Drug: Drug Class: Mechanism of Action: Indications ... · Increases in Tone and Peristalsis of GIT...
Transcript of Drug: Drug Class: Mechanism of Action: Indications ... · Increases in Tone and Peristalsis of GIT...
M1 M2 M3 Nm NnGq Gi Gq Ionotropic Ionotropic
PhospholipaseCIP3,DAG,Ca2+---------------------
Agonist:MuscarineAntagonist:Atropine
InhibitAdenylylCyclaseReducecAMP
-----------------------------------Agonist:MuscarineAntagonist:Atropine
PhospholipaseCIP3,DAG,Ca2+---------------------
Agonist:MuscarineAntagonist:Atropine
OpeningofNa/KChannels-----------------------------------------
Agonist:NicotineAntagonist:Tubocurarine
OpeningofNa/KChannels-----------------------------------------
Agonist:NicotineAntagonist:Tubocurarine
Reflexes:CarotidSinus
------------------------IncreasedAVERAGEBP:
VagalReflexSlowsHR
----------------DecreasedAVERAGEBP:
SympatheticReflexIncreasesHR
CNSAutonomicGanglia
Heart:HeartRate(NOTBP)SmoothMuscles
DecreaseinHeartRate(NegativeChorontropy)DecreaseinConduction(NegativeDromotropy)
SmoothMuscles(Eye):ContractionofSphincterMuscle(Miosis)IncreasedOutflowofAqueousHumor(ReductionofIntraocularTension)
ContractionofCiliaryMuscle(RelaxesSuspensatoryLigaments-->Spasmof
AccommodationforNearVision)-----------------------------------------
Bladder:ContractionofDetrusorMuscle
RelaxationofTrigone/SphincterMuscles-----------------------------RespiratoryTract:
ConstrictionofBronchus(Bronchospasm)IncreasesRespiratorySecretions
------------------------GIT:
IncreasesTone+PeristalsisIncreasesSecretionofGITGlands
CausesIntestinalContractions+DiarrheaInvoluntaryDefecation
IncreasedSweat,Lacrimal,SalivarySecretions
NeuromuscularJunction(SkeletalMuscle)
Ganglia(Sympathetic+ParasympatheticPre-Ganglionic)
AdrenalMedulla
Drug: DrugClass: MechanismofAction: Indications: AdverseEffects: Contraindications:
Hemicholinium IndirectCholinergicAntagonistsAcetylcholineInhibitor
BlocksTransportofCholineintotheNerveCellBlocksAcetyl+Choline-->Acetylcholine
ShutsDownEntireParasympthethicSystemShutsDownEntirePre-GanglionicSynapses(SNS+PNS)
Vesamicol IndirectCholinergicAntagonistsAcetylcholineInhibitor
BlocksUptakeandStorageofAcetylcholineintotheVesicles
BotulinumToxin IndirectCholinergicAntagonistsAcetylcholineInhibitor
BlockstheReleaseofAcetylcholinefromtheVesicles
SpiderVenom IndirectCholinergicAgonistsOver-ReleaseofAcetylcholine
CausesReleaseofAcetylcholine
ButyrylCholinesterase
IndirectCholinergicAntagonistsAcetylcholineInhibitor
PseudocholinesteraseBreaksDownAcetylcholineinthePre-SynapticCleft
PresentinPlasma,Liver,andIntestines
Acetylcholine
DirectCholinergicAgonists:CholineEsterShortDurationPoorlyAbsorbed
PoorlyLipidSolublePoorBBBPenetration
ActsonbothMuscarinic+NicotinicReceptorsDirectAdministration:
Ach-->BloodVessels(M3)Causes:
Arginine-->NitricOxide/EDRFGTP-->cGMP-->VASODILATION
NoTheraputicImplications:DiffuseAction(MoreSideEffects)RapidHydrolysis(WithinSeconds)
---------------------DirectAdministration:
Tx:Hypertension
DirectAdministration:M2-M3SideEffectsReflexTachycardia(SympatheticReflex(M2)
DecreaseinConductionofHeart(M2)IncreasesinToneandPeristalsisofGIT(M3)IncreasesinSecretionsofGITGlandsIntestinal
Contractions-->DiarrheaandInvoluntaryDefecation(M3)ConstrictionofBronchioles+RespiratorySecretions(M3)
Methacholine
DirectCholinergicAgonists:CholineEsterShortDurationPoorlyAbsorbed
PoorlyLipidSolublePoorBBBPenetration
NONICOTINICACTIONConstrictsBronchioles
