传出神经系统药理(英文版)

Pharmacology

Whatis

efferentnervoussystem(ENS)?

pharmacologyofefferentnervoussystemceptoreffectorCNSANSENS（2）Motornervoussystem

pharmacologyofENSSection1structureandfunctionClassificationofanatomy（1）Autonomicnervoussystem

Sympatheticnerveparasympatheticnerve突触间隙Synapticcleftsynapse

pharmacologyofENSSection2transmitterandreceptortransmitters（1）Noradrenaline(NA)Norepinephrin(NE)TransmittersSynthesis,releasingandeliminationofNAsynthesisreleasingelimination12NANA（2）Acetylcholine(Ach)

pharmacologyofENSSection2transmitterandreceptortransmittersAChEAChSynthesis,releasingandeliminationofAChsynthesisreleasingelimination（2）adrenoceptors

αreceptor：α1andα2βreceptor：β1、β2andβ3

pharmacologyofENSSection2transmitterandreceptorreceptors（1）cholinceptorsMuscarinereceptor(MR):M1andM2Nicotinereceptor

(NR)：N1and

N2（3）dopaminereceptors:D1andD2（2）noradrenergicnerve(adrenergicnerve)

pharmacologyofENSSection2transmitterandreceptorClassificationoftransmitters（1）cholinergicnerveACh

pharmacologyofENSSection3biologicaleffectandmechanism

biologicaleffectofENS

pharmacologyofENSSection3biologicaleffectandmechanismmolecularmechanismof

biologicaleffect

Ligandgatedionchannelreceptor，regulateNa+、K+、Ca2+flux.G-protein-coupledreceptors）drugactionandsignaitransduction

pharmacologyofENSSection4

actionmannersandclassificationofdrugsactionmanners（1）Direct:（2）Indirect:agonist

antagonistaffectreleaseaffecttransportandstorage

pharmacologyofENSSection4

actionmannersandclassificationofdrugsclassificationofdrugsacetylcholineChapter6cholinoceptoragonists

andcholinesteraseinhibitingdrugsSection1

cholinoceptoragonists

1.M、N-cholinoceptoragonistscarbaylcholine2.N-cholinoceptoragonistsnicotinepilocarpineChapter6cholinoceptoragonists

andcholinesteraseinhibitingdrugsSection1

cholinoceptoragonists

3.M-cholinoceptoragonistsstimulatesM-receptor3、M-cholinoceptoragonistspilocarpine1.EyePharmacologiceffects3.M-cholinoceptoragonistspilocarpine1.eyea.miosis(constrictpupil)

b.decreaseintraocularpressurec.cyclospasm(spasmofaccommodation)M

circularmuscleradialmuscle3、M-cholinoceptoragonistspilocarpine1.eye2.glands

increasesecretionofsweatglandandsalivarygland3.smoothmuscle3.M-cholinoceptoragonistspilocarpine1.glaucomaclinicalusesopen-angleglaucomaclose-angleglaucoma

2.iritiscorneaciliarymuscleiriscanalschlemnsuspensoryligamentslensChapter6cholinoceptoragonists

andcholinesteraseinhibitingdrugsSection2

cholinesteraseinhibitorsreversiblecholinesteraseinhibitorsnon-reversiblecholinesteraseinhibitorsneostigminephysostigmineorganophosphatesChapter6cholinoceptoragonists

andcholinesteraseinhibitingdrugsSection2

cholinesteraseinhibitorshydrolysisofAChAchAChEcholineaceticaciddrugsneostigmineChapter6cholinoceptoragonists

andcholinesteraseinhibitingdrugsSection2

cholinesteraseinhibitorsreversibleinhibitAChEreversiblecholinesteraseinhibitorsAchM-receptorN-receptorreversiblecholinesteraseinhibitors

neostigmine1.contractingskeletalmuscle

Pharmacologiceffectsverystrong--directactivatingN2receptors--releaseAchatthemotornerveendings2.stimulatingGItractandgallbladdersmoothmuscle

reversiblecholinesteraseinhibitors

neostigmine1.myastheniagravisclinical

uses2.postoperativeileusandurinaryretentioncholinergiccrisis3.paroxysmalsupraventriculartachycardia

