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Pharmacology II > Lecture 20: Inhibitors of Cell Wall Synthesis > Flashcards

Lecture 20: Inhibitors of Cell Wall Synthesis Flashcards

1
Q

What is the major difference between bacterial and mammalian cells

A

Presence of rigid cell wall

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2
Q

The cell wall in bacterial cells protects cells from ____

A

Osmotic rupture

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3
Q

What structure in the bacterial cell wall is particularly important for rigidity and resistance to osmotic lysis

A

Peptidoglycan

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4
Q

Gram ___bacteria have a thick peptidoglycan layer and no outer membrane

A

Positive

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5
Q

Gram ___bacteria have a thin peptidoglycan layer and an outer membrane

A

Negative

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6
Q

Penicillin, cephalosporins, monobactams, and carbapenems are what type of antibiotics

A

B-lactams

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7
Q

What is the mechanism of action for b-lactams

A

Prevent the crosslinking/ transpeptidation

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8
Q

What antibiotic is a glycopeptide

A

Vancomycin

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9
Q

Are Cell wall inhibitors bacteriocidal or bacteriostatic

A

Bacteriocidal

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10
Q

Cell wall inhibitors eventually result in cell death due to ___

A

Osmotic lysis

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11
Q

Protein synthesis inhibitors prevent the action of ___, therefore should not be used together

A

Cell wall inhibitors

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12
Q

Natural penicillin is extracted from culture of ___and semisynthetic penicillins are manufactured from ____

A

Penicillium chrysogenum, penicillin nucleus (6-amino penicillanic acid- 6-APA)

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13
Q

What is the chief structural requirement for the biological activity of penicillin

A

Penicillin nucleus

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14
Q

The antibacterial activity of penicillin resides in the ___

A

Intact b-lactam ring

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15
Q

___can split the B-lactam ring by enzymes or acids and result in loss of antibacterial action

A

B-lactamases

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16
Q

Natural penicillins have the highest antibacterial activity against ___

A

Gram positives

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17
Q

Natural penicillins cover what bacteria

A
  1. Gram positive
  2. Some gram negative
  3. Some anaerobes
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18
Q

Do natural penicillins have antipseudomonas activity

A

No

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19
Q

How are natural penicillins eliminated

A

Via kidney

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20
Q

Natural penicillins have poor ___penetration, unless their is inflammation

A

CNS

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21
Q

What natural penicillin has a short half life ~2hrs and is administered IV, IM

A

Penicillin G potassium

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22
Q

What natural Pencillin has a low concentration for 30days and is used prophylactically, administered IM

A

Penicillin G benzathine

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23
Q

What natural penicillin is used for everyday practice, longer half life ~10-20hrs, given IM

A

Penicillin G procaine

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24
Q

What natural penicillin is relatively acid resistant and therefore orally useful

A

Penicillin V

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25
Q

Natural penicillins are the drug of choice for what 4 bacteria

A
  1. Group A beta hemolytic streptococci
  2. Spirochetes
  3. Many Gram positive anaerobes
  4. Gram negative aerobic cocci
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26
Q

Penicillinase resistant penicillins (antistaphylococcal penicillins) have lower activity against what bacteria

A

Gram positive

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27
Q

Penicillinase resistant penicillins have coverage against what bacteria

A
  1. Some gram negative
  2. Some anaerobe
  3. Less gram positive
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28
Q

Penicillinase resistant penicillins is the drug of choice against ___

A

Penicillinase producing S. Aureus

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29
Q

Penicillinase resistant penicillins have ___metabolism and ___excretion

A

Hepatic, renal

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30
Q

What are the 3 examples of penicillinase resistance penicillins

A
  1. Oxacillin
  2. Cloxacillin
  3. Methicillin
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31
Q

What is methicillin used for

A

Diagnostic tool to determine if organism is resistant to methicillin which is a change in penicillin binding protein or if B-lactamase activity

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32
Q

What is oxacillin used for

A

Treatment of bone, soft tissue, and skin infections by penicillinase producing staphylococci

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33
Q

Oxacillin is used in what species

A

Dogs and horses

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34
Q

What is cloxacillin used for

A

Intramammary administration in dry and lactating dairy cattle

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35
Q

Extended spectrum penicillins have lower coverage of what bacteria

A

Gram positive

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36
Q

What bacteria do extended spectrum penicillins cover

A
  1. Gram negative bacteria
  2. Anaerobic coverage when combined with penicillinase inhibitor
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37
Q

