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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 parasympathetic 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 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 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 effect 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 action 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 cholinoceptor 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-cholinoceptor 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 agonistspilocarpine1. glaucomaclinical usesopen-angle glaucoma close-angle glaucoma 2. iritiscorneaciliary muscleiriscanal schlemnsuspensoryligamentslensChapter 6cholinoceptor agonists Section 2 cholinesterase inhibitorsreversible cholinesterase inhibitorsnon-reversible cholinesterase inhibitorsneostigminephysostigmineorganophosphatesChapter 6cholinoceptor agonists Section 2 cholinesterase inhibitors hydrolysis of AChAchAChEcholineacetic aciddrugs neostigmineChapter 6cholinoceptor agonists Section 2 cholinesterase inhibitorsreversible inhibit AChEreversible cholinesterase inhibitorsAchM-receptorN-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. myasthenia 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 thrill or paralysis reversible cholinesterase inhibitors neostigminemechanical intestinal obstructioncontraindicationsurinary obstructionbronchial asthmareversible cholinesterase inhibitorsphysostigmine eyea. miosisb. decrease intraocular pressurec. Cyclospasmreversible cholinesterase inhibitorsgalanthaminetensilontacrinedonepezilChapter 7cholinoceptor antagonists1. M-cholinoceptor antagonists2. N1-cholinoceptor antagonists3. N2-cholinoceptor antagonistsdepolarizing drugsnondepolarizing drugssuccinylcholinetubocurarineM-cholinoceptor antagonists atropinePharmacologic effects1. inhibiting the secretion 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 antagonists 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 atropinePharmacologic 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 (2.05.0mg) 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. inhibiting 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-cholinoceptor 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 atropineAdverse drug reactioncontraindicationsglaucoma pyloric obstructionprostatic hypertrophyuse with cautionold peopleM-cholinoceptor antagonistsAnisodamine (654-2)scopolamineChapter 8Adrenoceptor-activating drugscatecholCatecholamines,CAAdrenoceptor-activating drugs1. -receptor agonists2. 、-receptor 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. 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 pressure 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 cerebral 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-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+ 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, NorepinephrinePharmacologic 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 reactioncontraindicationsMetaraminolPharmacologic 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. relaxation 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 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,Phenoxybenzamine1-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, antagonize 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 vasoconstrictor- NA i.v3.anti-shock 4.stubborn congestive heart failure5.pheochromocytoma preoperative managementclinical uses coronary heart disease digestive ulcer serious arteriosclerosis renal inadequacyAdverse drug reactioncontraindications S 2. -receptor antagonists Nonselective blockers propranolol； Selective 1 blockers atenolol； Metoprolol and blockers labetalol 1. -blocking effects a. Heartl contraction forcel heart ratel conduction l decrease myocardial oxygen consumptionCOPharmacologic 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 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 failureAdverse drug reactioncontraindications ANY QUESTIONS？ THANK YOU！
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