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1、Pharmacology,Department of Pharmacology School of Pharmacy Jilin University SUI Da-yuan 睢大筼,What is efferent nervous system(ENS)?,Chapter 5 pharmacology of efferent nervous system,ceptor,effector,CNS,ANS,ENS,（2）Motor nervous system,Chapter 5 pharmacology of ENS,Section 1 structure and function,Class
2、ification of anatomy,（1）Autonomic nervous system Sympathetic nerve parasympathetic nerve,突触间隙Synaptic cleft,synapse,Chapter 5 pharmacology of ENS,Section 2 transmitter and receptor,transmitters,（1）Noradrenaline(NA)Norepinephrin(NE),Transmitters,Synthesis,releasing and elimination of NA,synthesis,rel
3、easing,elimination,1,2,NA,NA,（2）Acetylcholine(Ach),Chapter 5 pharmacology of ENS,Section 2 transmitter and receptor,transmitters,AChE,ACh,Synthesis,releasing and elimination of ACh,synthesis,releasing,elimination,（2）adrenoceptors receptor：1 and2 receptor：1、2 and3,Chapter 5 pharmacology of ENS,Sectio
4、n 2 transmitter and receptor,receptors,（1）cholinceptors Muscarine receptor(MR):M1 and M2 Nicotine receptor(NR)：N1 and N2,（3）dopamine receptors:D1 and D2,（2）noradrenergic nerve(adrenergic nerve),Chapter 5 pharmacology of ENS,Section 2 transmitter and receptor,Classification of transmitters,（1）choline
5、rgic nerve,ACh,Chapter 5 pharmacology of ENS,Section 3 biological effect and mechanism,biological effect of ENS,see under table,Chapter 5 pharmacology of ENS,Section 3 biological effect and mechanism,molecular mechanism of biological effect,Ligand gated ion channel receptor，regulate Na+、K+、Ca2+flux.
6、,G-protein-coupled receptors）,drug action and signai transduction,Chapter 5 pharmacology of ENS,Section 4 action manners and classification of drugs,action manners,（1）Direct:,（2）Indirect:,agonistantagonist,affect release affect transport and storage,Chapter 5 pharmacology of ENS,Section 4 action man
7、ners and classification of drugs,classification of drugs,acetylcholine,Chapter 6cholinoceptor agonists and cholinesterase inhibiting drugs,Section 1 cholinoceptor agonists,1.M、N-cholinoceptor agonists,carbaylcholine,2.N-cholinoceptor agonists,nicotine,pilocarpine,Chapter 6cholinoceptor agonists and
8、cholinesterase inhibiting drugs,Section 1 cholinoceptor agonists,3.M-cholinoceptor agonists,stimulates M-receptor,3、M-cholinoceptor agonists,pilocarpine,1.Eye,Pharmacologic effects,3.M-cholinoceptor agonists,pilocarpine,1.eye,a.miosis(constrict pupil),b.decrease intraocular pressure,c.cyclospasm(spa
9、sm of accommodation),circular muscle,radial muscle,3、M-cholinoceptor agonists,pilocarpine,1.eye,2.glands increase secretion of sweat gland and salivary gland,3.smooth muscle,3.M-cholinoceptor agonists,pilocarpine,1.glaucoma,clinical uses,open-angle glaucoma close-angle glaucoma,2.iritis,Chapter 6cho
10、linoceptor agonists and cholinesterase inhibiting drugs,Section 2 cholinesterase inhibitors,reversible cholinesterase inhibitors,non-reversible cholinesterase inhibitors,neostigminephysostigmine,organophosphates,Chapter 6cholinoceptor agonists and cholinesterase inhibiting drugs,Section 2 cholineste
11、rase inhibitors,hydrolysis of ACh,Ach,AChE,choline,acetic acid,drugs,neostigmine,Chapter 6cholinoceptor agonists and cholinesterase inhibiting drugs,Section 2 cholinesterase inhibitors,reversible inhibit AChE,reversible cholinesterase inhibitors,Ach,M-receptorN-receptor,reversible cholinesterase inh
12、ibitors,neostigmine,1.contracting skeletal muscle,Pharmacologic effects,very strong,-direct activating N2 receptors-release Ach at the motor nerve endings,2.stimulating GI tract and gallbladder smooth muscle,reversible cholinesterase inhibitors,neostigmine,1.myasthenia gravis,clinical uses,2.postope
