Inhibitors of Cell Wall Synthesis Flashcards

1
Q

Synonym for Inhibitors of Cell Wall synthesis drugs?

A

Beta-Lactam antibiotics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is specific structure of penicillin?

A

Beta Lactam ring = 4 membered ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is important about beta lactam ring in penicillin?

A

It is strained, therefore reactive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is cephalosporin?

A

A fungally derived drug with a beta lactam ring (penicillin is bacterial derived)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is the characteristic of the beta lactam ring if it is broken?

A

It will not work

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What type of bacteria are cell-wall synthesis inhibitors most effective against?

A

Most gram positive, some gram negative

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What bacteria are Inhibitors of Cell-Wall synthesis drugs effective against (3 specific)?

A

Spirochete, treponema palidum (syphilis) and actinomycoses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What organisms are Inhibitors of Cell Wall synthesis drugs not effective against (5)?

A

Protozoa, fungi, viruses, tubercule bacillus and rickettsia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

When are inhibitors of Cell Wall synthesis most effective?

A

During early infection when bacteria are actively dividing and building cell wall

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What does a bacterial cell wall do (very general)?

A

Encases bacterial cell membrane; after water flows in, the cell wall becomes rigid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is the general fluid [ ] of cell interior of gram positive bacteria?

A

Hypertonic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What does penicillin inhibit in bacteria?

A

Inhibits cross linking of cell wall units

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What happens when the cell wall has holes punched in it by beta lactam drugs?

A

Membrane ruptures due to inflow of water to hypertonic cell causing rupture

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is required on the bacteria to aide the beta lactam drugs?

A

Bacterial surface enzymes (autolysins) that cleave previously synthesized cell wall; these are usually reserved for reproduction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

In the absence of bacterial autolysins what is the character of Beta Lactam drugs: bacteriocidal or bacteriostatic.

A

Bacteriostatic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the three stages of bacterial cell wall synthesis?

A
  1. Production of cell wall building blocks
  2. Precursor carried from inside cell membrane to
    outside
  3. Cross linking of cell wall
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Which Beta lactam drug inhibits the production of Cell Wall Building blocks (Stage I)? Treats what infection?

A

Cycloserine; tuberculosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What 2 beta lactam drugs inhibit the precursors being carried from inside the cell membrane to the outside (Stage II)?

A

Vancomycin and bacitracin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What 2 beta lactam drugs stop the cross-linking of the cell wall (Stage III)?

A

Penicillin and cephalosporin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

How does penicillin inhibit the cross linking of the cell wall?

A

It is similar to the D-alanyl-D-alanyl terminus of polypeptide side chain of peptidoglycan and occupies D- ala-D-ala substrate site of transpeptide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Beta lactam antibiotics interfere with what steps of cell wall synthesis?

A

Final steps

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What do autolysins normally do (2)?

A

Normally nick cell walls for attachment of new peptidoglycan units or separation of daughter cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Four ways bacteria can become resistant to Penicillin

A
  1. Lack of accessibility to target
  2. Production of penicillinases or beta lactamases
  3. Altered penicillin binding protein
  4. Drug efflux pumps
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What is an example of lack of accessibility to target for penicillin resistance?

A

Gram negative bacteria having outer membrane inhibiting access to cell wall

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What is absolute requirement for inhibition of transpeptidase?

A

Intact beta-lactam ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What is the difference between beta-lactamase and penicillinase?

A

Penicillinase only breaks down penicillin beta lactam ring

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

How can gram negative bacteria, who have low production of penicillinases still eliminate antibiotic without being swamped?

A

Gram negative limits access of beta lactam antibiotics via the peptidoglycan cell wall

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

If an antibiotic binds to Penicillin Binding Protein 2 or Penicillin Binding Protein 3 what will its effects be on the bacteria?

A

Prevents cell division (septum formation) and loss of rod like structure (filament formation)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What do PBP 2 and 3 do specifically?

A

3: Septum formation (cleave in rod)
2: Needed for rod shape

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

What does binding to PBP 1 affect?

