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Pharm Exam 4 > Penicillin and Cephalosporin > Flashcards

Penicillin and Cephalosporin Flashcards

1
Q

What is a synonymn for “Inhibitors of Cell Wall synthesis drugs”?

A

Beta Lactam Antibiotics

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2
Q

What is the specific structure of penicillin?

A

Beta Lactam ring = 4 membered ring

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3
Q

What is important about beta lactam ring in penicillin?

A

It is strained and reactive.

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4
Q

What is a cephalosporin?

A

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

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5
Q

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

A

It doesn’t work.

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6
Q

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

A

Most are gram positive with some gram negative

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7
Q

What bacteria are Inhibitors of Cell Wall synthesis drugs effective against?

A 
Spirochetes 
Treponema palidum (syphilis) Actinomycoses
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8
Q

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

A 
Protozoa
Tubercule bacillus
Fungi 
Rickettsia
Viruses
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9
Q

When are inhibitors of Cell Wall synthesis most effective?

A

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

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10
Q

Why are Cell Wall synthesis inhibitor drugs not as effective in later stage infections?

A

Construction of bacterial cell wall is slower

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11
Q

What does a bacterial cell wall do?

A

Encases bacterial cell membrane

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12
Q

What is the character of the cell interior of gram positive bacteria?

A

Hypertonic

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13
Q

What does penicillin inhibit in bacteria?

A

Inhibits cross linking of cell wall units

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14
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.

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15
Q

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

A

Bacterial surface enzymes (autolysins) that cleave previously synthesized cell wall

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16
Q

In the absence of bacterial autolysins what Is the character of Beta Lactam drugs bacteriocidal or bacteriostatic?

A

Bacteriostatic

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17
Q

What are the 3 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
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18
Q

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

A

Cycloserine

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19
Q

Cycloserine (Stage I cell wall synthesis inhibitor) is used in treating what infection?

A

Tuberculosis

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20
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

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21
Q

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

A

Penicillin and Cephalosporin

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22
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.

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23
Q

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

A

The final steps

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24
Q

Cell death requires the action of what?

A

Autolysins

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25
Q

Autolysins act how normally?

A

They normally nick cell walls for attachment of new peptidoglycan units.

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26
Q

What are 4 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
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27
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.

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28
Q

What is the absolute requirement for inhibition of transpeptidase?

A

Intact beta-lactam ring

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29
Q

What is the difference between penicillinase and beta lactamase?

A

Penicillinase only breaks down penicillin beta lactam ring.

Beta lactamase breaks down both penicillin and cephalosporin beta lactam ring

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30
Q

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

A

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

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31
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) Loss of rod like structure (filament formation)

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32
Q

If an antibiotic binds to Penicillin Binding Protein 1 what will its effects be on the bacteria?

A

Inhibits cell wall synthesis

Organism undergoes osmotic lysis

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33
Q

If antibiotic binds PBP 2 and PBP 3 is the effect bacteriocidal or bacteriostatic?

A

Bacteriostatic

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34
Q

If antibiotic binds PBP 1 is the effect bacteriocidal or bacteriostatic?

A

Bacteriocidal

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35
Q

What stage of cell wall synthesis is PBP 1 involved in?

A

Cross linking step on stage III of cell wall synthesis

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36
Q

What can PBP 1 do to itself to resist penicillin?

A

Change affinity for penicillin

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37
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

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38
Q

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

A

synthesize new PBP’s with altered penicillin affinity

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39
Q

What does a drug efflux pump do?

A

Pumps the drug out once it gets in cell

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40
Q

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

A

Broad spectrum can be effective against some gram negatives by getting through the outer membrane to attack the inner membrane peptidoglycan

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41
Q

Are penicillins widely distributed or narrowly distributed throughout the body

A

Widely distributed

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42
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

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43
Q

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

A

Inflammation

44
Q

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

A

Intramuscular

45
Q

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

A

Intravenous

46
Q

How much penicillin is absorbed by oral administration?

A

20-25%

47
Q

How is penicillin eliminated?

A

Renal

48
Q

How much of penicillin is excreted as active drug?

A

Two thirds

49
Q

What is the half-life of all penicillins?

A

Approximately 1 hr

50
Q

Why is probenecid used?

A

It decreases renal excretion of drugs to increase antibiotic plasma concentration during serious infection.

51
Q

Use of penicillin is limited primarily by what?

A

Resistance

52
Q

Is penicillin one of the more highly toxic or least toxic drugs in medicine?

A

One of the least toxic

53
Q

Use of penicillin limited primarily by

A

Resistance

54
Q

What are 5 toxicities associated with penicillin?

A
  1. Resistance
  2. Hypersensitivity
  3. Anaphylactic shock
  4. CNS effects
  5. Superinfection
55
Q

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

A

Resistant

56
Q

What respiratory problem increases one’s risk of penicillin hypersensitivity

A

Asthma

57
Q

Would a penicillin hypersensitivity result in anaphylaxis?

A

No. It would only cause a rash.

58
Q

What would be the signs of penicillin anaphylaxis?

A 
Bronchoconstriction
Abdominal pain
Nausea 
Vomiting
Weakness
Fall in BP
59
Q

What are immediate indicators of anaphylaxis?

