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Pharmacotherapy V > Beta-Lactam Characteristics > Flashcards

Beta-Lactam Characteristics Flashcards

1
Q

What are the two anti-pseudmonal penicillins?

A

Ticarcillin, piperacillin

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2
Q

What beta-lactams are NOT excreted by the kidneys?

A

Nafcillin, oxacillin, ceftriaxone, cefoperazone

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3
Q

What beta-lactam does NOT demonstrate cross-reactivity?

A

Aztreonam

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4
Q

What PKPD do beta-lactamase drugs exhibit?

A

Time > MIC, time-dependent bactericidal

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5
Q

What are the two drugs of choice for MSSA?

A

Nafcillin and cefazolin

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6
Q

What cephalosporins demonstrate activity against anaerobes?

A

2nd generation cephalosporins cefoxitin, cefotetan, and cefmetazole

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7
Q

What is the only penicillin that can cover Klebsiella?

A

piperacillin

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8
Q

What five penicillins have a significant sodium load?

A

pen G sodium, piperacillin, ticarcillin, nafcillin, carbenicillin

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9
Q

What penicillin might you use for a respiratory tract infection, listeria, or enterococcus?

A

Aminopenicillins – ampicillin, amoxicillin

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10
Q

What type of penicillin is used for PSSP and syphilis?

A

Natural penicillins – pen G, pen VK

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11
Q

What are the four primary adverse reactions seen with the penicillins?

A

Neurotoxicity, hematologic toxicity, allergenicity, interstitial nephritis (nafcillin esp)

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12
Q

What gram-negative bacteria are covered by first-generation cephalosporins?

A

PEK = Proteus mirabilis, E. coli, K. pneumoniae

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13
Q

What gram-negative bacteria are covered by second-generation cephalosporins?

A

HENPEK = H. influenzae (BL-), Enterobacter (some), Neisseria, Proteus mirabilis, E. Coli, K. pneumoniae. M. catarrhalis

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14
Q

What is the “big hole” for cephalosporins?

A

Enterococcus – totally inactive

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15
Q

What is the anti-MRSA cephalosporin?

A

Ceftaroline

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16
Q

What cephalosporins cover pseudomonas?

A

Ceftazidime, cefoperazone, cefepime

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17
Q

What cephalosporins cover PRSP?

A

ceftriaxone, cefotaxime

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18
Q

What cephalosporin is active against KPC-producing bacteria?

A

Ceftazidime-avibactam

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19
Q

Which drug class demonstrates synergy when combined with a beta-lactam drug?

A

aminoglycosides

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20
Q

What cephalosporin has a much longer half life?

A

Ceftriaxone – 8 hours

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21
Q

What cephalosporins penetrate into the CSF?

A

cefuroxime, cefepime, 3rd generation (ceftazidime, ceftriaxone, cefpodoxime)

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22
Q

What is the only cephalosporin that does not cover pseudomonas?

A

ertapenem

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23
Q

What drug class demonstrate useful synergy with carbapenems when used for gram-negative aerobes?

A

aminoglycosides

24
Q

What carbapenem best penetrates the CNS?

A

meropenem

25
Q

What carbapenem has a longer half life and can be dosed once daily?

A

Ertapenem

26
Q

What is the spectrum of activity for aztreonam?

A

Gram-negative aerobes only.

NO gram-positive or anaerobic coverage

27
Q

Name some clinical roles for the carbapenems

A

Empiric therapy for hospital acquired infections, polymicrobial infections, SPICE/ESBL/AmpC bacteria, pseudomonas (except ertapenem)

28
Q

Name the clinical role for aztreonam

A

Infections due to gram-negative aerobes, especially in penicillin-allergic patients.

29
Q

What is the renal mechanism for penicillin excretion?

A

Tubular secretion

30
Q

How does the side chain lipophilicity and degree of protein binding affect penicillin characteristics?

A

lipophilic side chain = Increased protein binding

less degradation, less bioavailability, same half life

31
Q

Why is cephapirin unstable?

A

the acetyl group is hydrolyzed off, leaving a hydroxyl group that can react with the essential carbonyl group, resulting in an inactive ring version

32
Q

What is the key group on cefazolin and what is its purpose?

