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Pharm Cell Wall Drugs
KYCOM Block 10
88
Pharmacology
Graduate
09/18/2013

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Cards

Term
what are the 4 categories of B-lacctam drugs
Definition
penicillins, cephalosporins, carbapentems, monobactams
Term
what are the 4 types of penicillins, what is the penicillinase resistance status
Definition
natural - susceptible
anti-staph - resistant
amino - susceptible
anti-pseudomonas - susceptible
Term
what kind of antibiotic is penicillin (2)
Definition
B-lactam cell wall drug
bactericidal
Term
what are the 2 natural penicillins
Definition
penicillin G, penicillin V
Term
what are the 4 anti-staph penicillins
Definition
naficillin, methacillin, oxacillin, dicloacollin
Term
what are the 2 amino penicillins
Definition
amoxicilliin and ampicillin
Term
what are the 2 anti-pseudomonas penicillins
Definition
piperacillin
ticaricillin
Term
what parts of the body does penicillin distribute to (3)
Definition
bones, CNS, placenta (not tertogenic)
Term
how are penicillins metabolized and excreted
Definition
little metabolism
WA excreted in PCT of kidney (adjust for renal dysfunction)
Term
what are the three parts to the MOA of all penicillins
Definition
inactivate PBP on cell memrane stopping cell wall synthsis, allowing autolysins to proceede, breaking cross links in peptidoglycan

stop trans-peptidase preventing cross linking

active against peptidoglycan wall
Term
what 4 ways can a microbe get resistance to a B-lactam
Definition
has no cell wall

plasmid B-lactaminase transfer

porin mutation: drug can't get through LPS to PBP

modify PBP so drug cannot bind
Term
what 3 side effects to penicillins cause, what triggers them
Definition
hypersensitivity: triggered by penicilloic acid. maculopapular rash, angioedema, anaphylaxis

GI reaction (especially ampicillin)

acute interstitial nephritis (rare)
Term
can someone have penicillin after an allergic reaction, how does this change other drug perscriptions
Definition
if they had a mild reaction (rash) they don't get penicilliin anymore but can have other B-lactams

if they had a severe reaction (anaphylaxis) they can never have all B-lactam drugs
Term
what are the 2 MOA of B-lactaminase inhibitors
Definition
irreversibly bind B-lactaminase and alter its structure

allows for antibiotics to kill, not killers
Term
do B-lactaminase inhibitors penetrate the CNS well
Definition
no
Term
what are B-lactaminase / penicillin combos, what is their method of administration (4)
Definition
cavulanic A / amoxicillin - oral

