14.+psikofarmakologi

8/10/2019 14.+Psikofarmakologi

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PSYCHOPHARMACA


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classifcation I. Antipsychotics II. Antidepressants

III. Antianxiety and Drug orinso!nias

I". Drug or #ipolar disorder


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I. ANTIPSYCHOTIC (AP)

SYNONIMS: antischizophrenic drug neuro!eptics

"a#or tran$ui!izer C%ASSI&ICATION:

T#pica! AP : ch!orpro"azine 'uphenazine ha!operido! thioridazine

At#pica! AP :c!ozapine o!anzapine risperidone

$uetiapine aripriprazo!


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M CHANISM O& ACTION *!oc+ing the , - receptors , /

("eso!i"0ic 1 "esocortica! dep. path2a#) 3 At#pica! : c!ozapine

2ea+ ,- 0!oc+er potentantips#chotic 0!oc+ , 4 receptor and 5 HT -

6ar#ing pattern o7 se!ecti8it# in rec. 0!oc+inge9ect

Ta+e se8era! 2ee+s to c!inica! response e8en

though their rec. 0!oc+ing is i""ediate

The connection 0et2een rec. 0!oc+. acti8it# to

c!in. response : re"ains unc!ear


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PHA MACO%O;ICA% && CTS

S!o2 response to e de!usion

Antie"etic acti8it# : ? 0!oc+. , @ rec.

Th/effect70% of pts30% resistant


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$%%$C& O' R$C$P&RS "ary a!ong di(erent AP ) Chlorpro!a*ine+ , - /0H& 1A2D 12D -

) Haloperidol+ D 12 , - 2/0H& 1A2D - 2H - ) Clo*apine+

D3 , - 2/0H& 1A2D 1 D - ) Olan*apine+

/0H& 1A2H - 2 D 32D 1 2 , - 2D -


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) Aripipra*ole+ D 1 /0H& 1A 2D 3 2 , - H - 22D -

) 4uetiapine +H-2 , - 2M -56 2D 1 2/0H& 1A


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PSYCHO7O8ICA7 $%%$C&S In nonpsychotic patients Sleepiness5 restlessness5 autono!ic

e(ect unli9e sedati:e0hypnotics andi!paired per or!ance inpsycho!otor and psycho!etric testsIn Psychotic patients+ alle:iatepsychosis and i!pro:e per or!ance


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$7$C&RO$'C$PHA7O8RAPHIC$%%$C&S

Shi t the pattern o $$8 re;uencies+slo


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Phar"aco+ineticA0sorption and *ioa8ai!a0i!#

Chlorpro!a*ine a#sorption erratic interindi:idual :ariation up to >? old 5

#ioa:aila#ility+chlorpro!a*ine+ 1/@

thiorida*ine 6/@5#oth undergo frst pass!eta#olis!

haloperidol /@0 relation #et


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DIS&RIG &IO' Highly lipid solu#le


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Meta#olis! and $xcretion Most AP are co!pletely !eta#oli*ed Meta#olites usually not acti:e except

!esorida*ine


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A,A. 1 9ind o !otor distur#ance +

-FAcute dystonias K Par9inson0li9esy!pto!s L nigrostriatal #loc9 D 1 rec.5tre!or5 rigidity Eesp. ec9 !uscleF5a9atisiaEuncontrolla#le restlessnessF

&hJ anticholiergic drugs+ trihexyphenidyl #eperiden 5

diphenhydra!ine) 7e:odopa and dopa!inergic agonist

should ne:er #e use E


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AD$

1F &ardi:e dis9inesia0 in:oluntary !o:e!ent o ace

K li!#s5 appearing !onthsJyears a ter

treat!ent &hJ usually unsuccess ul

$xtrapyra!idal AD$ are less li9ely to occur


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G.Cardio:ascular ad:ersee(ects

Chlorpro!a*ine5 thiorida*ine+orthostatic hypotensionN!eanarterial pressure5 peripheralresistance and stro9e :olu!e N

H Rate 5 prolonged 4& inter:alsertindole5


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C.$ndocrine AD$ In


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D. Other AD$ anti!uscarinic ad:erse e(ects +

0 Al*hei!er E!e!ory i!pair!entF0 prostate hypertrophy0 glauco!a5

orthostatic hypotension + associated < al a

adrenergic #loc9ing e(ect L all and racturein the elderly

0-. p 3 -.Gertra! 8 Qat*ung -?th

ed.


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0 Indonesian population + asco!!on


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DR 8 CHOIC$ Gased !ainly on di(erences and AD$ In using typical AP 9no


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A representati:e group o AP drugs ispresented in+

Ta0!e - /. p 4B/.*ertra" ;atzung /D th ed.


