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Systemic Pharm I > Cell Wall Synthesis Inhibitors > Flashcards

Cell Wall Synthesis Inhibitors Flashcards

1
Q

Natural 1st Gen Penicillins

A

penicillin G, penicillin V

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2
Q

Penicillinase-Resistant 2nd Gen Penicillins

A

dicloxacillin, methicillin, nafcillin, oxacillin

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3
Q

Which 2nd Gen penicillin is never used for treatment?

A

methicillin, only clinical MRSA identification

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4
Q

Aminopenicillins 3rd Gen

A

amoxicillin, ampicillin

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5
Q

Extended Spectrum 4th Gen Penicillins

A

piperacillin, ticarcillin

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6
Q

Which penicillin do optometrists prescribe most?

A

amoxicillin

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7
Q

1st Gen Cephalosporins

A

cefadroxil, cefazolin, cephalexin

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8
Q

2nd Gen Cephalosporins (5)

A

cefaclor, cefotetan, cefoxitin, cefprozil, cefuroxime

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9
Q

3rd Gen Cephalosporins (8)

A

cefdinir, cefditoren, cefixime, cefotaxime, cefpodoxime, ceftazidime, ceftibuten, ceftriaxone

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10
Q

4th Gen Cephalosporins

A

cefepime

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11
Q

5th Gen Cephalosporins

A

ceftaroline, ceftolozane

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12
Q

What are the three beta-lactamase inhibitors used in antibiotic combos?

A

clavulanic acid, sulbactam, tazobactam

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13
Q

“Other” cell wall synthesis inhibitors…

A

bacitracin, daptomycin, telavancin, vancomycin

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14
Q

Why do antibiotics work?

A

selectively interfere with synthesis of bacterial cell wall which bacterial cells cannot live without and human cells do not possess

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15
Q

What do these antibiotics require?

A

a cell that is actively dividing (should not be combined with a bacteriostatic antibody)

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16
Q

What is the main difference between gram + and - bacteria?

A

(+) have cell wall most exterior (-) have outer lipopolysaccharide membrane in addition to cell wall

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17
Q

What two cell components do cell wall inhibitors target?

A

peptidoglycan and transpeptidase

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18
Q

What cell wall component do penicillins and cephalosporins target?

A

transpeptidase

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19
Q

What cell wall component do bacitracin and vancomycin target?

A

peptidoglycan

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20
Q

Penicillins are…

A

among the most widely effective and least toxic drugs known but have limited use due to increased resistance

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21
Q

What are penicillin drug difference attributed to?

A

side chains

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22
Q

What differences do side chains manifest?

A

antimicrobial spectrum, stability to stomach acid, cross-hypersensitivity, susceptibility to degradative enzymes

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23
Q

What is constant in antibiotic chemical structure?

A

the beta lactam ring

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24
Q

What are transpeptidase enzymes?

A

PBPs, a group of bacterial enzymes that are anchored in the cytoplasmic membrane and extend into the periplasmic space

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25
Q

What is the function of transpeptidase enzymes?

A

assembly, maintenance, and regulation of the peptidoglycan portion of the bacterial cell wall

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26
Q

What is the MOA of beta-lactam antibiotics?

A

form a covalent bond with transpeptidase and inhibit catalytic activity of these enzymes which prevents elongation and cross linking of peptidoglycan and leads to autolysis

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27
Q

T/F each bacterial species has a unique set of PBPs to which particular antibiotics bind

A

true

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28
Q

Penicillins easily cross the cell wall of…

A

gram (+) bacteria

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29
Q

“Easy to kill” gram (-) bacteria have…

A

proteins inserted to act as channels to allow entry of antibiotic

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30
Q

“Hard to kill” gram (-) bacteria have…

A

very restrictive porins and thus are resistant to many antibiotics including penicillin

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31
Q

Hard to kill gram (-) bacteria example

A

pseudomonas

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32
Q

Where are natural penicillins obtained from and what are they susceptible to?

A

obtained from mold fermentation, susceptible to inactivation by beta-lactamases

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33
Q

Of the two natural penicillins, which one is injected and more available systemically?

A

penicillin G

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34
Q

What are penicillinase-resistant penicillins used for?

A

use restricted to the treatment of infections caused by penicillinase-producing staph

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35
Q

What is important to remember about methicillin?

A

it is NOT used for treatment due to causing interstitial nephritis and is used only to identify resistant strains of S. aureus aka MRSA (methicillin resistant staph aureus)

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36
Q

What is used to treat MRSA?!

