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Unit 2- Pharm > Inhibitors of Cell Wall Synthesis I > Flashcards

Inhibitors of Cell Wall Synthesis I Flashcards

1
Q

All inhibitors of cell wall synthesis are

A

bactericidal

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2
Q

Cell walls protect against

A

cell lysis

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3
Q

Five groups of inhibitors of cell wall synthesis?

A 
Cycloserine
Bactracin
Penicillins
Vancomycin
Fosfomycin
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4
Q

Gram positive bacteria has

A

thick peptidoglycan

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5
Q

Gram negative bacteria has

A

outer membrane + thin peptidoglycan layer

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6
Q

Major difference between bacterial and mammalian cells is presence of a

A

rigid cell wall external to the cell membrane

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7
Q

Cell wall protects bacterial cells rom

A

osmotic rupture - which would result from the fact that the cell is usually hyperosmolar to host environment

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8
Q

Peptidoglycan is composed of

A

a backbone of two alternating sugars, NAG and NAM

a chain of four AA that are linked to NAM

a peptide bridge that cross-links the tetrapeptide chain

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9
Q

Transglycosulation joins

A

NAM and NAG together

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10
Q

Transpeptidation joins

A

alanine with diaminopimetic acid

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11
Q

Peptidoglycan is the ____ of cells

A

armor

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12
Q

What makes the peptidoglycan really strong?

A

transpeptidation

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13
Q

What does transglycosulation and transpeptidation?

A

penicillin-binding proteins

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14
Q

Inhibition of any stage of the synthesis, export, or assembly or peptidoglycan lead to inhibition of bacterial cell growth and

A

cell death

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15
Q

Peptidoglycan is synonymous with

A

cell wall

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16
Q

How is peptidoglycan formed?

A
  1. addition of subunits (a sugar with its five attached AA)
  2. transport through cytoplasmic membrane to the cell surface
  3. subsequent cross-linking by cleavage of the terminal stem-peptide AA
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17
Q

Where are precursor units (NAM, NAG) assembled?

A

cytoplasm

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18
Q

What carries NAM and NAG across inner membrane?

A

lipid carrier

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19
Q

Where does peptidoglycan form?

A

outside of the inner membrane

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20
Q

Peptidoglycan synthesis:

Transglycosylation

Enzymatic action performed by:

A

joining of NAG and NAM

PBPs

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21
Q

Peptidoglycan synthesis:

Transpeptidation

Enzymatic action performed by:

A

cross links pentapeptides

PBPs

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22
Q

In peptidoglycan synthesis, NAG reduced to

A

NAM

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23
Q

In peptidoglycan synthesis, transport across

A

inner membrane

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24
Q

In peptidoglycan synthesis, amino acid mimicry

A

pentapeptide chain

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25
Q

Transpeptidation is inhibited by

A

penicillins

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26
Q

If you give someone B-lactam antibiotics, what does not occur?

A

transpeptidation

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27
Q

If transpeptidation does not occur, what happens?

A

cell lyses

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28
Q

Inhibitors of cell wall synthesis are:

A

bactericidal to growing cells because they must be remodeling cells for it to work

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29
Q

Inhibitors of cell wall require what three things for activity and cell lysis.

A

Penicillin-binding proteins, active growth, and autolysins

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30
Q

Beta-lactam antibiotics prevent what?

A

cross-linking reaction called transpeptidation

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31
Q

If an infection has gone into latency, will inhibitors of cell wall synthesis work?

A

No.

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32
Q

Virtually all antibx that inhibit cell-wall synthesis are

A

bactericidal

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33
Q

cell death is due to

A

osmotic lysis

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34
Q

loss of cell wall integrity following treatment is due to the bacteria’s own cell wall remodeling enzymes called _______ that cleave peptidoglycan bonds in the normal course of cell growth

A

autolysis

35
Q

In the presence of agents that inhibit cell wall growth, ______ proceeds without normal cell-wall repair; weakness and eventual lysis occur.

A

autolysis

36
Q

Protein synthesis inhibitors _____ action of the cell wall synthesis inhibitors.

A

prevent

37
Q

If you put an inhibitor of cell growth with a static drug, will it be effective?

A

No - not effective b/c cell has stopped growing

38
Q

If cell has stopped growing ______ antibiotics are useless.

A

beta-lactam

39
Q

If a cell is being remodeled on the outside, what is happening on inside?

If using beta-lactam antibiotics, what happens?

A

Making new units on inside

Degradation continues

Layer thickness does not change

Making of new structures ceases

40
Q

Are beta-lactam antibiotics useful with non-growing cells?

A

no.

41
Q

8 criteria for properties of inhibitors of cell wall synthesis?

