抗精神失常藥課件

第18章抗精神失常藥

藥學(xué)系藥理教研室1謝謝觀賞2019-6-29第18章抗精神失常藥

藥學(xué)系藥理教研室1謝謝觀賞2019-6Chapter18

AntipsychoticdisordersdrugsZhuxiaoguang2謝謝觀賞2019-6-29Chapter18

Antipsychoticdisobjecter掌握

氯丙嗪的藥理作用、作用機(jī)制、臨床應(yīng)用與主要不良反應(yīng)等。熟悉抗精神失常藥的概念和分類;其他抗精神病藥的作用特點(diǎn);碳酸鋰、米帕明的藥理作用特點(diǎn)。了解精神失常的概念、分型.3謝謝觀賞2019-6-29objecter掌握氯丙嗪的藥理作用、作用機(jī)制、臨床應(yīng)Why?4謝謝觀賞2019-6-29Why?4謝謝觀賞2019-6-29神經(jīng)兮兮

神經(jīng)稀稀

神經(jīng)搭錯(cuò)5謝謝觀賞2019-6-29神經(jīng)兮兮神經(jīng)稀稀神經(jīng)搭錯(cuò)5謝謝觀賞2019-6-29Neuropathypsychopathynote（神經(jīng)?。ň癫。?謝謝觀賞2019-6-29Neuropathypsychopathynote（神經(jīng)?。㊣ntroduction1、ConceptPsychoticdisorders

variousreason

severementaldisorders.7謝謝觀賞2019-6-29Introduction1、ConceptPsychotic2、classification1、schizophrenia精神分裂癥2、mania-depressivedisorder躁狂抑郁癥

3、anxiety焦慮癥4、others8謝謝觀賞2019-6-292、classification1、schizophreni1）themostfamiliar,2）inpatient60~70%;3）thoughtandbehavior----cloven(分裂)4）limbicsystem(邊緣系統(tǒng))

DAfunction.Schizophrenia

(Itype,IItype)9謝謝觀賞2019-6-291）themostfamiliar,SchizophrMania-depressivedisorder

mania5-HT↓NANA↓1）Mania-depressive

2）depression5-HT↓10謝謝觀賞2019-6-29Mania-depressivedisordermania3、anxiety焦慮癥4、others青春期、周期性、更年期11謝謝觀賞2019-6-293、anxiety焦慮癥4、others青春期、11謝謝觀10月10日是世界精神衛(wèi)生日健康體魄+健康心理美好人生12謝謝觀賞2019-6-2910月10日是世界精神衛(wèi)生日健康體魄+健康心理美好人生12謝ClassificationofdrugsAntipsychoticdrugschlorpromazineAntimanicdrugs

lithiumcarbonateAntidepressants

imipramineAnxiolytics

diazepam氯丙嗪碳酸鋰米帕明地西泮13謝謝觀賞2019-6-29ClassificationofdrugsAntips§1

AntipsychoticDrugs吩噻嗪類：chlorpromazine硫雜蒽類：chlorprothixene丁酰苯類：haloperidol其他類：sulpiride，clozapine…14謝謝觀賞2019-6-29§1AntipsychoticDrugs吩噻嗪類：chchlorpromazine,CPZ

氯丙嗪

（wintermin冬眠靈）[pharmacokinetics]

1、po.slowandirregular,Fvariable,im.absorb

quickly；2、passBBBeasily,

distributioniswide(inbrainhigher);

3、metabolizemainlyinliver;4、elimination：kidney.15謝謝觀賞2019-6-29chlorpromazine,CPZ氯丙chlorpromazine[actions＆uses]I.

