Professional Documents
Culture Documents
ANTIBAKTERI
(pengantar antibiotik & penghambat sintesis dinding sel bakteri) Dripa Sjabana, dr., M.Kes
dripa@fk.unair.ac.id
PO4 3-
peptidoglikan protein
RNA DNA
glukosa
NH4 +
Folat Analog pirimidin & purin
SO4 2-
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dripa@fk.unair.ac.id
PBP
Katzung (2004)
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TRANSPEPTIDASE
Figure 44.3 Schematic diagram of the biosynthesis of peptidoglycan in a bacterial cell (e.g. Staphylococcus aureus) with the sites of action of various antibiotics. The hydrophilic disaccharide-pentapeptide is transferred across the lipid cell membrane attached to a large lipid (C55 lipid) by a pyrophosphate bridge (-P-P-). On the outside, it is enzymically attached to the 'acceptor' (the growing peptidoglycan layer). The final reaction is a transpeptidation, in which the loose end of the (gly)5 chain is attached to a peptide side-chain of an M in the acceptor and during which the terminal amino acid (alanine) is lost. The lipid is regenerated by loss of a phosphate group (Pi) before functioning again as a carrier. (M, N-acetylmuramic acid; G, N-acetylglucosamine.) dripa@fk.unair.ac.id
Downloaded from: StudentConsult (on 3 May 2005 08:34 AM) 2005 Elsevier
-lactam AB
inhibitor
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Autolytic enzimes
bacterial
bacterial lysis
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PENICILLIN
Subsituted 6-aminopenicillanic acid
CEPHALOSPORIN
Subsituted 7-aminocephslosporic acid
Figure 44.2 Schematic diagram of a single layer of peptidoglycan from a bacterial cell (e.g. Staphylococcus aureus) showing the site of action of the β-lactam antibiotics (more detail in Fig. 44.3). In Staphylococcus aureus the peptide cross-links consist of five glycine residues. Gram-positive bacteria have several layers of peptidoglycan. (NAMA, N-acetylmuramic acid; NAG, N-acetylglucosamine.)
A = thiazolidine ring
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Downloaded from: StudentConsult (on 3 May 2005 08:34 AM) 2005 Elsevier
Katzung (2004)
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Penicillin
Penicillin G (iv), VK (po) Antistaphylococcus
Cloxacillin, dicloxacillin (po) Nafcillin, oxacillin (iv)
MONOBACTAM
Subsituted 3-amino-4-methylmonobactamic acid
Extended-spectrum
CARBAPENEM
Subsituted 3-hydroxyethylcarbapenemic acid
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Cephalosporin
1st generation:
Cefadroxil, cefazolin, cephalexin, cepharpirin, cephradine Very active againts gram(+) cocci.
(1)
Cephalosporin
3rd generation:
(2)
2nd generation:
Cefaclor, cefamandole, cefonicid, cefuroxime, cefprozil, loracarbef, ceforanide, cephamycins, cefoxitin, cefmetazole, cefotetan Extended gram(-) coverage
Cefoperazone, cefotaxime, ceftazidime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, ceftibuten, moxalactam Expanded gram(-) coverage, + bbb.
4th generation:
cefepime More resistant to hydrolysis by chromosomal beta-lactamases (eg. enterobacter) and some extended spectrum betalaktamases
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Monobactam
Aztreonam Spektrum ~ aminoglycoside
Jelaskan hubungan:
Sulphonamide PABA Folate Bakteri vs. manusia ?
dripa@fk.unair.ac.id
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Jelaskan hubungan:
Trimethoprim Tetrahydrofolate Thymidylate Dihydrofolate reductase Bakteri vs. manusia ?
Bacaan lanjut
Katzung BG ed.(2004). Farmakologi Dasar & Klinik, ed.8, buku 3. Jakarta: Salemba Medika, hal.3-33. Rang HP et al. (2003). Pharmacology, ed.5. London: Elsevier, p.620-643.
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