Wall Bacteria Cell-1

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Farmakologi dan Toksikologi 3

2nd meet
1. Inhibition of synthesis or damage to the peptidoglycan cell wall
2. Inhibition of synthesis or damage to the cytoplasmic membrane
3. Modification in synthesis or metabolism of nucleic acids
4. Inhibition or modification of protein synthesis
5. Modification in energy metabolism
R. F., Clark, M. A., dan Cubeddu, L. X., 2009. Pharmacology. Lippincott Williams & Wilkins.
Wecker, L., Crespo, L. M., dan Brody, T. M., 2010. Brodys human pharmacology: molecular to clinical. Philadelphia, PA: Mosby/Elsevier.
Wecker, L., Crespo, L. M., dan Brody, T. M., 2010. Brodys human pharmacology: molecular to clinical. Philadelphia, PA: Mosby/Elsevier.
Therapeutic Overview
-Lactams

Penicillins, Cephalosporins, Carbapenems, and Monobactams

Bactericidal: inhibit many gram-positive and gram-negative organisms

Agents differ by:


Organism inhibited
Pharmacokinetics
Bacterial resistance
VancomycinBactericidal; inhibits many methicillin-resistant
staphylococci

BacitracinBactericidal; topical use only for gram-positive bacteria


Wall structure of microbial cells
NAM: N-Acetylmuramate
NAG: N-Acetylglucosamine
1. Penicillin-binding proteins
2. Inhibition of transpeptidase:
3. Production of autolysins (not affected by -
Lactams)
NAM & NAG dihubungkan o/peptida yg
kecil sehingga membentuk ikatan yg kuat
krn d perantarai o/serangkaian enzim
(trans-, carboxy & edopeptidase) PBP
PBP bekrja mengkatalisis pembentukan
ikatan silang antara rantai peptidoglikan
Obat AB analog dgn PBP
Enzim transpeptidase bekerja
mengkatalisis reaksi transpeptidasi.
Enzim transpeptidase pd membran
sitoplasma dpt mengikat AB shg enzim tdk
dpt mengkatalisis reaksi transpeptidasi
ik. Silang tdk terbentuk dinding rapuh
Komplek protein transpeptidase dan AB
beta lactam akan menstimulasi
pembentukan autolisins digesti dinding
sel bakteri
1. Altered PBPs
2. production of -Lactamase

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