A

Inhibits synthesis of cell wall so organism undergoes osmotic lysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

If Ab binds PBP 2 and 3, is the effect bacteriostatic or -cidal? PBP 1?

A

Static; PBP 1 is bacteriocidal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

In what stage of cell wall synthesis is PBP 1 involved?

A

Cross linking step on Stage III of cell wall synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

What can PBP 1 do to itself to resist penicillin?

A

Change its affinity for penicillin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

What will happen if bacteria increases levels of Penicillin binding protein?

A

It will soak up the penicillin to decrease the effect of penicillin on PBP 1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

What else can bacteria do to alter their penicillin binding protein to resist penicillin?

A

Synthesize new PBP’s with altered penicillin affinity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What does a drug efflux pump do?

A

Pumps out the drug once it gets into the cell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What is characteristic of broad spectrum penicillin versus narrow spectrum penicillin?

A

Broad spectrum can be effective against some gram negatives by getting through the Outer envelope of gram negative bacteria to attack transpeptidases in cell wall

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

Are penicillins widely distributed or narrowly distributed throughout the body?

A

Widely distributed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Where do penicillins not distribute well and therefore cannot be used for treatment in these areas of the body?

A

Joints, ocular tissue, cerebrospinal fluid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

What can cause penicillin to reach higher levels in the central nervous system?

A

Inflammation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

What administrative route is most common parenteral route that gives predictable blood level for penicillin?

A

Intramuscular

42
Q

What penicillin administrative route to use for treatment of severe infection requiring fast action and high blood levels?

A

Intravenous

43
Q

How much penicillin is absorbed by oral administration?

A

20-25%

44
Q

How is penicillin eliminated?

A

Renal

45
Q

What fraction of penicillin is excreted as a still active drug? Half life?

A

2/3; ~1hr

46
Q

Why is probenecid used?

A

Decreases renal excretion of drugs to increase antibiotic plasma concentration during serious infection

47
Q

Use of penicillin is limited primarily by ___?

A

Resistance

48
Q

Five toxicities ass’d w/ penicillin?

A

Resistance, hypersensitivity, anaphylactic shock, CNS effects or superinfection

49
Q

Staph infections acquired in hospital are usually susceptible or resistant to penicillin?

A

Resistant

50
Q

What respiratory problem increases one’s risk of penicillin hypersensitivity?

A

Asthma

51
Q

Would a penicillin hypersensitivity result in anaphylaxis?

A

No, just a rash

52
Q

What would be six signs of penicillin anaphylaxis?

A

Bronchoconstriction, abdominal pain, nausea, vomiting, weakness, fall in BP

53
Q

What are immediate indicators of anaphylaxis?

A

Dizziness, weakness, sweating and palpitations

54
Q

After a sensitization dose to penicillin, what are likely symptoms?

A

Rash, fever, swollen joints several days after taking penicillin

55
Q

When would a person be at risk for penicillin to affect CNS?

A

Pt has impaired renal function or infused w/ unusually high dose

56
Q

What is the major risk w/ long-term penicillin therapy?

A

Superinfection

57
Q

4 General classes of penicillins?

A

Pencillin G (benzylpenicillin), Gastric-acid-resistant penicillin, penicillinase-resistant pencillin, or broad-spectrum penicillin

58
Q

Standard reference penicillin?

A

Pencillin G (benzylpenicillin)

59
Q

Is Penicillin G adminstered orally?

A

No, inactive at low pH

60
Q

Can penicillin G get by penicillinases in bacteria, e.g. against Staph aureus?

A

No, pencillinase sensitive

61
Q

Is penicillin G broad or narrow spectrum?

A

Narrow, gram + only (similar to Pen V)

62
Q

Penicillin G are used in the treatment of what three bacterial infections?

A

Syphillis, rheumatic fever and gonorrhea

63
Q

Name for Gastric Acid Resistant Penicillin?

A

Penicillin V (acid stable)

64
Q

SIgnificance of Penicillin V?

A

Can be given orally and produces higher blood levels than Penicillin G (2-5x)

65
Q

4 Penicillinase-Resistant Penicillins?

A

Methicillin, cloxacillin, nafcillin, dicloxacillin

66
Q

Advantage and disadvantage of Penicillinase Resistant Penicillins?

