48/49: Antibiotics II Flashcards
peptidoglycan is composed of…
chains of repeating monomers of the disacchride subunits: NAM-NAG-pentapeptide
enzymes join monomers together to form NAM-NAG chains
transglycosylase
enzymes bind the NAM-NAG chains into a rigid structure by adding pentaglycine crosslinks between pentapeptide residues on adjacent chains
transpeptidase
what are peniclinin-binding proteins?
peptidoglycan is maintained by the enzymes that create the bonds between NAM-NAG peptidoglycan monomers and between NAM-NAG chains in the layer
selective b-lactam antibiotics bind selectively to different PBPs and this contributes to the sensitivity of bacterial strains to individual penicillins and cephalosporin antibacterial agents
b-lactam compounds include (4)
penicillins
cephalosporins
monobactams
carbapenems
these agents are bactericidial
susceptible to b-lactamase
MOA penicillins
bind to and inhibit PBP enzymes
key adverse effects of penicillins
hypersensitivity 5-7%
rash, hives, itching, respiration difficulty, anaphylaxis
ampicillin amoxicillin piperacillin ticarillin azlocillin
all “broader” penicillins
penicillin G and V methicillin nafcillin oxacillin = narrower spectrum
which penicillins are b-lactamase resistant?
the group of vey narrow spectrum
methicillin
nafcillin
oxacillin
all the rest are sensitive
______ used in combination with penicillins to increase effectiveness
clavulanic acid (b-lactamase inhibitor)
amoxicillin & clavulanic acid = augmentin
advantages of cephalosporins over penicillins
- more resistant to b-lactamase
- less % adverse effects
generally used if penicillins are not well tolerate
MOA cephalosporins
bind to and inhibit the PBPs
key adverse effect cephalosporins
hypersensitivity 2%
rash, hives, itching, respiration difficulty, anapylaxis
4th generation cephalosporins have a more _____ spectrum than 1st gen
broad
broader spectrum with increasing generation
1st g: +
2nd g: + and some -
3rd g: + and -
4th g: + and -
which cephalosporins can enter the CNS?
3rd and 4th gen
cefdinir
cfixime
ceftriaxone
cefepime
and 2g: cefuroxime
which cephalosporin gen is b-lactamase resistant?
4th gen
cefepime
only mono bactam agent
aztreonam
only gram -
penetrates CSF
b-lactamase resistant
MOA aztreonam
bind to and inhibit PBPs
key adverse reaction monobactams
hypersensitivity
are carbapenems resistant to b-lactamase?
yes but susceptible to similar enzyme carbamenemase
______ inactivated in kidney so it is administered with cilastatin to prevent this inactivation
imipenem
MOA carbapenems
bind to and inhibit the PBPs
key adverse effects carbapenems
GI
nausea, vomiting, & diarrhea
MOA vancomycin
prevents elongation of the peptidoglycan cell wall structure by binding to pentapeptide and acting as steric inhibitor