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187 Cards in this Set

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What is the MOA of b-lactams?
inhibition of cell wall synthesis (irreversible binding); prevents crosslinking of peptidoglycan
B-lactams are bactericidal or bacteriostatic?
bactericidal
b-lactams are time dependent or concentration dependent?
time dependent
What are the requirements for susceptibility to b-lactams?
actively growing and making a cell wall, not producing inactivating enzymes, lactams must be able to enter porin channels to reach peptidoglycan layer (gram -)
What organisms do b-lactams offer no coverage for?
atypicals, MRSA (except ceftaroline - 5th gen cephalosporin)
What anti-hyperlipidemic drug has a beta-lactam ring?
ezetimibe
What structure do b-lactams bind to kill bacteria?
penicillin binding proteins
Who discovered penicillin?
alexander flemming (1928)
What are the two types of natural pcn?
PCN G and PCN V (VK)
What are the routes for PCN G?
IM and IV (although does come oral but not in notes)
What are the routes for penicillin V?
PO`
What does the short acting form of PCN G have?
procaine
What does the long acting form of PCN G have?
benzathine
What is the dosing unit for pcn?
million units
Gram stain for streptococci and PCN usage?
Gram +, used frequently for streptococci
Gram stain for staphylococci and PCN usage?
gram +, has resistance issues to regular PCN
Gram stain for enterococci and PCN usage?
gram +, has resistance issues to regular PCN
Gram stain for streptococcus pneumoniae and PCN usage?
gram +, only used in highly susceptible strains
Gram stain for N. meningitidis and PCN usage?
gram - cocci and frequently used
What anaerobes is natural PCN used for?
Peptostreptococcus sp, and Actinomyces
What spirochete is natural PCN used for?
Treponema pallidum (syphillis)
What are the common clinical uses for natural PCN?
Upper respiratory tract infections *URI* (strep throat), meningitis, skin infections (S. pyogenes with clindamycin added), endocarditis (with gent), bone infections
What is the drug of choice for syphillis?
PCN (all stages of disease)
What is the dosing frequency for PCN?
q 4 to 6 h
LA form of PCN contains?
benzathine
CR form of PCN contains?
mix of benzathine and procaine
What are the resistance mechanisms to b-lactams?
-overproduction of PBPs,
-production of PBPs with reduced affinity to PCN or beta-lactams (usually gram +)
-B-lactam inactivatin enzymes
-inactivation of porins (gram -)
-efflux pumps (gram -)
What are the anti-staphylococcal PCNs / penicillinase-resistant PCNs?
Oxacillin, nafcillin, dicloxacillin, cloxacillin, methicillin (last two not on market anymore)
What are the routes of admin for oxacillin?
IV, PO
What are the routes of admin for nafcillin?
IV
What are the routes of admin for Dicloxacillin?
PO
What addition was made to the anti-staphylococcal PCNs (chemically) to be reistant to b-lactamases?
addition of large R group to sterically block b-lactamases
What is the drug of choice for MSSA?
anti-staphylococcal PCNs (oxacillin, nafcillin, dicloxacillin)
What to treat Streptococci with, Oxacillin or PCN?
PCN
What is the antimicrobial spectrum for anti-staphylococcal pcns?
staphylococci (as the majority are PCN resistant today), streptococci, limited anaerobic activity
What organisms does anti-staphylococcal pcns not have coverage against?
Enterococcus, gram - organisms
What are the two aminopenicillins?
Ampicillin, amoxicillin
Route of admin for ampicillin?
IV, PO
Route of admin for amoxicillin?
PO
Greater stability in gastric acid, amox or amp?
amox
Advantage of aminopenicillins over anti-staphylococcal pcns?
Gram - coverage with aminopenicillins
Antimicrobial spectrum coverage of aminopenicillins?
-Gram + (Streptococci and Enterococci, Listeria monocytogenes; DOES NOT cover Staph well)
- Gram - (E. coli, Proteus mirabilis, H. influenzae, Salmonella sp, Shigella sp)
-Some anaerobic coverage
What is the drug of choice for Enterococci?
Aminopenicillins
What is the drug of choice for Listeria?
aminopenicillins
What is the drug of choice for otitis media?
aminopenicillins (specifically high dose Amoxicillin)
What caution should be taken with administration of ampicillin?
ampicillin has a high level of sodium and should use caution with high dose and long term use or in selected populations
What are the carboxypenicillins?
Carbenicillin, Ticarcillin
What are the urediopenicillins?
Azloxillin, Mezocillin, Piperacillin
What are the carboxypenicillins and ureodiopenicillins referred to as?
extended spectrum penicillins
What is the antimicrobial spectrum for the extended spectrum penicillins?
increased gram - including pseudomonas, less activity with staph, strep and entero; excellent anaerobe activity
What is more potent for Pseudomonas and Enterococci, Piperacillin or Ticarcillin?