A

vancomycin!! because it is resistant to all beta-lactam antibiotics

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37
Q

What are extended spectrum penicillins used for? (aminopenicillins)

A

designed to maintain gram (+) coverage and add “easy” gram (-) coverage

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38
Q

What do optometrists usually prescribe?

A

amoxicillin (oral) + a penicillinase inhibitor

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39
Q

What are 4th gen extended-spectrum penicillins used for?

A

gram (-) coverage, aka antipseudomonal penicillins

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40
Q

What are the natural forms of bacterial resistance?

A

no cell wall, cell wall impermeable to the drug

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41
Q

What is the acquired form of bacterial resistance?

A

plasmid transfer of genetics for resistance to multiple agents

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42
Q

What are three acquired resistance properties?

A

beta-lactamase activity, decreased permeability and altered PBPs

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43
Q

Explain b-lactamase activity resistance

A

enzyme hydrolyzes the b-lactam ring of drug resulting in loss of bactericidal activity

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44
Q

Explain decreased permeability resistance

A

bacteria possess an efflux pump to push antibiotic back outside the cell

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45
Q

Explain altered PBPs

A

different PBPs have a lower affinity to antibiotics requiring a clinically unattainable concentration of the drug

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46
Q

Which form of acquired resistance does MRSA have?

A

altered PBPs

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47
Q

Describe the absorption of penicillins

A

most are incompletely absorbed after oral administration (some have only injection because of poor GI absorption)

48
Q

Why do antibiotics affect intestinal flora?

A

they are incompletely absorbed and have sufficient quantities to affect flora

49
Q

Which penicillin is almost completely absorbed?

A

amoxicillin

50
Q

T/F penicillinase-resistant penicillins are destroyed in acidic environment

A

true

51
Q

Why can’t you take penicillinase-resistant penicillins with food?

A

must be taken 30-60 minutes before or 2-3 hrs after because you cannot have an acidic stomach environment

52
Q

T/F penicillins cross the placenta AND are teratogenic

A

false- they do cross the placenta but are NOT teratogenic

53
Q

T/F penetration to bone or CSF is insufficient unless inflammation is also present

A

true

54
Q

Is penicillin metabolism significant or insignificant?

A

insignificant

55
Q

How are most penicillins excreted?

A

the kidneys

56
Q

What percent of patients have hypersensitivity to penicillin?

A

5-10%

57
Q

What are three signs of penicillin hypersensitivity?

A

rash, angioedema, anaphylaxis

58
Q

T/F cross-allergic reactions with other beta-lactam antibiotics can happen

A

true, but rare… happens with 1st generation cephalosporins

59
Q

What are adverse reactions to penicillins?

A

hypersensitivity, diarrhea, nephritis, neurotoxicity, hematologic toxicities

60
Q

What is an important hematologic consideration with penicillin prescription?

A

penicillin causes decreased coagulation and should not be given to patients on a blood thinner (like warfarin)

61
Q

T/F cephalosporins are closely related to penicillins and are also B-lactam antibiotics?

A

true

62
Q

Cephalosporin MOA

A

the same as penicillin, cell wall synthesis disruption via transpeptidase

63
Q

T/F cephalosporins tend to be more resistant to certain B-lactamases than penicillins are

A

true

64
Q

First gen cephalosporins are used for…

A

gram positive coverage (including staph aureus)

65
Q

Second gen cephalosporins are used for…

A

gram positive coverage, improved gram negative coverage, and anaerobic coverage ex: cefaclor or cefoxitin

66
Q

Third gen cephalosporins are used for…

A

gram negative coverage (some pseudomonal coverage by ceftazidime)

67
Q

Fourth gen cephalosporins are used for…

A

broad spectrum coverage, gram + and - with full Pseudomonas coverage but no anaerobic coverage (cefepime)

68
Q

Fifth gen cephalosporins are used for…

A

gram negative and anaerobic with activity against S. aureus including MRSA (ceftaroline), S. pneumonia, and Pseudomonas (ceftolozane/tazobactim)

69
Q

Which generation of cephalosporins are considered advanced?

A

5th gen

70
Q

Which generation of cephalosporins have no oral formulations?

A

5th gen, injection only

71
Q

What are the six basic uses of cephalosporins?

A

skin infections, intra-abdominal infections, pneumonia, serious infections, MRSA, pseudomonas

72
Q

Which cephalosporin generation treats skin infections?

A

1st gen, gram (+)

73
Q

Which cephalosporin generation treats intra-abdominal infections?

