reaction that catalyzes bond on peptides in the peptidoglycan layer & the enzyme
transpeptidation - PBP
the back bone of the peptidoglycan layer is made of
sugars
NAG-NAM-NAG
MOA of BL ABX
inhibition of PBP
beta lactam ring is meant to mimic ______
transition intermediation of transpeptidation
beta lactam ring is highly susceptible to what kind of attack by what amino acid residue
nucleophilic attack by serine residue
what is the beta lactic rings hybridation
sp2
inhibition of the PBP is two step process what are they
competitive and tight binding
serine residue attacks attacks BL ring
what kind of inhibition do BL ABX do
suicide inhibition of PBP
beta lactam ABX display: 1). ______ 2.) ________
PAE & bacteriocidal
pen g has what kind of absorption
poor - unstable in acidic conditions - BL carbonyl protonates
pen v has what kind of absorption
good because of EWG on side chain -O-
amoxicillin has what kind of absorption
good! - ionization of amino group
ampicillin has what kind of absorption
bad
what kind of transporter is oral absorption mediated by
dipeptide transporter - pen v and amoxicillin
spectrum of pen G and pen v
gram+
strep pyogenes
pen g drug of choice for atypicals
treponema pallium (syphillis)
spectrum of amoxicillin and ampicillin
better gram -
h influ (otitis media)
moraxella
serine beta lactase MOA
uses water to restore enzyme and degrades ABX
serine BLi's
clavulanic acid
sulbactam
tazobactam
serine BLi's MOA
block degradation of susceptible penicillins - results in irreversible inhibition - known as suicide inhibitiors
chemical rearrangement preventing restoration of the enzyme