13、rative ileus and urinary retention,cholinergic crisis,3.paroxysmal supraventricular tachycardia,4.overdosage of muscle relaxants,reversible choliesterase inhibitors,neostigmine,large dosage,Adverse drug reaction,nausea,cholinergic crisis,vomiting,abdominal pain,muscle thrill or paralysis,reversible
14、cholinesterase inhibitors,neostigmine,mechanical intestinal obstruction,contraindications,urinary obstruction,bronchial asthma,reversible cholinesterase inhibitors,physostigmine,eye,a.miosis,b.decrease intraocular pressure,c.Cyclospasm,reversible cholinesterase inhibitors,galanthamine,tensilon,tacri
15、ne,donepezil,Chapter 7cholinoceptor antagonists,1.M-cholinoceptor antagonists,2.N1-cholinoceptor antagonists,3.N2-cholinoceptor antagonists,depolarizing drugs,nondepolarizing drugs,succinylcholine,tubocurarine,M-cholinoceptor antagonists,atropine,Pharmacologic effects,1.inhibiting the secretion of g
16、land salivary gland sweat gland bronchial secretary gland stomach gland,M-cholinoceptor antagonists,atropine,Pharmacologic effects,2.relaxing visceral smooth muscle stomach intestine detrusor of bladder urinary tract bronchial muscle biliary tract uterus,M-cholinoceptor antagonists,atropine,Pharmaco
17、logic effects,3.eye mydriasis increases intraocular pressure cycloplegia,circular muscle,Radial muscle,M-cholinoceptor antagonists,atropine,Pharmacologic effects,4.heart small dose:-decreases heart rate large dose:-increases the heart rate,M-cholinoceptor antagonists,atropine,Pharmacologic effects,5
18、.dilating blood vessels and improve microcirculation therapeutic dose:-no significant effect large dose:-dilating blood vessels,M-cholinoceptor antagonists,atropine,Pharmacologic effects,6.CNS therapeutic dose(0.51.0mg)maximal dose(1.02.0mg)more large dose(2.05.0mg)toxic dose(over 10mg),M-cholinocep
19、tor antagonists,atropine,clinical uses,1.relieving spasm of smooth muscle-visceral colic pain,gastric and intestinal colic pain bladder irritating symptoms gallbladder colic pain renal colic pain,M-cholinoceptor antagonists,atropine,clinical uses,2.inhibiting secretion of gland,preanaesthetic medica
20、tion for controlling the side effect of ethersevere night sweat and slavers adjunctive therapy for peptic ulcers,M-cholinoceptor antagonists,atropine,clinical uses,3.ophthalmology,iridocyclitis examining eye ground examining eyesight,M-cholinoceptor antagonists,atropine,clinical uses,4.cardiovascula
21、r disorder,slow type arrhythmia-bradycardia,S-A block,A-V block-Adams-Stokes syndrome induced by antimony intoxication,M-cholinoceptor antagonists,atropine,clinical uses,5.antishock,6.organophosphate intoxication,M-cholinoceptor antagonists,atropine,Adverse drug reaction,contraindications,glaucoma,p
22、yloric obstruction,prostatic hypertrophy,use with caution,old people,M-cholinoceptor antagonists,Anisodamine(654-2),scopolamine,Chapter 8Adrenoceptor-activating drugs,catechol,Catecholamines,CA,Adrenoceptor-activating drugs,1.-receptor agonists,2.、-receptor agonists,3.-receptor agonists,4.dopamine r
23、eceptor agonists,Noradrenaline,Metaraminol,Adrenaline,Ephedrine,Isoprenaline,Dobutamine,Salbutamol,Dopamine,、-adrenoceptor agonists,Adrenaline Adr,Epinephrine,Pharmacologic effects,1.stimulating the heart contraction force heart rate conduction,CO,2.contract and relax blood vessels skin,mucous membr
24、anes-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 pressure small dose=larger dose,4.relaxation of bronchial smooth