CNS1、Antipsychoticeffects(抗精神病作用)

characteristics

1)longuse,can’tproducetolerance;2)symptomatictreatment(對(duì)癥治療);3)theonsetofeffectisslow(6W-6M).16謝謝觀賞2019-6-29chlorpromazine[actions＆us

mechanism

fourimportantdopaminergicpathways:

1)mesolimbicpathway

中腦－邊緣系統(tǒng)

2)mesocorticalpathway

中腦－皮質(zhì)通路

3)nigrostriatalpathway

黑質(zhì)－紋狀體通路

4)tubero-infundibularpathway

結(jié)節(jié)－漏斗通路CPZ(－)D2-R→

antipsychoticeffects17謝謝觀賞2019-6-29mechanismfourimportantClinicaluses

psychoticdisorder：1）schizophrenia-----

firstchoice;2）otherpsychoticstates:

manicstates;delirium(譫妄)states.noeffectondepression.(Itype＞IItype)18謝謝觀賞2019-6-29Clinicalusespsychoti

2、Antiemeticeffects

(鎮(zhèn)吐作用)

Antiemeticeffectisstrong;Butnoeffectonmotionsickness.(暈動(dòng)性嘔吐)CPZlowdosage㈠CTZ（催吐化學(xué)感受區(qū)）(+)vomitingcenterlargedosage㈠vomitchemoreceptortriggerzone19謝謝觀賞2019-6-292、Antiemeticeffects(鎮(zhèn)吐作用)

nauseaandvomit

inducedbyuremia(尿毒癥),cancer,pregnanttoxemia(妊娠毒血癥),radiation(輻射)

andsomedrugs.

stubbornhiccup

頑固性呃逆

Clinicaluses20謝謝觀賞2019-6-29nauseaandvomitinduce

3、influenceoftemperatureregulationcharacteristics:1)

temperaturenormalpersonandpatientswithfever;2)actioncorrelativewithenvironmentaltemperature(環(huán)境溫度);

3）

producefever,dispel

fever(散熱).21謝謝觀賞2019-6-293、influenceoftemperatureClinicaluses1）hypothermalanesthesia

低溫麻醉

2）artificialhibernation

人工冬眠

CPZ+pethidine(哌替啶)

+promethazine(異丙嗪)hibernationmixture22謝謝觀賞2019-6-29Clinicaluses1）hypothermal配合物理降溫使體溫降至34℃以下機(jī)體進(jìn)入“冬眠”狀態(tài)。BMR，對(duì)各種病理刺激的反應(yīng)性，組織對(duì)缺氧的耐受力。

mostlyusedfor

嚴(yán)重感染、中毒性休克、高熱驚厥、甲狀腺危象等輔助治療。人工冬眠23謝謝觀賞2019-6-29配合物理降溫使體溫降至34℃以下機(jī)體進(jìn)入“冬眠4、theeffectsofCNSdepressants

e.g.generalanaesthetics,sedative-hypnotics,analgesics(鎮(zhèn)痛藥),alcohol,……24謝謝觀賞2019-6-294、theeffectsofCNSdepres

II.autonomicnervesystem

1、cardiovascular(-)-R(-)血管運(yùn)動(dòng)中樞dilatethebloodvesseldirectlyBP↓orthostatichypotension

體位性低血壓adrenalinereversalcannotuseinthehypertension:tolerance2、(-)M–Rdrymouth,constipation(便秘),blurredvision(視力模糊)…25謝謝觀賞2019-6-29II.autonomicnervesystem1III.endocrinesystemCPZ

(-)D2-R

(tubero-infundibularpathway)

prolactininhibitoryfactor(催乳素釋放抑制因子);

thesecretionofgrowthhormone;thesecretionofGnRH(促性腺激素);

thesecretionofACTH;……（內(nèi)分泌系統(tǒng)）26謝謝觀賞2019-6-29III.endocrinesystemCPZ([adversereactions]1、

commonadversereaction1)㈠CNS,2)M-R㈠,3)-R㈠:BP,

orthostatichypotension…4)localirritative(刺激性).27謝謝觀賞2019-6-29[adversereactions]1、common

