Cell Wall Inhibitors Flashcards
Classes of beta lactams
Penicillins
Cephalosporins
Monobactams
Carbepenems
Penicillins- MOA
Resemble D-ala-D-ala- bind to transpeptidase and inhibit the transpeptidation reaction
Activate autolytic enzymes
Penicillins- Static vs Cidal
Cidal
Penicillines- kinetics
metabolized in liver- Req dose change in renal failure
get into bile
DO NOT GET INTO CNS (unless there is inflammation) AND ACID LABILE SO INACTIVE IN ABSCESSES
Penicillin- excretion
Renal used to be given with probenecid to keep it in the blood
Penicillin- AE
IgE mediated anaphylaxis IgM/G- Type III hypersensitivity Diarrhea neuromuscular irritability hematologic changes drug fever interstian nephritis
Narrow spectrum penicillins- Drugs
Pen G- Procaine, Benzocaine
Pen V- Phenoxy Penicillin
Narrow Spectrum- use
Strep (GAS) non penicillinase staph aureus Anaerobes- actinomyces, clostridium N. Meningitis Treponemes
Narrow spectrum- when change dose
renal failure
Pen G-
IV
procain and benzathine- repository forms for longer half life
Procain causes strange beh
Pen V
oral
phenoxy penicillin
Very Narrow Spectrum- drugs
Methacillin Nafcillin Oxacillin Cloxacillin Dicloxacillin
Very narrow- uses
staph except MRSA
Very Narrow- IV vs Oral
IV- methicillin, nafcillin, oxacillin
Oral- nafcillin, oxacillin, cloxacillin, dicloxacillin (clox and diclox- longer t1/2)
Very narrow -Kinetics
change dose in liver failure
Methacillin
change dose in Renal failure
AE- interstitial nephritis, rarely used except in lab tests
Nafcillin
MAJOR dose change in liver failure
AE- Neutropenia, Phlebitis
Oxacillin
AE- neutropenia, LFT’s
Extended Spectrum
Amoxicillin
Ampicillin
Pipercillin
Ticarcillin
Ampicillin/ Amoxicillin- use
com acquired- ENT and lung infxns
Ticarcillin/Pipercillin- use
serious gram- infxn use with aminoglycosides- E. Faecelis, Pseudomonas B. Fragilis Indole + proteus
Extended spectrum- kinetics
Change dose in renal failure- except piperacillin
Amoxicillin
oral
AE- major acuse of pseudomembranous colitis
Ampicillin
IV
Can be a major cause of pseudomembranous colitis
Pipercillin
IV
Ticarcillin
IV
Extended spectrum + beta lactamase inhibitor
Amoxicillin + CA
Ampicillin + Sublactam
Pipercillion + tazobactam
Ticarcillin + CA
Extended spectrum+ beta lactamase uses
used when dealing with beta lactamase producing organisms bacteroides moraxella H. Flu S. Aureus
Amox + CA
Oral
Upper and lower RTI- H. flu, moraxella
AE- diarrhea, pseudo membranous colitis
Amp + sublactam
IV
Dirty surgical prep
aspiration pneumonia
pip+ tazo
Ticar + CA
IV
shotgun therapy before know exact pathogen
Cephalosporins- trends
1 --> 3rd gen dec in G+ coverage, but inc in G- inc in CNS penetration inc resistance to betalactamase 4th gen combines best of 3 w/ gram + coverage 5th gen
Cephalosporins- kinetics
Renal Excretion with major dose change in renal failure except- cefotaxime, ceftriaxone (they are hepatic)
Cephalosporin AE
super infection
pseudomembranous colitis
1st gen cephalosporin- drugs
Cefazolin
Cephaloxin
1st gen cephalosporin- use
Gram +
cost effective
Cefazolin
staph/strep
clean surgical prophylaxis
possible UTI
2nd gen cephalosporin
Cefotetan
Cefoxitin
Cefuroxime
Cefotetan