25、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 cerebral artery ischemic heart disease congestive heart failure hyperthyrea dia
26、betes,Adverse drug reaction,contraindications,Ephedrine,Pharmacologic effects,-similar to adrenaline-action is weak and longer-enhances the release of NA-central actions,-prevent hypotension-bronchial asthma-nasal congestion-allergy,clinical uses,Dopamine,Pharmacokinetics,-precursor of NA and Adr-me
27、tabolized by COMT and MAO-enhances the release of NA-no effect with P.O.(iv ggt)-no effect on CNS(not penetrate BBB),Pharmacologic effects,low dose(1)increase cardiac contractility-1+NA release SBP(2)vasoconstriction(1)DBP=vasodilation(D1)(3)increase in glomerular filtration rate,renal blood flow an
28、d Na+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 failure,clinical uses,-adrenoceptor agonists,Noradrenaline NA,Norepinephrine,Ph
29、armacologic effects,1.stimulating the heart 2.contract blood vessels 3.increasing blood pressure,1.Hypotension2.early phase of neurogenic shock 3.upper gastrointestinal tract bleeding,clinical uses,hypertension atherosclerosis coronary heart disease oliguria and anuria,Adverse drug reaction,contrain
30、dications,Metaraminol,Pharmacologic effects,-acts on 1 receptor-causes NA release-increases BP and cardiac output-decreases heart rate,-adrenoceptor agonists,Isoprenaline,Isoproterenol,Pharmacologic effects,1.stimulating the heart2.relax blood vessels3.decreasing blood pressure4.relaxation of bronch
31、ial smooth muscle 5.metabolic effects,1.bronchial asthma2.cardiac arrest 3.Atrio ventricular conduction block 4.shock,clinical uses,coronary heart disease myocarditis hyperthyroidism,Adverse drug reaction,contraindications,NA Adr Iso DA,min,Peripheral resistance,Arterial pressure,P R,拟肾上腺素药基本作用的比较,1
32、、2-receptor agonists Phentolamine,Tolazoline,Phenoxybenzamine1-receptor agonistsPrazosin,Dorazosin,Terazosin,Chapter 9Adrenoceptor Blocking Drugs,S 1.-receptor antagonists,S 2.-receptor antagonists,1、2-receptor agonists Propranolol,Timolol,Pindolol1-receptor agonistsAtenolol,Metoprolol,Acebutolol,S
33、1.-receptor antagonists,block receptor,antagonize the effects of-agonists after pretreatment with-antagonist-Adr shows decrease BP called“epinephrine reversal”,1、2-receptor antagonists,Phentolamine,Pharmacologic effects,1.reduces peripheral resistance-block 1-relax blood vessels2.cardiac stimulation
34、-reflex cardiac mechanisms-blocks presynaptic 2 enhanced NA release 3.M,H 1,H 2 agonist,1.peripheral vascular spasm diseases 2.local vasoconstrictor-NA i.v3.anti-shock 4.stubborn congestive heart failure5.pheochromocytoma preoperative management,clinical uses,coronary heart disease digestive ulcer s
35、erious arteriosclerosis renal inadequacy,Adverse drug reaction,contraindications,S 2.-receptor antagonists,Nonselective blockers propranolol；Selective 1 blockers atenolol；Metoprolol and blockers labetalol,1.-blocking effects,a.Heart contraction force heart rate conduction decrease myocardial oxygen
36、consumption,CO,Pharmacologic effects,b.blood vessel and BP(1)contract peripheral blood vessel(2)contract coronary artery(3)lower blood pressurec.bronchial smooth muscled.metabolic effects,2.Endogenous sympathomimetic effect-receptor agonist-some drugs 3.Membrane stabilizing action local anaesthetic
37、effect-decrease membrane ion channel permeability,1.prevention of angina pectoris 2.prevention of cardiac arrhythmias 3.treatment of hypertension 4.hyperthyrea,clinical uses,sinus bradycardia bronchial asthma atrioventricular block congestive heart failure,Adverse drug reaction,contraindications,ANY QUESTIONS？,THANK YOU！,
