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HHD Pharm Cell Wall 2
Whitlock penicillins, cephalosporins etc
36
Medical
Professional
04/06/2009

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Term
pencillin
Definition
targe: pencillin binding proteins
action: bactericidal
properties:
substituent on 6-aminopenicllanic acid influence, porn penetration, susceptibility to beta lactamase
affinity for and pattern of binding to PBPs
Term
reistanace to penicillin
Definition
mostly beta lactamases
sometimes altered targets: MRSA, PRSP grm negative impaired access
efflux pumps

impaired access
efflux pumps
Term
penicillins are classified by
Definition
their abtibacterial specturm and their susceptibility to beta lactamase
Term
penicillin G affects
Definition
active vs. group A sterptococci
t pallidum
some enteroccoci
penumococci
meningococci
anaerobes
Term
very narrow specrtrun pencillinase resistant
Definition
nafcillin
oxacillin
staph uysed to be methicillin but nthat is renal toxic
Term
MRSA
Definition
no beta lactamase response due to change in target protein
Term
extended spectrum beta lactamase drugs
Definition
aminopenicllins, carboxypenicillins, ureidopenicllins
Term
aminopenicllins
Definition
ampicillin
amoxicillin

like penicillin G also active against some e.coli, h.influenzae, l.monocytogenes, p. mirablis and enterococcal
Term
carboxypenicillin
Definition
ticarcillin-extends to gram negative including pesudomonas and proteus species
Term
ureidopenicillin
Definition
klebsiella
pipercillinlike ticarcillin
Term
beta lactamase inhibitors
Definition
sulbactam
tazobactam
claculanic acid

contain an extra beta lactam ring that is a suicide substrate for beta lactamase
Term
a beta lactam drug plus a beta lactamase inhibotor can be
Definition
synergistic
Term
cephalosporins
Definition
target penicllin binding proteins (cell wall trasnpeptidases)
action: bactericidal
properties: substituent on 7 aminocephalosporic acid influence porin penetration
beta lactase susceptible
target binding

resistance: beta lactamase, altered target, impaired access

adverse effects:
hypersensitivity:imiited cross allergeicity with penicllins but do not use in patients with anaphylaxis
GI problems

parenteral admin
no CNS
renal excretion
Term
cephalosporins classified by
Definition
generation
Term
1st generation cephs
Definition
cefazolin
kills most gram positive coci (penicillinase producing bugs)
no kill MRSA no kill enterococus
plus ecoli, k. pneumonia, P. mirablis
Term
2nd generation
Definition
increased effect against gram negative organisms, such as H.influenzae and b. fragilis
Term
cefazilin
Definition
propholaxis before surgery
Term
third generation
Definition
big guns
gram negative action
eneteric and psudomonas
4th generation cefepinme for multi drug resistant
Term
1st generation
Definition
skin organisms
Term
2nd generation uses
Definition
respiraotry and mixed anerobes
Term
serious empirical therapy
Definition
3rd generation
Term
gonhorrohea
Definition
ceftriaxone 3rd generation
Term
monobactam (aztreonam)
Definition
target:PBP
action: bactericidal towards gram-aerobes

spectrum similar to aminoglycosides
synergistic with aminogylcosides
gram positive and anawerobes are itnriinsiclaly resistant
Term
aztreonam
Definition
not used as often as dr. whitlock would think
Term
carbapenam
Definition
imipenem/cilastatin
meropenem
ertapenem
target: penicllin binding proteins
action: bactericidal
properties kill many gram positive organisms and gram negative organisms as awell as some PRSP

resistance emerging-reducing drug use

low susceptibilty to beta lactamazes

adverse effects: hypersensitivity
GI
CNS (seizures esp. in renal failure0
IV administration
renal elimination
renal dehydropeptidase

uses: mixed infections, empirical therapy in immunocopmromised infections
Term
vancomycin acts at the
Definition
polymerization step
Term
vancomycin binds to the
Definition
d-ala d-ala of the cell wall and prevents polymerization
forms five hydrogen bonds
Term
gram negatives are resistant to vancomycin why?
Definition
it is too big to pass through the pores
Term
how can enterococci and stphylococci become resistant to vancomycin?
Definition
the terminal alanine turns into d-lac and this makes only four hydrogen onds and htis makes the bond very weak.

now the corss linking takes place
Term
vancomycin stat line
Definition
target: dala dala
action: bactericidal
properties: kills many gram positive cocci and bacilli
resistance: gram - and mutated strept and staph with d lactate plasmid
red man syndrome
ototoxicity
pharmacokinetics: poorbioavialbaility
adminster IV for
renal elimination

uses: serious infections with beta lactam resistant gram positive
possible nephrotoxicicity
Term
what to use against MRSA
Definition
Vancomycin
Term
what stops monomer production
Definition
fosfomycin
cycloserine (inhibits alanine)
bacitracin (inhibits phosphorylation)
Term
bacitracin
Definition
gram positve
neprotoxic
Term
cycolserine
Definition
cns toxic
dala dala stopper
tuberculosis
Term
fosfomycin
Definition
UTI
can be used during pregnancy inhibits enolpyuruvate transferase an early step in cell wall synthesis
Term
daptomycin
Definition
target cell membrane
action: bactericidal towards gram positive
concentration dependent killing with PAE
active veruss MRSA, VRSA

use: bada ass bugs endocarditis
resistance: staph aureus w decreased suceptibility during therapy
adverse effects: GI myopathy
pharmako: IV admin
urinary excretion
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