IncreaseinRespiratorySecretions
VeryLittleTheraputicImplication:VeryShort-Lived
UsedinDiagnosisofBronchialHyperactivity+AsthmaticConditions
(MetacholineChallenge)
Carbachol
DirectCholinergicAgonists:CholineEster
RelativelyShortDurationPoorlyAbsorbed
PoorlyLipidSolublePoorBBBPenetration
CanCauseRelesaeofEpinephrinefromAdrenalMedulla(NicotinicAction)
LocalMioticAgent(ConstrictsthePupil)ReducesIntraocularTension
UsedLocallyforGlaucomaTreatment(EyeDrops) NoSideEffectsduetoLocalityoftheEyeDrops
Bethanechol
DirectCholinergicAgonists:CholineEster
RelativelyShortDurationPoorlyAbsorbed
PoorlyLipidSolublePoorBBBPenetration
NONICOTINICACTIONStimulatesAtonicBladder(Postpartum-Postoperative)
NON-OBSTRUCTIVEUrinaryRetention
Postpartum-PostoperativeAtonicBladder
CongenitalMegacolonParalyticIleus(Post-Op,Neurogenic)
GeneralizedEffectsofCholinergicStimulation:Sweating,Salivation,Flushing,DecreasedBP,Nausea,
AbdominalPain,Diarrhea,Bronchospasm
PilocarpineTertiaryAmineCrossesBBB
DirectCholinergicAgonists:CholinomimeticAlkaloid
LongDurationFarLessPotentPenetratesBBB
ObtainedfromLeavesofPilocarpusMicrophyllusAppliedTopicallytotheCornea
ProducesRapidMiosisContractionoftheCiliaryMuscle
(SpasmofAccommodation)
DrugofChoice:Emergency:
LoweringIntraocularTensionofbothNarrowAngle(ClosedAngle)andWide
Angle(OpenAngle)Glaucoma-------------------
Sjogren'sSyndrome:PromotesSalivationinPatientswith
XerostomiaCanalsobecausedbyIrradiationof
theHeadandNeck
Diaphoresis(ProfuseSweating)Salivation
CanEnterBBB-->CNSDisturbances-->Convulsions
ArecholineDirectCholinergicAgonists:CholinomimeticAlkaloid
LongDuration
Drug: DrugClass: MechanismofAction: Indications: AdverseEffects: Contraindications:
EdrophoniumQuaternary
DoesNOTCrossBBB
IndirectCholinergicAgonists:Anticholinesterase
ReversibleShort-Acting
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------CombinewithChEandCarbamylatedEnzymeisSlowto
HydrolyzeandFreetheEnzyme(10-20Minutes)
DIAGNOSISofMyastheniaGravisTensilonTest
UsedtoDifferentiateMyastheniaGravisfromCholinergicCrisis
NoCNSSideEffects+GeneralizedCholinergicStimulation
PhysostigmineTertiary
DOESCrossBBB
IndirectCholinergicAgonists:Anticholinesterase
ReversibleIntermediate-Acting
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------CombinewithChEandCarbamylatedEnzymeisSlowto
HydrolyzeandFreetheEnzyme(30Minutes)
OralAbsorptionisGood.Uncharged,LipidSoluble,CrossesBBB
Tx:Glaucoma(LowerIntraocularTensionand
ProduceMiosis)Tx:Bladder/IntestinalAtony
Tx:AntidoteinAtropineOverdose
CanEnterBBB-->CNSDisturbances-->Convulsions
Atria AV Node SA Node
NeostigmineQuaternary
DoesNOTCrossBBB
IndirectCholinergicAgonists:Anticholinesterase
ReversibleIntermediate-Acting
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------CombinewithChEandCarbamylatedEnzymeisSlowto
HydrolyzeandFreetheEnzyme(30Minutes-2Hours)
PoorOralAbsorptionTx:
ProminentActiononSkeletalMusclesTx:
ParlyticIleus/CongenitalMegacolonTx:UrinaryRetention
Tx:AntidoteinTubocurarineOverdose
Tx:MyastheniaGravis
NoCNSSideEffectsTubocurarine:RelaxesSkeletalMuscles
(DuringSurgeries)
DemecariumQuaternary
DoesNOTCrossBBB
IndirectCholinergicAgonists:Anticholinesterase
ReversibleIntermediate-Acting
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------CombinewithChEandCarbamylatedEnzymeisSlowto
HydrolyzeandFreetheEnzyme(30Minutes-2Hours)
Tx:OpenAngleandClosed-Angle
GlaucomaNoCNSSideEffects
PyridostigmineAmbenoniumQuaternary
DoesNOTCrossBBB