ANTABUSE LIKE RXN WITH ALCOHOL t 1/2= 3.5 hours comm acquired aerobes serious intrabdominal and pelvic infections combination of anaerobes- bacteroides
Cefoxitin
used for- intraabdominal/ pelvic infections
combination of anaerobes- bacteroides
comm acquired aerobes
Cefuroxime
can get into CNS
Staph/ Strep, serious pediactric meningitis and pneumonia
serious adults pneumonia
3rd gen cephalosporins
Cefotaxime
Ceftazadime
Ceftriaxone
Cefoperazone
3rd generation distribution
CNS
3rd gen useage
hospital acquired gram - EXCEPT PSEUDOMONAS
use in combo with other agents against anerobes
Cefotaxime
significant hepatic metabolism- so less dose change during renal failure
DOC IN MENINGITIS
Ceftriaxone
Biliary excretion t1/2= 8 hrs cost effective in outpt therapy same use as cefotaxime AE- BILLIARY SLUDGE, diarrhea
Cetazidime
PSEUDOMONAS- synergy with aminoglycosides against pseudomonas
hospital acquired gram-
Cefoperazone
Antabuse like rxn to alcohol
4th gen- drug
Cefepime
Cefepime
combines gram + of 1st gen w/ other charecteristics- H. flu, pseudomonas
only use for serious hospital acquired infections
5th gen
Cefatroline- can be used against MRSA
Monobactam
Azobactam
Monobactam- admin
IV
monobactam- use
aerobic gram negative rods (only aminoglycosides also work on these)
Monobactam- advantages
Aminogloycosides are the only other drug that work on aerobic gram negative rodes, but are assoc with nephrotoxicity, monobactams avoid this
NO CROSS ALLERGENICITY WITH OTHER BETA LACTAMS
Carbepenems
Imipenem
Meropenem
Ertapenem
Carbepenems- admin
IV
Carbepenem- spectrum
broadest spectrum penicillins work agaisnt anything except MRSA…ish
Carbepenems- use
Shotgun therapy
can cause emergence of resistant MRSA or Candida
Imipenem
UTI when combined with Cilastatin- for urinary concentration
AE- seizures esp in those with renal damage or elderly
Ertapenem
out pt IV tx
Vancomycin- admin
IV- systemic infxn
Oral- pseudomembranous colitis
Vancomycin- kinetics
t1/2= 6 hrs so can be given every half day or day
Renal excretion- adjust in renal failure
distributes everywhere except- CNS, eye, prostate
Vanco- spectrum
cidal for all gram +
Vanco- use
MRSA/MRSE/PRSP
serious staph/strep when allergic to beta lactams
bac endocarditis
pseudomembranous colitis
Vanco- AE
REDMAN SYNDROME- erythema, itching, hypotension- histamine mediated, means administering the drug to quickly
Dose related nephro and ototoxicity- related to time in trough
Vanco- MOA
binds to D-ala-D-ala- inhibiting transglycosylation
Vanco MOR
pasmid mediated changing of D-ala-D-ala to D-ala-D-lactate
Telavancin
Vanco on steroids
inc MRSA activity AND nephrotox
CI in pregnancy
Daptomycin- kinetics
t1/2 = 9 hrs
concentration dependent killing with long post antibiotic effect= 1/day dosing
renal excretion
Daptomycin- spectrum
cidal against gram +
Daptomycin- use
resistant gram + infxn esp when need cidal ie infective endocarditis
Daptomycin- CI
inactivated in lung so dont use for lung infxn (inactivated by surfactant)
Daptomycin- AE
skeletal muscle myalgia, waekness and inc muscle enzymes
synergistic tox w/ statins
watch kidney enzymes
Fosfomycin- MOA
inhibits enolpyruvate transferasae- preventing formation of N- acetylmuranic acid so bac cant make the peptidoglycan background
Fosfomycin- use
concentrates in Urinary system so good for UTI.