A

Less susceptible to penicillinases; narrow spectrum

67
Q

Methicillin (penicillinase resistant penicillin) is oral or IV admin?

A

IV. Not absorbed orally

68
Q

Is Methicillin as effective as Penicillin G against organisms not producing penicillinase?

A

No, only 50% as effective as Pen G

69
Q

3 Broad Spectrum Penicillins?

A

Ampicillin, amoxicillin, and carbenicillin

70
Q

What are Broad-Spectrum Penicillins more active against, Gram - or Gram +?

A

Gram -, reduced against gram +

71
Q

Are Broad Spectrum Penicillins susceptible to penicillinases?

A

Yes

72
Q

What is the penicillin-related drug that is front line for tuberculosis treatment?

A

Cycloserine

73
Q

Which stage of cell wall synthesis does the anti- tuberculosis drug Cycloserine target?

A

First stage

74
Q

What penicillinase-resistant penicillin can be given orally?

A

Dicloxacillin

75
Q

This penicillin-related drug is last line of defense treating MRSA and also used in Endocarditis.

A

Vancomycin

76
Q

Only place Vancomycin administered?

A

Hospital

77
Q

Which stage of Cell Wall synthesis does Vancomycin inhibit?

A

Intermediate

78
Q

This intermediate stage cell wall synthesis inhibitor is toxic systemically, but used topically? What type of bac does it kill: gram + or -?

A

Bacitracin; gram +

79
Q

Bacitracin normally paired with what other 2 drugs as a topical ointment (triple-biotic, Neosporin)?

A

Polymyxin and neomycin

80
Q

3 agents that can be given in combination with Penicillin or Cephalosporin to increase their activity by breaking down bacterial resistant Beta-lactamase or Penicillinase?

A

Clavulanate, sulfabactam and taxobactam

81
Q

Cephalosporins are cell wall inhibitors that are bacterial or fungal derived?

A

Fungal

82
Q

Cephalosporins are resistant to…

A

Pencillinase

83
Q

How are Cephalosporins and penicillins similar?

A

Both have beta-lactam rings

84
Q

What bacteria types are Cephalosporins effective against?

A

Gram + and -

85
Q

Most cephalosporins are administered IV or IM. Which 2 cephalosporins are administered orally?

A

Cephalexin and cefaclor

86
Q

What is the distribution for Cephalosporins?

A

Well-distributed except CNS

87
Q

Are most cephalosporins readily metabolized or minimally metabolized?

A

Minimally metabolized

88
Q

How are cephalosporins excreted?

A

Kidney

89
Q

2 things that can block cephalosporin excretion in the kidney?

A

Probenecid (med specifically given to decrease excretion to increase drug potency) and renal failure

90
Q

What causes the hypersensitivity in penicillin and cephalosporins?

A

Beta-lactam ring

91
Q

Adverse reaction of cephalosporins systemically

A

Nephrotoxicity

92
Q

3 infections Cephalosporins used for?

A

Meningitis, streptococcal, staphylococcal

93
Q

Why use Cephalosporin?

A

Gram - infection that is penicillin resistant

94
Q

When is Cephalosporin used prophylactically?

A

During and after surgery for endocarditis

95
Q

3 classifications of Cephalosporins

A

1st, 2nd and third generations

96
Q

2 characteristics of 1st Generation Cephalosporins?

A

Good against G+, modest against G-

97
Q

First Generation Cephalosporin that can be administered orally?

A

Cephalexin

98
Q

2 characteristics of 2nd Generation Cephalosporins?

A

Good against G-. not very active against G+

99
Q

2 characteristics of 3rd Generation Cephalosporins?

A

Active against G-, especially those producing penicillinase

100
Q

3 ways bacteria can be Cephalosporin resistant?

A

Drug can’t reach target, produce enzyme to disrupt active ring or alter ab binding protein

101
Q

Pseudomonas and proteus Gram negative bacteria can produce this for Cephalosporin resistance.

A

Cephalosporinase