4.overdosageofmusclerelaxantsreversiblecholiesteraseinhibitors

neostigminelargedosageAdverse

drugreactionnauseacholinergiccrisisvomitingabdominalpainmusclethrillorparalysisreversiblecholinesteraseinhibitors

neostigminemechanicalintestinalobstructioncontraindicationsurinaryobstructionbronchialasthmareversiblecholinesteraseinhibitorsphysostigmineeyea.miosisb.decreaseintraocularpressurec.CyclospasmreversiblecholinesteraseinhibitorsgalanthaminetensilontacrinedonepezilChapter7cholinoceptorantagonists1.M-cholinoceptorantagonists2.N1-cholinoceptorantagonists3.N2-cholinoceptorantagonistsdepolarizingdrugsnondepolarizingdrugssuccinylcholinetubocurarineM-cholinoceptorantagonists

atropinePharmacologic

effects1.

inhibitingthesecretionofgland

salivaryglandsweatglandbronchialsecretaryglandstomachglandM-cholinoceptorantagonists

atropinePharmacologiceffects2.

relaxingvisceralsmoothmuscle

stomachintestinedetrusorofbladderurinarytractbronchialmusclebiliarytractuterusM-cholinoceptorantagonists

atropinePharmacologiceffects3.

eye

mydriasisincreasesintraocularpressurecycloplegiaM

circularmuscleRadialmuscleM-cholinoceptorantagonists

atropinePharmacologiceffects4.

heart

smalldose:

---

decreasesheartrate

largedose:---

increasestheheartrate

M-cholinoceptorantagonists

atropinePharmacologiceffects5.

dilatingbloodvesselsandimprovemicrocirculation

therapeuticdose:

---nosignificanteffect

largedose:

---

dilatingbloodvessels

M-cholinoceptorantagonists

atropinePharmacologiceffects6.

CNS

therapeuticdose(0.5~1.0mg)

maximaldose

(1.0~2.0mg)

morelargedose

(2.0~5.0mg)

toxicdose(over10mg)

M-cholinoceptorantagonists

atropineclinicaluses1.

relievingspasmofsmoothmuscle

---visceralcolicpaingastricandintestinalcolicpainbladderirritatingsymptomsgallbladdercolicpain

renalcolicpain

M-cholinoceptorantagonists

atropineclinicaluses2.

inhibitingsecretionofglandpreanaestheticmedicationforcontrollingthesideeffectofetherseverenightsweatandslavers

adjunctivetherapyforpepticulcers

M-cholinoceptorantagonists

atropineclinicaluses3.

ophthalmologyiridocyclitisexaminingeyeground

examiningeyesight

M-cholinoceptorantagonists

atropineclinicaluses4.

cardiovasculardisorderslowtypearrhythmia

---bradycardia,S-Ablock,A-Vblock

---Adams-StokessyndromeinducedbyantimonyintoxicationM-cholinoceptorantagonists

atropineclinicaluses5.

antishock6.organophosphateintoxicationM-cholinoceptorantagonists

atropineAdversedrugreactioncontraindicationsglaucoma

pyloricobstructionprostatichypertrophyusewithcautionoldpeopleM-cholinoceptorantagonistsAnisodamine(654-2)scopolamineChapter8Adrenoceptor-activatingdrugscatecholCatecholamines,CAAdrenoceptor-activatingdrugs1.α-receptoragonists2.α、β-receptoragonists3.β-receptoragonists4.dopaminereceptoragonistsNoradrenaline,MetaraminolAdrenaline,EphedrineIsoprenaline,Dobutamine,SalbutamolDopamineα、β-adrenoceptoragonists

AdrenalineAdr,EpinephrinePharmacologic

effects1.

stimulatingtheheartcontractionforceheartrateconductionCO2.

contractandrelaxblood

vessels

skin,mucousmembranes--constrictionsplanchnicvessels

renalandmesenteric--constriction

cerebralandpulmonary--weakconstriction

skeletalmuscle--dilatationcoronaryarteryvessels

--dilatation3.