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Su""ar# AP are :ery use ul + or pats K care gi:ers

less hospitali*ation

$(ecti:e in ?@ o pts

Atypical + pro#le!


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Su""ar# Atypical +

0 2 !eta#olic side e(ects +)


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C#tochro"e P 45D enz#"es in8o!8ed inps#chophar"aco!ogica! drug

-,B : a"itript#!ine desipra"ine i"ipra"ineha!operido! nortript#!ine

risperidone thioridazine8en!a7a


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4uestion to #e ans


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/. $xplain actors in uencing the useo drugs


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I. ANTI, P SSANTC7ASSI%ICA&IO'A.%irst 8eneration &ricyclic AD

I!ipra!ine A!itriptyline

) Clo!ipra!ineG. Second 8eneration+ ) A!oxapine5 Maprotiline5 &ra*odone5 Gupropion

C. &hird 8eneration+"enla axine5 Mirta*apine5'e a*odone K Duloxetine


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D. Selecti:e Serotonin Reupta9eInhi#itor ESSRIF

&!uo


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A. &ricyclic Antidepressant

Mechanis! o action Gloc9 the a!ine transporters Eupta9e pu!pF Gloc9 reupta9e o '$ E'$&F5 /H& ES$R&F E

dopa!inF catechola!ine+ !aniaN catechola!ine +depression

'ot clearly understood


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G.. Second generation oAntidepressant

AD that exhi#it less C"S side e(ects ) desi!ipra!ine+ !eta#olit o

i!ipra!ine ) nortriptyline+ !eta#olit o triptyline AD that exhi#it less C"S side e(ects #ut

!ore sedation+ tra*odone and #upropion A!oxapine a !eta#olite o

antipsychotic loxapine+ retain AP actiono the parent drug


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Maprotyline5structure rese!#lesdesi!ipra!ine is a potent '$

reupta9e inhi#itor5 causingsedation5anti!uscarinic andC"S side e(ects .


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C. &hird 8eneration o AD "enla axine+ 0 potent inhi#itor o serotonin transporterN K


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Mirtazapine "ore rapid in action no "ore eEcacious than

other A, !i+e!# to cause 2eight gain su0stantia! se


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C#tochro"e P 45D enz#"es in8o!8ed inps#chophar"aco!ogica! drug

-,B : a"itript#!ine desipra"inei"ipra"ineha!operido! nortript#!ine

8en!a7a


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,rug Interaction

high!# protein 0ound : 7ree drug in

co"0. : aspirinphen#!0utazone

inhi0itor o7 C#p -,B : nortript#!ine

desipra"in

TCA a!coho! se8ere esp. depression

TCA antih#pertensi8e adrenergicneuron

0!oc+ing agents (guanadre!): *P

3 Shou!d 0e "onitored c!inica!!#

conc. by

- fluvoxamine- paroxetine


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,. SS I (Se!ecti8e Serotonin eupta+eInhi0itor)

&!uo


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A,

== than TCA : C6S anti"usc.

acute to


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Indication : "aKor depression an


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AD$ Paroxetine+ highest a nity to serotonin

receptorsT.indirectly result in a net declinein dopa!inergic trans!ission leading toextrapyra!idal side e(ects Edistonia5a9athisiaF

Sexual unctionEdelayed eUaculation andanorgas!iaF

paroxetine2 uoxetine5 sertraline2u oxa!ine


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,. Monoa"ine o


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III. ANLIO%YTIC > HYPNOTIC, ;S

A. * N O,IA PIN S Mechanis" o7 action

7aci!itate ;A*A action ( receptor 0inding) :h#perpo!arization C! channe! opening

sa7e 0ecause its action depend onendogenous ;A*A 0ar0iturate : direct action in o8erdose

Phar"aco!ogica! e9ects reduction o7 an


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A, Acute o8erdosage

!ess dangerous on!# rare!# in the present o7 other CNS depressant

esp. a!coho! : se8ere resp. disorder orin COP,3 cou!d 0e counteract 0# antagonist 'u"azeni!

Co""on side e9ect : dro2siness con7usion i"paired coordination

a"nesia esp. 2ith !ong acting drug

i"pair"ent o7 Ko0 per7or"ance and dri8ings+i!!


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Chronic use :

To!erance : !ess than 0ar0iturate

,ependence de"onstrate 0# s#"pto"s o7 an


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Indication H#pnotic :

!orazepa" te"azepa"

3 not 7or chronic use to!erance An

14.+psikofarmakologi

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