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112 Cards in this Set

  • Front
  • Back
name the groups and subgroups of the Beta lactams
penecillins - native penecillins, antistaphs, extended spectrum, antipseudemonals
carbapenams
monobactams
cephalosporins
name the native penicililns
pen G
Pen V - probenecid
name the antistaphylococcal penicillins
nafcillin
oxacillin
cloxicillin
dicloxicillin
name the extended spectrum penicillins
ampicillin
amoxacillin
antipseudomonal penicillins
name the antipseudemonal penicillins
ticarcillin
piperacillin
name the first generation cephalosporins
cefazolin
cephalexin
name the 2nd gen cephalosporins
cefoxitin
cefaclor
cefprozil
name the 3rd gen cephalosporins
ceftriaxone
ceftazidime
cefotaxime
cefdinir
name the 4th gen cephs
cefepime
name the B-lactamase inhibitors
clavulanic acid
sulbactam
tazobactam
name the carbapenem we have to know
imipenem (+cilastatin)
name the monobactam we have to know
aztreonam
name the 2 "other cell wall/membrane inhibitiros we need to know
vancomycin
bacitracin
what are the 4 steps in which beta mactams work
1. bind to PBP
2. PBP is unable to crosslink peptidoglycan chans
3. bacteria are unable to sythesize stable cell wall
4. weakened cell wall leads to lysis of bacteria from osmotic pressure
describe difference between gram pos and gram neg
gram pos- cell wall composed of many sheaths of peptidoglycan layers - they have peptide cross -links, also have teichoic acid and lipoteichoic acid
Gram NEG - small peptidoglycan layer with outer cell wall composed ofporins and other proteins - lipid rich- target the periplasmic space
what does the structure of gram positive peptidoglycan layers have that gram negative does NOT

what do both have that are important
gram positive - (gly)5

both have ala-ala
what does vancomycin bind to ?
ala-ala of the NAM side chain
what does cycloserine do?
blocks the formation of alanine-alanine before it is added to the N-acetylmuramic acid (NAM)

it is a 2nd line agent for TB
describe the formation of the cell wall
NAM is formed with its tetrapeptide side chain
combined with bactoprenox
then combined with NAG + (gly)5
Moves out of cell
Bactoprenol is removed and brought back into cell to be recycled
what drug binds to the Ala-Ala structure?

what does this prevent
vancomycin

prevents cross linking and elongation of peptidoglycan layer, i.e. blocks transglycosylase
what is bactoprenol?
what does it connect to?
carrier protein that carries the NAG-NAM peptidoglycan piece outside of bacterial cell
Connects to NAM 1st. then NAG and gly5 are added
it is brought back in and recycled
what inhibits bactoprenol recycling?
bacitracin
How do penecillins work?
they are structurally similar to Ala-Ala structure on NAM,
and bind to transpeptidase
this blocks the cross linking of peptidoglycan chains
what is a penicillin binding protein?

what are the different types of PBP, as in their function?
anything that binds penicillins
-there are several types, can be membrane bound or cytoplasmic

functions - catalyze transpeptidase rxn, maintain shape, form septum during division, inhibit autolytic enzyme
what is autolysis in bacteria?

how can we effect with drugs?
it is the normal breakdown of the bacterial cell wall in order for the cell to grow

if we inhibit the autolysis inhibitors --> chews up cell wall
what is the most important thing to know about pharmacokinetics of penicillins
they are TIME DEPENDENT killers!!!
effect is directly proportional to amount of time the drug concentraion at site of infection is above minimal inhibitory concentration
what is the major chemical structure in all the beta lactams?

what is the product of its breakdown?
beta lactam ring

penilcilloic acid
what part of B-lactam structures defien their spectrum of antibacterial activity?

how can we change the spectrum of B-lactams by changing these? (5)
R groups

increase acid stability
resist beta-lactamases
improve psectrum to include G-
increase activity against pseudomonas
iomprove activity against anaerobes
describe the characteristics of Pen G

what does it target?
acid labile - poor oral, ioavailability, low cost, safe - large thx index

Targets Gram +, few Gram _ (nisseria meningococci), Some anaerobes and spirochetes (syphillis)
Characteristics of pen V

used to treat what?
more acid stable, can be taken orally "V is not IV"

used ot treat resp tract infections, otitis media, sinusitis, skin, UTI
Also prophylaxis in rheum fever
what is Pen G used to treat?
infections - sepsis, pnemonia, pericarditis, endocarditis, menengitis, anthrax - which are caused by susceptible orgamisms - Gram +, bu tusually not staph aureus, Some gram Neg like nisseria gonorhea, some anaerobes some spirocehetes
what bugs have acquired resistance to Pen G
Staph Aureus (90)%
streptococci (5%)
most of neisseria gonococci is resistant - PenG no long DOC
what parts of the body does Pen G not readily reach?
prostate
ocular
CSF - does not cross BBB, but inflammation causes leaky membrane which allows for penicillin tx
How is Pen G cleared and what is half life?

