Antagonisme Farmakodinamika New

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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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