A

2nd gen, anaerobic

74
Q

Which cephalosporin generation treats pneumonia?

A

3rd (or 4th)

75
Q

Which cephalosporin generation treats serious infections (especially immunocompromised patients)?

A

4th gen

76
Q

Which cephalosporin generation treats MRSA?

A

5th gen, ceftaroline

77
Q

Which cephalosporins treat pseudomonas?

A

ceftazidime (3rd), cefepime (4th), ceftolozane (5th)

78
Q

T/F cephalosporins are susceptible to staphylococcal penicillinase

A

false

79
Q

T/F cephalosporins have poor oral absorption

A

true

80
Q

What is true of the cephalosporin distribution?

A

only a few have penetration to CSF even if there is inflammation

81
Q

Where are cephalosporins secreted from?

A

kidney, except ceftriaxone

82
Q

Where is ceftriaxone eliminated?

A

liver/bile

83
Q

What is the risk of cross-reactivity to penicillin?

A

1% chance with first generation, use generation 3 or later for patients with PCN allergy

84
Q

What do B-lactamase inhibitors do?

A

do not have antibacterial activity themselves, blind to penicillinase and inactivate it to protect antibiotics

85
Q

What are the three b-lactamase inhibitors?

A

clavulanic acid, sulbactam, tazobactam

86
Q

What makes augmentin?

A

clavulanic acid and amoxicillin

87
Q

What is vancomycin?

A

an “other” cell wall inhibitor effective against multiple drug resistant organisms aka MRSA

88
Q

What is bacitracin?

A

an “other” cell wall inhibitor that causes nephrotoxicity and is only given topically as ointment (no oral/injection)

89
Q

What is the MOA of vancomycin and bacitracin?

A

inhibits cell wall synthesis via peptidoglycan damaging the underlying cell membrane

90
Q

What are vancomycin and bacitracin not effective against?

A

gram (-) cell wall synthesis

91
Q

T/F vancomycin is restricted to treatment of serious infections

A

true, b/c plasma mediated resistance is developing

92
Q

What is the administration of vancomycin?

A

slow IV infusion (oral only for enterocolitis)

93
Q

What eliminates vancomycin from the body?

A

kidneys

94
Q

What are the four adverse effects of vancomycin?

A

fever, chills, phlebitis at injection site, and flushing or shock

95
Q

Why does flushing/shock happen with vancomycin and how can you prevent it?

A

happens if infusion is rapid due to rapid release of histamine, for prevention pre-treat with antihistamine

96
Q

What is the synthetic derivative of vancomycin?

A

telavancin

97
Q

What is telavancin used for?

A

alternative treatment for gram (+) infections, esp. skin

98
Q

What is the MOA of telavancin?

A

inhibition of cell wall synthesis

99
Q

What is the spectrum of telavancin?

A

used with gram (+) staph and strep including MRSA

100
Q

T/F telavancin is more effective than vancomycin

A

false, it is the same not better

101
Q

What are the pharmacokinetic considerations for telavancin?

A

hepatic metabolism uncertain, IV infusion, monitor renal function

102
Q

What are adverse effects of telavancin?

A

taste disturbances, nausea, vomiting, insomnia, foamy urine, caution in cardiac conditions

103
Q

T/F you can prescribe telavancin to pregnant women

A

FALSE

104
Q

What is the MOA of bacitracin?

A

interferes with peptidoglycan and cell wall synthesis

105
Q

Which bacteria, + or -, is bacitracin used for?

A

gram + coverage

106
Q

T/F toxicity and allergic reactions are common with bacitracin

A

false

107
Q

T/F bacitracin can be used during pregnancy

A

true

108
Q

What is the administration of bacitracin?

A

topical only because of nephrotoxicity systemically

109
Q

What medication is used mainly for infectious blepharitis and overnight coverage of bacterial corneal ulcers?

A

bacitracin

110
Q

What is an alternative medication for treating gram (+) infections including MRSA?

A

daptomycin

111
Q

What is the MOA of daptomycin?

A

induces rapid depolarization of cell membrane

112
Q

What can daptomycin treat?

A

gram (+), skin structure infections

113
Q

What inactivates daptomycin?

A

pulmonary surfactants, never use it for pneumonia

114
Q

What are pharmokinetic considerations of daptomycin?

A

90 % bound to protein AND no hepatic metabolism

115
Q

What are adverse effects of daptomycin?

A

constipation, nausea, headaches, myalgia, insomnia

Systemic Pharm I (13 decks)

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