what must we watch for? and what drug must we be careful in using?
via active transport pump in kidneys, very quickly HL=~30min

probenecid (gout tx)
what are the two Pen G drugs that are given as "repository penicillins"
Pen G procaine
Pen G benzathine
most common adverse effect of Pen G
allergic Rxn - can be any types of the 4 hypersens rxns

most ppl that say they are allergic are not.
name the 4 types of hypersens rxns
1. anaphylaxis
2. antibody-dependent cyto toxicitiy
3. immune complex disase
4. cell mediated or delayed hypersens.
breakdown product of penecillins

what can it act as?
penicilloic acid

can act as a hapten --> to cause a hypersens rxn
what are the non-allergic side effects of penecillin G
diahrrea and GI intolerance

NEUROTOX - seizures, coma, hyper-reflexia
Super infections (more common with broader spectrum)
what are common superinections and what do they cause?
clostridium difficile - pseudomembranous collitis
staph aurerus - enterocolitis
candida albicans - vaginal, oral thrush
what are the general 5 modes of resistance to Pen G?
1. gram neg's are generally resistant - thick outer cell wall
2. penicillinase production (B-lactamse - most common_
3. cell lysis cascade is not activated (streph, staph, listeria)
4. mycoplasma - no cell wall
5. transpeptidase is altered (MRSA)
what is the major mode of resistance against B- lactams?

what are the different kinds
bacterial production of B-lactamase

chromosome encoded - inducible
plasmid encoded - constitutively expressed - most mediate resistance to pens and 1st and 2nd gen cephs
what is the attack point of the B-lactamase

beta lactamases of what types of bacteria chew up pens and cephs well
beta lactam ring - essential for PBP binding

pseudomonas, enterobacter
what are ESBLs? expain them

what are most common producers of ESBLs
extended spectrum beta-lactamases

certain B lactamases that hydrolyze pens, cephs (ALL) monobactams
primarily seen in gram Negs

most common - klebsiella pneumonia and e. coli
what is special about the antistaphylococcal penicillins

extends spectrum to what?
they are resistant to the beta lactamases - their side chains don't fit in B-lactamase active site
extends spectrum to include B-lactamase producting Staphylococci - NOT MRSA
DOC for MSSA
adverse effects of antistaphylococcal pens?
same as Pen G
also:

blood dyscrasia - agranulocytosis
acute interstitial nephritis
Oxacillin - hepatotoxicity!
deescribe the spectrum of extended spectrum penicillins?

what are they , and how are they administered
ampicillin &amoxicililn &antipseuds

penetrate gran negative more readily - E Coli, N. meningitidis

not effective against B-lactamase producers - use B-lacatamase inhibitors

amoxicillin - better bioavailability than Amp
amox: one of oral pens tha tFOOD DOES NOT INTERFERE with absorption
what is one of the only penecillins that food does NOT effect with its absorption
amoxicillin

O in the amox is for ORAL
what is the spectrum of the extended spectrum pens?
Same as Pen G + extends to :
HELPS
Haemophilus influenza
E. Coli
Listeria
Proteus
Salmonella
what are clinical uses of Extended specturm penicillins

what is one of the drugs often used in combo with? why?
sinusitis, otitis, UTIs, pneumonia SOUP
HELPS FOR SOUP

amox used with aminoglycoside (gentamicin) - synergism for broad range of coverage in serious infections
what is ampicililn a DOC for?
listeria meningitis
wht are the antipseudomonal pens and what is their spectrum??? what are they sensitive to?
ticarcillin and piperacillin.

they are sensitive to B-lactamase - so we use with B-lactamase inhibitors

spectrum similar to ampicillin but extends to include other gram Negatives -

Pen G + HELPS + Pseudomonas, klebsiella and Serratia
if we have an ifection of klebsiella, pseudomonas, or serratia... what penecillin do we use to treat it?
antipseudomonas - they are all gram negs

PEN G + HELPS + kleb, pseud, serratia
how are the antipseudomonal pens given? why?
with aminoglycoside... because of increasing emergence of resistance
what are clinical uses of the antipseudomonal pens?