2.extrapyramidalsystemreactions

錐體外系反應(yīng)1)parkinsonism帕金森綜合征2)acutedystonia急性肌張力障礙

3)akathisia靜坐不能

4)tardivedyskinesia遲發(fā)性運(yùn)動(dòng)障礙中樞抗膽堿藥

CPZ

()

nigrostriatalpathwayD2-R

28謝謝觀賞2019-6-292.extrapyramidalsystemre3.allergicreactions4.acutetoxication

po.largedose:1~2g/time，

clinicalsymptoms：narcoma，Bp

shock，

（麻醉性昏睡）cardiacdamage,arrhythmia……

[contraindications]p.16029謝謝觀賞2019-6-293.allergicreactions29謝謝觀賞201briefsummaryCPZ

blocking中腦-皮質(zhì)通路D2-R中腦-邊緣葉通路D2-R抗精神病作用黑質(zhì)-紋狀體通路DA-R錐體外系反應(yīng)結(jié)節(jié)-漏斗通路DA-R影響內(nèi)分泌30謝謝觀賞2019-6-29briefsummaryCPZ中腦-皮質(zhì)通路D2-R抗

otherantipsychoticdrugsp.161-163

硫雜蒽類

tardan泰爾登

丁酰苯類

haloperidol

氟哌啶醇

其他口服長(zhǎng)效類

penfluridol

五氟利多

sulpiride

舒必利

clozapine

氯氮平

risperidone

利培酮31謝謝觀賞2019-6-29otherantipsychoticdrugs§2Antimanicdrugslithiumcarbonate

碳酸鋰

[characteristics]

1.absorbedwell；widedistribution；2.Na+enhancetheexcretionofLi+;

incept

Na+renaldischarge

Li+3.onsetofeffectisslow,

individualvariation（個(gè)體差異）;32謝謝觀賞2019-6-29§2Antimanicdrugslithiumca4.mechanismiscomplex;p.1645.maniaandthemanicstateofschizophreniaclinicalfirstchoice;6.adversereaction

safemarginisnarrow;commonadversereaction

acutetoxication:CNS(–)coma…,death.

withdrawal,treatment:

iv.0.9%NaClTDM

important!33謝謝觀賞2019-6-294.mechanismiscomplex;p§3AntidepressantdrugsImipramine米帕明（丙咪嗪）［characteristics］

1.po.absorbedwell；widedistribution；

2.Antidepressantselectivity

high;actionslow;

normal----CNS(–)

depressed----uplift(情緒高漲)34謝謝觀賞2019-6-29§3AntidepressantdrugsImipr３.mechanism：inhibitthereuptakeofNA、5-HTinthebrain.4.Clinicaluses:differenttypesofdepression,enuresis(遺尿癥),

anxietyandphobia(恐怖癥).5.Adversereactions:M-R(–),CNSsymptom…

[druginteraction]

p.16535謝謝觀賞2019-6-29３.mechanism：inhibitthereupOtherdrugs

p.166-170amitriptyline阿米替林

maprotiline馬普替林

mianserin米安色林

……36謝謝觀賞2019-6-29Otherdrugsp.166-1701.DescribetheactionsandusesofCPZ.2.PleaseexplaintheeffectsandadversereactionsofCPZbyreceptortheory.3.Listthenameusedformaniaordepressive.questions37謝謝觀賞2019-6-291.Describetheactionsanduse38謝謝觀賞2019-6-2938謝謝觀賞2019-6-29第18章抗精神失常藥

藥學(xué)系藥理教研室39謝謝觀賞2019-6-29第18章抗精神失常藥

藥學(xué)系藥理教研室1謝謝觀賞2019-6Chapter18

AntipsychoticdisordersdrugsZhuxiaoguang40謝謝觀賞2019-6-29Chapter18

Antipsychoticdisobjecter掌握

氯丙嗪的藥理作用、作用機(jī)制、臨床應(yīng)用與主要不良反應(yīng)等。熟悉抗精神失常藥的概念和分類;其他抗精神病藥的作用特點(diǎn);碳酸鋰、米帕明的藥理作用特點(diǎn)。了解精神失常的概念、分型.41謝謝觀賞2019-6-29objecter掌握氯丙嗪的藥理作用、作用機(jī)制、臨床應(yīng)Why?42謝謝觀賞2019-6-29Why?4謝謝觀賞2019-6-29神經(jīng)兮兮

