Farmakodinami Maret 2015
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Transcript of Farmakodinami Maret 2015
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FARMAKODINAMI
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DOSIS (R/)
DOSIS YG DIMINUMFaktor-2 FKA D M E
KONSENTRASI OBAT DI TEMPAT KERJA
Fisio o!ikPato o!ikG"#"tikU$%rI#t"raksi
Faktor-2 FD r"s"&tor 'o$"ostatik
EFEK / RESPON P
terapeutik toksik
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Sinergisme : Efek kombinasi dari 2 (/lebih)macam obat yang saling menunjangAddisi : Bentuk sinergisme obat dimanaefeknya merupakan efek penambahanobat tersebut (mis !"!#2)
$otensiasi : Bentuk sinergisme obat dimanaefeknya lebih besar dari efek
penambahan masing%masing obat(mis !"!&2)Antagonis : Efek 2 macam obat yangberla'anan
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Bound Free Free Bound
LOCUS OF ACTION“RECEPTORS ”
TISSUERESERVOIRS
SYSTEMICCIRCULATION
Free ru!
Bound ru!
ABSORPTION E"CRETION
BIOTRANSFORMATION
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OBAT + RESEPTOR
INTERAKSI OBAT DENGAN RESEPTOR PADA
SEL SUATU ORGANISME
PERUBAHAN BIOKIMIAWI DAN FISIOLOGI
RESPON
(KHAS UTK MASING-MASING OBAT)
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Far$ako i#a$i $"$&" a*ari +E,"k o at ( ioki$ia.i ,isio o!is) &a asisti$ io o!ik s"rta $"ka#is$" k"r*a#0a
E,"k o at +
S" a! "sar ok i#t"raksi o at !r"s"&tor1 s" a!ia# a!i t k $" a %i r"s"&t
R"s"&tor o at +Makro$o "k% (&rot"i#) &a a sisti$
io o!ik 0a#! a&at $"r% a' ,%#!si sisti$ts ok i#t"raksi#0a ! o at
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RESEPTOR UNTUK LIGAND ENDOGEN
OBAT hormon
nerotr n!m"ter
AGONIS # SUBSTANSI $ANG EFEKN$A MEN$ERUPAI
SEN$AWA ENDOGEN%LIGAND ANTAGONIS # MENGHAMBAT EFEK SUATU AGONIS DI
TEMPAT IKATAN AGONIS
Kom&et"t"'
Non om&et"t"'
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Agonis obat yang mampu berikatandg reseptor dan menimbulkan efek
(afinitas +, aktivitas intrinsik +)
Antagonis obat yang mampu berikatandg reseptor tetapi tidak dapat menimbulkan efek
(afinitas +, aktivitas intrinsik - )
Antagonis kompetitif ikatan dg reseptor dpt digeser oleh agonis
(Emax sama, ED5 beda)Antagonis ireversibel ikatan dg reseptor kuat,
Emax lebih rendah
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*+,-.*A A*,A0.*-S,S
! $hysiologic Antagonists
2 +hemical Antagonist
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Agonists and Antagonists
$hysiologic A*,A0.*-S,A drug that binds to a non%related receptor1 producingan e ect opposite to that produced by the drug ofinterest
-ts intrinsic acti3ity is # !1 but on another receptor
Glucocorticoid Hormones Blood Sugar
Insulin Blood Sugar
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Agonists and Antagonists
+hemical A*,A0.*-S,A chelator (se4uester) of similar agent that interactsdirectly 'ith the drug being antagoni5ed to remo3e it orpre3ent it from binding its receptor
A chemical antagonist does not depend on interaction'ith the agonist6s receptor (although such interactionmay occur)
Heparin, an anticoagulant, acidicIf there is too much bleeding and haemorrhaging
Protamine sulfate is a base. It forms a stable
inactive complex with heparin and inactivates it.
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!olar !olar
!olar !olar
"onpolar "onpolar
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RESEPTOR RESEPTOR
#RESEPTOR TRANSMEMBRAN$ I%T& EN'IM$ %ANAL ION$ I%T& ($PROTEIN
#RESEPTOR I SITOSOL
%OMUNI%ASI SEL
INTRA SEL ANTAR SEL
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TRANS U%SI SINYAL
MOLE%UL LI(AN ) ST *essen!er
RESEPTOR
+ TAR(ET SEL,
EFE%TOR - nd *essen!er+.AMP/ IP0/ A(,
EFE% BIOLO(I
Komunikasi sel
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+lassi7cation 8eceptor
,ransduction9echanisms1. Ion channel linked receptors e.g. Achnicotinic (Na + ) and GABA (Cl -)
2. G protein & second messenger generationaden!late c!clase stim"lation or inhi#ition -cA$%
g"an!late c!clase - cG$% phospholipase C -
I% 'AG. ome receptors are themsel es protein
kinases*. Intracell"lar receptors (e.g. corticosteroids
th!roid hormone)
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#ransmembrane $ignaling#ransmembrane $ignaling
%e&hanisms%e&hanisms drug
'ut'ut
nn
genegene
!!
**
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Re*e&tor *t" t"on
o' G &rote"n
G &rot re, . t"ono' n en/0me or "on *h nne.
1h n,e "n the*on!2o' !e*on3me!!en,er
In *t" t"onme*h n"!m
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The M 4or E''e*tor! n3 Intr *e.. . rThe M 4or E''e*tor! n3 Intr *e.. . r
Se*on3 Me!!en,er! "n GP1R S0!tem!Se*on3 Me!!en,er! "n GP1R S0!tem!