cavulanic A / tricarcillin - IV or IM

taxobactam / piperacillin - IV or IM

sublactam / ampicillin - parentrail
Term
what are the five categories of cephalosporins, what is their penicillinase resistance status
Definition
1st generation - none really
2nd generation - some
3rd generation - basically all resistant
4th generation - resistant
5th generation - resistant?
Term
what 2 drugs are 1st generation cephalosporins
Definition
cefazolin
cephalexin
Term
what 4 drugs are 2nd generation cephalosporins
Definition
cefaclor
cegoxitin
cefuroxime
cefmandole
Term
what 4 drugs are 3rd generation cephalosporins
Definition
ceftaxime
ceftazidime
ceftriaxone
cefoperazone
Term
what 1 drug is a 4th generation cephalosporin
Definition
cefepime
Term
what 2 drug is a 5th generation cephalosporin
Definition
cefaroline
Term
what type of antibiotic is a cephalosporin (2)
Definition
b-lactam cell wall drug
bactericidial
Term
how are cephalosporins administered, why
Definition
IV or IM because they are absorbed poorly
Term
what pharmological principals to cephalosporins have in common with penicillins
Definition
MOA, resistance issues, side effects, metabolism, clearance
Term
what happens when a patient overuses cephalosporins
Definition
enterococcal superinfections
Term
what three drugs are cerbapenems, what are their B-lactaminase resistances
Definition
imipenem
neropenem
entrapenem
all resistant
Term
how are carbapenems administered
Definition
iv
Term
what side effect do carbapenems do that isnt the same as penicillin
Definition
seizures (especially imipenem)
Term
what pharmological principals to carbapenems have in common with penicillins
Definition
MOA, resistance issues, side effects, metabolism, clearance
Term
what drugs are monobactams, what are their B-lactaminase resistance status
Definition
azerotonam - resistant
Term
what pharmological principals to monobactams have in common with penicillins
Definition
MOA, resistance issues, metabolism, clearance
Term
why are monobactams different from all the other B-lactams
Definition
they only have one ring (B-lactam), their allergies do not cross react with other B-lactam drugs
Term
what side effects do monobactams cause (2)
Definition
phelbitis and skin rash
Term
how are monobactams administered
Definition
IV or IM
Term
what are the four non-B-lactam cell wall drugs, what type of antibiotic are they
Definition
vancomycin- bactericidia
bacitracin
polymyxins
tricoplanin- bacteriacidial
Term
vancomycin MOA
Definition
binds to D-ala-D-ala terminal stopping protein elongation inhibitng cell wall synthesis
Term
vancomycin resistance (3)
Definition
VRSA, VREnterococcus
change binding site to D-ala-D-lactate
Term
how is vancomycin administered
Definition
IV
oral for GI infection (not absorbed. C. diff)
Term
vancomycin excretion
Definition
kidney, adjust for failre
Term
vancomycin side effects (4)
Definition
fever, chills, phlebitis, red man syndrome
Term
what is the cause of red man syndrome, what is the solution
Definition
if IV infusion is too wuick, histamine flushes face via macrophages causing hypotension

infuse of 1h
Term
baitracin: administration, for what microbes, how to use
Definition
topical
for gram positive bacteria
use with neomycin and polymyxins
Term
polymyxins: administration, for what microbes, how to use
Definition
topical
for gram negativebacteria
use with neomycin and polymyxins
Term
trichoplanin: what drug is this like, what does it kill (2)
Definition
simillar to vancomycin, kills gram positive and MRSA
Term
what is penicillin G combined with (5) and why, when combined like this how is it administered, what is this combination good at treating
Definition
depot forms: procaine or benzathine to increase duration and increase stability

Na or K to increase stability

given IV to treat syphillis
Term
what is the benifit of a penicillin V over G, how is it administered
Definition
oral
more resistant to gastric A
Term
what is the most often used anti-staph drug, why, how is it administered
Definition
naficillin, it has lower nephrotoxicity, IV
Term
what penicillins are not excreted by the kidney
Definition
all 4 anti-staph penicillins, do not need to be adjusted in renal failure
Term
what penicllins are only oral (3)
Definition
penicillin V, amoxicillin, amoxicillin/clavuonic A
Term
what penicillins reach the meninges well
Definition
ampicillin
Term
how are aminopenicillins administered
Definition
orally
IV/IM for ampicillin/B-lactaminase inhibitor
Term
what is the most absorbed penicillins, why is this good and bad
Definition
amoxicillin
good because it gets into the body well
bad because it has no effect on gut infections unlike all the other penicillins
Term
what penicillins are only IV/IM (4)
Definition
antipseudomonals, ampicillin/sublactam, ticaricillin/clauvonic acid, piperacillin/tazobactam
Term
what penicillins are oral, IV, and IM (2)
Definition
ampicillin
anti-staph penicillins
Term
what do aminopenicillins need to wrk
Definition
amino-glycosides
Term
which cephalosporins are not metabolized in the kidney, where is it excreted
Definition
ceftriaxone, excreted into bile. use for renal disease
Term
which cephalosporins are not IV/IM, they are oral (3)
Definition
cephalexin, cefaclor, cefuroxime
Term
which cephalosporins penetrate the CNS (6)
Definition
cefuroxime - not as good
ceftaxime, ceftaxidime, fectriaxone, cefperazone
cefepime
Term
which cephalosporins are good for surgical prophylaxis
Definition
1st gen
Term
which cephalospirins are good for skin, UTI, respiratory infections, otitis media
Definition
1st gen, 2nd gen
Term
which cephalosporins work for anaerobes
Definition
gen 3 and 4
Term
what are the side effects of 2nd gen cephalosporins (2)
Definition
cefmandole: disulfiram (acetylaldehyde accumulation) and anti vitamin K (bleeding)

the rest: same as penicillins
Term
which cephalosporins are used for biliary tract infections
Definition
3rd gen
Term
what are 5th generation cephalosporins used for (5)
Definition
acute bacterial and skin structure infections (ABSSI)

community acquired bacterial pneumonia (CABP)