what kind of px do we treat in?
pneumonia, UTI, peritonitis, skin and soft tissue infections with susceptible organism

immunocompromised pxs
what is the broadest spectrum penecillin we can give
piperacillin with tazobactam - a beta lactamase inhibitor
what are the adverse effects of antipseudomonal penicililns? name them again
liek that of Pen G but most importantly....
Super infection b/c so broad spectrum
Can potentiate aminoglycoside-associated nephrotoxicity
Sodium overload
what kind of px must we be careful with when giving antipsuedomonal pens? why?
pts with CHF or renal insufficiency... sodium overload, the drug is given with sodium formula
what are the resistance mechanisms involving antipseudomonal pens? why?
since they target Gram Neg and gram Pos -

Pos- beta-lactamase outside cell wall & changes in PBP
Neg- change in entry though porins, beta lactamases in periplasmic space, EFFLUX PUMP
why and how do beta lactamase inhibitors work

name them again
they contain a beta lactam ring so it fits in their binding site and INACTIVATES THEM

clavulanic acid
sulbactam
tazobactam
what kind of beta lactamase are beta lactamase inhibitors effective for?
plasmid encoded beta lectamases, NOT CHROMOSOMAL (induced by gram NEG bacilli by 2nd and 3rd gen cephs)
what are the 4 main combo preps with beta lactamase inhibitors
amoxicillin + clavulanic acid (augmentin) only ORAL one!!!!

ampicillin+sulbactam
Ticarcillin + clavulinic acid
Piperacillin + tazobactam
what is the MOA of cephalosporins
same as penecillins, b-lactams that block cell wall cynthesis. resemble the structure of NAG-NAM and attract transpeptidase

BACTERICIDAL
how are cephs cleared by the body?
via the kidneys
what is the spectrum of cephs?
like ampicillin
G+ & HELPS
H. flu, ecoli, lissteria, proteus, salmonella
what are cephalosporins not active against? (2)
enterococcus or MRSA
what are the extended spectrum B-lactamases?
what can they break down?
E.coli, Klebsiella, pseudomonas, enterobacter
discuss the role of allergic reaction about cephalosporins
cephs seem to cause less allergic reactions, some cross sensitivity (~10%)

good alternative to pxs who are allergic to pens
describe the coverage of cephalosporins against gram positives vs gram negs
as you go up in generation 1->4
decrease in Gram+ coverage and increase in Gram- coverage
how do cephs compare to penecillins in resistance to Beta-lactamases

Describe each generation
cephs are more resistant to B-lactamases
they all act on MSSA

resistance to b-lactamases increases with higher generation
describe half life differences in each generation of cephalosprins
half life increases with generation 3>2>1
renal elimination goes down in higher gens
what drugs can penetrate CSF
3rd and 4th Generation cephalosporins only
what are the major adverse effects of cephalosporins

what is it due to?
Which drugs specifically???
hypoprothrombinemia - coagulation prob

alcohol intolerance

dude to MTT group on R-
Cefotetan(2nd)
Cefoperazone(3rd)
Genearl primary uses of 1st fgeneration cephalosporins
Rarely DOC for any infection

Maybe- UTIs caused by Klebsiella and Pen/sulf resistant organisms. staphylococcal or streptococcal infections; cellulutis or soft tissue infections

******PROPHYLAXIS FOR SURGERY (cefazolin)
what are 1st generation cephs active against, what are they not active against
active against G+ and Proteus, E.coli, Klebsiella

PenG+ PEcK

not effective agaisnt MRSA, enterococcus, or pseudomonas
what are what are the 2nd gen cephs and what are their coverage?
cefoxitin, cefaclor, cefprozil

Active: G+, H. influenza, enterobacter, neisseria, proteus, e.colii, klebsiella
G+ HEN PEcK
Not active: enterococci, MRSA or pseudomonas
what are primary uses for 2nd generation cephs?
sinusitis, bronchitis, otitis media
lower respiratory tract infections

mixedd anaerobic infections, eg peritonitis, diverticulitis
Lyme dz - but 3rd gen better
what are adverse reactions of 2nd generation cephalosporins
allergic rxns
blood dyscrasias - anemia, eosinophilia

Pseudomembranous colitis - due to superinfection
what happens as you move up in ceph classes
increase in Gram neg and anaerobe coverage
increase in ability to cross BBB
increase in B-lactamase resistance
compare halflives of 3rd gen to others, specific
Generally they have longer halflives
what is excretion of 3rd gen cephs
what is the exception
all renally
EXCEPT ceftriaxone - liver!!!
3rd gen ceph coverage
less against G+

more G-:
PSEUDOMONAS, kleb, E. coli, Proteus, serratia
describe serratia
gram negative
facultataive anaerobe
enterobacter family
rod shaped
tend to colonize respiratory and UTI
what is the general clinical use of 3rd gen cephs? specifically what type or presentation
how administered?
SERIOUS Gram (-) infections!
with aminoglycoside