A

dizziness, weakness, sweating, palpitations

60
Q

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

A

Rashes, fever, swollen joints several days after taking penicillin

61
Q

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

A

When the patient has impaired renal function or is infused w/ unusually high dose

62
Q

What is the risk with long term penicillin therapy

A

Superinfection

63
Q

What are 4 General classes of penicillins?

A
  1. Penicillin G(benzylpenicillin)
  2. Gastric Acid Resistant Penicillin
  3. Penicillinase Resistant Penicillins
  4. Broad Spectrum Penicillins
64
Q

Standard reference penicillin

A

Penicillin G (benzylpenicillin)

65
Q

Is penicillin G administered orally?

A

No. It is inactive at low pH?

66
Q

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

A

No it is penicillinase sensitive.

67
Q

Is penicillin G broad or narrow spectrum?

A

Narrow. Gram positive only.

68
Q

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

A

Syphillis, Rheumatic Fever, and Gonorrhea

69
Q

What is the name for Gastric Acid Resistant Penicillin

A

)Penicillin V (acid stable)

70
Q

What is the importance of Penicillin V?

A

Itcan be given orally and produces higher blood levels than Pen G

71
Q

How are Penicillin G and Penicillin V similar?

A

Both are narrow spectrum.

72
Q

What are 4 Penicillinase Resistant Penicillins

A
  1. Methicillin
  2. Cloxacillin
  3. Nafcillin
  4. Dicloxacillin
73
Q

What is the advantage and the disadvantage of Penicillinase Resistant Penicillins

A

Less susceptible to penicillinases

Narrow spectrum

74
Q

Is methicillin (penicillinase resistant penicillin) administered orally or intravenously?

A

Intravenously (it is not absorbed orally)

75
Q

Is methicillin as effective as Penicillin G against organisms not producting penicillinase?

A

No. Only 50% as effective as Pen G

76
Q

Name 3 Broad Spectrum Penicillins.

A

Ampicillin
Amoxicillin
Carbenicillin

77
Q

Are Broad Spectrum Penicillins active against gram negative or gram positive bacteria?

A

Gram negative (effectiveness is reduced against gram positive)

78
Q

Are Broad Spectrum Penicillins susceptible to penicillinases?

A

Yes

79
Q

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

A

Cycloserine

80
Q

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

A

First Stage (Stage I)

81
Q

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

A

Vancomycin

82
Q

What is the only place where vancomycin is administered?

A

At the hospital

83
Q

Which stage of Cell Wall synthesis does Vancomycin inhibit?

A

Intermediate

84
Q

What intermediate stage cell wall synthesis inhibitor is toxic systemically, but used topically?

A

Bacitracin

85
Q

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

A

Polymyxin

Neomycin

86
Q

What are 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
Taxobactam

87
Q

Cephalosporins are cell wall inhibitors that are fungally or bacterially derived?

A

Fungally

88
Q

Cephalosporins are resistant to what?

A

Penicillinase

89
Q

How are cephalosporins and penicillins similar?

A

Both have beta-lactam rings

90
Q

What bacteria types are Cephalosporins effective against?

A

Gram positive and Gram negative

91
Q

Most cephalosporins are administered intravenously or intramuscularly. Which 2 cephalosporins are administered orally

A

Cephalexin and Cefaclor

92
Q

What is the distribution for Cephalosporins?

A

Well distributed except to CNS

93
Q

Are most cephalosporins readily metabolized or minimally metabolized?

A

Minimally metabolized

94
Q

How are cephalosporins excreted?

A

Kidney

95
Q

What are 2 things that can block cephalosporin excretion in the kidney?

A
  1. Probenecid (med specifically given to decrease excretion to increase drug potency)
  2. Renal Failure
96
Q

What is the factor causing the hypersensitivity in penicillin and cephalosporins?

A

Beta-lactam ring

97
Q

What is an adverse systemic reaction to cephalosporins?

A

Nephrotoxicity

98
Q

What are 3 infections against which cephalosporins are used?

A
  1. Meningitis
  2. Streptococcal
  3. Staphylococcal
99
Q

What type of infection/situation necessitates the use of cephalosporins?

A

Gram negative infection that is penicillin resistant

100
Q

When is Cephalosporin used prophylactically?

A

During and after surgery for endocarditis.

101
Q

What are 3 classifications of cephalosporins?

A

1st Generation
2nd Generation
3rd Generation

102
Q

What is the main character of 1st Generation Cephalosporins?

A

Good against gram positive

Moderate against gram negative

103
Q

First Generation Cephalosporin that can be administered orally?

A

Cephalexin

104
Q

What is the character of 2nd Generation cephalosporins?

A

Good against G-

Not very active against G+

105
Q

What is the character of 3rd Generation cephalosporins?

A

Active against gram negative, especially those producing penicillinase

106
Q

What are 3 ways bacteria can be Cephalosporin resistant?

A
  1. Drug can’t reach target
  2. Produce enzyme to disrupt active ring
  3. Alter antibiotic binding protein
107
Q

What can pseudomonas and proteus gram negative bacteria produce for Cephalosporin resistance?

A

Cephalosporinase

Pharm Exam 4 (8 decks)

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