INTERAKSI OBAT DENGAN RESEPTOR

Oleh
Dr La Ode Sumarlin, M.Si

Program Studi Kimia

UIN Syarif Hidayatullah Jakarta
 Kinetika Interaksi Obat-Reseptor

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 Kinetics……..

• A+R [AR] Response

• Rate of association= k1 [A][R]

• Rate of dissociation = k2 [AR]
• At equilibrium:
– Rate of association = rate of dissociation
– k1 [A][R] = k2 [AR]
– k2/k1 = [A][R]/ [AR] = kD

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 Kinetics…. (some assumptions)

1. Reaksi antara agonis dan reseptor adalah reversibel

2. Kedua reaktan tersedia dalam bentuk bebas atau
terikat dan tidak termasuk bentuk lain, mis hasil
degradasi yang tidak terlibat dalam reaksi tersebut
3. Semua tempat di reseptor mempunyai affinitas
yang sama terhadap agonis dan independen

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 Plot terhadap waktu….
• d([AR]/dt = k1[A][R] – k2[AR]

• Plotting of [AR] as function of time yields an

hyperbolic curve and asymptotic relationships
for the formation of [AR] as equilibrium was
approach

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INTERAKSI OBAT-RESEPTOR

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PERBEDAAN KONFIGURASI

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EFEK Obat & Ikatan Protein

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Agonist & Antagonist

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 Affinity & efficacy

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Competitive antagonism

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 Tipe antagonism
• Competitive antagonism: atropine, ipratropium,
hyoscine for ACTH-receptor
• Irreversible antagonism: phenoxybenzamine for α-
adrenoceptor
• Non-competitive antagonism: Ca-channel blockers
• Chemical antagonism: protamine vs heparin
• Physiological antagonism: prostacyclin against
thromboxane A2

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Type of receptors

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Activation of receptor

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The role of Second messengers

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