Gram neg. sepsis, pneumonia, meningitis
nosocomial infections
complicated UTI
IMMUNOCOMPROMISED host
ghonnoreah and lyme disease DOC
what does nosocomial mean?
hospital acquiered
when is a 3rd gen ceph a DOC? that we have learned so far (5)
klebsiella pneumoniae (ceftazidime)
E.coli - wound
Gonorrhea - ceftriaxone
lyme dz - ceftriaxone
hospitalized pneumonia pxs!
a person is being treated for Community acquired pneumonia as an outpatient, what drug?
NOT a 3rd gen ceph,
azithromycin, clindamycin, or doxycycline
describe 4th gen ceph spectrum
wider spectrum, more resistant to beta-lactamases
describe the uses of 4th gen ceph
clinical uses
more effective against PSEUDOMONAS than 3rd
also against Staph and Strep pneumoniae

And Haemophilis and neisseria
describe neisseria

what disesases and strands
what do we use against this?
gram negative diplococci bacteria

n. ghonorrhea
n. meningitidis

4th gen ceph
describe cefapime the drug
not oral
renally eliminated
crosses BBB
No disulfram side effects, but similar to all other cephs otherwise
name the carbapenem and its MOA and spectrum
imipenem
MOA - same as pens and cephs - has Ala-ala to attract transpeptidase
specturm - broader than B-lactams - bactericidal to almost ALL bacteria except enterococcus faecium, MRSA and c. difficil
what is resistant to imipenem
MRSA
c. difficile
enterococcus faecium
what is special about imipenems action
it has post antibiotic effect after it falls below minimum inhibitory concentration
what is primary use for carbapenems
(lots to know)
and when do we use it?
treatment of tough drugs
ESBL-producing microbes (kleb and ecoli)
Alt tx for G- pneum and bacteremia, compilcated UTI, serious pseudomonas infections
emprical tx of nosocomial and mixed infections caused by MDR

LAST RESORT KINDA THING
what are the two most common ESBL-producing bugs
e.coli and klebsiella
when is carbapenem DOC?
enterobacter infections
ESBL producing klebsiella
what is carbapenem always used with?
what does it do?
cilastatin

blocks carbapenem being rapidly BROKEN down in renal proximal tubule, by dehydropeptidase
characteristics of carbapenems
distribution and limitations
Crosses BBB

gram neg porins may resis entry
hydrolyzed by metallo-B-lactamases

pseudomonas develops resistance quickly
not effective against MRSA, c. difficile, enterococcus faecium
side effects of iminpenem
NVD - only one we've seen
seizures!! especially in renal insufficiency - spikes drug
hypersensitivity - cross reactive with pens - 10-50%?
what is the monobactam we need to know?
MOA?
aztreonam
MOA same as other B-lactams, but only to Gram neg PBP
Spectrum of aztreonam?
GRAM NEG ANAEROBES ONLY****
what are the gram negative aerobes?

what is not?
serratia
pseudomonas
enterobacter
neisseria

not - enterobacter, kleb, etc
what is aztreonam not effective against?
gram positive and anearobes
when do we use aztreonam?

specific px?
SERIOUS gram neg infections
Useful in MDR infections

in px's allergic to pens and cephs - no cross reactivity
vancomycin MOA
binds tightly to ala-ala structure of NMG-NAG complex to inhibit transglycosylse activity
how is vancomycin administered?

special cases?
paretnally

except in GI infection - C. difficile, and enterocollitis (s. aureus) - not orally bioavailable
spectrum of vancomycin

when do we use? when DOC?
GRAM POSITIVE ONLY

used only in SERIOUS infections:
MRSA (DOC)
enterococci (DOC)
c. difficile (alt to metronidazole)
what is DOC for collitis due to C. difficile
metronidazole

alternate is vanc
Side effects of vanc?

when to use caution?
ototoxicity
nephrotoxicity
extreme flushing due to histamine relase - not a type I allergic rxn

use cautiously with aminoglycosides (other agents with oto and nephro tox)
what do we sometimes give with vancomycin to increase effect
aminoglycoside for synergistic effect
bacitracin MOA and coverage?
MOA - binds bactoprenol - doesnt allow the carrier protein for NAG-NAM to re-enter cell

coverage - GRAM POSITIVE ONLY