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Antidepressants: Classification
Antidepressants: Classification
Antidepressants: Classification
A
NTIDEPRESSANTS
CLASSIFICATION
Doser angeg iveninm
g/day.
SelectiveSerotoninReuptakeInhibitor
(InhibitionofmonoaminereceptorsbySSRileadstodecreasemonoaminereuptake
SSRI andincreasesNeurotransmitterinSynapticCleft.Thisleadstodownregulationof
5HT1A Receptor.TheGenomereactiontothisinformationleadstoadecreased
ommon 5HT1A Receptorexpression.5HTreleaseisincreasedandbuildsupinthesynapse.
C
Thisleadstopostsynaptic5HT1A Receptortodesentesize.)
F eatures
Mechanismofactionsandsomeimportantpoints.
Fluoxetine SERTi+ 5HT2Ci+NETi 5HT2Cileadstoincreasedcognitionand
[20-60mg] attention,reducedfatigue,antibulimiaeffect
butalsocausesagitation,insomnia,anxiety.
Longestacting.
italopram
C R+SEnantiomers H1inhibition leadstosedation,andQTc
[20-40mg]
(H1i+SERTi) prolongation.
Escitalopram
SEnantiomer(SERTi) PureSERTinhibition
[10-20mg]
aroxetine
P SERTi+M1A ntagonism + M1Inhibition s edationandanticholinergic
[20-50mg]
NETi action.
NOSinhibitionc ausessexualdysfunction.
SerotoninPartialagonist/ReuptakeInhibitor
(InhibitionofmonoaminereceptorsbyblockingSERTandalongwithithaspartial
SPARI agonisticactionon5HT1A Receptorleadingtomorerapidincreasein5HTlevelin
synapticcleft.)
C ommon
F eatures
SNRI SerotoninNorepinephrinereuptakeInhibitor
Common (InhibitionofmonoaminereceptorsbyblockingSERTandNETandincreasein5HT
F eatures andNElevelinsynapticcleft.
AddonactionNETiincreasesDAintheprefrontalcortex(notinanyotherareasof
thebrain)DA+NE+5HTthisiscalledas2.½Mechanism.)
enlafaxine
V SERTi+ NETi SERTiMostpotentandrobustatlower
[75-375mg] doses.
NETiactionprogressivelyincreasesasdose
increases.
Moderatelypotentandrobustonlyathigher
doses.
uloxetine
D SERTi+ NETi Relievesdepressioninabsenceofpainand
[60-120mg] viceversa.
Fibromyalgia,ChronicMusculoskeletalpain
Diabeticperipheralneuropathicpain.
Milnacipran SERTi+ N
ETi MorepotentNETthanSERTinhibitorandthis
[100-200mg] Day1 :1 2.5m
go
nce activityleadstogoodcognitiveimprovement.
Days2
-3:2
5m g/day( 12.5m
gt wiced aily) Sideeffects:Increasedsweatingandurinary
Days4
-7:5
0m g/day( 25m
gt wiced aily) hesitancy.
AfterD
ay7
:1
00m
g/day( 50m gt wiced aily)
upropion
B DATi+NETi ● UsedtoaugmentSSRIorSNRIin
[150-300mg] Bupropionisaweakreuptakeinhibitor casewhensignsandsymptomsof
propertybutisefficaciousasits residualPositiveeffectsareseen.
inhibitorypropertiesismadeupby ● Usefulintreatmentofreduced
6-HYDROXYmetaboliteofBUPROPION positiveeffectandDopamine
(Radafaxine) deficiencysyndrome.
● Bupropiondoesnotcausesexual
OccupiesDATinStriatumandNucleus dysfunctionasitlackssignificant
Accumbensinamannertomitigate
SERTinhibition.
cravingbutnotsufficienttocauseabuse.
● Nonabusableandusefulin
treatmentofNicotineDeAddiction.
NASSA Nor-AdrenergicandSpecificSerotoninAntidepressant.
Common (InhibitionofmonoaminereceptorsbyblockingNETandDATincreaseinNEand5HT
F eatures
levelinsynapticcleft.
AddonactionNETiincreasesDAintheprefrontalcortex(notinanyotherareasof
thebrain)DA+NE+5HTthisiscalledas2.½Mechanism.)
ianserin
M 5HT2A+5HT2C+5HT3 Sameasabovebutadditionaleffectonalpha
[30-90mg] 1receptors.
Antagonist+α1+ α2
antagonist+H1
Antagonist.
Mirtazapine α2antagonist+ 5HT2A + α2antagonistactionsyielddualincreaseof
[15-45mg] both5HTandNErelease.(SNRIalso
5HT2C+5HT3A
ntagonist+ increasesboth5HTandNEreleasebythe
H1Antagonist. monoaminetransporterblockage.)
Thesetwomechanismsaresynergisticsoby
blockingbothofthemwillleadtoagreater
disinhibitorysignalforthesetwo
neurotransmitters.Forthisreason
MirtazapineisoftencombinedwithSNRIfor
caseswhodon'trespondtoSNRIalone.This
combinationisoftencalledasCALIFORNIA
ROCKETFUEL.
