Antibiotics II: Inhibitors of Cell Wall Synthesis Flashcards
Beta-lactams: bactericidal or bacteriostatic?
bactericidal
Beta-lactams: time-dependent or concentration-dependent?
time-dependent
Mechanism of cell wall disruption by beta-lactams?
irreversibly inhibits transpeptidase; most effective in log phase of growth; target PBPs (penicillin-binding proteins)
G+ mechanism of resistance
secretion of beta-lactamases
standard, narrow-spectrum
Penicillin G, Penicillin V
Targets of penicillin
G+»>G-; anaerobic bacteria
DOC for syphilis
penicillin G
Penicillinase-resistant, narrow spectrum
Nafcillin
Use for Nafcillin
Pen G-resistant staph (MSSA) endocarditis, SSTIs (no G- activity)
Aminopenicillins, broad-spectrum
Amoxicillin
MOA for amoxicillin
activity against G- bacteria due to increased penetration through porins
Major use of amoxicillin
URIs
Antipseudomonal, extended-spectrum
ticarcillin, piperacillin
DOC for nosocomial G- infections
ticarcillin, piperacillin
beta-lactamase inhibitor
clavulanic acid
half-life of beta-lactams
short (30-90 min)
single dose repository prep given IM used for syphilis and prevention of rheumatic fever
pen G benzathine
Reaction common during therapy for syphilis
Jarish-Herxheimer (inflammatory response after lysis of organism)
large IV doses cause sodium overload –> CHF
ticarcillin
Pneumococcal, Streptococcal
Pen G
Meningococcal, Neisseria, syphilis, anaerobes, Listeria
Pen V
Staph. aureus, Staph. epidermis
Nafcillin
H. influenzae, S. pneumoniae, E. coli
Amoxicillin
P. aeruginosa, Enterobacter, B. fragilus, Klebsiella
Ticarcillin, Piperacillin
1st generation vs. 5th generation cephalosporins
increasing activity against G- bacteria and anaerobes
increasing resistance to Beta-lactams
increasing penetration into CNS
1st generation cephalosporin
cefazolin
used immediately before surgery to prevent surgical site infections
cefazolin
2nd generation cephalosporin
cefoxitin
3rd generation cephalosporin
ceftriaxone
Tx. of meningitis and gonorrhea + empiric chlamydia
ceftriaxone
4th generation cephalosporin
cefepime
empirical treatment of hospitalized patients when resistance due to extended spectrum beta-lactamases is suspected
cefepime
Uses - multi-drug resistant infections, anaerobic and mixed infections
imipenem/cilastatin
reason to combine imipenem with cilastatin
cilastatin is dipeptidase inhibitor that prevents renal inactivation
narrow spectrum drug with activity against G- aerobic bacteria
aztreonam
considered safe to give to patients with penicillin allergy
aztreonam
tricyclic glycopeptide antibiotic
vancomycin
MOA: prevent polymerization of cell wall precursors; blocks addition of NAM-NAG to polymer chain
vancomycin
active only against G+ bacteria (S. aureus and S. epidermis)
vancomycin
tx for VRSA and VRE
linezolid, daptomycin, quinupristin/dalfopristin
treatment of CDAD
vancomycin, metronidazole(1st choice)
alternative to penicillin in allergic patients w/ severe G+ infections
vancomycin
Adverse reactions to vancomycin
ototoxic and nephrotoxic; “red man syndrome”, thrombophlebitis
bactericidal phosphoenolpyruvate analogue
fosfomycin
treatment of uncomplicated G- UTIs
fosfomycin
inhibits production of murein monomers
fosfomycin
enters bacterium via glycerophosphate transporter
fosfomycin
inhibits bactoprenol dephosphorylation (lipid carrier)
bacitracin
drugs that make up Neosporin
bacitracin, neomycin, polymyxin B
Resistance to Vancomycin
variations in peptide terminus produce 1000-fold decrease in binding affinity