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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
Autolysins act how normally?
They normally nick cell walls for attachment of new peptidoglycan units.
26
What are 4 ways bacteria can become resistant to penicillin?
1. Lack of accessibility to target 2. Production of penicillinases or beta lactamases 3. Altered penicillin binding protein 4. Drug efflux pumps
27
What is an example of lack of accessibility to target for penicillin resistance?
Gram negative bacteria having outer membrane inhibiting access to cell wall.
28
What is the absolute requirement for inhibition of transpeptidase?
Intact beta-lactam ring
29
What is the difference between penicillinase and beta lactamase?
Penicillinase only breaks down penicillin beta lactam ring. | Beta lactamase breaks down both penicillin and cephalosporin beta lactam ring
30
How can gram negative bacteria, who have low production of penicillinases still eliminate antibiotics without being swamped?
Gram negative limits access of beta lactam antibiotics to the peptidoglycan cell wall
31
If an antibiotic binds to Penicillin Binding Protein 2 or Penicillin Binding Protein 3 what will its effects be on the bacteria
Prevents cell division (septum formation) Loss of rod like structure (filament formation)
32
If an antibiotic binds to Penicillin Binding Protein 1 what will its effects be on the bacteria?
Inhibits cell wall synthesis | Organism undergoes osmotic lysis
33
If antibiotic binds PBP 2 and PBP 3 is the effect bacteriocidal or bacteriostatic?
Bacteriostatic
34
If antibiotic binds PBP 1 is the effect bacteriocidal or bacteriostatic?
Bacteriocidal
35
What stage of cell wall synthesis is PBP 1 involved in?
Cross linking step on stage III of cell wall synthesis
36
What can PBP 1 do to itself to resist penicillin?
Change affinity for penicillin
37
What will happen if bacteria increases levels of penicillin binding protein?
It will soak up the penicillin to decrease the effect of penicillin on PBP 1
38
What else can bacteria do to alter their penicillin binding protein to resist penicillin
synthesize new PBP’s with altered penicillin affinity
39
What does a drug efflux pump do?
Pumps the drug out once it gets in cell
40
What is character of broad spectrum penicillin versus narrow spectrum penicillin?
Broad spectrum can be effective against some gram negatives by getting through the outer membrane to attack the inner membrane peptidoglycan
41
Are penicillins widely distributed or narrowly distributed throughout the body
Widely distributed
42
Where do penicillins not distribute well and therefore cannot be used for treatment in these areas of the body?
joints ocular tissue cerebrospinal fluid
43
What can cause penicillin to reach higher levels in the central nervous system?
Inflammation
44
What administrative route is most common parenteral route that gives predictable blood level?
Intramuscular
45
What administrative route to use for treatment of severe infection requiring fast action and high blood levels?
Intravenous
46
How much penicillin is absorbed by oral administration?
20-25%
47
How is penicillin eliminated?
Renal
48
How much of penicillin is excreted as active drug?
Two thirds
49
What is the half-life of all penicillins?
Approximately 1 hr
50
Why is probenecid used?
It decreases renal excretion of drugs to increase antibiotic plasma concentration during serious infection.
51
Use of penicillin is limited primarily by what?
Resistance
52
Is penicillin one of the more highly toxic or least toxic drugs in medicine?
One of the least toxic
53
Use of penicillin limited primarily by
Resistance
54
What are 5 toxicities associated with penicillin?
1. Resistance 2. Hypersensitivity 3. Anaphylactic shock 4. CNS effects 5. Superinfection
55
Staph infections acquired in hospital are usually susceptible or resistant to penicillin?
Resistant
56
What respiratory problem increases one’s risk of penicillin hypersensitivity
Asthma
57
Would a penicillin hypersensitivity result in anaphylaxis?
No. It would only cause a rash.
58
What would be the signs of penicillin anaphylaxis?
``` Bronchoconstriction Abdominal pain Nausea Vomiting Weakness Fall in BP ```
59
What are immediate indicators of anaphylaxis?
dizziness, weakness, sweating, palpitations
60
After a sensitization dose to penicillin, what are likely symptoms?
Rashes, fever, swollen joints several days after taking penicillin
61
When would a person be at risk for penicillin to affect CNS?
When the patient has impaired renal function or is infused w/ unusually high dose
62
What is the risk with long term penicillin therapy
Superinfection
63
What are 4 General classes of penicillins?
1. Penicillin G(benzylpenicillin) 2. Gastric Acid Resistant Penicillin 3. Penicillinase Resistant Penicillins 4. Broad Spectrum Penicillins
64
Standard reference penicillin
Penicillin G (benzylpenicillin)
65
Is penicillin G administered orally?
