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Target and mechanisms
Common routes of resistance.
Groups of bacteria effected and spectrum of activity
Target: Cell wall
Resistant to Blactamases produced by Staphylococcus.
Target: Penicillin binding proteins (PBPs) interfere with production of peptidoglycan and cell wall synthesis.
Target: Cell wall
Mechanism: Penicillin binding proteins (PBPs) interfere with production of peptidoglycan and cell wall
Modification of PBP - occurs in Staphylococcus aureus. Outer membrane most gram negative bacteria inherently impermeable to these drugs. B-lactamase activity. Modification of PBP - occurs in Staphylococcus aureus and Enterococci. Outer membrane most gram-ve
Grouped 1-3, with decreasing activity against gram positive and increased activity against gram
bacteria inherently impermeable to these drugs.
Target: Cell membrane
Gram positive bacteria intrinsically resistant as do not have LPS.
Mechanism: target LPS in outer membranes
Gram negative. Use requires injection.
LPS modification. Sulphonamide
A number of structures for this groups this is the simplest.
Target: DNA synthesis Mechanism: Competitive blocking of paraamenobenzoic acid (PABA) incorporation to folic acid. Inhibit Dihydrofolate synthase (DHF).
Altered by synthetic pathway employing sulphonamide resistant enzyme.
No longer used except in conjunction with trimethoprim.
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