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110 Cards in this Set

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the 4 types of beta-lactams
-penicillins
-cephalosporins
-aztreonam
-carbapenems
MOA of penicillin
-bind to penicillin binding proteins and inhibit cell wall synth
-activate endogenous autolytic system of bact.-->cell lysis and death
-bactericidal and time-dependent killing
MOR to penicillin
-inactivation by b-lactamase enzymes
-alteration of PBP
-decreased cell wall permeability/no porin channels
structure of penicillins
house with a garage
classification of penicillins
-Natural
-Penicillinase-Resistant
-AMINOpenicillins
-UReidopenicillins
-Beta-lactam/BLase inhibitors
-Carboxypenicillins?
penicillins have _____ tissue penetration
good; except eye, prostate and CNS (better w/ inflamed meninges)
oral penicillin agents are ____ by gastric acid
destroyed
food ____ absorption of penicillins
delays
the most acid stable penicillin is... and the other two are
amoxicillin, dicloxacillin and ampicillin
benzathine is used to treat...and levels are ____ MIC and last for ___
syphillis; below; weeks
procaine is used to treat...and levels are... and last for ...
neurosyphillis; high; 12-24 hrs.
protein binding of penicillin is ....
widely variable between agents 15-97%
metabolism of penicillins is....
minimal to none
penicillin is eliminated by...except for ... and ... which are elimnated by..
kidney; nafcillin and oxcillin; liver
does pen. require renal dose adjusting?
YES!
pen. half lives are ... and require...daily dosing
short; multiple
name all the natural penicillins
G - IV, benzathine, procain
VK (oral)
spectrum of natural penicillins
G+ - strep (B&G always susc.), staph (mostly resistant now), enterococci, l. monocytogenes
G- - n. meningitides
Anaerobes - fair (not B. fragilis)
other - trep. pallidum (syphillis)
name the penicillinase-resistant pens.
oxacillin
nafcillin
dicloxacillin (PO)
cloxacillin (PO)
what is the drug of choice for staph. aureus that is not MRSA
oxacillin/nafcillin
name the aminopenicillins
-ampicillin (PO and IV)
-amoxicillin (PO)
what is the most preferred aminopenicillin and why?
amoxicillin b/c of better bioavailability
name the carboxypenicillins
ticarcillin
carbenicillin (PO)
what was the first class of drugs to treat pseudomonas aur.?
carboxypenicillins
name the ureidopenicillins
-piperacillin
-mezlocillin (not available?)
are there any ureidopenicillins available orally?
nope
T/F ureidopenicillins are not effective against pseudomonas?
False, they are very effective
name the beta-lactam/Blactamase inhibitors
-ampicillin/sulbactam
-ticarcillin/clavulanate
-piperacillin/tazobactam
-amoxicillin/clavulanate (PO)
what coverage does BL/BLase inhibitors have that other BLs don't?
anaerobes!
what is the most dangerous hypersensitivity rxn associated w/ BLs?
immediate (anaphylaxis) - IgE mediated
what BLs can cause an hepatic ADRs
ox and naf (metabolized by liver)
serum sickness is mediated by ____ and has what symptoms and when is the onset
IgG; rash, fever, leukopenia, arthralgia, pupura, lymphadenopathy; 1-2 weeks
the delayed IgG mediated hypersensitivity is seen with _____ and has what symtpoms/onset
beta-lactams; maculopapular rash; after several days of therapy
what beta-lactam can cause electrolyte abnormalities?
carboxypenicillins
the GI ADRs seen in beta-lactams could be caused by a ____ infxn
C. diff
what BL is prone to causing diarrhea as an ADR
clavulanate from augmentin (ticarcillin and clavulanate)
Drug interactions of BLs
-Oral contraceptives
-warfarin
-probenicid
structure of cephalosporins
'house with a basement'
cephalosporins do not cover...
-MRSA
-Enterococci
t/f oral absorption is good for cephs
t
what gens of ceph penetrate CSF
3 and 4
the distribution of ceph is similar to ...
pen
what cephs are partially metabolized
-ceftriaxone
-cefoperazone
1st gen cephs
-cefazolin
-cephalexin (po versrion of cefazolin)
-cefadroxil
-cefeclor
half lives of cephs are generally ____ than PCN an require ____ frequent dosing
longer;
less
most cephs are eliminated by the ____ and require ____
kidneys
renal dose adjustment
what drugs are cephamycins, what group are they in, what extra coverage do they have and what are they commonly used for
-cefotetan and cefoxitin
-2nd gen ceph
-G- anaerobes
-GI surgery propylaxis
name the 2nd gen cephs
-cefuroxime
-cefotetan
-cefoxitin
what extra coverage to 2nd gen cephs have"?
h. influenzae and m. catarrhalis
name the 3rd gen cephs
-ceftriaxone
-cefotaxime
-ceftazidime
name the 4th gen ceph
cefepime
what special coverage do ceftriaxone and cofotaxime have?
