Inhibitors of Cell Wall Synthesis II Flashcards

1
Q

4 classes of beta-lactams

A

penicillins
cephalosporins
monobactams
carbapenems

ALL CIDALS!

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2
Q

3 other inhibitors of CWS (not beta-lactams)

A

vancomycin
phosphomycin
bacitracin

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3
Q

Cephalosporins mechanism of action

A

activate cell wall autolytic enzymes through blocking of terminal cross-linking of peptidoglycan

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4
Q

ICWS all do what?

A

all lyse cells

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5
Q

R2 substitutions determine degree of

A

antibacterial activity

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6
Q

R1 affects

A

pharmacokinetic properties

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7
Q

Chemically, cephalosporins are a group of antibiotics closely related to _______ and have what structures?

A

penicillin

beta-lactam ring structures

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8
Q

What advantage do cephalosporins have over penicillins?

A

7-methyl-group in cephalosporins which increases resistance to beta-lactamase

– never 100% resistance due to different types of beta-lactamase

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9
Q

First generation cephalosporins have what kind of spectrum?

A

narrow

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10
Q

First generation cephalosporins:

good activity against what kind of bacteria?

A

G+

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11
Q

First generation cephalosporins:

relatively moderate activity against what kind of bacteria?

A

Gram - (E. Coli, Kiebsiella, Proteus)

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12
Q

What kind of bacteria is susceptible to first generation cephalosporins?

A

Most G+ cocci

MSSA (enterococci, MRSA, and S. epidermis are resistant)

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13
Q

First generation cephalosporins:

some are:

A

acid resistant

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14
Q

First generation cephalosporins:

increased _______

A

beta-lactamase resistance

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15
Q

First generation cephalosporins:

how are they excreted?

A

renal excretion

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16
Q

What is the DOC for surgical prophylaxis?

A

cefazolin (parentally given)

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17
Q

Are first generation cephalosporins the DOFC for MSSA?

A

no - penicillinase-resistance still DOFC

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18
Q

Second generation cephalosporins:

lower activity against what type of bacteria?

A

G+

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19
Q

Second generation cephalosporins:

somewhat increased activity against what type of bacteria

A

G-

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20
Q

Second generation cephalosporins:

do they have antipseudomonal activity?

A

no

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21
Q

Second generation cephalosporins:

do they have beta-lactamase resistance?

A

yes - increased beta-lactamase resistance

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22
Q

Second generation cephalosporins:

are they acid resistant?

A

some are

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23
Q

Second generation cephalosporins:

how are they excreted?

A

mostly through renal excretion

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24
Q

What are the two first generation cephalosporins?

A

cefazolin - IV, IM

cephalexin - oral

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25
Q

What are the three second generation cephalosporins?

A

cefaclor - oral
cefuroxime - IV, IM
cefprozil - oral

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26
Q

Third generation cephalosporins:

what kind of spectrum

A

broad

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27
Q

What are the four third generation cephalosporins?

A

Ceftriaxone - IV/IM
Cefotaxime Sodium - IV/IM
Ceftazidime - IV/IM
Cefixime - oral

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28
Q

What is the only third generation cephalospore that is oral?

A

cefixime

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29
Q

Special characteristics of ceftriaxone?

Treats what?

A

CNS penetration

Neisseria

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30
Q

Special characteristics of cefotaxime sodium?

A

CNS penetration

31
Q

Ceftazidime used to treat what bacteria?

A

P. aeruginosa

32
Q

Third generation cephalosporins:

less active against

A

Gram + cocci

33
Q

Third generation cephalosporins:

much more active against

A

enterobacteriaceae (penicillinase producing strains)

34
Q

Third generation cephalosporins:

what kind of activity does ceftazidime combined with aminoglycosides treat?

A

pseudomonas aeruginosa activity

35
Q

Third generation cephalosporins:

how are they administered?

A

IV/IM and oral

36
Q

Third generation cephalosporins:

increased:

A

beta-lactamase resistance

37
Q

Third generation cephalosporins:

how are they excreted?