Do extended spectrum penicillins have antipseudomonal activity

A

No

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38
Q

Extended spectrum penicillins are susceptible to ___

A

B-lactamase (why combine with penicillinase inhibitors to provide anaerobic coverage)

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39
Q

Can you give extended spectrum penicillins orally

A

Yes- acid resistant

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40
Q

Extended spectrum penicillins have ___excretion

A

Urinary

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41
Q

What are the two examples of extended spectrum penicillins

A

Amoxicillin and ampicillin

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42
Q

What are ampicillin and amoxicillin used for

A

Tx sensitive bacterial infections, particularly respiratory infections

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43
Q

Which has better absorption: ampicillin or amoxicillin

A

Amoxicillin

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44
Q

Ampicillin and amoxicillin are FDA approved for what species

A

Dog, cats, cattle

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45
Q

What coverage do antipseudomonal penicillins provide

A
  1. Extended spectrum penicillins (gram negative, anaerobes if combined with penicillinase inhibitors)
  2. Enteric gram negative bacilli (not Klesibella)
46
Q

Antipseudomonal penicillins major use is the treatment of ___

A

Pseudomonas aeruginosa

47
Q

Antipseudomonal penicillins are susceptible to ___

A

B-lactamase

48
Q

Can you give antipseudomonal penicillins orally

A

No-acid sensitive

49
Q

Antipseudomonal penicillins have ___excretion

A

Renal

50
Q

What are the two examples of antipseudomonal penicillins

A

Piperacillin
Ticarcillin

51
Q

Which has better antipseudomonal activity, piperacilin or ticarcilin

A

Piperacillin

52
Q

What are the 3 beta-lactamase inhibitors that can be combined with other products

A
  1. Clavulanic acid
  2. Sulbactam
  3. Tazobactam
53
Q

B-lactamase inhibitors are not active against

A

Methicillin resistant, penicillinase-producing staphylococci- because change in PBP not B-lactamase activity

54
Q

What are some mechanisms of resistance to penicillin (5)

A
  1. B-lactamase
  2. Decreased permeability
  3. Alteration in PBPs
  4. Autolytic enzymes not being activated- tolerance
  5. Lack of peptidoglycan cell wall- mycoplasma and chlamydia
55
Q

90% of penicillin is excreted via the __

A

Tubular system

56
Q

Tubular secretion of penicillins can be partially blocked by ___ which can provide ___systemic level of penicillin in severe infections

A

Probenecid, higher

57
Q

What is the major penicillin toxicity

A

Allergies- hypersensitive rxn- anaphylaxis

58
Q

Are first generation cephalosporins narrow or broad spectrum

A

Narrow

59
Q

What do first generation cephalosporins have activity against

A
  1. Good activity against gram positive
  2. Moderate activity against gram negative
60
Q

First generation cephalosporins have good activity against some gram positive cocci except ___ and ___

A

Enterococci, methicillin resistant S. Aureus

61
Q

Which generation of cephalosporins have good activity against E. Coli, Klebsiella pneumonia, and Proteus mirabilis

A

First

62
Q

What are the 4 example of first generation cephalosporins

A
  1. Cefazolin
  2. Cefadroxil monohydrate
  3. Cephalexin
  4. Cephapirin
63
Q

What is cefazolin used for

A

Surgical prophylaxis

64
Q

What is cefadroxil monohydrate used for

A

Susceptible infections of skin, soft tissue, and GU in dogs and cats

65
Q

What is cephalexin used for

A

Susceptible skin infections in dogs

66
Q

What is cephapirin used for

A

Mastitis in lactating and dry cows

67
Q

What spectrum are second generation cephalosporins

A

Intermediate

68
Q

Second generation cephalosporins have increased activity against ___

A

Gram negative

69
Q

What are the two examples of second generation cephalosporins

A
  1. Cefoxitin
  2. Cefaclor
70
Q

Are third generation cephalosporins narrow or broad spectrum antibiotics

A

Broad

71
Q

Third generation cephalosporins are less active than first generation against __, but much more active against ___, including ___ producing strains

A

Gram positive cocci, enterobacteriaecae, including penicillinase producing strains