IndirectCholinergicAgonists:Anticholinesterase
ReversibleLong-Acting
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------Pyridostigmine:3-6HoursAmbenonium:4-8Hours
Tx:ChronicManagementofMyastheniaGravis
Tx:ParlyticIleus/CongenitalMegacolon
Tx:UrinaryRetention
NoCNSSideEffects
TacrineDonepezil
RivastigmineGalantamineTertiary
DoesCrossBBB
IndirectCholinergicAgonists:Anticholinesterase
ReversibleLong-Acting
Anti-ChE Tx:Alzheimer'sDisease CanEnterBBB-->CNSDisturbances-->Convulsions
Organophosphates:Echothiophate
THIOLS
IndirectCholinergicAgonists:Anticholinesterase
IrreversibleInsectisides/NerveGasPoisons
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------ParalysisofMotorFunction(BreathingDifficulty)ConvulsionsProduceIntenseMiosis(Therapeutic)
Aging:ThePhosphorylatedEnzymeslowlyreleasesoneofitsethylgroups.Thismakesitimpossibleforenzymereactivator(Pralidoxime)tobreakthebondbetweenthedrugandenzyme
=Irreversible.------------------------
Tx:Open-AngleGlaucoma
CataractsDUMBBELSS:D:DiarrheaU:UrinationM:Miosis
B:Bradycardia+BronchoconstrictionE:Excitation(CNS+Muscle)
L:LacrimationS:Salivation+Sweating
Organophosphates:ParathionMalathion
(Insecticides)THIOLS
IndirectCholinergicAgonists:Anticholinesterase
IrreversibleInsectisides/NerveGasPoisons
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------CompoundsreactwithEsteraticSite,whichishydrolyzed
extremelyslowlywithwaterornotatall.
Aging:ThePhosphorylatedEnzymeslowlyreleasesoneofitsalkylgroups.Thismakesitimpossibleforenzymereactivator(Pralidoxime)tobreakthebondbetweenthedrugandenzyme
=Irreversible.Tx:NOTHING
DUMBBELSS:D:DiarrheaU:UrinationM:Miosis
B:Bradycardia+BronchoconstrictionE:Excitation(CNS+Muscle)
L:LacrimationS:Salivation+Sweating
Organophosphates:ParathionMalathion
Diazinon(TIK-20)Echothiophate
SomanSarinTabun
IndirectCholinergicAgonists:Anticholinesterase
IrreversibleInsectisides/NerveGasPoisons
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------B
Aging:ThePhosphorylatedEnzymeslowlyreleasesoneofitsalkylgroups.Thismakesitimpossibleforenzymereactivator(Pralidoxime)tobreakthebondbetweenthedrugandenzyme
=Irreversible.Tx:NOTHING
DUMBBELSS:D:DiarrheaU:UrinationM:Miosis
B:Bradycardia+BronchoconstrictionE:Excitation(CNS+Muscle)
L:LacrimationS:Salivation+Sweating
Carbamates:CarbarylPropoxur
IndirectCholinergicAgonists:Anticholinesterase
IrreversibleInsectisides/NerveGasPoisons
AgentsthatInhibitAcetylcholineasteraseProtectsAcetylcholinefromHydrolysis
-------------------------------------
CholinesteraseReactivators:Pralixdoxime
CholinesteraseReactivators
BindswithAnionicSiteofChEandundergoesreactiontocauseHydrolysisofPhosphoserineBond,resultinginfree
enzyme.ButyouNEEDTOGIVEATROPINEorPatientwillnot
survivethesymptoms
OPPoisoning:Shouldbeadministeredasearlyaspossible
(24hoursismaximum).BeforeAgingTakesPlace(LossofAlkylGroup)
TreatmentisineffectiveinthecaseofPhysostigmineorNeostigmine
(Carbamates)CanAlsoGiveAtropine:Counteract
MuscarinicEffects
Drug: DrugClass: MechanismofAction: Indications: AdverseEffects: Contraindications:
AtropineHyoscine
GlycopyrrolateTertiaryAmineDoesCrossBBB
CholenergicAntagonist:NaturalAlkaloid
ObtainedfromAtropaBelladonaTachycardia(BlocksM2)
NOCHANGEinBPMydriasis(PupilDilation)(M3)
Cycloplegia(ParalysisofAccommodation)(M3)Constipation(M3)Bronchodilation(M3)UrinaryRetention(M3)
DecreasedSecretions(M3)BodyTemperatureIncreases:AtropineFever
Compensatory:DilatesBloodVesselsonFace(AtropineFlush)(M3)
