中枢神经系统药理学教案.docx
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中枢神经系统药理学教案
大理学院药学院药理学教研室
彭芳教案
课 程:
药理学
教 材:
李端主编《药理学》(第五版,人民卫生出版社,2003)
杨宝峰《药理学》(第六版,人民卫生出版社,2003)授课对象:
04级药学本科1~2班
授课时间:
2006年9月25日-10月16日
教师:
彭芳
职称:
教授
参考书籍:
杨藻宸:
《医用药理学》
杨宝峰《药理学》(规划教材,北京大学出版社,2003)
中枢药理(12学时)
教学内容
授课学时
授课时间
镇静催眠药(双语教学)
2.0
9月25日
抗癫痫药和抗惊厥药
1.5
9月25日
治疗中枢神经系统退行性疾病药
局部麻醉药
1.0
0.5
9月28日
抗精神失常药
2.5
10月9日
镇痛药
2.5
10月12日
解热镇痛抗炎药(双语教学)
2.0
10月16日
药学院药理学教研室教案
Chapter12Sedative-Hypnotics
[Aims]:
1.TounderstandtheclasificationandrepresentativedrugsofSedative-HypnoticDrugs.2.Masteringthepharmacologicalactionandclinicalapplicationofbenzodiazepines.
3.Understandingthetraitsofbarbiturates.
[TeachingContentsandlearningtimedistribution]:
1.Benzodiazepines:
55minute
2.Barbiturates:
20minute
3.Theothersedative-hypnotics:
5minute
[AssistantTeaching]:
makeuseofprojector
[Vocabularylist]:
benzodiazpine;diazepam
[Review]:
1.Trytorelatetheactionandusesofbenzodiazepines.
2.Whatisadvantageofbenzodiazepinesforhypnoticactionascomparewith
barbitals?
[Teachingcontents]:
Ⅰ.GeneralIntroduction
A.Definition
Hypnoticsaredrugsusedtoproducedrowsinessandsleep,whilesedativesareusedtocalmanxiousanxiousandrestlesspatients.
B.Twophasesofsleep
1.Rapideyemovementsleep(REM,paradoxicalsleep)--20minineachrun
2.Non-rapideyemovementsleep(NREM,orthodoxsleep)
--90minineachrun
--dividedtofourstages
--stage3and4--slowwavesleep,somnambulismandnightterrors
C.Physiologicalsleepconsistsof4-5cyclesofalternativeREMandNREM
Ⅱ.Benzodiazepines(BZD)
A.Classification
1.Short-acting(t1/2<5hrs):
triazolam,midazolametc
2.Intermediate-acting(t1/2=5-15hrs):
lorazepam,oxazepametc
3.Long-acting( t1/2>15hrs):
diazepam,flurazepametc
B.Pharmacokinetics
1.Intramuscularinjectionunreliable,givenorally
2.Mostmetabolismsinliver
3.Somemetaboliteshalf-livesgreaterthantheparentdrugs
C.Pharmacologicaleffects
1.Antianxiety
Diazepamshowsanxiolyticeffectsandalsoexerts“taming”effect.Withsmallerdosethansedativedose,diazepammayrelievethepatientfromtension,agitation,fear,
anxiety,restlessnessandgastrointestinaltractdisturbancesorinsomniainducedbyanxiety.
2.Sedationhypnosis
Allthesedative-hyponoticswillinducesleepifhighenoughdosesaregiven.Thelatencyofsleeponsetisdecreased.Thedurationofsleepisprolonged(especiallystage2NREMsleep).Slow-wavesleep(stage3,stage4NREMSLEEP,anddeltawave)isshortened.TheeffectonREMisshortened,butsmall.
Advantages
-Therapeuticindexishigh–
largedosagedosenotinduceanesthesia
-Nohepaticenzymeinductioneffect
-withdrawaldrug,reboundissmall
3.Anticonvulsanteffectsandantiepilepticeffects:
-Inhibitdevelopmentandspreadofepileptiformactivity
-Anticonvulsant--withoutCNSdepression
4.Musclerelaxation
-Inhibitpolysynapticreflexes
-Inhibitinternuncialtransmission
-Depresstransmissionattheskeletalmyoneuraljunction--highdoses
D.Mechanismofaction
BZDagonistsincreasetheamountofchloridecurrentgeneratedbyGABAAreceptoractivated---potentiatingtheeffectsofGABA
E.ClinicalUses
1.Antianxiety:
BZDcanrelievetheanxietyofgeneralizedanxietydisorderandinsomepatientspanicattacksyndrome.
2.SedativeandHypnotic:
usedtotreatinsomniaandpreanestheticmedication
.Thecomplaintofinsomniaembracesawidevarietyofsleepproblemsthatincludedifficultyinfallingasleep,frequentawakeningsandshortdurationofsleep.Insomecases,thepatientwillneedandshouldbegivenahypnoticforalimitedperiod.
3.Anticonvulsantantiepileptic:
Dizepamisusedtotreattetanus, eclampsia,
convulsioninducedbydrugintoxicationandfever(children).Diazepamgivenintravenouslyorrectallyishighlyeffectiveforstoppingcontinuousseizureactivity,especiallygeneralizedtonic-clonicstatusepilepticus.Itisthefirstchoiceofdrugtotreatstatusepilepticus.
4.Skeletalmusclerelaxant:
Dizepamreducesmuscletone.Itisusedtoreducemusclerigidityinducedbycerebralpalsy,cerebralvascularaccidentorspinalcorddamage,andisalsousedtorelievemusclespasminducedbyjointpathologicalchanges.
F.AdverseEffects
1.Generallyreactions:
d
rowsiness、lethargy—mostcommonly
2.Acutetoxicity:
respiratoryandcirculatory
depressants
3.Physicalandpsychologicaldependence--longtimeuse
G.Characteristicsofdifferentdrugs
1.Oxazepam
(1)Intermediateacting,t1/2=5-10h
(2)Weakhypnoticandmusclerelaxant
(3) Strongantianxietyeffect
(4) Usedtotreatanxiety
(5)Dependence--repeateduse
2.Lorazepam
(1)Sameasoxazepam
(2)Hasdependence
(3)Treatanxietyandinsomnia
(4)Statusepileptics,IV
3.Flurazepam
(1)Longacting,t1/22