A

the thio-linked thiodiazole is stable to hydrolysis so it does not inactivate the cephalosporin. However, it still forms a good leaving group so it is potent parenterally

33
Q

What are the oral cephalosporins?

A

1st gen: cephalexin
2nd gen: cefuroxime, cefaclor
3rd gen: cefixime

34
Q

What sets oral cephalosporins apart?

A

Unreactive side chains at C-3 (next to carboxyl group)

35
Q

What role does a methoximino group plan on a cephalosporin?

A

Conveys resistance to hydrolysis via steric hindrance. However, only syn isomer is helpful.

36
Q

What does the prime ether on C-7 do for a cephalosporin?

A

Enhances stability against beta-lactamase (steric hindrance)

37
Q

How does an amine group off of C-7 help a cephalosporin?

A

The positive charge draws away electron density, making it more stable to acidic hydrolysis and potentially orally active (cephalexin/ceclor)

38
Q

Important aspects of cefazolin

A 
1st generation
DOC for MSSA, surgical prophylaxis
parenteral
tho-linked thiadiazole is stable to hydrolysis, but still good leaving group that activates B-lactam ring
strong inducer of AmpC
39
Q

Important aspects of cephalexin

A

1st generation
orally active
methyl group on C-3 not chemically reactive
ampicillin-type amino side chain stabilizes it in acid
Strong inducer of AmpC

40
Q

Important aspects of cefoxitin

A

2nd generation
parenteral
covers anaerobes - methoxy group off BL ring
Strong inducer of AmpC

41
Q

Important aspects of cefotetan

A

2nd generation
covers anaerobes
NMTT side chain can cause hypoprothrombinemia and disulfiram reaction

42
Q

Important aspects of cefuroxime

A

2nd generation
parenteral or oral (carbamate group more stable to acid, poor leaving group. prodrug available)
Oxime ether makes resistant to BL hydrolysis
penetrates the BBB

43
Q

Important aspects of cefotaxime

A 
3rd generation (not for SPICE)
good activity against PRSP
44
Q

Important aspects of ceftriaxone

A 
3rd generation (not for SPICE)
Good activity against PRSP
No pseudomonas coverage
Half life 8 hours, not adjusted for renal function
45
Q

Important aspects of ceftazidime

A

3rd generation (not for SPICE)
Covers Pseudomonas
Parenteral
Oxime ether enhances stability vs BL enzymes
charged pyridinium group is good leaving group

46
Q

Important aspects of cefoperazone

A 
3rd generation (not for SPICE)
Has MTT side chain -- disulfiram plus thrombocytopenia
Does not need to be adjusted for renal function
Covers pseudomonas
47
Q

Important aspects of cefprozil

A

2nd generation

48
Q

Important aspects of cefpodoxime

A

3rd generation (not for SPICE)

49
Q

Important aspects of cefepime

A

4th generation
parenteral with good leaving group
Syn-methoxyimino makes stable vs BL, improves gram-negative activity
Covers pseudomonas and BL-producing enterobacter

50
Q

What does SHEP stand for, and which drug class does it describe the spectrum for?

A

Shigella, salmonella, H. influenzae (BL-), E. Coli, Proteus

aminopenicillins

51
Q

What does SHEP-MEPP stand for, and which drug class does it describe the spectrum for?

A

Shigella/salmonella, H. influenzae, E. coli, Proteus, Morganella, Enterobacter, Providencia, Pseudomonas
Carboxypenicillin – ticarcillin

52
Q

What penicillin has the gram-negative spectrum SHEP-MEPP + KS?

A

Penicillin–covers serratia and klebsiella in addition to stuff covered by ticarcillin.

53
Q

When do penicillins have a PAE?

A

for gram-positive bacteria

54
Q

What are the primary clinical uses for the aminopenicillins?

A

Listeria, enterococcus

55
Q

Which carbapenem shows best CSF penetration?

A

Meropenem

56
Q

Could aztreonam be used for meningitis?

A

Yes, penetrates well

Pharmacotherapy V (10 decks)

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