Bloodpressure

(1)systolicbloodpressure(2)diastolicbloodpressure

smalldose

↓=

largerdose

4.

relaxationofbronchialsmoothmuscle

5.

metaboliceffects

-increasemetabolism-energy-increaseinsulinsecretion-increaseoxygenconsumption

1.Cardiacarrest2.Allergicshock

3.Bronchialasthma

4.

Localapplication

clinicaluses◆hypertension◆sclerosisofcerebralartery◆ischemicheartdisease◆congestiveheartfailure◆

hyperthyrea◆diabetesAdversedrugreactioncontraindicationsEphedrinePharmacologic

effects---similartoadrenaline---actionisweakandlonger---enhancesthereleaseofNA

---centralactions---preventhypotension---bronchial

asthma---nasalcongestion---allergyclinicalusesDopaminePharmacokinetics---precursorofNAandAdr---metabolizedbyCOMTandMAO---enhancesthereleaseofNA---noeffectwithP.O.(ivggt)---noeffectonCNS(notpenetrateBBB)Pharmacologic

effectslowdose(1)increasecardiaccontractility--β1+NAreleaseSBP(2)vasoconstriction(α1)DBP=vasodilation(D1)(3)increaseinglomerularfiltrationrate,renalbloodflowandNa+excretion(D1)

largedoseα1>D1(1)sometypesofshock

---cardiogenic,septicshockandhemorrhagicshockespeciallywithcardiacdysfunction,oliguriaoranuria(2)acuterenalinsufficiency---withdiuretics(3)congestiveheartfailureclinicalusesα-adrenoceptoragonistsNoradrenalineNA,NorepinephrinePharmacologic

effects1.

stimulatingtheheart

2.

contractblood

vessels

3.

increasingbloodpressure1.Hypotension2.earlyphaseofneurogenicshock

3.uppergastrointestinaltract

bleeding

clinicaluses

▲

hypertension

▲

atherosclerosis

▲

coronaryheartdisease

▲

oliguriaandanuriaAdversedrugreactioncontraindicationsMetaraminolPharmacologic

effects---actsonα1receptor

---causesNArelease---increasesBPandcardiacoutput---decreasesheartrate

β

-adrenoceptoragonists

Isoprenaline,IsoproterenolPharmacologic

effects1.

stimulatingtheheart2.

relaxblood

vessels3.

decreasingbloodpressure4.

relaxationofbronchialsmoothmuscle

5.

metaboliceffects1.bronchial

asthma2.cardiacarrest3.Atrio–ventricularconductionblock

4.shock

clinicaluses

■

coronaryheartdisease

■

myocarditis

■

hyperthyroidismAdversedrugreactioncontraindications

NAAdrIsoDA

minPeripheralresistanceArterialpressurePR拟肾上腺素药基本作用的比较α1、α2-receptoragonists

Phentolamine,Tolazoline,Phenoxybenzamineα1-receptoragonistsPrazosin,Dorazosin,TerazosinChapter9AdrenoceptorBlockingDrugsS1.α-receptorantagonistsS2.β-receptorantagonistsβ1、β2-receptoragonists

Propranolol,Timolol,Pindololβ1-receptoragonistsAtenolol,Metoprolol,AcebutololS1.α-receptorantagonists

★blockα–receptor,antagonizetheeffectsofα-agonists

★afterpretreatmentwithα-antagonist--AdrshowsdecreaseBP

–called“epinephrinereversal”

α1、α2-receptorantagonistsPhentolaminePharmacologic

effects1.reducesperipheralresistance--blockα1

--relaxblood

vessels2.cardiacstimulation

--reflexcardiacmechanisms--blockspresynapticα2

enhancedNArelease3.M,H1,H2agonist1.peripheralvascularspasmdiseases2.localvasoconstrictor--NAi.v3.anti-shock4.stub