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Reseptor MAOI

Reseptor MAOI. (Enzim sbg target aksi obat). MAO. Mono amin oksidase : Adlh enzim yg mengkatalisis oksidasi senyawa monoamin. Tdpt dlm bentuk terikat dg membran luar mitokondria pd hampir semua jenis sel. Menjadi target aksi obat gol MAOI Ada 2 subtype : MAO-A dan MAO-B.

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Reseptor MAOI

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  1. Reseptor MAOI (Enzim sbg target aksi obat)

  2. MAO • Mono amin oksidase : • Adlh enzim yg mengkatalisis oksidasi senyawa monoamin. • Tdpt dlm bentuk terikat dg membran luar mitokondria pd hampir semua jenis sel. • Menjadi target aksi obat gol MAOI • Ada 2 subtype : MAO-A dan MAO-B. • MAO-A : pd saraf astroglia, hati, saluran gastrointestinal, plasenta. • MAO-B : pd saraf astroglia dan platelet darah. • Penting dlm menginaktivasi neurotransmitter monoamin. MAO-A : mendegradasi dopamin, serotonin, norepinefrin, epinefrin. • MAO-B : mendegradasi dopamin, senyawa fenetilamin.

  3. MAO Inhibitor (MAOI) • Meningkatkan kadar neurotransmitter amin pd kondisi patologis (cth. Depresi) • Cth obat : tranilsipromin, fenelzin, Isokarboksasid. • Bersifat irreversibel dan tdk selektif, shg bnyk efek samping, cth. cheese reaction akibat interaksi dg makanan yg mengandung as. Amino tiramin. Peningkatan krisis hipertensi akibat terpicunya pelepasan norepinefrin o/ tiramin yg di-uptake o/ saraf.

  4. Cheese Reaction Saraf adrenergik Tiramin di usus Tirosin L-Dopa MAO di dinding usus (80% MAO-A dan 20% MAO-B) di liver (50% MAO-A dan 50% MAO-B Noradrenalin Uptake tiramin Memicu pelepasan NA Tiramin di darah Endothelial MAO-A Uptake NA

  5. Cheese Reaction • Normalnya tiramin yg ada pd makanan akn di inaktivasi o/ MAO di dinding usus dan di hati. • Tiramin yg tdk dimetabolisir akan msk ke dlm sirkulasi darah. Sebagian di metabolisir o/ MAO di sel endotelial vaskuler. • Jk asupan tiramin tinggi, tiramin di uptake o/ saraf adrenergik dan memicu pelepasan noradrenelin yg menyebabkan efek vaskuler  hipertensi • MAOI irreversibel meningkatkan kadr tiramin yg msk dlm sirkulasi shg memicu pelepasan NA di saraf. • MAOI reversibel dpt berkompetisi dg tiramin u/ berikatan dg enzim. Shg tiramin dimetabolisir dg normal o/ enzim.

  6. MAO Inhibitor • MAOI yg selektif thd subtipe MAO: • Selegilin, pargilin, rasagilin selektif menghambat MAO-B. Digunakan pd pengobatan pd penyakit Parkinson ( degenerasi saraf dopaminergik di otak yg menyebabkan gejala spt tremor, gerakan lambat dan kaku, ketdk seimbangan tubuh) • Obat ini kurang menyebabkan efek samping cheese reaction

  7. MAO Inhibitor • Inhibitor thd MAO-A ttp bersifat reversibel. (RIMA = reversible MAO-A inhibitor) Cth. Moklobemid Lebih aman dan tdk menyebabkan cheese reaction Tjd kompetisi antara obat dan tiramin shgtiramin dpt dimetabolisir dg cara yg normal di usus dan hati, tdk terakumulasi dlm sirkulasi.

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