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What is the MOA of beta-lactams?
bactericidal
Penicillin-binding proteins (PBP) make up the cell
bind to (PBP)
inhibit cell wall synthesis
What is penicillinase-resistant penicillins?
have substitutions to the beta-lactam ring that sterically inhibit penicillinase
Which Penicillins are given IV?
Pen G
Nafcillin
Oxacillin
Ampicillin (also oral)
Ticarcillin
Piperacillin
Unasyn (Amp/sulbactam)
Timentin (Ticarcillin/clavulanate)
Zosyn (Pip/tazobactam)
Which Penicillins are given PO?
Pen VK
Dicloxacillin
Amoxicillin
Ampicillin (IV also)
Carbenicillin (only used for UTIs)
Augmentin (Amox/clavulanate)
Which Penicillins are given IM?
benzathine Pen G
procaine Pen G
Pen G benzathing + Pen G procaine
What are the natural penicillins?
Pen G (and all variations)
Pen VK
(Veetids)
What are the spectrum of activity for natural PCNs?
Streptococcus pyogenes
Streptococcus pneumoniae
Streptococcus viridans
Clostridium perfringes
(gas gangrene)
Why are natural PCNs are ineffective against
staphylococcus aureus
?
because they are readily hydrolyzed by penicillinases
(Beta-lactamases)
to become resistant to penicillin
Which natural PCN are more active toward
Gram-negative
organisms?
Pen G
is 5-10x more active than Pen V
What are the penicillinase-resistant penicillins
or
antistaphylococcal penicillins?
methicillin
nafcillin
oxacillin
dicloxacillin
What are the spectrum of activity for penicillinase-resistant penicillins/antistaphylococcal penicillins?
MSSA
streptococci
(but not enterococci)
What are the extended-spectrum aminopenicillins?
ampicillin
amoxicillin
(Trimox, Amoxil)
What are the extended-spectrum antipseudomonal penicillins?
carbenicillin
ticarcillin
piperacillin
What are the beta-lactamase inhibitors?
clavulanic acid
sulbactam
tazobactam
What are the beta-lactam/beta-lactamase inhibitor combinations?
Augmentin
(amoxicillin clavulanate)
Unasyn
(ampicillin sulbactam)
Timentin
(ticarcillin clavulanate)
Zosyn
(piperacillin tazobactam)
What are the main coverage of
Augmentin
&
Timentin
?
H. flu
Moraxella catarrhalis
Klebsiella pneumonia
MSSA
Anaerobes
How are beta-lactam/beta-lactamase inhibitors formulated?
amount of beta-lactam changes as dose increases
amount of beta-lactamase is constant
2x250 does not equal 1x500, the inhibitor concentration would be too high = more SE
How are Penicillins eliminated?
renally:
glomerular filtration and active tubular secretion
Oxacillin
(renal and bile)
Nafcillin
(bile)
What type of killing do Penicillins posess?
time-dependent killing
What are the SE of Penicillins?
NVD (infectious and non-infectious D)
hypersensitivity
anemia
decreased platelets
increased INR
acute interstitial nephritis
(methicillin, nafcillin)
excess sodium load
(ticarcillin worst)
excess potassium load
(Pen G)
superinfection
What pregnancy class are Penicillins?
class B
DOC in pregnancy
What are the DI of Penicillins?
oral contraceptives (use condoms for 1 wk after antibiotics)
warfarin (increased INR d/t loss of gut flora)
What is the MOA of cephalosporins?
bactericidal
inhibition of
mucopeptide synthesis
in bacterial cell wall
cause cell wall lysis
How are cephalosporins dosed?
IV
PO
IM
How are cephalosporins grouped?
grouped into generations based on their antimicrobial coverage
What cephalosporins are 1st generation?
cefazolin
(Ancef)
cephalexin
(Keflex)
cefadroxil
(Duricef)
Which 1st generation cephalosporins are given PO?
cephalexin
(Keflex)
cefadroxil
(Duricef)
What are the groups of microorganisms that 1st generation cephalosporins cover?
Gram (+) more than Gram (-)
What cephalosporins are 2nd generation?
cefoxitin
(Mefoxin)
cefuroxime
(Zinacef)
cefotetan
(Cefotan)
cefaclor
(Ceclor)
cefprozil
(Cefzil)
Which 2nd generation cephalosporins are dosed PO?
cefaclor
(Ceclor)
cefprozil
(Cefzil)
Which 2nd generation cephalosporins are dosed both IV & IM?
cefuroxime
(Zinacef)
cefotetan
(Cefotan)
What cephalosporins are 3rd generation?
cefdinir
(Omnicef)
ceftriazone
(Rocephin)
ceftazidime
(Fortaz)
cefotaxime
(Claforan)
Which 3rd generation cephalosporins are dosed PO?
cefdinir
(Omnicef)
Which 3rd generation cephalosporins are dosed IV & IM?
ceftriazone
(Rocephin)
ceftazidime
(Fortaz)
What cephalosporins are 4th generation?
cefepime
(Maxipime)
IV & IM
What cephalosporins are 5th generation?
ceftaroline
(Teflaro)
IV only
What kind of killing does cephalosporins possess?
time-dependent killing
above the MIC
Which cephalosporins are good for anaerobes?
cefoxitin
(Mefoxin)
cefotetan
(Cefotan)
Which cephalosporins are good for pseudomonas?
ceftazidime
(Fortaz)
cefepime
(Maxipime)
Which cephalosporins are good for
MRSA
,
MRSE
, and
enterococcus
?
ceftaroline
(Teflaro)
Which cephalosporin is best for use in neonates?
cefotaxime
(Claforan)
How are cephalosporins eliminated?
mostly renal:
glomerular filtration and active tubular secretion
ceftriaxone
(
bile
30-40%)
Which cephs can penetrate the CNS?
cefuroxime
(2nd-gen)
cefotaxime
(3rd-gen)
ceftriaxone
(3rd-gen)
ceftazidime
(3rd-gen)
How protein bound are cephs?
ceftriaxone
is
concentration dependent
: increasing dose increases fraction unbound, so higher doses and longer interval is better
What are the SE of cephs?
hypersensitivity
increased INR/bleeding/hypoprothrombinemia in cephs that have MTT side-chain
(cefotetan)
NVD
HA
dizziness
neurotoxicity (high dose in renal impaired)
bilirubin encephalopathy (
ceftriaxone
- highly PPB)
Which ceph should not be used in neonates?
ceftriaxone
displaces bilirubin
What are the DI of cephs?
do not administer
ceftriaxone
with
calcium-containing IV fluids
in neonates (increased risk of precipitation)
How can bacteria becomes immune or resistance to cephalosporins?
through the production of
beta-lactamases
Author
skylinezts
ID
102628
Card Set
Antibacterial Agents
Description
Antibacterial Agents
Updated
2011-09-19T06:08:18Z
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