Penecillin Flashcards
structure of penicillin
house with a garage
4-member B-lactam ring next to 5-member sulfa ring
B-lactam MOA
bind the cell wall and inhibit cell wall/peptidoglycan synthesis (penicillin binding proteins). inhibits transpeptidase which makes cross links in peptidoglycan.
B-Lactam: Bacteriocidal or Bacteriostatic? concentration dependent or time dependent? Elimination half-life? Elimination route (primarily)?
Bacteriocidal (except against entercoccus species)
Time-dependent
Which B-lactams aren’t eliminated by the kidney?
nafcillin, oxacillin,
ceftriaxone, cefoperazone
Most common mechanism of B-lactam resistance?
B-lactamase (hydrolyzes B-lactam ring)
B-lactamase activity in gram pos?
destroy B-lactams extracellularly
B-lactamase activity in gram neg?
destroy B-lactams in the periplasm (between inter and outer membrane) after B-lactams enter through porins
Natural penecillins examples (with attributes)?
IV: Penicillin G (still used) Benzapine (long-lasting, used 1x/week for latent syphilis) Procaine (short acting) Oral: Penicillin VK (more readily absorbed)
Bacteria treated by Natural Penicllins?
Gram+ = Group Strep and viridians strep
gram- cocci = neisseria spp
Anaerobes = clostridium (not C.Diff)
syphilis
Penicllinase-resistant Penicllin examples?
IV: Nafcillin, Oxacillin, Methicillin (Ox and Meth not used)
Oral: Dicloxacillin (not absorbed well orally)
Bacteria treated by Penicillinase-resistant Penicillins?
Gram+ = MSSA (Methicilline susceptible staph aureus)
made specifically for staph aureus’s penicillinase
What gene causes staph aureus to be resistant to penicillinase-resistant penicillin (MRSA)? And how does it convey resistance? What is only drug that can treat MRSA?
mecA gene. changes the binding site.
Ceftaroline.
Aminopenicillins: Why created? examples?
Gram neg activity (especially for Ecoli)
IV: Ampicillin
Oral: Amoxicillin (Ampicillin can be given but it isn’t)
Bacteria treated by Aminopenicillins?
Gram+ = same as penicillin, but better with enterococci. Only drug that treats Listeria monocytogenes (Gram+) Gram- = proteus mirabilis, Ecoli (most), salmonella, shigella, H.flu
Carboxypenicillins: why made? examples?
Gram neg bacteria
IV: Ticarcillin (only available in combination)