenerate active enzyme from the organophosphorus-cholinesterase complex and also antagonize the twitching.diarrhea 腹泻 twitchings 颤搐6 Chapter 7 Anticholinergic Drugs (M antagonist) Anticholinergic drugs can combine with cholinergic receptors and inhibit Ach or cholinergic drugs to combine with the receptors. They are divided into M-cholinoceptor blocking drugs and N-cholinoceptor blocking drugs.M -eceptor antagonist:atropinnon selectively Mreceptor antagonist1 pharmacological effects:Glands: inhibit the secretion of salivary gland, sweat gland and bronchial secretory. Eye: pupil dilation, increase intraocular pressure, cycloplegiaSmooth muscle: relaxation of viseral smooth muscle, stomach and intestine , bladder detrusor and urinary tract smooth muscle and weak effect on biliary tract and uterus.Cardiaovascular system : increase HR, dilate blood vessel , Bp decrease and improve microcirculation.CNS: stimulating effect.2 clinical uses:visceral colic: gastric and intestinal colic pain and bladder irritating symptoms. Combined with pethidine for treatment of gallbladder colic and renal colic pain preanaesthetic medication ， ophthalmologic disorders , bradycardia anti-shock especially for infectious shock. Organophosphate intoxication.salivary 唾液的intestine 肠cycloplegia 调节麻痹detrusor 逼尿肌colic 绞 痛urinary 尿 的biliary胆汁的gallbladder 胆囊ophthalmologic眼科的preanaesthetic medication 麻醉前给药pethidine 度冷丁uterus子宫bradycardia 心动过缓 visceral内脏的Chapter 8 Adrenergic DrugsAdrenergic drugs are a group of drugs, which have similar chemical structures and pharmacological actions. They may combine with and activate adrenoceptors and produce adrenomimetic effects, they are called adrenomimetic drugs. These drugs are amines, their effects are similar to that of exciting sympathetic nerves, thus they are also called sympathomimetic drugs.1 mixed a and B agonists: adrenaline(epinephrine)1.1Pharmacological effects:(1) Cardiovascular system:blood vessel: a constrict mucous membranes and skin vessels.Constrict renal and mesenteric blood vesselB 2 dilate vessel of skeletal muscle, coronaryheart: a powerful stimulant effect on heartB i HR T( positive chro no tropic effect)contraction T (positive inotropic effect)con ducti on T in crease the secreti on of reninBp: small dose or therapeutic dose increases systolic and diasto，lic.(2) Smooth muscle: relaxation of most kinds of bronchial smooth muscle(3) Metabolic effects: hyperglycemia1.2 Clinical usesCardiac arrest:Anaphylaxis: anaphylactic shockBronchial asthma:Local application: use with local anesthetics to constrict the regional blood vessels1.3 Side effects: restlessness,anxiety, insomnia, palpitation, sweating, very highdose :severe headache,elevation of BP, the danger of cerebral hemorrhage, arrhythmia and ventricular fibrillation1.4 Contraindications: hypertension, sclerosis of cerebral artery, ischemic heartdisease, congestive heart failure, hyperthyroidism. and diabetes.2 a receptor agonist: norepinephrine, NAIt has very strong a receptor activating effect,2.1 pharmacological effects:(1) very strong blood constriction a 1 receptor. NA has relatively little effect onB 2, dilation of coronary blood vessels, increase coronary blood flow.(2) heart: mild activation on heart(B 1), increases cardiac contractility, cardiac8output, heart rate, conduction(3) Blood pressure: increase systolic and diastolic pressure.2.2 clinical uses(1) hypotension induced by drug intoxication( chlorpromazine, A iscontraindicated)(2) early phase of neurogenic shock(3) upper gastrointestinal tract bleeding3 B receptor : isoprenaline(isoproterenol)3.1 pharmacological effects: B 1, B 2 receptor agonist(1) cardiovascular system :positive inotropic and chronotropic effects, conductionincrease, diastolic pressure falls, systolic blood pressure may remain unchanged or rise, mean arterial pressure falls.