72
Q

What are the 4 examples of third generation cephalosporins

A
  1. Ceftiofur
  2. Cefovecin
  3. Cefixime
  4. Cefpodoxime
73
Q

What is ceftiofur used for

A

Respiratory infections for cattle, swine, and horses

74
Q

What is cefovecin used for

A

Cats and dogs with skin and soft tissue infections

75
Q

What is cefixime used for

A

Extra label for skin, soft tissue and urinary infections in dogs and cats

76
Q

What is cefpodoxime used for

A

Labeled for skin and soft tissue infections in dogs

77
Q

Fourth generation cephalosporins are more resistant to ___

A

B-lactamases

78
Q

What is the 1 example of fourth generation cephalosporins

A

Cefepime

79
Q

What is cefepime used for

A

Potentially used for treating neonatal foals and dogs with severe infections

80
Q

What 4 organisms do cephalosporins have no activity against

A
  1. MRSA
  2. Listo. Monocytogenes
  3. Enterococci
  4. Atypical- Myocplasma and chlamydia
81
Q

What two organisms do cephalosporins have no effect against but penicillin does

A

Listo. Monocytogenes
Enterococci

82
Q

Most cephalosporins are excreted by the ___

A

Kidney

83
Q

What is the mechanism of action of polymixin B

A

Produces a detergent that disrupts the cell membrane

84
Q

What are the uses for polymixin B

A
  1. Topically to treat gram negative bacterial infections of skin, eye and ear in all species
  2. Combined with bacitracin for broad spectrum effects
  3. Administered orally to cattle and swine to tx gram negative enteric infections
85
Q

What are some adverse effects of polymixin B

A

Nephrotoxicity if given parenterally

86
Q

Monobactams: Aztreobam are drugs with ___ring

A

Monocyclic beta-lactation

87
Q

Aztreonam is relatively resistant to ___

A

B-lactamases

88
Q

What is Aztreonam active against

A

Gram negative rods, including pseudomonas

89
Q

Aztreonam have no activity against ___and ___

A

Gram positive and anaerobes

90
Q

What are some side effects of Aztreonam

A

Phlebitis, skin rash, abnormal liver function

91
Q

Aztreonam has not cross sensitivity with ___derivatives

A

Pencillin

92
Q

What class do imipenem; cilastatin and meropenem belong to

A

Carbapenems, B-lactam antibiotics

93
Q

Imipenem is rapidly inactivated by ___ and must be given with ___

A

Dehydrogenase, cilastatin (dehydrogenase inhibitor)

94
Q

Are carbapenems broad or narrow spectrum

A

Broad

95
Q

What do carbapenems: imipenem; cilastatin and meropenem have activity against

A
  1. Anaerobes
  2. Gram positive
  3. Gram negative rods
96
Q

What carbapenem can cause seizures at high levels

A

Imipenem

97
Q

What is the mechanism of action of vancomycin

A

Inhibits cell wall synthesis by:
1. Binding to D-Ala-D-Ala terminus of peptidoglycan and prevents crosslinking
2. Inhibits transglycosylation which inhibits elongation of peptide chain

98
Q

How does resistance develop to vancomycin

A

D-Ala-D-Ala mutation replaced by D-Ala-D-lactate

99
Q

Gram ___are resistant to vancomycin and can be combined with ___for synergistic effect

A

Negative, Aminoglycosides

But also has synergistic toxicity

100
Q

What antibiotic is very useful in MRSA and gram positive infections in Pencillin allergic patients

A

Vancomycin

101
Q

T or F: vancomycin is absorbed orally

A

False

102
Q

What are some adverse reactions with vancomycin

A
  1. Hypersensitivity
  2. Nephro and ototoxicty
  3. Uremia after high dose can be fatal
103
Q

What antibiotic is very useful for susceptible Gram positive systemic life threatening infections

A

Vancomycin

104
Q

T or F: vancomycin can be used in food producing animals

A

False, banned

105
Q

What is the mechanism of action of Bacitracin

A

Interferes with final dephosphorylation step of lipid carrier so can’t transport peptidoglycan to outer cell wall

106
Q

Bacitracin is active against what bacteria

A

Gram positive

107
Q

Parenteral bacitracin use is rare due to risk of ___

A

Nephrotoxicity

108
Q

Bacitracin is commonly used topically in addition with ___ and ___ to prevent ___

A

Neomycin and polymixin
Prevent superficial skin and eye infections following minor injuries

109
Q

Which antibiotic has the properties in series A
A. Imipenem/Cilastatin
B. Vancomycin
C. Pencillin
D. Ampicillin
E. Cefazolin

A

D. Ampicillin

110
Q

Which antibiotic has properties in series C:
A. Imipenem/ Cilastatin
B. Vancomycin
C. Penicillin G
D. Ampicillin
E. Cefazolin

A

B. Vancomycin

111
Q

Which antibiotic has the properties in series A
A, Aztreonam
B. Vancomycin
C. Penicillin G
D. Cefixime
E. Oxacillin

A

C. Penicillin G

Pharmacology II (36 decks)

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