医学传出神经系统药理英文睢大员

1、 sui da-yuan 睢大筼睢大筼 what is efferent nervous system (ens)? chapter 5 pharmacology of efferent nervous systemceptoreffectorcnsansens（2）motor nervous systemchapter 5 pharmacology of enssection 1 structure and function classification of anatomy（1）autonomic nervous system sympathetic nerve parasympathet

2、ic nerve突触间隙突触间隙synaptic cleftsynapsechapter 5 pharmacology of enssection 2 transmitter and receptortransmitters（1）noradrenaline (na) norepinephrin (ne)transmitterssynthesis,releasing and elimination of nasynthesisreleasingelimination12nana（2） acetylcholine (ach)chapter 5 pharmacology of enssection

3、2 transmitter and receptortransmittersacheachsynthesis,releasing and elimination of achsynthesisreleasingelimination（2）adrenoceptors receptor：1 and2 receptor：1、2 and3chapter 5 pharmacology of enssection 2 transmitter and receptor receptors（1）cholinceptors muscarine receptor (mr): m1 and m2 nicotine

4、receptor (nr)：n1 and n2（3）dopamine receptors: d1 and d2（2）noradrenergic nerve (adrenergic nerve)chapter 5 pharmacology of enssection 2 transmitter and receptor classification of transmitters（1）cholinergic nerveachchapter 5 pharmacology of enssection 3 biological effect and mechanism biological effec

5、t of enssee under tablechapter 5 pharmacology of enssection 3 biological effect and mechanismmolecular mechanism of biological effect ligand gated ion channel receptor， regulate na+、k+、ca2+ flux.g-protein-coupled receptors）drug action and signai transductionchapter 5 pharmacology of enssection 4 act

6、ion manners and classification of drugsaction manners（1）direct:（2）indirect:agonistantagonistaffect release affect transport and storagechapter 5 pharmacology of enssection 4 action manners and classification of drugsclassification of drugsacetylcholinechapter 6cholinoceptor agonists section 1 cholin

7、oceptor agonists 1. m、n-cholinoceptor agonists carbaylcholine2. n-cholinoceptor agonists nicotinepilocarpinechapter 6cholinoceptor agonists section 1 cholinoceptor agonists 3. m-cholinoceptor agonistsstimulates m-receptor3、m-cholinoceptor agonistspilocarpine1. eyepharmacologic effects3. m-cholinocep

8、tor agonistspilocarpine1. eyea. miosis (constrict pupil) b. decrease intraocular pressurec. cyclospasm (spasm of accommodation)m circular muscleradial muscle3、m-cholinoceptor agonistspilocarpine1. eye2. glands increase secretion of sweat gland and salivary gland3. smooth muscle3. m-cholinoceptor ago

9、nistspilocarpine1. glaucomaclinical usesopen-angle glaucoma close-angle glaucoma 2. iritiscorneaciliary muscleiriscanal schlemnsuspensoryligamentslenschapter 6cholinoceptor agonists section 2 cholinesterase inhibitorsreversible cholinesterase inhibitorsnon-reversible cholinesterase inhibitorsneostig

10、minephysostigmineorganophosphateschapter 6cholinoceptor agonists section 2 cholinesterase inhibitors hydrolysis of achachachecholineacetic aciddrugs neostigminechapter 6cholinoceptor agonists section 2 cholinesterase inhibitorsreversible inhibit achereversible cholinesterase inhibitorsachm-receptorn

11、-receptorreversible cholinesterase inhibitors neostigmine1. contracting skeletal muscle pharmacologic effectsvery strong-direct activating n2 receptors -release ach at the motor nerve endings2. stimulating gi tract and gallbladder smooth muscle reversible cholinesterase inhibitors neostigmine1. myas

12、thenia gravis clinical uses2. postoperative ileus and urinary retentioncholinergic crisis3. paroxysmal supraventricular tachycardia 4. overdosage of muscle relaxantsreversible choliesterase inhibitors neostigminelarge dosageadverse drug reactionnauseacholinergic crisisvomitingabdominal painmuscle th

13、rill or paralysis reversible cholinesterase inhibitors neostigminemechanical intestinal obstructioncontraindicationsurinary obstructionbronchial asthmareversible cholinesterase inhibitorsphysostigmine eyea. miosisb. decrease intraocular pressurec. cyclospasmreversible cholinesterase inhibitorsgalant

14、haminetensilontacrinedonepezilchapter 7cholinoceptor antagonists1. m-cholinoceptor antagonists2. n1-cholinoceptor antagonists3. n2-cholinoceptor antagonistsdepolarizing drugsnondepolarizing drugssuccinylcholinetubocurarinem-cholinoceptor antagonists atropinepharmacologic effects1. inhibiting the sec

15、retion of glandl salivary glandl sweat glandl bronchial secretary gland l stomach glandm-cholinoceptor antagonists atropinepharmacologic effects2. relaxing visceral smooth muscle l stomach intestinel detrusor of bladder urinary tractl bronchial musclel biliary tractl uterusm-cholinoceptor antagonist

16、s atropinepharmacologic effects3. eye l mydriasisl increases intraocular pressure l cycloplegiam circular muscleradial musclem-cholinoceptor antagonists atropinepharmacologic effects4. heartl small dose: - decreases heart rate l large dose: - increases the heart rate m-cholinoceptor antagonists atro

17、pinepharmacologic effects5. dilating blood vessels and improve microcirculationl therapeutic dose: -no significant effectl large dose: - dilating blood vessels m-cholinoceptor antagonists atropinepharmacologic effects6. cns therapeutic dose ( 0.51.0mg ) maximal dose (1.02.0mg) more large dose (2.05.

