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Lindsey's D&D Unit 3 > Antibacterial Agents II: Cell Wall Synthesis Inhibitors > Flashcards

Antibacterial Agents II: Cell Wall Synthesis Inhibitors Flashcards

1
Q

Name the 5 main β-lactam and cell wall synthesis inhibiting Abx.

A
  1. penicillins
  2. vancomycin
  3. cephalosporins
  4. carbapenems
  5. monobactams
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2
Q

What are the 3 stages of peptidoglycan synthesis?

A
  1. synth. of cell wall subunits in the cytosol
  2. linear polymerization of subunits at cell membrane
  3. cross-linking of peptidoglycan polymers at the cell wall
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3
Q

What inhibits stage 1 of peptidoglycan synthesis (synth. of cell wall subunits in the cytosol)?

A

fosfomycin, cycloserine

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4
Q

What inhibits stage 2 of peptidoglycan synthesis (linear polymerization of subunits at the cell membrane)?

A

bacitracin, vancomycin

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5
Q

What inhibits stage 3 of peptidoglycan synthesis (cross-linking of peptidoglycan polymers at the cell wall)?

A

penicillins, cephalosporins

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6
Q

Choose: Penicillins are BACTERICIDAL/BACTERIOSTATIC.

A

bactericidal

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7
Q

_____ is the generic term for enzymes that hydrolyze β-lactams, including penicillinases and cephalosporinases.

A

β-lactamase

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8
Q

β-lactamase is the generic term for enzymes that hydrolyze β-lactams, including ____ and _____.

A

penicillinases; cephalosporinases

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9
Q

β-lactamase is the generic term for enzymes that ____, including penicillinases and cephalosporinases.

A

hydrolyze β-lactams

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10
Q

How does MRSA occur?

A

alterations of penicillin binding proteins (PBPs) so they no longer bind

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11
Q

How are Penicillins absorbed, distributed, metabolized, and excreted?

A

A: good on empty stomach
D: throughout body- poorly into tissues- high conc in liver, kidney, skin
M: increased in kidney failure
E: kidney tubular secretion; breast milk

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12
Q

What is probenecid?

A

drug that blocks tubular secretion of penicillin to prolong it’s activity

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13
Q

Describe Penicillin G.

A

prototypical penicillin; powerful; inexpensive; hydrolyzed by acid and penicillinase enzyme

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14
Q

Describe Penicillin V.

A

acid-resistant; better absorbed than G; oral route ok; mild to moderate infections

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15
Q

Describe the penicillinase-resistant penicillins.

A

less potent than G; acid resistance and binding varies; eliminated by hepatic and renal routes; for gram + and gram - cocci; ex: methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin

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16
Q

Describe the extended spectrum penicillins.

A

increased hydrophobicity allows penetration thru porins; acid resistant but NOT penicillinase resistant; ex: ampicillin, amoxicillin

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17
Q

Describe the Anti-pseudomonal penicillins.

A

not resistant to penicillinase; effective against Pseudo. aeruginosa, enterococci, Bacteriodes fragilis; parenteral only; ex: ticarillin, piperacillin

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18
Q

What drug is not resistant to penicillinase; effective against Pseudo. aeruginosa, enterococci, Bacteriodes fragilis; parenteral only; ex: ticarillin, piperacillin?

A

the Anti-pseudomonal penicillins

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19
Q

What drug has increased hydrophobicity to allow penetration thru porins; acid resistant but NOT penicillinase resistant; ex: ampicillin, amoxicillin?

A

the extended spectrum penicillins

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20
Q

What drugs are less potent than G; acid resistance and binding varies; eliminated by hepatic and renal routes; for gram + and gram - cocci; ex: methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin?

A

the penicillinase-resistant penicillins

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21
Q

What drug is acid-resistant; better absorbed than G; oral route ok; for mild to moderate infections?

A

Penicillin V

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22
Q

What drug is the prototypical penicillin; powerful; inexpensive; hydrolyzed by acid and penicillinase enzyme?

A

Penicillin G

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23
Q

Name the 3 β-Lactamase Inhibitors.

A
  1. clavulanic acid
  2. sulbactam
  3. tazobactam
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24
Q

The ____ will extend the antibacterial spectrum of the accompanying penicillin ONLY if bacterial resistance is due to β-lactamase destruction AND the inhibitor is active against that particular β-lactamase.

A

β-lactamase inhibitor

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25
Q

The β-lactamase inhibitor will ____ of the accompanying _____ ONLY if bacterial resistance is due to β-lactamase destruction AND the inhibitor is active against that particular β-lactamase.

A

penicillin; extend the antibacterial spectrum

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26
Q

The β-lactamase inhibitor will extend the antibacterial spectrum of the accompanying penicillin ONLY if
_____ AND the inhibitor is active against that particular β-lactamase.