(2) bronchial smooth muscle: relaxation3.2 clinical uses(1) cardiac arrest and heart block (2) asthma(3) shock: now seldom used4 DA activates DA receptor, B 1 and a receptor. DA causes an in crease of cardiac contractility. It also causes the release of NA from nerve endings, in induces vasoconstriction(a1).it elevates BP and has weakB2 effects. The effect on D1 receptor of kidney, and mesentery induces dilation of renal and mesenteric blood vessels.Adrenomimetic 拟肾上腺素cutaneous 皮肤的mesenteric肠系膜的metabolic代谢systolic 收缩的sclerosis 硬化diastolic 心脏舒张的ischemic 缺血hemorrhage 出血hyperglycemia 高血糖症 arrhythmia 心律失常ventricular 心室的fibrillation 心 室 纤维颤动diabetes糖尿病hyperthyroidism 甲亢hypotension 低血压9Chapter 9 Adrenoceptor Blocking Drugs1 a adre no ceptor block ing drugsNon selective a receptor blocking drugs: phentolaminePharmacological effects: decreaseperipheral resistance, dilate blood vessel, decrease BP, weak cardiac stimulation effect. After pretreatment with a -antagonist, Adr(E) shows its decrease of BP, which is called“epinephrine reversa”l.Clinical uses: peripheral vascular diseases such as Raynauds Syndrome, thromboangitis) , excess local vasoconstrictor, anti-shock, pheochromocytoma, myocardiac infarction and stubborn congestive heart failure.Side effect: hypotensionPhentolamine should be used with particular caution in patients with coronary artery (because of its reflex cardiac stimulation) or a history of peptic ulcer( agonist at M and H2 receptor which increase the gastric acid release).a 1 receptor blocker: prazosin, it is effective in the management of hypertension with less tachycardia than occurs in phentolamine.2 B receptor blocking drugsNon selective : propranolol, pindolol, sotalol, timololPharmacological effects:(1) B blocking effects: heart: decreaseHR, cardiac contractility and cardiac output,slowed AV conduction.(negative chronotropic and inotropic), hypoglycemia blood vessel: weakly increase peripheral resistance. Inhibit release of renin Decrease BP, lead to bronchoconstriction(2) endogenous sympathomimetic effect: (pindolol)(3) membrane stabilizing action:(4) other effects: anti-platelet aggregationClinical uses: angina pectoris(in stable and unstable not in variant because of coronary constriction ) , cardiac arrhythmias, hypertension, glaucoma(timolol reduces the production of aqueous humor)Selective B 1 antagonist: atenolol, metoprolol3 a and B antagonist: labetalolpheochromocytoma 嗜 铬 细 胞 瘤renin 肾素 endogenous 内源性的 platelet 血小板aggregation 聚集 angina pectoris 心10 心律失常绞痛 arrhythmia Chapter 10 Sedative-HypnoticsHypnotics are drugs used to produce drowsiness and sleep, while sedatives are used to calm anxious and restless patients.1 Benzodiazepine: diazepamPharmacological effects:(1) Anti-anxiety, (2) sedation hypnosis(prolong stage 2 NREM sleep. Shorten3,4 NREM, weakly shorten REM), (3) anti-convulsant effect and anti-epileptic effects.(Bz combines with Bz receptor, strengthen the function of GABA. (4) central muscle relaxationClinical uses: sedative and anti-anxiety, insomnia, tetanus, convulsion induced by fever and drug intoxication, relieve muscle spasm. Antagonist of Diazepam is flumazenil.Bz has no anesthetic effect.Mechanism: Benzodiazepine(BDZ) receptors appear to be located in GANAA receptor sites. BDZ combine with GABA-BDA receptor hloride ion channel complex and potentiate the effect of GABA.Adverse effects: drowsiness, fatigue, dizziness, tolerance, dependence, addiction2 barbitutates:Pharmacological effects: sedati on, hyp no tics(pro long stage n NREM sleep, shorte n REM), anti-convulsant effect and anti-epileptic effects, anesthesia, used for anxiety, epilepsy, anesthesia , pre-anesthetic medication.Mechanism: barbiturates have combining point on GABAA receptor-Cl- complex. After combing with the complex, they enhance the binding of GABA to GABA A receptors. Increase the duration of Cl- channel openings. Then increase Cl- influx, induce hyperpolarization.More and strong side effect: hangover, rebound, tolerance, dependence, addictioninsomnia 失眠惊厥 anaesthetic眼花influx 流 入（ 使 ） 超极化tetanus 破 伤 风 麻醉的 dizz in ess hyperpolarizeconvulsion 头昏11Chapter 11 Antiepileptic Drugs1 classification of seizure type：Partial seizures: simple; complex; psychomotor.Generalized seizures: grand mal; absence(petit mal)Status epilepticus2 antiepileptic drugs2.1 phenytoin: is a weak acid, an enzyme inducer. At low dose, the elimination is according to first order kinetics. At high dose, it is according to zero order kinetics.Pharmacological effect and mechanism: it has a broad range of action against most types of seizures(grand mal and psychomotor epilepsy) excep