藥理學(xué)老師c18劉antipsychot

AntimentaldisorderDrugs

CLASSIFICATION1.Antipsychoticdrugs2.AntimanicDrugs3.Antidepressants4.Antianxietydrugs

ξ1

Antipsychoticdrugs

HypothesisforSchizophrenia:

HyperactivityofDAreceptorinbraindopaminergicpathwaysinCNSNigral-striatumpathway:thecenterofextrapyramidalsystemofmotorfunction

hyperactivity:hyperkineticsyndromeweakness:PDMesolimbic-mesocorticalpathway:toregulateemotionwithcognition,thinking,perception,inference.Tuberoinfundibularsystem:Toregulatethehormonesecretionofpituitarygland.

ClassificationofAntipsychotics

Chlorpromazine(Wintermin)[Pharmacologicaleffects]1.centralnervoussystem(1)Antipsychoticeffects:

Toamelioratethesymptomssuchasdelusions,hallucinationsandmania

Theinfluencetoaveragepeople’spsychomotilityandbehavior:sedation,apathy(感情淡漠),slowreaction

Mechanism:toblockD2receptorof

mesolimbicandmesocorticalpathway.

(2)Antiemeticeffect:CPZhaspowerfuleffectonvomitbroughtfromvariouscause(exceptfromkinetia)

Mechanism:Inlittledose,itinhibitD2receptorsonCTZInhighdose,itmaydepressthemedullaryvomitingcenterdirectly.

(3)Temperatureregulation:Inlowtemperature,itcandecreasebodytemperaturetobehindthenormal.Inhightemperature,thebodytemperaturewillincreaseNotonlydecreasebodytemperatureoffeverpatient,butalsodecreasenormalbodytemperature.

(4)enhancecentraldepressivedrugaction

2.Antagonisticsystem:

α-adrenergicreceptorblockingeffect:vasculardilatation,bloodpressuredecrease.

Mreceptorblockingeffect:Highdosecancausedrymouth,constipation,blurredvision.3.Endocrinesystem:

Decreasesprolactininhibitoryfactory;increasethesecretionofprolactin

Mechanism:

blocktheD2receptoroftuberoinfundibularpathwayCLINICALUSES:1.Psychoticdisorder:UsedtotreatvarioustypesofschizophreniaManiaandotherschizophreniawithexcitationanddelusion2.Antiemeticeffectsandtreatingstubbornhiccup.Nauseaandvomitinginducedbyuremia,cancer,pregnanttoxemia,radiation.3.HypothermicanesthesiaandartificialwintersleepTodecreaseoxygenconsumptionofheartandbrainandpreventshockinoperation.SIDEEFFECTS1.generalsideeffects

centraldepressiveaction

Mreceptorblockingeffect:Highdosecancausedrymouth,

constipation,blurredvision.

α-adrenergicreceptorblockingeffect:Orthostatichypotension,stuffynose.2.Extrappyramidalsystemreactions

A.ParkinsonismB.AcutedysmyotoniaC.Akathisia(靜坐不能)

Mechanism:CPZblockDreceptorofnigrostriatal

pathway.Centralanticholinegicdrugscanbeusedtotreatit,butlevo-dopacannotbeusedtotreatit.

D.Tardivedyskinesiamaybeseenwithchronictherapy.Anticholinergicdrugdeterioratethesymptom.

Mechanism:

UpregulationofDreceptor3.Cardiovasculareffects:Orthostatichypotension,whichcanresultinsyncopeandreflextachycardia.4.Allergicreaction5.Others

galactorrhea(溢乳)hepaticΞ2antimanicdrugsLithiumcarbonateCorrecttheoveractivityofcatecholaminergicsystems[mechanism]1.Inhibitreleaseoftransmittersatthesynapse2.EnhancethereuptakeofNA.3.Inhibiteinositolphosphatase(肌醇磷酸酶),decreaseIP3-PIP2[Adversereaction]TIislower,lightsafeMEC=0.6-1.2mmol/LMTC=1.4mmol/LANTIDEPRESSANTSEtiologicalfactorofdepression:deficiencyofNAand5-HT,andDAClassificationofantidepressants,

tricyclicsantidepressive

[pharmacodynamics]1.

antidepressive(slowly)

tricyclicblocktheamine(norepinephrineorserotonin)reuptakepumps,whichterminateamineneurotransmission.2.

autonomicnervoussystemblockMreceptor.3.

Cardiovascularsysteminhibitedreflexofcardio-vascular,hypotension,arrhythmia.[adversereaction]

1.

similartoatropine2.

cardiovascularheartrateincrease,posturehypotrension,arrhythmia3.

nervoussystem4.

othersemetictetrecyclicantidepressive

Characteristic:fast;tolerance;lightadversereaction.MAOI

MAO-Aistheamineoxidiseprimarilyresponsiblefornorepinephrineserotonin,andtyraminemetabolism.MAO-Bismoreselectivefordopamine.asaresult,theirreversibleMAOinhibitoraresubjecttoaveryhighriskofhypertensivereactiontotyramineingest