MRSA, enterococci, listeria
Term
what does imipenem have to be combined with to work, why
Definition
cilastatin (dihydropeptidase inhibitor) to protect from nephrotixic metabolites forming
Term
what is the broadest spectrum B-lactam of the amm
Definition
imipenem
Term
what is used for surgery prophylaxis in a MRSA high area
Definition
non b-lactam cell wall drugs (vancomycin)
Term
what is used for endocarditis prophylaxis
Definition
non b-lactam cell wall drugs (vancomycin)
Term
what are anti-staph penicillins used for
Definition
staph (MSSA). AEROBIC
Term
what are natural penicillins used for
Definition
gram positive cocci - strep, enterococcus (but use amino penicillin first), staph (but use anti-staph first), syphillis (pen G). AEROBIC
Term
what are amino penicillins used for
Definition
strep, enterococci, listeria (ampicillin). AEROBIC
Term
what are anti-pseudomonal penicillins used for
Definition
MUST be used for pseudomonas, can be used fo all gram negative that are AEROBIC
Term
which penicillins can be used as "broad spectrum" why. how do you determine which one do use
Definition
enough gram negative coverage.
if it is an unknown gram negative use anti-pseudomonas. if it is known to not be pesudomonas than use amino penicillin
Term
explain the general trend of gram negative and positive coverage in penicillins
Definition
better gram positive - antistaph, natural, amino, antipseudomonas - better gram negative
Term
what is the best penicillin for strep
Definition
natural
Term
what is another name for syphillis, what is the best drug for it
Definition
treponema, benzathine pen G
Term
what penicillin kills lysteria
Definition
ampicillin
Term
what are the general trands of the cephalosporins for their clinical actions
Definition
become more broad from 1 to 4 because they increase in gram negative coverage

none kill listeria, enterococci, or MRSA (5th gen kills MRSA)
Term
what cephalosporins killa anaerobic
Definition
second generation kills bacteroides and clostridium (not diff)
Term
what do 1st gen cephalosporins kill(6)
Definition
staph, strep, E. coli, klebsiella, proteus
best gram positive coverage of the cephalosporiins
Term
what do 2nd gen cephalosporins kill (4)
Definition
clostridium not diff, bacteroides, everything 1st gen killed, more gram negatitive than 1st gen
Term
what does 3rd and 4th gen cephalosporins kill (7)
Definition
all CNS infections but listeria
more gran negative rods and cocci than 1st and 2nd gen without anaerobic (enteric, pseudomonas, gonorrhea)

3rd does meningitis biliary tract infections

everything 1st gen killed
Term
what drug combo is preferred for an unknown CNS infection
Definition
ampicillin (to cover listeria) + 3rd gen cephalosporin to cover everything else
Term
what is the back up drug for listeria
Definition
TMP-SMX
Term
carbapenem clinical use (6), what are they not good at (2)
Definition
emperic therapy: b lactaminase resistant, gram positive or negative, klebsiella pneumonia, anaerobes, pseudomonas

not good at enterococci, MRSA
Term
monobactams clinical use (3), what are they not good at (2)
Definition
aerobic gram negative rods including enterics and pseudomonas

not good at gram positive, anaerobes
Term
what is the clinical use of vancomycin (7)
Definition
MRSA!!, SERIOUS gram positive infections when allergic to b-lactam, C. diff!! that didnt respond to metronidazole, surgical prophylaxis in MRSA high area, gram positive, arobic, anaerobic
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