18、0mg) toxic dose (over 10mg) m-cholinoceptor antagonists atropineclinical uses1. relieving spasm of smooth muscle -visceral colic painl gastric and intestinal colic pain l bladder irritating symptoms l gallbladder colic pain l renal colic pain m-cholinoceptor antagonists atropineclinical uses2. inhib

19、iting secretion of glandl preanaesthetic medication for controlling the side effect of etherl severe night sweat and slavers l adjunctive therapy for peptic ulcers m-cholinoceptor antagonists atropineclinical uses3. ophthalmology l iridocyclitis l examining eye ground l examining eyesight m-cholinoc

20、eptor antagonists atropineclinical uses4. cardiovascular disorder l slow type arrhythmia -bradycardia, s-a block, a-v block -adams-stokes syndrome induced by antimony intoxication m-cholinoceptor antagonists atropineclinical uses5. antishock6. organophosphate intoxicationm-cholinoceptor antagonists

21、atropineadverse drug reactioncontraindicationsglaucoma pyloric obstructionprostatic hypertrophyuse with cautionold peoplem-cholinoceptor antagonistsanisodamine (654-2)scopolaminechapter 8adrenoceptor-activating drugscatecholcatecholamines,caadrenoceptor-activating drugs1. -receptor agonists2. 、-rece

22、ptor agonists3. -receptor agonists4. dopamine receptor agonists noradrenaline, metaraminoladrenaline , ephedrineisoprenaline, dobutamine, salbutamoldopamine、-adrenoceptor agonists adrenaline adr, epinephrinepharmacologic effects1. stimulating the heartl contraction forcel heart ratel conduction co2.

23、 contract and relax blood vessels skin, mucous membranes -constriction splanchnic vessels renal and mesenteric -constriction cerebral and pulmonary - weak constriction skeletal muscle -dilatation coronary artery vessels -dilatation 3. blood pressure (1) systolic blood pressure (2) diastolic blood pr

24、essure small dose = larger dose 4. relaxation of bronchial smooth muscle 5. metabolic effects - increase metabolism-energy - increase insulin secretion - increase oxygen consumption 1. cardiac arrest2. allergic shock 3. bronchial asthma 4. local application clinical uses hypertension sclerosis of ce

25、rebral artery ischemic heart disease congestive heart failure hyperthyrea diabetesadverse drug reactioncontraindicationsephedrinepharmacologic effects-similar to adrenaline -action is weak and longer-enhances the release of na -central actions -prevent hypotension-bronchial asthma -nasal congestion-

26、allergyclinical usesdopaminepharmacokinetics-precursor of na and adr-enhances the release of na -pharmacologic effectslow dose (1) increase cardiac contractility - 1 + na release sbp (2) vasoconstriction (1) dbp = vasodilation (d1) (3) increase in glomerular filtration rate, renal blood flow and na+

27、 excretion (d1) large dose 1 d1 (1) some types of shock - cardiogenic, septic shock and hemorrhagic shock especially with cardiac dysfunction, oliguria or anuria (2) acute renal insufficiency - with diuretics (3) congestive heart failureclinical uses-adrenoceptor agonists noradrenaline na, norepinep

28、hrinepharmacologic effects 1. stimulating the heart 2. contract blood vessels 3. increasing blood pressure1. hypotension2. early phase of neurogenic shock 3. upper gastrointestinal tract bleeding clinical uses hypertension atherosclerosis coronary heart disease oliguria and anuriaadverse drug reacti

29、oncontraindicationsmetaraminolpharmacologic effects- acts on 1 receptor - causes na release- increases bp and cardiac output- decreases heart rate -adrenoceptor agonists isoprenaline, isoproterenolpharmacologic effects1. stimulating the heart2. relax blood vessels3. decreasing blood pressure4. relax

30、ation of bronchial smooth muscle 5. metabolic effects1. bronchial asthma2. cardiac arrest 3. atrio ventricular conduction block 4. shock clinical uses coronary heart disease myocarditis hyperthyroidismadverse drug reactioncontraindications na adr iso da minperipheral resistancearterial pressurep r对

31、不 同 肾 上 腺 素 受 体 作 用 的 比 较 作 用 方 式 分 类 受 体 1受 体 2受 体 直 接 作 用 于 受 体 释 放 递 质 去 甲 肾 上 腺 素 + + + 间 羟 胺 + + + + + 去 氧 肾 上 腺 素 + + 甲 氧 明 + - - + - 肾 上 腺 素 ， + + + + 多 巴 胺 ， + + + + 麻 黄 碱 ， + + + + + 异 丙 肾 上 腺 素 - + + + 多 巴 酚 丁 胺 + + + + 拟肾上腺素药基本作用的比较1、2-receptor agonists phentolamine, tolazoline,phenoxyben

32、zamine1-receptor agonistsprazosin, dorazosin,terazosinchapter 9adrenoceptor blocking drugs s 1. -receptor antagonists s 2. -receptor antagonists1、2-receptor agonists propranolol, timolol, pindolol1-receptor agonistsatenolol, metoprolol, acebutolol s 1. -receptor antagonists block receptor, antagoniz

33、e the effects of -agonists after pretreatment with -antagonist - adr shows decrease bp called “epinephrine reversal” 1、2-receptor antagonistsphentolaminepharmacologic effects1. reduces peripheral resistance - block 1 - relax blood vessels2. cardiac stimulation - reflex cardiac mechanisms - blocks presynaptic 2 enhanced na release 3. m, h 1 ,h 2 agonist1.peripheral vascular spasm diseases 2.local v