神經(jīng)稀稀

神經(jīng)搭錯(cuò)43謝謝觀賞2019-6-29神經(jīng)兮兮神經(jīng)稀稀神經(jīng)搭錯(cuò)5謝謝觀賞2019-6-29Neuropathypsychopathynote（神經(jīng)?。ň癫。?4謝謝觀賞2019-6-29Neuropathypsychopathynote（神經(jīng)?。㊣ntroduction1、ConceptPsychoticdisorders

variousreason

severementaldisorders.45謝謝觀賞2019-6-29Introduction1、ConceptPsychotic2、classification1、schizophrenia精神分裂癥2、mania-depressivedisorder躁狂抑郁癥

3、anxiety焦慮癥4、others46謝謝觀賞2019-6-292、classification1、schizophreni1）themostfamiliar,2）inpatient60~70%;3）thoughtandbehavior----cloven(分裂)4）limbicsystem(邊緣系統(tǒng))

DAfunction.Schizophrenia

(Itype,IItype)47謝謝觀賞2019-6-291）themostfamiliar,SchizophrMania-depressivedisorder

mania5-HT↓NANA↓1）Mania-depressive

2）depression5-HT↓48謝謝觀賞2019-6-29Mania-depressivedisordermania3、anxiety焦慮癥4、others青春期、周期性、更年期49謝謝觀賞2019-6-293、anxiety焦慮癥4、others青春期、11謝謝觀10月10日是世界精神衛(wèi)生日健康體魄+健康心理美好人生50謝謝觀賞2019-6-2910月10日是世界精神衛(wèi)生日健康體魄+健康心理美好人生12謝ClassificationofdrugsAntipsychoticdrugschlorpromazineAntimanicdrugs

lithiumcarbonateAntidepressants

imipramineAnxiolytics

diazepam氯丙嗪碳酸鋰米帕明地西泮51謝謝觀賞2019-6-29ClassificationofdrugsAntips§1

AntipsychoticDrugs吩噻嗪類：chlorpromazine硫雜蒽類：chlorprothixene丁酰苯類：haloperidol其他類：sulpiride，clozapine…52謝謝觀賞2019-6-29§1AntipsychoticDrugs吩噻嗪類：chchlorpromazine,CPZ

氯丙嗪

（wintermin冬眠靈）[pharmacokinetics]

1、po.slowandirregular,Fvariable,im.absorb

quickly；2、passBBBeasily,

distributioniswide(inbrainhigher);

3、metabolizemainlyinliver;4、elimination：kidney.53謝謝觀賞2019-6-29chlorpromazine,CPZ氯丙chlorpromazine[actions＆uses]I.

CNS1、Antipsychoticeffects(抗精神病作用)

characteristics

1)longuse,can’tproducetolerance;2)symptomatictreatment(對(duì)癥治療);3)theonsetofeffectisslow(6W-6M).54謝謝觀賞2019-6-29chlorpromazine[actions＆us

mechanism

fourimportantdopaminergicpathways:

1)mesolimbicpathway

中腦－邊緣系統(tǒng)

2)mesocorticalpathway

中腦－皮質(zhì)通路

3)nigrostriatalpathway

黑質(zhì)－紋狀體通路

4)tubero-infundibularpathway

結(jié)節(jié)－漏斗通路CPZ(－)D2-R→

antipsychoticeffects55謝謝觀賞2019-6-29mechanismfourimportantClinicaluses

psychoticdisorder：1）schizophrenia-----

firstchoice;2）otherpsychoticstates:

manicstates;delirium(譫妄)states.noeffectondepression.(Itype＞IItype)56謝謝觀賞2019-6-29Clinicalusespsychoti

2、Antiemeticeffects

(鎮(zhèn)吐作用)

Antiemeticeffectisstrong;Butnoeffectonmotionsickness.(暈動(dòng)性嘔吐)CPZlowdosage㈠CTZ（催吐化學(xué)感受區(qū)）(+)vomitingcenterlargedosage㈠vomitchemoreceptortriggerzone57謝謝觀賞2019-6-292、Antiemeticeffects(鎮(zhèn)吐作用)

nauseaandvomit

inducedbyuremia(尿毒癥),cancer,pregnanttoxemia(妊娠毒血癥),radiation(輻射)

andsomedrugs.