A

by kidney

38
Q

What is the drug of choice for N. gonorrhoeae?

A

Ceftriaxone

39
Q

In what populations do you not want to use ceftriaxone i?

A

neonates, billirubin displacement

40
Q

Third generation cephalosporins can/cannot penetrate CNS without inflammation

A

can

41
Q

What is the DOFC for pseudomonas?

A

antipseudomonas penicillins BUT can use ceftazidime if penicillin allergy

42
Q

Fourth generation cephalosporins:

comparable to what generation

A

3rd generation

43
Q

Fourth generation cephalosporins:

more resistant to

A

some beta-lactamases

44
Q

Fourth generation cephalosporins:

given how?

A

IV

45
Q

Fourth generation cephalosporins:

is/is not antipseudomonal?

A

IS

46
Q

Fourth generation cephalosporins:

what kind of coverage: gram+ or gram-

A

Gram+ coverage

47
Q

Fourth generation cephalosporins:

how are they excreted?

A

renal

48
Q

Which generation of cephalosporins have the broadest coverage

A

fourth generation

49
Q

What do fourth generation cephalosporins treat against?

A

enterobacteriaceae, MSSA, pseudomonas

50
Q

What generation of drugs do you use for empirical therapy?

A

fourth generation - particularly when resistance to beta-lactamases are anticipated

51
Q

Name one fourth generation cephalosporin?

A

Cefepime - IV

52
Q

Fifth generation cephalosporins bind to:

A

MRSA PBP

53
Q

Fifth generation cephalosporins do/do not have antipseudomonal activity.

A

do not

54
Q

Fifth generation cephalosporins

activity against what kind of bacteria?

A

G+ and G-, approved for CABP

55
Q

Fifth generation cephalosporins

what kind of excretion?

A

renal

56
Q

Fifth generation cephalosporins

what kind of special coverage?

WHY is this special?

A

MRSA and VRSA coverage

THE ONLY BETA LACTAM ACTIVE AGAINST MRSA

57
Q

Name of one fifth generation cephalosporin

A

ceftaroline fosamil - IV

58
Q

What makes fifth generation cephalosporin unique?

A

mechanistically, ceftaroline can bind to PBP2A with very high affinity - this is the mutated PBP that other beta-lactams cannot bind to

59
Q

ceftraline fosamil is an exception why?

A

it is because ONLY beta-lactam active against MRSA

still not drug of first choice against MRSA

60
Q

First or second generation cephalosporins are DOFC for which three bacteria?

A

E coli
Kiebsiella
Proteus

61
Q

Second of third generation cephalosporins are DOFC for which bacteria?

A

Moraxella catarrhalis

62
Q

Ceftriaxone or cefixime treat which bacteria?

A

neisseria gonorrheae

KNOW THIS

63
Q

What generation of drugs treat salmonella?

A

third generation cephalosporins

64
Q

What drug treats penicillin-resistant s. pneumoniae?

A

ceftriaxone

65
Q

What is used to treat borrelia burgdorferi?

A

ceftrioxone (LATE DISEASE ONLY)

66
Q

Level of safety for cephalosporins?

A

fairly

67
Q

Which has more toxicity - cephalosporins or penicillins?

A

cephalosporins

68
Q

Risk of ______ with cephalosporins with enterococci, G-bacilli, pseudomembranous colitis or candida

A

superinfection

69
Q

What type of reaction can people have after alcohol consumption with cephalosporins?

A

disulfiram-like reaction

(makes drinking intolerable due to hangover)

should not drink on this medicine

70
Q

What percentage of cross sensitivity with penicillin does cephalosporin have?

A

10%

71
Q

G.I symptoms commonly associated with cephalosporins?

A

anorexia, N/V, diarrhea

72
Q

Dose dependent renal tubular necrosis is associated with what class of drugs?

A

cephalosporins

73
Q

Why would you not want to treat something with cephalosporin and aminoglycosides?

A

synergistic nephrotoxicity (BIG DEAL)

74
Q

What is the DOFC for pseudomonas?

A

2 penicillins better than cephamine due to cephamine’s renal effects