Piperacillin
What is more potent for Stenotrophomonas maltophilia (gram -) , Piperacillin or Ticarcillin?
Ticarcillin
Name the b-lactamase inhibitors
Clavulanic acid, sulbactam, tazobactam
What organism is sulbactam have activity against?
Acinetobacter sp
What are the side effects of Clavulanic acid?
Gi sides, cholestasis
What is another name for amoxicillin/clavulanic acid? Route of admin?
Augmentin, PO
What is another name for ampicillin/sulbactam? Route of admin?
Unasyn, IV
What is another name for Ticarcillin/clavulanic acid? Route of admin?
Timentin, IV
What is another name for Piperacillin/Tazobactam? Route of admin?
Zosyn, IV
MOA of b-lactamase inhibitors?
Suicide binding (irreversible)
Does ampicillin cover MSSA?
no
Does amoxicillin cover MSSA?
no
Does Augmentin cover MSSA?
yes
Does Unasyn cover MSSA?
yes
What is the difference between the MOA in MRSA resistance compared to MSSA?
MSSA uses b-lactamases but MRSA has a change in the PBP so b-lactamase inhibitors won't work
Augmentin or Unasyn work for S. pneumoniae?
no
What is the antimicrobial spectrum coverage of Augmentin and Unasyn?
-Expanded Gram + (MSSA)
-Expanded Gram - (Citrobacter, Enterobacter, Serratia, H influenzae, M catarrhalis - last two mislisted in the notes)
-Better anaerobic coverage (Bacteroides sp)
"Clinical Pearl" type of infections that b-lactam/ b-lactamases augmenting and unasyn are used for?
nosocomial acquired pneumonia, otitis media, sinusitis, skin and bone infections, ob/gyn, infections of (or near) mouth, intrabdominal infections
Drug of choice for otitis media?
Amox mono (not augmentin as clavulanic acid causes increased diarrhea and cholestasis)
What is the antimicrobial spectrum for b-lactam/b-lactamase inhibitors timentin and zosyn?
What augmentin or unasyn covers:
-Expanded Gram + (MSSA)
-Expanded Gram - (Citrobacter, Enterobacter, Serratia, H influenzae, M catarrhalis - last two mislisted in the notes)
-Better anaerobic coverage (Bacteroides sp)

PLUS
pseudomonas, serratia, acinetobacter
"Clinical Pearls" type of infections for zosyn?
nosocomial infections +/- AG FQ, respiratory, intrabdominal, diabetic foot, ssti
"Clinical Pearls" type of infections for timentin?
-2nd line for Stenotrophomonas maltophilia (cf patients)
-rarely used due to Na overload, teratogenicity, decreased platelet aggregation (increased chance of bleeding)
What PCN has the best coverage against pseudomonas: oxacillin, ampicillin, piperacillin, penicillin?
piperacillin
Which b-lactam group does not require renal adjustments?
anti-staphylococcal; mostly excreted in bile
Which pcn groups have rash associated with them?
all
Which pcn groups have allergic reactions associated with them?
all
Which pcn groups have diarrhea associated with them?
All, natural pcn sometimes not though; ampicillin has higher than normal
Which pcn groups have increased liver enzymes associated with them?
pcn, amino-pcn, anti-staph pcn
Which pcn groups have interstitial nephritis associated with them?
pcn and anti-staph pcn (methicillin)
Which pcn groups have extravasation associated with them?
Nafcillin
Which pcn groups have seizure associated with them?
PCN, amino-pcn
What are the b-lactams that have a decrease in absorption when ingested with food?
PCN V, amox, dicloxacillin, cloxacillin
PCNs that strongly interact with warfarin?
Nafcillin/dicloxacillin (strong cyp3a4 inducers)
PCNs that interact with birth control?
PCN and aminopenicillins (but really all PCNs)
What is the drug interaction with probenecid and PCN?
inhibits tubular secretion of PCN and increases half life
PCN anaphylaxis is mediated by which immunoglobulin?
IgE
PCN allergy crossreactivity with 1st gen cephalosporins?
10%
PCN allergy crossreactivity with 2nd and 3rd gen cephalosporins?
1-5%
PCN allergy crossreactivity with carbapenems?
5%
PCN allergy crossreactivity with monobactams?
Rare
What constitutes an immediate PCN allergy?
- <1h
-anaphylaxis, wheezing, bronchospasm, angioedema, hypotension, urticaria
-IgE mediated
What constitutes an accelerated PCN allergy?
- 1-72h
-urticaria, fever, laryngospasm, angioedema
-IgE mediated
What constitutes a delayed PCN allergy?