stubbornhiccup

頑固性呃逆

Clinicaluses58謝謝觀賞2019-6-29nauseaandvomitinduce

3、influenceoftemperatureregulationcharacteristics:1)

temperaturenormalpersonandpatientswithfever;2)actioncorrelativewithenvironmentaltemperature(環(huán)境溫度);

3）

producefever,dispel

fever(散熱).59謝謝觀賞2019-6-293、influenceoftemperatureClinicaluses1）hypothermalanesthesia

低溫麻醉

2）artificialhibernation

人工冬眠

CPZ+pethidine(哌替啶)

+promethazine(異丙嗪)hibernationmixture60謝謝觀賞2019-6-29Clinicaluses1）hypothermal配合物理降溫使體溫降至34℃以下機(jī)體進(jìn)入“冬眠”狀態(tài)。BMR，對(duì)各種病理刺激的反應(yīng)性，組織對(duì)缺氧的耐受力。

mostlyusedfor

嚴(yán)重感染、中毒性休克、高熱驚厥、甲狀腺危象等輔助治療。人工冬眠61謝謝觀賞2019-6-29配合物理降溫使體溫降至34℃以下機(jī)體進(jìn)入“冬眠4、theeffectsofCNSdepressants

e.g.generalanaesthetics,sedative-hypnotics,analgesics(鎮(zhèn)痛藥),alcohol,……62謝謝觀賞2019-6-294、theeffectsofCNSdepres

II.autonomicnervesystem

1、cardiovascular(-)-R(-)血管運(yùn)動(dòng)中樞dilatethebloodvesseldirectlyBP↓orthostatichypotension

體位性低血壓adrenalinereversalcannotuseinthehypertension:tolerance2、(-)M–Rdrymouth,constipation(便秘),blurredvision(視力模糊)…63謝謝觀賞2019-6-29II.autonomicnervesystem1III.endocrinesystemCPZ

(-)D2-R

(tubero-infundibularpathway)

prolactininhibitoryfactor(催乳素釋放抑制因子);

thesecretionofgrowthhormone;thesecretionofGnRH(促性腺激素);

thesecretionofACTH;……（內(nèi)分泌系統(tǒng)）64謝謝觀賞2019-6-29III.endocrinesystemCPZ([adversereactions]1、

commonadversereaction1)㈠CNS,2)M-R㈠,3)-R㈠:BP,

orthostatichypotension…4)localirritative(刺激性).65謝謝觀賞2019-6-29[adversereactions]1、common

2.extrapyramidalsystemreactions

錐體外系反應(yīng)1)parkinsonism帕金森綜合征2)acutedystonia急性肌張力障礙

3)akathisia靜坐不能

4)tardivedyskinesia遲發(fā)性運(yùn)動(dòng)障礙中樞抗膽堿藥

CPZ

()

nigrostriatalpathwayD2-R

66謝謝觀賞2019-6-292.extrapyramidalsystemre3.allergicreactions4.acutetoxication

po.largedose:1~2g/time，

clinicalsymptoms：narcoma，Bp

shock，

（麻醉性昏睡）cardiacdamage,arrhythmia……

[contraindications]p.16067謝謝觀賞2019-6-293.allergicreactions29謝謝觀賞201briefsummaryCPZ

blocking中腦-皮質(zhì)通路D2-R中腦-邊緣葉通路D2-R抗精神病作用黑質(zhì)-紋狀體通路DA-R錐體外系反應(yīng)結(jié)節(jié)-漏斗通路DA-R影響內(nèi)分泌68謝謝觀賞2019-6-29briefsummaryCPZ中腦-皮質(zhì)通路D2-R抗

otherantipsychoticdrugsp.161-163

硫雜蒽類

tardan泰爾登

丁酰苯類

haloperidol

氟哌啶醇

其他口服長(zhǎng)效類

penfluridol

五氟利多

sulpiride

舒必利

clozapine

氯氮平

risperidone

利培酮69謝謝觀賞2019-6-29otherantipsychoticdrugs§2Antimanicdrugslithiumcarbona