farmakodinami maret 2015

8/16/2019 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

farmakodinami maret 2015

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