-rash, interstitial nephritis, hemolytic anemia, stephens-jonson syndrome, drug fever, neutropenia, thrombocytopenia
-IgG and IgM mediated
What agent does not beed to be renally adjusted: ampicillin, nafcillin, piperacillin/tazobactam, tazobactam?
nafcillin
What organisms in our notes do cephalosporins have no activity against?
enterococcus, lsteria, atypicals
Only 5th gen cephalosporin?
ceftaroline
What are the 1st gen cephalosporins?
IV
-Cefazolin, cephalothin, cephadrine
PO
-Cephalexin, cefadroxil
(only generation to have ceph instead of all "cef")
What is another name for ancef? what gen?
cefazolin, 1st gen
What is another name for cephalexin? what gen?
keflex, 1st gen
what is another name for duricef? what gen?
cefadroxil, 1st gen
What is the spectrum of activity for the first gen cephalosporins?
-Staph (MSSA and some coag-neg staph
-Streptococci, but not S/ pneumoniae
-Limited gram - (only enterobacteriaceae that don't make b-lactamases)
-no anaerobic (except peptostreptococcus)
"clinical pearl" infections treated with 1st gen cephalosporins?
-SSTI
-uncomplicated UTI
-surgical prophylaxis
-Lack of coverage for S. pneumoiae, H influenzae, and M catarrhalis limits use in respiratory tract infections, sinusitis, and otitis media
What are the 2nd gen cephalosporins?
IV
-Cefuroxime (zinacef), cefmetazole
PO
-Cefuuroxime (ceftin, zinacef), cefprozil (cefzil), cefaxlor (ceclor), loracarbef (lorabid)
What is the spectrum of activity for the second gen cephalosporins?
-increased gram - activity compared to 1st gen
-decreased gram + compared to first gen
-limited anaerobic
What are the cephamycins?
special 2nd gen cephs, Cefoxitin (mefoxin) and Cefotetam(cefotan); jave anaerobic coverage
What is the spectrum of activity for cephamycins?
Anaerobic coverage, especially gram - Bacteroides
decreased gram + coverage esp MSSA
What are the general uses for 2nd gen cephalosporins today?
mild to moderate community acquired infections
What are the uses for cephamycins?
surgical prophylaxis, intrabdominal, pelvic, ob.gyn infections
What are the 3rd gen cephalosporins?
IV
-ceftriaxone (rocephin), cefotaxime (claforan), ceftizoxime (ceftizox), ceftazidime (fortaz), cefoperazone
What is the spectrum of activity for 3rd gen cephalosporins?
-Enhanced gram - activity (enterobacteriaecae, Enterobacter, Citrobacter, Providencia)
-increased activity against H influenzae and M catarrhalis
-!!Pseudomonas activity: Ceftazidime only

-Limited gram + activity
S. Pneumoniae (ceftriaxone and cefotaxime only - have identical coverage)
Dosing schedule for ceftiaxone?
once daily due to protein binding
Drug of choice for inpatient community acquired pneumonia?
ceftriaxone/cefotaxime (3rd gen) +/- macrolide
Which 3rd gen cephalosporin should not be used in neonates? Why? Which should be used?
Ceftriaxone should not be used due to kernicterus in less than 3 months old; should use Cefotaxime instead
Drug of choice for gonorrheal infections?
ceftriaxone/cefotaxime
Which cephalosporin should be used for S. pneumoniae meningitis?
Ceftriaxone/cefotaxime
What are the oral 3rd gen cephalosporins?
Cefixime(suprax), cefpodoxime(vantin), ceftibuten(cedax), cefdinir(omnicef)
What is the microbial spectrum for 3rd gen ceph orals?
same as 3rd gen iv but no pseudomonas; cefixime and ceftibuten lack Staph activity
Primary use for 3rd gen ceph orals?
URI or Otitis media; can be used for STDs (gonorrhea with cefixime)
What are the 4th gen cephalosporins?
cefepime (maxipime)
What is the microbial spectrum for the 4th gen cephs?
-broadest of cephs (zqitterions)
-increased gram neg including pseudomonas
-increased gram + including S pneumoniae
-stable aginst many b-lactamases (can be used on Enterobacter, Citrobacter, Proteus vulgaris)
-Minimal anaerobic coverage
What is the drug of choice in febrile neutropenia?
cefepime(maxipime) (4th gen ceph)
Possible uses of cefepime other than febrile neutropenia?
meningitis, nosocomial infections (still need anaerobe coverage)
What are the 5th gen cephalosporins?
ceftaroline (teflaro) IV
FDA indications for ceftaroline?
-SSTI caused by MSSA, MRSA, Streps, E coli, Klebsiella
-CAP caused by MSSA, not MRSA, Streps, H flu, Klebsiella
What is ceftobiprole?
unapproved cephalosporin with MRSA, pseudomonas, enterococcus, and increased S. pneumoniae coverage
1st gen ceph absorption?