PCN resistant pneumococci
what extra coverage do the 3rd gen cephs have
n. gonorrheae and enterobacteriaceae and pcn resistant pneumococci
what is special about ceftazidime
pseudomonal coverage
what does cefepime cover
everything but anaerobes
hypersensitivities of cephs
cross react w/ pcn -- serious IgE rxns
ADRs of ceph
hypoprothrombinemia and bleeding
-agents with MTT inhibit vit. K clotting factors -->disulfram (antabuse) rxns
-other rxns like pcn
t/f cephs have few drug interactions
t
name the carbapenems
-imipenem/cilastatin
-meropenem
-ertapenem
what 3rd gen cef has p. aureginosa coverage?
ceftazidime
spectrum of 3rd gen ceph
G+ staph, strep (*esp pcn resistant pneumococci***)
G- same as 2nd gen + neis. gonorrhea + enterobactericeae
Ana - None
name the 4th gen cef
cefepime
spectrum of cefepime
G+ cocci
G- PEcK + Hi + McNgEb
ana - none
hypersensitivity of cefs
x-reactive w/ pcn - create serious IgE rxns in 7%
ADRs of cefs
-Hypoprothrombinemia/Bleeding from agents w/ MTT side chain
-disulfram like rxns
t/f cefs have lots of drug interactions
false
name the carbapenems
-imipenem/cilastatin
-meropenem
-ertapenem
wtf is cilastatin
-not a beta-lactamase inhibitor and has no antimicro action
-prevents degradation of imipenem in brush border of kidney
carbapenem dist. and absorption
-poor oral absorption
-good distribution
where is imipenem metabolized
by dihydropeptidase in brush border of kidney
carbs are eliminated how?
renally
carbs have ____ spectrum
broad
carbs cover MRSA t/f
false
carb spectrum
imi-/meropenem - very good G+, excellent G-, Excellent ana
erta- same but no pseudomonas or enterococcus
carb. hypersensitivity
x-react with pcn
ADRs of carb.
-seizures (renally dose adjust)
-hypersensitivity
name the monobactam
aztreonam
spectrum of aztreonam
Gram - ONLY!!
structure of aztreonam
garage w/ no house
t/f aztreonam has x-reactivity w/ pcn allergies
false - aztreonam has a different structure than pcn
t/f aztreonam distributes into eyes/prostate/CNS
false but has otherwise good distribution
the activity of sulfonamide is due to it's _____ ring in it's structure
benzene
folic acid is necessary for making _____
thymidine, purines and AAs
where do bact. get their folic acid derivatives and where do we get them from
bact. must synthesize them
we get them from our diet
what does PABA stand for
para-aminobenzoic acid
what is the activity of sulfonamide drugs linked to?
the benzene ring
sulfa drugs are bacterio____
static
t/f sulfa drugs affect mammalian cells
f - we get folate from our diets
t/f sulfa drugs are good for treating serious infxns such as bacteremias
false, they are bacteriostatic
MOA for sulfonamide
competitive inhibitor of dihydropteroate synthetase
MOA for trimethoprim
competitive inhibitor of dihydrofolate reductase (takes dihydrofolic acid to tetrahydrofolic acid)
Mech of resistance to sulfa
-overproduction of PABA
-use of alternate metabolic pathway (ie. exogenous FA intake
-mutations of dihydropteroate synthase ->poor affinity for sulfa
-losss of cell wall permeability
sulfasalazine is ____ absorbed and therefore used to treat...
poorly
ulcerative colitis/Crohn's DZ
sulfamethoxazole is used for...
UTI
nocardiosis
toxoplasmosis
malaria
what is co-trimoxazole
trimethoprim-sulfamethoxazole
Bactrim
Septra
TMP-SMX (TMP-SMZ)
why is tmp paired with smx?
synergism baby
what is the most effective ratio of SMX to TMP
20 parts SMX to 1 part TMP
TQ*** what is the dosing of SMP-TMX based on?
the TMP component!!!
tmp-smx is ____ absorbed
well
tmp is ____ lipid soluble than smx and has a ____Vd
more
larger
t/f tmp-smx distribute well into tissues including lung, CSF, urine
t
tmp is ___metabolized and is ____ excreted in urine and _____ renal dose adjustment
not
totally
requires
TQ**** t/f TMP-smx does not require renal dose adjustment
FFFFF
TQ**** T/F tmp-smx should be used to treat serious infxns such as bacteremias
F
smx is _____ metabolized and ____% is excreted unchanged in urine
acetylated
30
1/2 life of smx/tmp
8-10 hours
spectrum of tmp/smx
G+
staph (sometimes MRSA)
strep A,B,C and pneumonia (highly resistant
L. monocytogenes (2nd DOC)
G-
Hi, m. catarrhalis, enterobactericeae (resist.)
Misc.
-pneumocystis carinii
-nocardia
-GI pathogens (salmonella, shigella, v. cholera)
ADRs of tmp/smx
-hypersens.
-crytalluria ->stones
-hematologic
-G6PD deficiency*** -->hemolytic anemia
-bone marrow suppression
-hyperkalemia
-NVD
what ADRs are specific to tmp/smx
-hyperkalemia from tmp blocking K+ from being secreted
-NVD from large doses
drug intrxns of tmp-smx
-WARFARIN****TQ*** inc. INR and inc. risk of bleeding
-displace highly protein bound drugs
phenytoin - seizures
gyburide - oral hypoglycemic
-kernicterus in preggos -> displaces bilirubin from albumin ->newborn encephalopathy