Antibiotics: Cell Wall Synthesis inhibitors Flashcards
what are the cell wall synthesis inhibitor drugs?
- Beta lactam antibiotics
- Penicillins *
- Cephalosporins*
- Carbapenems
- Monobactam
- Vancomycin*
- Bacitracin
ß-lactams will work on what bacteria?
actively synthesizing peptidoglycan or in the log phase
how do ß-lactams work?
bind and inactivate bacterial enzymes essential for cross-linking between peptidoglycan chains
(inactivates transpeptidases and carboxypeptidases)
inactivation of enzymes for bacterial cross linking by ß-lactams will cause activation of what?
it will activate Autolysins that degrade cell wall and eventually kill the bacteria
ß-lactams drugs are considered what type of drugs?
bacteriocidal drugs
what are 3 ways that bacteria have adapted to evade ß-lactams?
- Hydrolysis of antibiotic by Beta-lactamases
- (cleave beta-lactam ring and destroy the antibitotic)
- Alteration of PBPs (penicillin-binding proteins)
- bacteria can alter their PBPs so that beta-lactams cannot bind them
- Reduced permeability of Gram negative outer membrane
- bacteria alter their porins and size of porin channels
- Prevent the large molecules of the beta-lactam drug from penetrating the cell wall
what are the enzymes that inactivate ß-lactams antibiotics?
1) Penicillinases – specific for penicillins
2) Cephalosporinases – target cephalosporins
3) Carbapenemases – inactivate carbepenems
4) Extended-Spectrum B-lactamases (ESBLs) - inactivate cephalosporins and penicillins
what is important about the penicillin structure?
it contains a ß-lactam ring
what is penicillin’s mode of action?
Inhibition of transpeptidases (PBPs) with subsequent Inhibition of cell wall synthesis & bacterial cell death
what side effects can penicillin have?
hypersensitivity
name the different types of penicillin.
1) Penicillin G, Penicillin V
2) Aminopenicillins
3) Extended spectrum Penicillins (Anti-pseudomonal
4) Penicillinase-Resistant Penicillins
5) Beta-lactamase Inhibitors
6) Penicillin + Beta-lactamase inhibitor
what penicillins are susceptible to penicillinase (ß-lactamase)?
penicillin G and V
Aminopenicillins
Extended spectrum Penicillins (Ureidopenicillins)
what are the penicillins that are penicillinase resistant?
Methicillin
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin
how is penicillin G administered?
through IV
how is penicillin V administered?
orally
how is penicillin G and V’s spectrum?
narrow
penicillin G and V are used for what type of bacteria?
gram positive bacteria
Methicillin, Nafcillin, Oxacillin, Cloxacillin, Dicloxacillin are used only for what bacteria?
staph infections
aminopenicillins like ampicillin and amoxicillin have this side effect…
diarrhea
name the aminopenicillins?
ampicillin and amoxicillin
how are Aminopenicillins: Ampicillin, amoxicillin, taken?
orally
what is another term for penicillinase?
ß-lactamase
Aminopenicillins: Ampicillin, amoxicillin, are used for what infection?
enterococci and listeria infections
what is an important anti-psudomonal penicillin?
pipercacillin
What are the penicillinase resistant penicillins?
Methicillin,
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin
how are cloxacillin and dicloxacillin administered?
orally
how are Methicillin, Nafcillin, Oxacillin administered?
Intavenous
what bacteria have developed resistance to methicillin?
MRSA, MRSE
methicillin resistance refers to resistance against what drugs?
met, naf, oxa, clox, diclox
what is the drug of choice for staph infection?
Methicillin, Nafcillin, Oxacillin, Cloxacillin, Dicloxacillin
(Naf for Staph)
what is the drug of choice to treat MRSA or methycillin resistance?
vancomycin
what is an example of a common staph infection?
abcesses
what is the drug of choice for listeria infections?
Aminopenicillins
what do ß-lactamase inhibitors do?
Inactivate some types of beta-lactamase enzymes produced by bacteria
Give an example of a ß-lactamase inhibitors
Clavulanic acid (clavulanate)
are they effective working alone? what do you do to correct this?
no, always used in combination penicillin
how effective are beta lactamase inhibitors when administered alone?
inactive at inhibiting bacteria on their own
how do you increase the effectivity of ß-lactamase inhibitors?
administer in conjunction with penicillin
do beta lactamase inhibitors all work will all beta lactamases
no
what is a Beta lactam + beta lactamase inhibitor combination?
penicillins that have been combined with beta lactamase inhibitors to increase effectiveness
what are the Beta lactam + beta lactamase inhibitors?
Amoxicillin + clavulanate (Augmentin)
Piperacillin + tazobactum
how is the antibiotic spectrum of Beta lactam + beta lactamase inhibitors?
broad
beta lactam + beta lactamase inhibitor has improved activity against?
Improved activity against beta-lactamase producing staphylococci and selected gram negative rods*