Bacterial Wall Synthesis Inhibitors Flashcards

(52 cards)

1
Q

How does bacterial cell wall synthesis inhibitor work?

A

Binds to/near active site of transpeptidase/penicillin-binding protein (PBP) thus inhibiting crosslinking of peptidoglycan cell wall

For actively growing bacteria, cell wall weakened, causing increased intracellular osmotic pressure, leading to cell lysis

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2
Q

What are the types of BCWI?

A

Beta-lactam
Glycopeptide

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3
Q

What are the types of beta lactam?

A

Penicillin, carbepenem, cephalosporin, monobactam

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4
Q

What are the types of penicillins?

A

Natural penicillin
Penicillinase-Resistant Penicillin
Aminopenicillin
Anti-pseudomonas Penicillin

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5
Q

Examples of natural penicillin?

A

Penicillin G (IV)
Penicillin V (PO)

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6
Q

Which natural penicillin has good F?

A

Penicillin V

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7
Q

Syphilis caused by Treponema pallidum can be treated with which penicillin?

A

Penicillin G

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8
Q

What penicillin can be used against MRSA?

A

Penicillinase-resistant penicillin: cloxacillin

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9
Q

What bacteria does cloxacillin cover?

A

Only gram-positive (staphylococci)

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10
Q

What to take note of when taking cloxacillin?

A

Best taken on empty stomach

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11
Q

Why is cloxacillin penicillinase resistant?

A

Bulky side chain limits the accessibility of beta-lactamases to the catalytic site of action

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12
Q

Why are aminopenicillinases broad spectrum?

A

They have additional hydrophilic groups to penetrate gram-negative bacteria via porins

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13
Q

Are Amoxicillin and ampicillin effective against Pseudomonas?

A

No

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14
Q

Are Amoxicillin and Ampicillin effective against Klebsiella?

A

No

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15
Q

Can IV Amoxicillin and Ampicillin be used for CNS infection?

A

Yes

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16
Q

Ampicillin or Amoxicillin hss better oral absorption?

A

Amoxicillin

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17
Q

Does piperacillin cover MRSA?

A

No

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18
Q

Is piperacillin effective against pseudomonas?

A

Yes

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19
Q

How is piperacillin cleared?

A

70% renal

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20
Q

How does beta-lactamase inhibitors work?

A

Bind and inactivate irreversibly to serine beta-lactamase via covalent bonds to protect beta-lactams from catalysis by restructuring and permanently inactivating it.

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21
Q

What are the BL Combination drugs?

A

Augmentin PO/IV (Amoxicillin + Clavulanate)
Unasyn IV (Ampicillin + Sulbactam)
Zosyn IV (Piperacillin + Tazobactam)

22
Q

How does resistance to penicillin arise?

A
  1. Altered PBP with reduced affinity to penicillin ( MRSA: PBP2a)
  2. Production of penicillinase
  3. Decrease porin production –> decreased ability if Abx to enter cell, decr drug conc
  4. Efflux pumps
23
Q

Adverse rxns for penicillins

A
  1. Hypersensitivity (Stevens Johnson syndrome and toxic epidermal necrolysis) + anaphylaxis
  2. GI symptoms (NV, Clostridioides difficile-associated disease(CDAD))
  3. Neurotoxicity
24
Q

What are the different generations of cephalosporins?

A

1st gen: cefazolin IV, cephalexin PO
2nd gen: Cefuroxime PO
3rd gen: Ceftriaxone , Ceftazidime
4th gen: Cefepime
5th gen: Ceftriziprole, Ceftaroline

25
Which cephalosporin has activity against Pseudomonas?
3rd gen: ceftazidime 4th gen: Cefepime
26
What cephalosporin is effective against MRSA?
Ceftaroline
27
What are the 1st and 2nd gen cephalosporins ineffective against?
1. Pseudomonas 2. Listeria Monocytogenes 3. Atypicals (Mycoplasma, Chlamydia, Legionella spp.) 4. MRSA 5. Enterococcus spp.
28
Which 3rd gen cephalosporin is effective aginst Pseudomonas?
Ceftazidime
29
What can be used for vancomycin-ressistant S. Aureus?
Ceftaroline
30
What can be used for Streptococcus pneumoniae?
Ceftaroline
31
What are 3 advantages of later gen cephalosporins compared to 1st/2nd gen
1. Greater resistance to beta-lactamase 2. Greater gram-negative coverage due to increased affinity for transpeptidase 3. Greater CNS penetration
32
Which cephalosporin is cleared hepatically?
Ceftriaxone: 40% in bile
33
What is IV incompatible with ceftriaxone?
Calcium-containing pdt (Ringer's or Hartmann's solution) --> Ca precipitate formation
34
What is Carbepenems used for?
Extended spectrum beta-lactamase producing bacteria (gram-negative + anaerobic spp.)
35
Imipenem is combined with ____, so that
Cilastatin Cilastatin inhibits dehydropeptidase 1 (DHP1) in the brush border of proximal renal tubule to prevent rapid hydrolysis of imipenem so that more of active form is recovered.
36
Which carbepenum cannot be used against P. aeruginosa and enterococcus spp.?
Ertapenem
37
What does imipenem and meropenem cover?
1. P. Aeruginosa 2. Enterococcus spp. 3. Staphylococci (incl. penicillinase-producing strains) 4. Streptococci (incl. penicillinase-producing strains) 5. Anaerobes (Bacteriodes fragilis)
38
When is carbepenem used?
Mod-severely ill patients with nosocomial infections Usually in hospitals
39
Can carbepenem be used for MRSA?
No
40
Is there cross allergy between carbepenem and penicillin?
Yes
41
What class of drug is aztreonam?
Beta lactam: Monobactam
42
What does Aztreonam cover?
**Gram negative only** - enterococcus - p. Aeruginosa - Haemophillus influenzae - Neisseria gonorrhoeae - Escherichia coli - Klebsiella pneumoniae
43
How is Aztreonam administered?
IV/IM
44
Does monobactam cause cross allergy with penicillin?
Not likely
45
How does vancomycin work?
Vancomycin binds with high affinity to D-Ala- D-Ala terminus of pentapeptide of NAM component od peptidoglycan and interferes with transglycosylation of cell wall precusor units, inhibiting cell wall synthesis.
46
What does vancomycin cover?
Gram positive only Due to its large molecular size(1500kDa), which limits its ability to penetrate outer membrane of gram negative bacteria
47
How is vancomycin administered?
IV PO (poor F) for Clostridioides difficiles associated disease
48
How is vancomycin cleared?
Renal
49
ADR of vancomycin
1. Thrombophlebitis with fever and chills 2. Red-neck/ Red Man Syndrome (prevented by prolonging infusion to 1-2hrs) 3. Nephrotoxicity 4. Ototoxicity
50
What BCWI can be used against MRSA?
1. Ceftobizime 2. Ceftaroline 3. Vancomycin
51
Why do 3rd gen cephalosporins require antimicrobial stewardship?
They drive ESBL production
52
What are first line agents for MSSA bateremia?
Cloxacillin, cephalexin