Beta lactams and cell wall inhibitors Flashcards
Penicillins- MOA
D-Ala-D-Ala analog –> inhibit the enzyme transpeptidase resulting in inhibition of the transpeptidation rxn. activating autolysis.
Penicillins- MOR
MRSA/PRSP- change PBP
Salmonella- efflux pump
Pseudomonas- change porin structure so drug cant penetrate
staph and gram neg- plasmid betalactamases.
Penicillin- classifications
Narrow spectrum- penicillinase susceptible
Very narrow spectrum- penicillinase resistant
Extended spectrum- penicillinase resistant
Narrow Spectrum penicillins- drugs
Penicillin G
Penicillin V
pehnoxyethyl penicillin
Narrow Spectrum penicillins- resistant strains
S. aureus
N. gonorrhea
Very narrow spectrum- drugs
Methicillin Nafcillin Oxacilin cloxacillin dicloxacillin
Very narrow spectrum- uses
Staph
Penicillinase resistant
Extended spectrum- drugs
amoxicillin
ampicillin
pipercillin
ticarcillin
extended spectrum- prenicillinase resistant?
No they are susceptible to penicillinase thus are used with beta lactamase inhibitors
extended spectrum + beta lactamase inhibitor pairings
amoxicillin- clavulonic acid
ampicillin- sublactam
pipercillin- tazobactam
ticarcillin- clavulonic acid
Cephalosporins- how many generations
4
Cephalosporins- What are the characteristics of the generations
Gram + coverage dec as you move up
Gram - coverage inc as you move up
resistance to beta-lactamases inc as you move up
CNS penetration- inc as you go up
Cephalosporins- MOR
inactivated by beta-lactamases esp staphylococci
Modificatino of PBP
MRSA / PRSP drug permeability
Cephalosporins- 1st generation - drug names
Cefazolin
Cephalexin
Cephalosporins- 2nd generation- drug names
Cetotetan
Cetoxitin
Cefuroxime
Cefaclor
Cephalosporins- 3rd generation - drug names
cetoxamine
ceftazadime
cetraixone
ceoperazone
Cephalosporins- 4th generation- drug names, characteristics and uses
Cerfepime
combines gram positive spectrum of 1st generation with the characteristics of the other generations
Monobactams- MOA
binds to PBP3
Monobactams- names
Aztreonam
Monobactams- uses
Aerobic Gram negative rods including pseudomonas
synergistic with aminoglycosides
Carbapenems- MOA
similar to other beta lactams
Carbapenems- Uses
Broad spectrum- So thy are used as a shotgun approach gram + cocci: Staph and strep Gram - rods: pseudomonas Anaerobes doesn't work agaisnt MRSA and listeria
Carbapenems- MOR
resistant to most beta lactamases
BUT is synthetic to metalo-beta-lactamases
Carbapenems- drugs
Imipenem
Meropenem
Ertapenem
Classes of beta- lactams
penicillins
cephalosporins
Monobactams
Carbapenems
Vancomycin- MOA
Binds to D-Ala-D-Ala inhibiting transglycosylase= inhibition of transglycosylation = elongation is blocked and damages membranes
Vancomycin- MOR
plasmid mediated changes of D-Ala-D-Ala to D-Ala-D-lactate.
plasmid mediated changes in permeability
Vancomycin- uses
Gram +’s- MRSA and PRSP
Endocarditis
beta-lactamase producers in people with a penicillin allergy- E. Faecalis
Oral is used to tx pseudomembranous colitis b/c it gets to colon unchanged
Daptomycin- clearance and monitoring
cleared by kidney
monitor CPK levels b/c can cause myopathy
Daptomycin- uses
VRE
VRSA
Fosfomycin- MOA
inhibits enolpyruvate transferase- prevents formation of N-Acetylmuramic acid
Fosfomycin- uses
Concentrates well in the Urinary tract system, and is excreted at levels greater than MIC therefore is good for UTI
fosfomycin- MOR
dec in intracellular concentration
Cefazolin- class
1st generation Cephlosporin
Cefazolin method of admin
IV
Cefazolin Uses
Clean surgical prophylaxis
UTI- Staph Saprophyticus, strep, or E.Coli
PEcK- Proteus, E Coli, Klebsiella
Cephalexin- class
1st generation Cephalosporin
Cephalexin- administration
Oral
Cephalexin- uses
skin & soft tissue infections
oral Cephalosporins- excretion, how well are they absorbed, AE
renal excretion
Absorbed well
superinfection, pseudomembranous colitis
Narrow Spectrum Penicillins- Uses
Strep Penumo- pharyngitis and meningitis non penicillinase staph anaerobes- closridia, actinomycosis niserria menigitidis treponemes GAS
narrow spectrum penicillins- which organ failure prompts dose change
Renal
penicillin G- class
narrow spectrum penicillin
penicillin G- how well is it absorbed, route of admin
IV
poorly absorbed
Types of Penicillin G- repository forms
Have additive that helps them hang around in muscle and last longer
Procaine
Benzocaine
Penicillin V- route of admin
Oral
Penicillin V- AE
Neurologic changes and acting funny
Pehnoxyethyl Penicillin- admin
Oral
Very narrow spectrum metabolism, exception
All are metabolized by the liver except for Methicillin,