No. It is inactive at low pH?
66
Can penicillin G get by penicillinases in bacteria, e.g. against Staph aureus?
No it is penicillinase sensitive.
67
Is penicillin G broad or narrow spectrum?
Narrow. Gram positive only.
68
Penicillin G are used in the treatment of what three bacterial infections?
Syphillis, Rheumatic Fever, and Gonorrhea
69
What is the name for Gastric Acid Resistant Penicillin
)Penicillin V (acid stable)
70
What is the importance of Penicillin V?
Itcan be given orally and produces higher blood levels than Pen G
71
How are Penicillin G and Penicillin V similar?
Both are narrow spectrum.
72
What are 4 Penicillinase Resistant Penicillins
1. Methicillin 2. Cloxacillin 3. Nafcillin 4. Dicloxacillin
73
What is the advantage and the disadvantage of Penicillinase Resistant Penicillins
Less susceptible to penicillinases | Narrow spectrum
74
Is methicillin (penicillinase resistant penicillin) administered orally or intravenously?
Intravenously (it is not absorbed orally)
75
Is methicillin as effective as Penicillin G against organisms not producting penicillinase?
No. Only 50% as effective as Pen G
76
Name 3 Broad Spectrum Penicillins.
Ampicillin Amoxicillin Carbenicillin
77
Are Broad Spectrum Penicillins active against gram negative or gram positive bacteria?
Gram negative (effectiveness is reduced against gram positive)
78
Are Broad Spectrum Penicillins susceptible to penicillinases?
Yes
79
What is the penicillin-related drug that is front line for tuberculosis treatment?
Cycloserine
80
Which stage of cell wall synthesis does the anti- tuberculosis drug Cycloserine target?
First Stage (Stage I)
81
What penicillin-related drug is last line of defense treating MRSA and also used in Endocarditis?
Vancomycin
82
What is the only place where vancomycin is administered?
At the hospital
83
Which stage of Cell Wall synthesis does Vancomycin inhibit?
Intermediate
84
What intermediate stage cell wall synthesis inhibitor is toxic systemically, but used topically?
Bacitracin
85
Bacitracin is normally paired with what other 2 drugs as a topical ointment (triple-biotic, Neosporin)?
Polymyxin | Neomycin
86
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?
Clavulanate Sulfabactam Taxobactam
87
Cephalosporins are cell wall inhibitors that are fungally or bacterially derived?
Fungally
88
Cephalosporins are resistant to what?
Penicillinase
89
How are cephalosporins and penicillins similar?
Both have beta-lactam rings
90
What bacteria types are Cephalosporins effective against?
Gram positive and Gram negative
91
Most cephalosporins are administered intravenously or intramuscularly. Which 2 cephalosporins are administered orally
Cephalexin and Cefaclor
92
What is the distribution for Cephalosporins?
Well distributed except to CNS
93
Are most cephalosporins readily metabolized or minimally metabolized?
Minimally metabolized
94
How are cephalosporins excreted?
Kidney
95
What are 2 things that can block cephalosporin excretion in the kidney?
1. Probenecid (med specifically given to decrease excretion to increase drug potency) 2. Renal Failure
96
What is the factor causing the hypersensitivity in penicillin and cephalosporins?
Beta-lactam ring
97
What is an adverse systemic reaction to cephalosporins?
Nephrotoxicity
98
What are 3 infections against which cephalosporins are used?
1. Meningitis 2. Streptococcal 3. Staphylococcal
99
What type of infection/situation necessitates the use of cephalosporins?
Gram negative infection that is penicillin resistant
100
When is Cephalosporin used prophylactically?
During and after surgery for endocarditis.
101
What are 3 classifications of cephalosporins?
1st Generation 2nd Generation 3rd Generation
102
What is the main character of 1st Generation Cephalosporins?
Good against gram positive | Moderate against gram negative
103
First Generation Cephalosporin that can be administered orally?
Cephalexin
104
What is the character of 2nd Generation cephalosporins?
Good against G- | Not very active against G+
105
What is the character of 3rd Generation cephalosporins?
Active against gram negative, especially those producing penicillinase
106
What are 3 ways bacteria can be Cephalosporin resistant?
1. Drug can’t reach target 2. Produce enzyme to disrupt active ring 3. Alter antibiotic binding protein
107
What can pseudomonas and proteus gram negative bacteria produce for Cephalosporin resistance?
Cephalosporinase

Pharm Exam 4 (8 decks)

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