90%
2ng gen ceph absorption?
90%
3rd gen ceph absoprtion?
poor, 25-40%
4th gen ceph absorption?
iv only
5th gen ceph absorption?
iv only
what is the distribution of 1st gen ceph?
well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
what is the distribution of 5th gen ceph?
well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
what is the distribution of 4th gen ceph?
well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
what is the distribution of 3rd gen ceph?
well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
what is the distribution of 2nd gen ceph?
well into tissues, abcesses, bone, muscle, lung, liver, kidney, body fluids including bile, pleural, peritoneal
2nd gen ceph dist into meningitis?
some with cefuroxime
3rd gen ceph dist into meningitis?
high
4th gen ceph dist into meningitis?
high
5th gen ceph dist into meningitis?
high
1st gen ceph excretion?
renal
2nd gen ceph excretion?
tubular secretion
3rd gen ceph excretion?
renal except ceftriaxone which is biliary and thus no renal adjustment
4th/5th gen ceph excretion?
tubular secretion
All ceph % metabolized?
<10%
Half life on all cephs?
1-2 h except ceftriaxone which is 6h
What are the common adverse rxns to cephs?
rash, diarrhea, allergic rxns, c. diff (decreased rxns in general compared to pcns with trend being 1st gen > 2nd>3rd>4th/5th)
What are the rare adverse rxn to cephs?
seizures, hematologic issues interstitial nephritis
Which cephs have a methylthiotetrazole side chain? what is the significance?
Cefotan, Cefmandole, cefoperazone, cefmetazole (It apPERs the MAN has a TAN, or is it a METAZtasis? -melanoma) Causes vit k antagonism and disulfiram type rxns
Cephs and food interactions?
food can delay the rate of absorption
Cephs and drug interactions?
MMT-side chain = warfarin &eoth; probenecid causes decrease in tubular secretions
What is the broadest abx spectrum beta lactams?
carbapenems
What coverage is included in general with carbapenems?
Gram - including MDR organisms (Pseudomonas, Acinetobacter, ESBLs), Gram + except MRSA and E. faecium (VRE usually), and anaerobes (except C. diff)
What are the four carbapenems?
ertapenem, imipenem/cilastin, meropenem, doripenem
What organisms does ertapenem not cover?
Acinetobacter, Pseudomonas, Enterococci (but it is highly protein bound and only needs qd dosing)
What is the Drug of choice for extended spectrum beta lactamases?
carbapenems
What type of excretion are the carbapenems?
renal and need renal adjust.
What is the purpose of cilastin?
protects imipenem from inactivation by renal dehydropeptidase 1 and protects kidney from metabolites
What is the half life for the carbapenems?
1h for all except ertapenem which is 4h (and gets 1g IV qd)
What are the drug interactions for carbapenems?
decreases levels of valproic acid
What are the adverse rxns associated with carbapenems?
seizures (imipenem>meropenem/ertapenem>doripenem), and have issues with superinfections due to lack of coverage for VRE, stenotropomonas maltophilia, MRSA, Candida (but has a lower propensity for C diff infections than other agents)
What is the coverage with aztreonam?
gram - aerobes only; limited acitivity against Pseudomonas, enterobacter, citrobacter; inactive against acinetobacter and stenotrophomonas
What class is aztreonam?
monobactam
What is the common use for aztreonam?
usually when pt has PCN allergy. Can be used in menigitis, but requires renal adj
Cross resistance with aztreonam?
ceph resistance (inactive against ESBL_
What is the brand name for aztreonam?
azactam
What is the brand name for ertapenem?
invanz
what is the brand name for inipenem/cilastin?
primaxin
what is the brand name for meropenem?
merrem
what is the brand name for doripenem?
doribax
what is the brand name for ceftaroline? gen?
teflaro; 5th
what is the brand name for cefepime? gen?
maxipime; 4th
what is the brand name for cefixime? gen?
suprax; 3rd
what is the brand name for cefpodoxime? gen?
vantin; 3rd
what is the brand name for ceftibuten? gen?
cedax; 3rd
what is the brand name for cefdinir? gen?
omnicef; 3rd
what is the brand name for ceftriaxone? gen?
rocephin; 3rd
what is the brand name for cefotaxime? gen?
claforan; 3rd
what is the brand name for ceftizoxime? gen?
ceftizox, 3rd
what is the brand name for ceftazidime? gen?
fortaz, 3rd
what is the gen for cefoperazone?
3rd
What is the brand name for cefuroxime? gen?
zinacef, 2nd
what is the gen for cefmetazole?
2nd
what is the brand name for cefazolin, gen?
ancef, 1st
what is the brand name for cephalexin, gen?
1st, keflex
what is the brand name for cefadroxil, gen?
duricef, 1st
what is the gen for cephalothin?
1st
what is the gen for cephadrine?
1st