Pharm - Cephalosporins Flashcards by amanda kastel

recap - what are the antistaph penicillins

methicillin
oxacillin
cloxacillin
nafcillin

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differentiate between the structure of penicillins vs cephalosporins

both have 4-membered beta lactam ring

however, in penicillins, the fused ring is a 5-membered thiazoline and in cephalosporins it is a 6-membered dihydrothiazine ring

also, penicillins have 1 R substituent and cephalosporins have 2

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differentiate between the resistance to B lactamases between penicillins and cephalosporins

cephalosporins are MORE RESISTANT to beta lactamases

(but, some strains e coli and klebsiella that have extended spectrum b lactamases can still break cephalosporins)

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which have broader spectrum - penicillins or cephalosporins

cephalosporins

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cephalosporins, tho they have broader spectrum than penicillins, are STILL not active against __ and ____

listeria and enterococci

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true or false

cephalosporins have similar MOA and resistance mechanisms as penicillins

true

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how many cephalosporin generations are there??

explain the trends as far as:
-gram positive activity
-gram negative activity
-B lactamase resistance

5 generations

-all have similar activity against gram positive

-as you move up the generations (1–>5) there is a broader spectrum and more activity against gram (-)

-as you move up the generations (1–>5) B lactamase resistance increases

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name 3 1st gen cephalosporins

cephalexin
cefadroxil
cefazolin

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how can you remember which cephalosporins are 3rd gen

“one”
“ten”
“ime”

and cefdinir

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4th gen cephalosporin

cefepime

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2 5th gen cephalosporins

ceftaroline
ceftolozane

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cefprozil and cefuroxime - what gen

2nd gen

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3 mechanisms of cephalosporin resistance

-decreased concentration at site of action

-alter TWO PBP’s (1A and 2X)

-hydrolyzed by b lactamases (cephalosporinases)

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when the two PBP’s are altered, it makes ____ resistant to ______

pneumococci resistant to 3RD GEN CEPHALOSPORINS

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First gen cephalosporins have HIGH ACTIVITY against

gram positive cocci
(streptococci and staphylococci)

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what can 1st gen cephalosporins NOT be used to fight

MRSA
pseudomonas
enterobacter, citrobacter

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how is cephalexin administered

orally

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how is cefazolin administered

IV infusion only

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how are 1st gen cephalosporins eliminated

RENALLY - MUST DC DOSE

same issue as penicillins w seizures

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same DDI for 1st gen ceph and penicillins

probenecid substantially increases serum levels

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cephalexin clinical uses

PO 1st gen cephalosporin

UTI, staph and strp infections like cellulitis or soft tissue abscess

NOT FOR SERIOUS SYSTEMIC INFECTIONS

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at which gen can cephalosporins start being used for respiratory infections including pneumonia

2nd gen

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2nd gen have high activity against what 2 bacteria

Klebsiella and H. influenzae
-cause respiratory infection!!

gram positive cocci

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true or false

similar to 1st gen, 2nd gen cephalosporins are not active against enterococci, pseudomonas, or enterobacter infections

TRUE

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true or false cefuroxime is a 1st gen cephalosporin

FALSE - 2nd gen

how is cefuroxime administered

can be oral (cefuroxime axetil) or parenteral by IV (cefuroxime)

how is cefproxil administered and what gen

2nd gen oral

most cephalosporins are ________ cleared and thus require.....

renally cleared and thus require dose adjustment in renal failure

major gen of cephalosporins used for meningitis

3rd gen

which particular 2nd gen is used in CAP

cefuroxime

ORAL cephalosporins 2nd gen clinical uses

lower resp tract infections sinusitis otitis

true or false 3rd gen cephalosporins CANNOT be used in enterobacter infections

TRUE 4th gen can

main clinical uses 3rd gen cephalosporins

meningitis sepsis serious infections

3rd gen cephalosporins have high activity against which 2 bacteria

haemophilus neisseria (both can cause meningitis)

true or false 2nd gen cephalosporins can be used for CAP

true -- specifically cefuroxime

true or false 3rd gen have high activity against citrobacter

true

which 3rd gen cephalosporin is NOT renally eliminated and thus does NOT require a dosage adjustment in renal failure

ceftriaxone removed by liver (biliary tract)

intramuscular __ + ___ is used to treat gonorrhea

ceftriaxone + azithro

true or false 2nd gen cephalosporins can be used for the treatment of sepsis

FALSE 3rd gen

ceftazidime generation

3rd gen (one/ime/ten)

_____ + _______ is used to treat neutropenic and febrile immunocompromised patients

ceftazidime + avibactam (b lactamase inhibitor ceftazidime = 3rd gen cephalosporin - used for serious infections!

name 2 cephamycins and what generation are they

part of 2nd gen cefoxitin and cefotetan

the ORAL 2nd gen cephalosporins are active against __ and ___

b lactamase producing H. influenzae or moraxella catarrhalis

3rd gen cephalosporins have moderate activity against _____ specifically which 3rd gen

pseudomonas aeruginoisa only ceftazidime

3rd gen cephalosporins distribute well in the ____, aside from _____

well in CSF, aside from ORAL 3rd gen cephalosporins

___ and ___ are approved for meningitis including meningitis caused be pneumococci, meningococci, H. influenzae, and susceptible enteric gram negative rods

ceftriaxone and cefotaxime (3rd gen)

can 4th gen, like 3rd, also be used for febrile neutropenia empiric therapy?

yes

name 4 bacteria that cefepime has good activity against

pseudomonas enterobacteriaceae staph aureus (NOT MRSA) streptococccal pneumonia 4TH GEN

true or false cefepime is only given by IV route

true

2 main clinical uses of cefepime

enterobacter infections empiric therapy of febrile neutropenia good for nosocomial infections!

how is it that 4th gen cephalosporin like cefepime has good activity against enterobacter

it's more resistant to the beta lactamases produced by them

TRUE OR FALSE ceftaroline fosamil is not active against MRSA

FALSE - it is

2 major clinical uses ceftaroline fosamil

CAP SSTI (MRSA)

ceftaroline fosamil is NOT active against ---

extended spectrum b lactamase producing organisms or ampc

true or false ceftaroline fosamil is a prodrug

true metabolized to ceftaroline

TRUE OR FALSE ceftaroline fosamil retains binding to PBP2a

TRUE - ACTIVE AGAINST MRSA!

true or false ceftaroline fosamil is susceptible to chromosomal b lactamases

true

name 2 cephalosporins that can be combined with a b lactamase inhibitor also name their class

ceftazidime (3rd gen) + avibactam ceftolozane (5th gen) + taxobactam could also add metronidazole to that

with is the clinical use of ceftolozane + tazobactam + potential metronidazole

for hospital acquired pneumonia complicated UTI abdominal infections

true or false ceftolozane is not renally excreted

false - it is - need dose adjustment

what is approximate chance of cross reactivity that someone allergic to penicillin will also be allergic to cephalosporins? which gens is this most likely for?

~1% more likely with 1st and 2nd gen cephalosporins

main toxicity of cephalosporins

RENAL toxicity - interstitial nephritis and tubular necrosis

which group can cause bleeding issues and what molecule is it on what is done to resolve

MTT - methylthiotetrazole on cefotetan (2nd gen cephamycin) given with vitamin K gives severe disulfuram like reactions and hypoprothombinemia and bleeding disorders

true or false cephalosporins can cause c diff diarrhea

true - bc kills normal flora and c diff can overgrow

cephalosporins can cause ___ penia and ______penia

leukopenia and thrombocytopenia decreased blood cell count

*what generation of cephalosporins are recommended for the treatment of bacterial meningitis

3rd gen