NARI NorepinephrineReuptakeInhibitor
Common (InhibitionofmonoaminereceptorsbyblockingNETandDATincreaseinNEand5HT
F eatures levelinsynapticcleft.
NafazodoneisalsoaSARI.
New:
SARE(Serotoninantagonistandreuptakeenhancer)
1. Tianeptine
2. Amineptine
TCA TricyclicAntidepressant.
(Inhibitionofreceptors5HT2A,5HT2C,SERTiandNETi)
Amitriptyline[50-200]mg Clomipramine[30-250mg]
DOSE
Imipramine[50-200mg] Nortriptyline[75-150mg]
Lofepramine[140-210mg] Trimipramine[50-300mg]
Dosulepin(Dothepin)[75-225mg] Doxepin[30-300mg]
TETRACYCLIC Mianserin Amoxapine
ANTIDEPRESSANT Maprotiline
BICYCLIC Viloxazine
ANTIDEPRESSANT
MAOi Monoamineoxidaseinhibitor( BrainMAO-Ainhibitionhastobedone
tomediateantidepressantefficacyasMAO-Apreferentiallymetabolizesserotonin
andnorepinephrine.)
Common ByinhibitionofMAO-Aitcausesan
OnlyMAO-Ainhibitionleadstorobust
Features increaseinthelevelofSerotonin,
increaseinthelevelof5HtandNEand
Nor-epinephrineandDopamineat moderateincreaseinthelevelsofDA.Asit
synapticclefts. increasestheselevelsinasufficientamount,
isabletomediatetheantidepressantaction.
OnlyMAO-BinhibitionleadstomoderateDA
MAO-A MAO-B
levelincreaseanditseffectisirrelevantas
Substrates: Substrates: farasNEand5HTisconcernedanditisthus
5HT,NE,DA, DA,Tyramine, notabletomediateitsactionas
Tyramine. Phenylethylamine. antidepressantactionbutisusedin
treatmentofParkinson’sDisease.
Location: Location:
Brain,S kin, Brain, BothMAO-AandMAO-Binhibitionleadsto
Liver, Lymphocytes, veryhighriseinconcentrationofDA,5HT
Placenta. platelets. andNEatthesynapticcleftleadingtorobust
antidepressantaction.
Thus,MAO-AandMAO-Binhibitionisoneof
thefewtherapeuticmeasuresavailableto
increasedopamineindepression,and
thereforetotreatrefractorysymptomsof
diminishedpositiveeffects.
Tranylcypromine[20-30mg] Moclobemide[150-300mg]
Melatonin MelatoninisassociatedwiththeCircadianrhythm.Lightisthemostpowerful
synchronizer.Whenlightentersthroughtheeyeitistranslatedviathe
Agonists Retinohypothalamictracttothesuprachiasmaticnucleuswithinhypothalamus.The
Suprachiasmaticnucleus,inturn,signalsthepinealglandtoturnoffMelatonin
ommon
C Production.Duringthedarknesstherearesignalstothepinealglandtoproduce
Features melatonin.Melatonin,inturn,canactontheSCNtoresetcircadianrhythm.
HerbalProduct:
● St.JohnsWort(ActiveCompound=Hyperphorin)
● InhibitsreuptakeofNE,5HT
NeweragentsfortreatmentofDepression
VORTIOXETINE SERTi+[5HT1A,5HT1B/1D] Theclinicalpropertiesofvortioxetinesuggest
[5-20 mg] partialagonist+5HT3 antidepressantpropertieswithoutsexual
Antagonist+5HT7A ntagonists dysfunction,pro-cognitiveeffects.
Itincreasesthelevelof5HT,NE,
DA,Histamine,Acetylcholine.
KETAMINE Bindstoopenchannel Alsohasactiononαreceptor,NET,SERT
[0.5-1mg/kg configurationofNMDA (Serotonintransporter),μ-opioidreceptor.
i.v.] receptor.Inthisreceptorthere
isacalciumchannelandinthat
channelthereisasitecalledas
PCP(wherephencyclidine
binds).Thisisthesiteof
binding.Ketamineblocksthis
Receptor.
DEXTROMETHORPHAN Hasthesameactionslike ItisaweakNMDAreceptorantagonist,with
ketamineandactsonall strongerSERT, αreceptor,NET,SERT,
thereceptorsasketamine. μ-opioidreceptor.
Itisbeingusedincombinationwith
Quinidine(asitincreasesitsbioavailability)
totreatpseudobulbaraffectandmayhave
sometherapeuticutilityindepressionas
well.
Ref:
● S tahl’sP
sychopharmacology4 thE dition
● M
audsleyP rescribingg uidelines1 2ea nd1 3e .
By:
ManishRoshanandRajvardhan
JuniorResident
Dept.ofPsychiatry,AIIMSDelhi