Effe&tor
adenylyl &y&lase
phospholipase
nd messenger
&y&li& A%! (&A%!)
&al&ium, DA , and
phosphoinositide ( !.)
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O1at dan E2ek
D + R DR Efek
a!onis
adr1eta
( P (TP ( P
(s
(TP
Adeni3atsik3ase
ATP .AMP
γ
En4i*
En4i*$PO5
EFE%
R-C-Protein kinase
-C
-R
ATP
A P
M *h "! ' 5 6 * & * " " "
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Me*h n"!m o' 5et -6 re*e&tor *t" t"on "n* r3" * m !*.e
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E''e*t o' 5et -7 re*e&tor *t" t"onon !mooth m !*.e
ff f l h k k ( )
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Effe&t of alpha-/ 0muskarinik.(%.) re&eptor a&tivationof smooth mus&le &ontra&tion
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ntra&ellular %e&hanism1 $teroid
P. !mP. !m
22
"u&leus"u&leus
2 2
**************************
2"A2"A
m2"Am2"A!rotein!rotein
Effe&tsEffe&ts
drugdrug
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Speed of responses
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Agonist 3s antagonist
A!% 6)
% $)A!
Ant% 6)
% $)
6
6
Response
Ant
R
R
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A,on"!t 8 Ant ,on"!t
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Agonist Antagonist
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PENGATURAN FUNGSI RESEPTOR
3 4A $ A# $E4 D 2A" $A" #E2 $ %E"E2 $ '4E6A '" $" A DE$E"$ # $A$
3 4A 2A" $A" A" !ADA 2E$E!#'2 3E27 2A" $E A2A72'" 7, % $A4 !E%3E2 A" 34' 7E2 8A" 7A !A"8A"$ !E2$E"$ # 9 #A$ (6 !E2A7# 9 #A$) #E26ADA! A '" $
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-ndi3idual patient3ariations in drugresponses
Body 'eight andcomposition
Age ofclient(young andold);iet and *utrition
Ethnic origin0enetics
$athophysiology(eg
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OBAT $ANG BEKER9A TIDAK MELALUI RESEPTOR #
!E2 3A6A" A$A% 3A$A A"#A$ DA %g('6) , Al ('6).
!E2 3A6A" $ :A# '$%'# 7 D 2E# 7 '$%'# 7
2EA,%A" #'4
4 $E2'4 %E" 2A" 'EDE%$E2E32A4
A" A" : " $ %E%32A" A"E$#E$ % % E#E2
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= B *0A* ;.S-S%8ES$.*0raded dose%responses0raded dose%responses
:ull agonist
Agonist &on&entration
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>Ema? E; @
4og &on&entration
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Ther &e t"* n3 To:"* E''e*t! re
Do!e-Re. te3# Pheno5 r5"t .
S.ee&S.ee& De thDe th
Dose of !henobarbitalDose of !henobarbital
ED5ED5 4D54D5
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Autonomic $harmacology
+entral *er3ous System (+*S)$eripheral *er3ous SystemSomatic *er3ous SystemAutonomic *er3ous System (A*S)
Sympathetic Branch$arasympathetic Branch
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Autonomic *er3ousSystem +haracteristics
“ F i g h t o r
F l i g
h t ” “F
eedorBreed”
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A*SAnatomy $hysiology
,he ner3es of the A*S e?it the +*Sand subse4uently enter speciali5edstructures called “autonomic ganglia”
$reganglionic 7bers$ass bet'een the central ner3ous system and
the ganglia$ostganglionic 7bers
$ass bet'een the ganglia and the e ectororgan
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Sympathetic 3ersus$arasympathetic
Sympathetic gangliaocated close to the spinal cord ormid'ay bet'een the spinal cord andthe e ector organ
$arasympathetic gangliaocated close to or 'ithin the 'alls of
the target organs
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+holinergic and Adrenergicibers+holinergic
ibers that release acetylcholineAll preganglionic and postganglionic of theparasympathetic di3ision
Adrenergicibers that release norepinephrine
9ost postganglionic 7bers of thesympathetic di3ision are adrenergic1 butsome are cholinergic
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*eurochemical ,ransmission
*o actual physical connection e?istsbet'een t'o ner3e cells or bet'een a ner3ecell and the organ it inner3ates
SynapseSpace bet'een ner3e cells
*eruroe ector junctionSpeciali5ed synapse bet'een t'o ner3e cells or aner3e cell and an organ
*eurotransmitter+hemical messenger that conducts a ner3ousimpulse across a synapse
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; ;
;
;
;
;
;
;
;
;
MEDULLA
SPINAL1ORD
A1H NI1
A1H NI1
A1H NI1
A1H NI1
A1H NI1
A1H NI1
A1H MUS
A1H MUS
ADRENAL MEDULLA
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*eurotransmission
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*eurotransmitters
Acetylcholine$reganglionic ner3es of sympatheticner3ous system$reganglionic and postganglionic ner3esof the parasympathetic ner3ous system
*orepinephrine$ostganglionic ner3es of the sympatheticner3ous system
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Acetylcholine
or cholinergic synapsesacetylcholine molecules combine 'ithcholinergic receptor molecules
*icotinic 8eceptors$roduces an e?citatory response
9uscarinic 8eceptors$roduce an e?citatory or inhibition1 dependingon 'here the target receptors are found
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*orepinephrine
or adrenergic synapsesnorepinephrine molecules combine'ith adrenergic receptor molecules
Alpha 8eceptors
Blood 3esselsBeta 8eceptors
=eart ungs
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farmako?fk@unibra @a&@idnurdianafarmako?yahoo@&om