A
  1. activity against gram (+)
  2. spectrum (gram (-), anaerobic, coverage)
  3. activity against pseudomonas aeruginosa
  4. penicillinase resistance
  5. acid resistance - oral absorption
  6. CNS penetration
  7. route of elimination
  8. unique adverse effects
42
Q

4 groups based on spectrums of penicillin

A
  1. natural penicillin
  2. penicillinase resistant
  3. extended spectrum
  4. antipseudomonal
43
Q

4 natural penicillins

A

pen G
pen V
benzathine penicillin
procaine penicillin G

44
Q

4 penicillinase resistant penicillins

A
  1. nafcillin
  2. dicloxacillin
  3. oxacillin (prostaphilin)
  4. methicillin
45
Q

2 extended spectrum penicillins

A
  1. ampicillin

2. amoxicillin

46
Q

2 antipseudomonal penicillins

A
  1. piperacillin

2. ticarcillin

47
Q

Penicillinase is a

A

method of bacterial resistance

48
Q

Penicillinase AKA

A

beta-lactamase

49
Q

What does penicillinase do?

A

enzyme that hydrolyzes beta-lactam ring so that it no longer bind to PBP (target)

50
Q

How do some bacteria defend against antibiotics?

A

penicillinase

51
Q

How does penicillin work?

A

it kills by interfering with the production of cell wall – weakened cell wall rupture and cell dies

52
Q

What type of penicillin has the highest antibacterial activity against certain G+ bacteria including G+ anaerobic bacteria

A

natural penicillins

53
Q

Natural penicillins have ____ G- coverage.

A

some

54
Q

Natural penicillins are readily activated by _______

A

beta lactamase

55
Q

Natural penicillins are not effective against strains of

A

s. aureus

56
Q

Natural penicillins have _____ antipseudomonal activity.

A

no

57
Q

Natural penicillins are eliminated by

A

active transport in the kidney

58
Q

Natural penicillins have ____ CNS penetration.

Exception?

A

poor

except in cases with inflammation – with inflammation, natural penicillins have more CNS penetration

59
Q

Penicillin G is adminstered how?

A

parentally.

not well absorbed orally

60
Q

Penicillin V is administered how?

A

relatively acid resistant - absorbed well orally

61
Q

Penicillin G treats gram (+) or (-)

A

(+)

62
Q

Penicillinase-Resistant Penicillins have what kind of activity against gram (+) and gram (-) bacteria?

A

lower activity against G+ bacteria and some G- coverage (more than natural penicillin)

63
Q

Penicillin G treats these three major illnesses?

A

pneumococcal pneumonia

syphilis

gonorrhea (typically pen G is not first choice)

64
Q

Some penicillinase-resistant penicillins are ____ stable and highy protein bound

A

acid

65
Q

Penicillinase-resistant penicillins are

A

resistant to penicillinase

66
Q

MSSA

A

methicillin sensitive staph aureus

67
Q

more than ____% of S aureus isolates are resistant (MRSA)

A

20%

68
Q

What kind of metabolism and excretion are associated with penicillinase-resistant penicillin?

A

hepatic metabolism

renal excretion

69
Q

What is a useful treatment for diabetics who have an infection with MSSA or MRSA and cannot take a lot of antiobiotics?

A

maggot therapy

70
Q

MRSA is (mechanism of resistance)

A

penicillinase resistant

71
Q

MRSA resistance is not associated with

A

production of beta-lactamase

72
Q

MRSA produces _____ _____ which decreases affinity of beta-lactam antibiotics to PBPs

A

alternate PBP

73
Q

_________ cannot be used to treat MRSA

A

beta-lactam

74
Q

What is the exception for beta-lactams to treat MRSA

A

ceftaroline

75
Q

beta-lactam induces cell lysis in normal cells

in MRSA, what does not allow beta-lactam binding?

A

alteration in PBP

76
Q

How does MRSA work?

A

changes the target of the drug so the drug cannot detect the altered PBP

77
Q

Extended spectrum penicillins have what kind of coverage?

A

lower G+ coverage
extended G- coverage (E. Coli, Salmonella, Shigella, H. Influenzae, Proteus)
No antipseudomonal activity

78
Q

resistance develops frequently or infrequently with extended spectrum penicillins

A

frequently

79
Q

extended spectrum penicilins are susceptible to

A

beta-lactamase

80
Q

extended spectrum penicillins are/are not acid resistant

A

are

81
Q

extended spectrum penicillins are excreted how

A

urinary excretion

82
Q

what is extended spectrum penicillins a drug of choice for

A

lysteria infections

83
Q

What are penicillinase-resistant penicillins a drug of choice for?

A

penicillinase-producing s. aureus (MSSA)

Unit 2- Pharm (9 decks)

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