A

bacterial resistance is due to β-lactamase destruction

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27
Q

The β-lactamase inhibitor will extend the antibacterial spectrum of the accompanying penicillin ONLY if
bacterial resistance is due to β-lactamase destruction AND _____.

A

the inhibitor is active against that particular β-lactamase

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28
Q

Tx for Strep. pharyngitis, pneumoniae (CAP), sinusitis, otitis media, rheumatic fever, necrotizing fasciitis?

A

Pen G, Pen V, amoxicillin

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29
Q

Tx for Enterococci bacteremia, UTI?

A

Pen G, ampicillin + AG, ampicillin

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30
Q

Tx for Staph. aureus localized cutaneous infection, bacteremia, device-assoc. infections, pneumonia? (MSSA and MRSA)

A

MSSA: oxacillin
MRSA: NO penicillins

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31
Q

Tx for Neisseria gonorrhea?

A

Pen G (lots of resistance, tho)

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32
Q

Tx. for Neiserria meningititis meningitis?

A

Pen G

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33
Q

Tx for Moraxella catarrhalis otitis media, CAP?

A

amox/clav

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34
Q

Tx for Bacillis anthracis anthrax?

A

Pen G

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35
Q

Tx for Cornye. diphtheria?

A

Pen G

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36
Q

Tx for H. influenzae meningitis, otitis media, sinusitis, CAP?

A

ampicillin, amox/clav

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37
Q

Tx for E. coli UTIs, intra-abd infections, diarrhea, hemorrhagic colitis?

A

ampicillin, amox/clav

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38
Q

Tx for Klebsiella UTIs, intra-abd. infections?

A

ampicillin, amox/clav

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39
Q

Tx for H. pylori peptic ulcer disease?

A

ampicillin, amox/clav

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40
Q

Tx for Salmonella gastroenteritis, typhoid fever?

A

ampicillin, amox/clav

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41
Q

Tx for Pseudomonas aeruginosa opportunistic infections?

A

amox/clav, piper/tazo, ticar/clav

42
Q

Tx for Clost. perfringens gas gangrene, food poisoning?

A

Pen G

43
Q

Tx for Bacteriodes fragilis intra-abd. and brain abscesses?

A

Piper/tazo, ticar/clav

44
Q

Tx for Treponema pallidum syphilis?

A

Pen G

45
Q

Tx for Borrelia burgorferi Lyme disease (early)?

A

amoxicillin

46
Q

____ are virtually non-toxic except for hypersensitivity reactions.

A

Penicillins

47
Q

Penicillins are ____ except for hypersensitivity reactions.

A

virtually non-toxic

48
Q

Penicillins are virtually non-toxic except for _____.

A

hypersensitivity reactions

49
Q

How does penicillin become an antigen for hypersensitivity rxns?

A

functions as a hapten and combines with a protein

50
Q

Most penicillin reactions are related to the _____, which creates cross-linking.

A

6-aminopenicillianic

51
Q

___ of pts report a penicillin allergy but only ___ overall actually experience a rxn to exposure.

A

10%; 1-2%

52
Q

What is a type 1 penicillin rxn?

A

IgE mediated antibodies; very rare but can be life-threatening; 30 min onset

53
Q

What is a type 2 penicillin rxn?

A

cytotoxic Abs of IgG or IgM (complement dependent); rare; ex: hemolytic anemia

54
Q

What is a type 3 penicillin rxn?

A

delayed allergic rxn; 72 hour onset; IgG or IgM immune complexes that activate complement and lodge in tissues

55
Q

What is a type 4 penicillin rxn?

A

T cell mediated allergy; delayed onset; skin eruptions and thrombocytopenia

56
Q

What is the most common penicillin reaction?

A

a maculopapular or morbilliform rash (mild and reversible)

57
Q

How does vancomycin work?

A

it inhibits cell wall synthesis in stage 2 (linear polymerization)

58
Q

How is vancomycin administered and excreted?

A

A: IV unless used for GI treatment
E: renal (t1/2: 6-10 days)

59
Q

When should a vancomycin be used?

A

when less toxic agents are ineffective or not tolerated (ie penicillin allergy)

60
Q

Tx for MRSA severe skin and soft tissue infection?

A

vancomycin

61
Q

Tx for Staph and Strep meningitis, pneumonia, endocarditis, sepsis?

A

vancomycin

62
Q

Tx for ampicillin-resistant Enterococci bacteremia, endocarditis?

A

vancomycin

63
Q

Tx for C. diff pseudomembranous colitis?

A

metronidazole, oral vancomycin

64
Q

What are the adverse rxns for vancomycin?

A

chills, fever, skin rash, ototoxicity (pretreat with acetaminophen and diphenhydramine)

65
Q

Why do you pretreat vancomycin with acetaminophen and diphenhydramine?

