antibiotik penghambat sintesis protein
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Transcript of antibiotik penghambat sintesis protein
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Penghambat sintesis
protein:
a. Yang bekerja di
Ribosom subunit 30s
b. Yang bekerja di
Ribosom subunit 50s
http://www.pc.maricopa.edu/Biology/rcotter/BIO%20205/LessonBuilders/Chapter%2012%20LB/cow95289_12_01.jpg
What we are going to discuss?
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Penghambat Sintesis Protein
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW,
USA
Empat cincin heksasiklik pada golonganTetrasiklin
Penghasil klortetrasiklin = Streptomycesaureofaciens
Penghasil oksitetrasiklin = Streptococcus rimosus
Pada aminoglikosida, dua atau lebih gugusgula amino terikat lewat ikatan glikosidikpada inti heksosa (aminosiklitol)
Aminoglikosida dihasilkan olehStreptomyces sp.
Cincin lakton pada golongan Makrolida
Penghasil eritromisin = Streptomyceserytheus
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Proses Translasi
Ribosom bergerak disepanjang untai
mRNA,membaca kodon (mRNA menempel pd
ribosom).
Molekul tRNA membawa asam amino
Kodon tRNA cocok (A, T, G, C) dgn kodon mRNA
Asam amino ditambahkan pada rantai asam amino
(polipeptida)
tRNA dilepas untuk dipakai lg
tRNA membentuk urutan asam amino yg benar
untuk membuat protein
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Mekanisme Kerja
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Mekanisme Kerja
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• Eritromisin berikatan pd ribosom 50S danmenghambat translokasi kompleks tRNA-peptidadr lokasi asam amino ke lokasi peptida. akibatnyarantai polipeptida tdk dapat diperpanjang krnlokasi asam amino tdk dapat menerima komplekstRNA-asam amino yg baru.
• Kloramfenikol berikatan dgn ribosom 50S danmenghambat pengikatan asam amino baru padarantai polipeptida oleh enzim peptidil transferase
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• Tetrasiklin berikatan dgn ribosom 30S danmenghalangi masuknya kompleks tRNA-asamamino pada lokasi asam amino.
• Aminoglikosida (streptomisin) berikatan pd ribosom 30S yg menyebabkan kode pd mRNA salah dibaca oleh tRNA ,tjd protein abnormal dan non fungsional bagi sel bakteri.
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Mekanisme Kerja
http://medchrome.com/wp-content/uploads/2010/12/Antimicrobials-mechanism-of-
action.jpg
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Tetrasiklin
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Spektrum Tetrasiklin
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Aminoglikosida
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Spektrum Aminoglikosida
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Spektrum Aminoglikosida
• Masuk ke dalam sel melalui mekanisme
oxygen-dependent transport system
(transpor aktif) sehingga hanya efektif pada
bakteri aerob
• Dapat dikombinasi dengan penghambat
sintesis dinding sel, mis. Vankomisin,
sehingga memberikan efek sinergis
• Galur mikroba dianggap resisten bila:
kadar efektif streptomisin > 32 µg/mL
kadar efektif kanamisin dan amikasin > 16
µg/mL
kadar efektif tobramisin & gentamisin > 8
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http://medchrome.com/basic-science/pharmacology/antibiotics-inhibitors-of-protein-synthesis/
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Makrolida
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Spektrum Makrolida
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Klindamisin
• Mekanisme kerja serupa denganEritromisin
• Spektrum kerja: S. aureus, S. pyogenes, S. pneumoniae, S. viridans, danBacteroides fragilis
• Efek samping: clindamycin-associated pseudomembranouscolitis (gejala= demam, nyeriabdomen, diare dengan darah, dan lendir pada tinja) yang disebabkan oleh toksin C. difficile
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Kloramfenikol
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Spektrum Kloramfenikol
• Digunakan secara luas untuk hampir semua
gram positif dan gram negatif.
• Bekerja sangat baik pada bakteri anaerob.
• Sayangnya, toksisitasnya yang cukup tinggi
terhadap hati membuat antibiotik ini hanya
digunakan pada kasus infeksi akibat
mikroba-mikroba yang telah resisten
terhadap antibiotik lainnya.
• Bersifat bakteriostatik (secara umum) dan
bakterisid jika konsentrasi ditingkatkan
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Quinupristin/dalfopristin
• Quinupristin/dalfopristin merupakankombinasi dua antibiotik golonganstreptogramins denganperbandingan 30:70 (30% Quinupristin & 70% dalfopristin)
• Digunakan untuk mengatasiVancomycin-resistant Enterococcusfaecium (VRE)
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Oksazolidindinon
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW, USA
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Efek Samping
Finkel, Richard., Clark, Michelle A. Cubeddu, Luigi X., 2009, Lippincott's Illustrated Reviews: Pharmacology, 4th Edition, LWW,
USA
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Mekanisme Resistensi
a.Effluks aktif antibiotik: pada kasus resistensi
terhadap tetrasiklin dan kloramfenikol.
b.Hidrolisis obat oleh enzim yang dihasilkan
oleh bakteri: pada kasus resistensi terhadap
aminoglikosida
c.Berubahnya reseptor obat pada sel bakteri:
pada kasus resistensi terhadap makrolida
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