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AGONIS-ANTAGONIS
FARMAKODINAMIKA
Fifteen Aprila F., S. Farm, Apt
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Pengertian AGONIS?
Agonis PARSIAL
Pengertian ANTAGONIS
Antagonis FISIOLOGIK
Antagonis RESEPTOR
Antagonis KOMPETITIF
Antagonis NON KOMPETITIF
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Receptor
Drugs
Some Effect
A Cell
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Obat yg bila menduduki reseptormenimbulkan ef farmakologi scr intrinsik.
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Agonis lemah
Ar/ agonis yg memp aktvitas intrinsik atau
efektivitas yg rendah shg ef maksimalnya
lemah.Disebut jgantagonis parsial
Obat ini mengurangi ef maksimal yg
ditimbulkan agonis penuh.
Ex : Nalorfin (antagonis/agonis parsial u/resptor morfin)
AGONIS PARSIAL
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menurunkan aktivitas intrinsik
menurunkan afinitas
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Kurva X : Efek maksimal yg dihslkan oleh A
Kurva Y : Efek maksimal yg dihslkan oleh A + Agonis
dg dosis yg menimbulkan efek maksimal < Emax (A)
Kurva Z : Efek maksimal yg dihslkan oleh A + Agonis
dg dosis yg menimbulkan efek maksimal > Emax (A)
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Drugs A
Antagonist
Dude, youre
in my way!
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Obat yg menduduki reseptor yg
sama, tp scr intrinsik tdk mampu
menimbulkan efek farmakologi.
So: antagonis akan menghalangi ik
reseptor dg agonis shg kerja agonis
terhambat.
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ANTAGONIS FISIOLOGIKTjd pd organ yg sama, pd sistem reseptoryg berbeda.Ex : efek bronkokonstriksi histamin pd bronkus dan
bronkodilatasi adrenalin (adrenoreseptor )pd bronkus.
ANTAGONIS PD RESEPTORTjd mll sistem reseptor yg sama.
Ar/ antagonis mengikat reseptor d tmp ikagonis (receptor/active site).Ex : efek histamin pd rx alergi dpt diatasi dg pemberianantihistamin yg bekerja pd reseptor yg sama)
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Antagonis KOMPETITIF
antagonis berik dg receptor site scr
reversibel shg dpt digeser o/ agonis kdr
tinggi. (Ex : -bloker & antihistamin)
Antagonis NON KOMPETITIF
penghambatan ef agonis tdk dpt diatasi dg
me kdr agonis (sifatnya irreversibel),akibatnya ef mak akan berkrg, ttp afinitas
agonis thd reseptornya tdk berubah.
(Ex : fenoksibenzamid pd reseptor adrenergik)
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Afinitas agonis thd
reseptor menurun
Kurva bergeser sejajar
ke kanan
Ef maksimal yg dicapai
agonis sama
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Ef maksimal yg dicapai agonis berkrg
Afinitas agonis thd reseptor tdk
berubah.
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Biol
ogicalEffect
Drug Concentration
Effective Dose
Drug Alone
Drug +Non-competitive
AntagonistDrug +
PartialAgonist
Drug +Competitive
Antagonist
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