A

b/c of the risk of ototoxicity

66
Q

Because of ototoxicity, pretreat with _____ and _____ before giving vancomycin.

A

acetaminophen; diphenhydramine

67
Q

What is Daptomycin?

A

a cyclic lipopeptide used to treat methicillin and vancomycin resistant staph and enterococci; restricted use

68
Q

Where does Daptomycin act? What does it do?

A

at the bacterial membrane- causes loss of intracellular ions

69
Q

Cephalosporins are a type of ____.

A

β-lactam antibiotics

70
Q

How do cephalosporins work?

A

similar to penicillins but less susceptible to penicillinase and less cross-reactivity

71
Q

How are cephalosporins absorbed, distributed, metabolized, and excreted?

A

A: orally or parenterally
D: penetrate well into most tissues and fluids, including the placenta; brain and CSF ONLY in 3rd gen
M/E: kidneys

72
Q

How many cephalosporins generations are there?

A

5

73
Q

What are the 1st generation cephalosporins?

A

Cefazolin, Cephalexin

74
Q

What do the 1st gen cephalosporins work for?

A

gram + and - cocci, some gram - bacilli

75
Q

_____ are more stable than penicillins to many beta-lactamases.

A

1st gen cephalosporins

76
Q

Why is Cefazolin now the prototype drug?

A

low cost, low tox, good penetration, lengthened t1/2 (90 min)

77
Q

Compared to Penicillin G, the _____ have greater activity against MRSA.

A

1st gen cephalosporins

78
Q

Compared to ____, the 1st gen cephalosporins have greater activity against MRSA.

A

Penicillin G

79
Q

Compared to Penicillin G, the 1st gen cephalosporins have greater activity against ____.

A

MRSA

80
Q

Name a 2nd generation cephalosporin.

A

Cefuroxime

81
Q

____ have greater activity against gram (-) bacteria and anaerobes, especially respiratory, but do not work against Pseudomonas.

A

2nd generation cephalosporins

82
Q

2nd generation cephalosporins have greater activity against _____ and _____, especially _____, but do not work against Pseudomonas.

A

gram (-) bacteria, anaerobes; respiratory

83
Q

2nd generation cephalosporins have greater activity against gram (-) bacteria and anaerobes, especially respiratory, but do not work against _____.

A

Pseudomonas

84
Q

Name 3 3rd gen cephalosporins.

A
  1. Cefdinir
  2. Ceftriaxone
  3. Ceftazidime
85
Q

Don’t give a _____ to a pt with a hx of penicillin allergy.

A

cephalosporin

86
Q

Don’t give a cephalosporin to a pt with a hx of _____.

A

penicillin allergy

87
Q

How is a 3rd gen cephalosporin different than 2nd gen?

A

expanded gram (-) bacilli coverage; also Enterobacter, Hemophilis, Neisseria and moderate antipseudomonal

88
Q

How is a 4th gen cephalosporin different than 3rd gen?

A

more resistant to chromosomal and extended spectrum β-lactamases; good against pseudomonas and S. pneumoniae; some anaerobic

89
Q

Name a 4th gen cephalosporin.

A

cefepime

90
Q

Name a 5th gen cephalosporin.

A

Ceftaroline

91
Q

What are the 5th gen cephalosporins similar to? How are they unique?

A

3rd gens; better gram (+) coverage including MRSA, S. pneumoniae, and E. faecalis; does NOT cover pseudomonas or anaerobes

92
Q

Tx for MSSA, Strep surgical prophylaxis, skin infections?

A

cephalexin (po), cefazolin (IV)

93
Q

Tx for Klebsiella pneumonia, UTIs?

A

cephalexin

94
Q

Tx for E. coli, Proteus UTIs?

A

cephalexin

95
Q

Tx for resistant E. coli, proteus, Klebsiella pneumonia, UTIs?

A

2nd gen cephalosporin

96
Q

Tx for H. influenza meningitis, otitis media, sinusitis?

A

Cefuroxime (IV), Cefaclor (po)

97
Q

Tx for M. catarrhalis otitis media, sinusitis?

A

Cefaclor (po)

98
Q

Tx for Bacteriodes peritonitis, diverticulitis?

A

Cefoxitin

99
Q

Tx for S. pneumoniae pneumonia, meningitis?

A

Cefotaxime, Ceftriaxone

100
Q

Tx for N. gonorrhea?

A

ceftriaxone

101
Q

Tx for Pseudo. aeruginosa UTIs, pneumonia?

A

Ceftazidime

102
Q

What are the adverse rxns for the cephalosporins?

A

allergies/hypersensitivities, GI upset, superinfections, can intensify oral coagulants

Lindsey's D&D Unit 3 (12 decks)

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