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Pharmacotherapy V > Beta-Lactam Characteristics > Flashcards

Beta-Lactam Characteristics Flashcards

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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?

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A

aminoglycosides

24
Q

What carbapenem best penetrates the CNS?

25
What carbapenem has a longer half life and can be dosed once daily?
Ertapenem
26
What is the spectrum of activity for aztreonam?
Gram-negative aerobes only. | NO gram-positive or anaerobic coverage
27
Name some clinical roles for the carbapenems
Empiric therapy for hospital acquired infections, polymicrobial infections, SPICE/ESBL/AmpC bacteria, pseudomonas (except ertapenem)
28
Name the clinical role for aztreonam
Infections due to gram-negative aerobes, especially in penicillin-allergic patients.
29
What is the renal mechanism for penicillin excretion?
Tubular secretion
30
How does the side chain lipophilicity and degree of protein binding affect penicillin characteristics?
lipophilic side chain = Increased protein binding | less degradation, less bioavailability, same half life
31
Why is cephapirin unstable?
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
What is the key group on cefazolin and what is its purpose?
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
What are the oral cephalosporins?
1st gen: cephalexin 2nd gen: cefuroxime, cefaclor 3rd gen: cefixime
34
What sets oral cephalosporins apart?
Unreactive side chains at C-3 (next to carboxyl group)
35
What role does a methoximino group plan on a cephalosporin?
Conveys resistance to hydrolysis via steric hindrance. However, only syn isomer is helpful.
36
What does the prime ether on C-7 do for a cephalosporin?
Enhances stability against beta-lactamase (steric hindrance)
37
How does an amine group off of C-7 help a cephalosporin?
The positive charge draws away electron density, making it more stable to acidic hydrolysis and potentially orally active (cephalexin/ceclor)
38
Important aspects of cefazolin
``` 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
Important aspects of cephalexin
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
Important aspects of cefoxitin
2nd generation parenteral covers anaerobes - methoxy group off BL ring Strong inducer of AmpC
41
Important aspects of cefotetan
2nd generation covers anaerobes NMTT side chain can cause hypoprothrombinemia and disulfiram reaction
42
Important aspects of cefuroxime
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
Important aspects of cefotaxime
``` 3rd generation (not for SPICE) good activity against PRSP ```
44
Important aspects of ceftriaxone
``` 3rd generation (not for SPICE) Good activity against PRSP No pseudomonas coverage Half life 8 hours, not adjusted for renal function ```
45
Important aspects of ceftazidime
3rd generation (not for SPICE) Covers Pseudomonas Parenteral Oxime ether enhances stability vs BL enzymes charged pyridinium group is good leaving group
46
Important aspects of cefoperazone
``` 3rd generation (not for SPICE) Has MTT side chain -- disulfiram plus thrombocytopenia Does not need to be adjusted for renal function Covers pseudomonas ```
47
Important aspects of cefprozil
2nd generation
48
Important aspects of cefpodoxime
3rd generation (not for SPICE)
49
Important aspects of cefepime
4th generation parenteral with good leaving group Syn-methoxyimino makes stable vs BL, improves gram-negative activity Covers pseudomonas and BL-producing enterobacter
50
What does SHEP stand for, and which drug class does it describe the spectrum for?
Shigella, salmonella, H. influenzae (BL-), E. Coli, Proteus | aminopenicillins
51
What does SHEP-MEPP stand for, and which drug class does it describe the spectrum for?
Shigella/salmonella, H. influenzae, E. coli, Proteus, Morganella, Enterobacter, Providencia, Pseudomonas Carboxypenicillin -- ticarcillin
52
What penicillin has the gram-negative spectrum SHEP-MEPP + KS?
Penicillin--covers serratia and klebsiella in addition to stuff covered by ticarcillin.
53
When do penicillins have a PAE?
for gram-positive bacteria
54
What are the primary clinical uses for the aminopenicillins?
Listeria, enterococcus
55
Which carbapenem shows best CSF penetration?
Meropenem
56
Could aztreonam be used for meningitis?
Yes, penetrates well

Pharmacotherapy V (10 decks)

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