Parkinson'sDisease:TremorsPreanestheticMedication
ReduceSecretionsBradycardiainAcuteMI
HighDoses:CNS:MinimalRestlessness,Excitement,Hallucinations
Toxicity:GiveAtropineChildrendonotcompensateforBodyTemperature
IncreasesbyVasodilation-->Fever-->DeathBlurredVision(Mydriasis+Cycloplegia)
DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
GlaucomaUrinaryRetention(BPHPatients)
ScopolamineTertiaryAmineDoesCrossBBB(BetterthanAtropine)
CholenergicAntagonist:NaturalAlkaloid
3-7DaysBlocksMuscarinicReceptorsinVestibulocochlearNerve
PreventsorReversesVestibularDisturbances(MotionSickness)
45Hours-1HourBefore:Preference
BlurredVision(Mydriasis+Cycloplegia)DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
HyoscineGlycopyrrolateDicyclomine
CholenergicAntagonist:SyntheticAlkaloid
Tachycardia(BlocksM2)NOCHANGEinBP
Mydriasis(PupilDilation)(M3)Cycloplegia(ParalysisofAccommodation)(M3)Constipation(M3)
Bronchodilation(M3)UrinaryRetention(M3)
DecreasedSecretions(M3)BodyTemperatureIncreases:AtropineFever
Compensatory:DilatesBloodVesselsonFace(AtropineFlush)(M3)
Antispasmodic
BlurredVision(Mydriasis+Cycloplegia)DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
IpratropiumTiotropium
CholenergicAntagonist:SyntheticAlkaloid
Tachycardia(BlocksM2)NOCHANGEinBP
Mydriasis(PupilDilation)(M3)Cycloplegia(ParalysisofAccommodation)(M3)Constipation(M3)
Bronchodilation(M3)UrinaryRetention(M3)
DecreasedSecretions(M3)BodyTemperatureIncreases:AtropineFever
Compensatory:DilatesBloodVesselsonFace(AtropineFlush)(M3)
BronchialAsthmaCOPD
BlurredVision(Mydriasis+Cycloplegia)DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
TropicamideHomatropineCyclopentolate
CholenergicAntagonist:SyntheticAlkaloid
Lasts.25DaysTachycardia(BlocksM2)
NOCHANGEinBPMydriasis(PupilDilation)(M3)
Cycloplegia(ParalysisofAccommodation)(M3)Constipation(M3)Bronchodilation(M3)UrinaryRetention(M3)
DecreasedSecretions(M3)BodyTemperatureIncreases:AtropineFever
Compensatory:DilatesBloodVesselsonFace(AtropineFlush)(M3)
Mydritic+CycloplegicAgent(OpthalmoscopicExams)
BlurredVision(Mydriasis+Cycloplegia)DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
TrihexyphenydylBenztropine
CholenergicAntagonist:SyntheticAlkaloid
Tachycardia(BlocksM2)NOCHANGEinBP
Mydriasis(PupilDilation)(M3)Cycloplegia(ParalysisofAccommodation)(M3)Constipation(M3)
Bronchodilation(M3)UrinaryRetention(M3)
DecreasedSecretions(M3)BodyTemperatureIncreases:AtropineFever
Compensatory:DilatesBloodVesselsonFace(AtropineFlush)(M3)
Parkinson'sDisease:Tremors
BlurredVision(Mydriasis+Cycloplegia)DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
OxybutyninTolterodineTrospiumSolifenacinDarifenacin
CholenergicAntagonist:SyntheticAlkaloid
Tachycardia(BlocksM2)NOCHANGEinBP
Mydriasis(PupilDilation)(M3)Cycloplegia(ParalysisofAccommodation)(M3)Constipation(M3)
Bronchodilation(M3)UrinaryRetention(M3)
DecreasedSecretions(M3)BodyTemperatureIncreases:AtropineFever
Compensatory:DilatesBloodVesselsonFace(AtropineFlush)(M3)
OveractiveBladder(UrinaryUrgency)BPH
BlurredVision(Mydriasis+Cycloplegia)DryMouthFever
ConstipationUrinaryRetention
TachycardiaAgitationsHallucinationsDelirium
Drug: DrugClass: MechanismofAction: Indications: AdverseEffects: Contraindications:Succinylcholine DepolarizingNMJBlockerTubocurarinePancuroniumRocuroniumMivacurium
Non-DepolarizingNMJBlockers(NmBlocker)
HexamethoniumTrimethaphanMecamylamine
Nicotine
GanglionicBlockers(NnBlockers)