Penicillins (Lec 12) Flashcards
Bacteria are hypo-, hyper- or isoosmolar to host environment?
hyperosmolar
rigid cell wall keeps them from lysing
G+ and G- cell walls made of?
peptidoglycan
Peptidoglycan made of?
backbone of alternating sugars:
N-acetylglucosamine (NAG)
N-acetylmuramic acid (NAM)
4 AA chain linked to NAM
Peptide bridge cross-linking
3 stages of peptidoglycan assembly
1) sugar subunits assembled in cyto
2) sugars transported thru membrane to cell surface
3) cross-linking AA peptides
Drugs that inhibit cell wall synth (ICWS) are (U) what kind?
Cause death how?
bactericidal
osmotic lysis
Autolysins are?
remodeling enzymes in bacterial cell wall,
cleave peptidoglycan bonds for normal cell growth
Bactericides effect autolysins how?
allow autolysins to cleave bonds without subsequent wall repair,
wall weakens and allows lysis
ICWS drugs are primarily what kind?
β-lactams
4 specific β-lactams
1) penicillins
2) cephalosporins
3) monobactams
4) carbapenems
4 non-β-lactam ICWS
1) vancomycin
2) phosphomycin
3) bacitracin
4) cycloserine
What drug is the Natural Penicillin prototype?
Penicillin G
What drug is the Penicillinase-Resistant Penicillin prototype?
Nafcillin
What drug is the Extended Spectrum Penicillin prototype?
Ampicillin
Amoxicillin
What drug is the Antipseudomonal Penicillin prototype?
Piperacillin
Natural Penicillins provide highest activity against what type of bacteria?
G+, some G-
Natural Penicillins inactivated by?
β-lactamase (penicillinase)
Penicillinase-Resistant Penicillins is drug of choice against?
penicillinase-producing s. arueus (MSSA)
- > 20% of s. aureus types are resistant (MRSA)
MRSA is resistant to penicillins how?
Produces Penicillin-Binding Protein 2a (not β-lactamase) ->
β-lactam antibiotics don’t bind to PBP2a ->
can’t cause cell lysis
Extended Spectrum Penicillins provided extended coverage against?
G-, G+
Extended Spectrum Penicillins not active against what G- bacteria?
pseudomonas
Extended Spectrum Penicillins is drug of choice against?
listeria
h. plyori (+bismuth + metronidazole0
Ampicillin rashes are not caused by?
hypersensitivity (allergy)
Antipseudomonal Penicillins active against?
G-: extended spectrum
Antipseudomonal Penicillins DOC for?
pseudomonas aeruginosa (+ aminoglycoside)
Antipseudomonal Penicillins should be used in combination with what to prevent resistance?
aminoglycosides
Addition of β-lactamase Inhibitors to Extended Spectrum Penicillins and Antipseudomonal Penicillins does what?
extends their spectrums to include many bacteria previously resistance because of β-lactamase prodxn
β-lactamase combination drugs are NOT active against?
MRSA
methicillin resistant penicillinase producing staphylococci
Bacterial Resistance to Penicillins:
5 methods
1) β-lactamase inactivates drug
2) G- decreased permeability to drug
3) Alternate PBPs that prevent drug binding
4) Drug inability to activate autolytic enzymes
5) Bacteria lack peptidoglycan wall
Pencillin toxicity caused by? (4)
1) allergy
2) electrolyte imbalance
3) GI disturbances
4) superinfections
PCN is DOC?
all G+ strep
enterococcus