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Microbiology > Agents Targeting Cell Wall (Gartenberg) > Flashcards

Agents Targeting Cell Wall (Gartenberg) Flashcards

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Biology 101 flashcards
1
Q

Bacterial Cell Wall Drugs

A
  • penicillins
  • ß-lactamase inhibitors
  • cephalosporins
  • monobactams
  • carbapenems
  • glycopeptides
  • lipopeptides
  • defensins
  • inhibitors of peptidoglycan precursors
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2
Q

transglyosylase & transpeptidase

A

transglycosylase combines NAG/NAM monomers in peptidoglycan, transpeptidase cross-links

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3
Q

ß-lactam antibiotics (mechanism, families (4))

A

-ex penicillin: mimic D-ala D-ala part of cross-link, irreversibly bind transpeptidase, preventing proper crosslinking, cell lysis (bactericidal). But only works vs growing bacteria!!

4 families:

  • Penicillin (5-member ring)
  • cephalosporins (6-member ring)
  • carbapenem (5-member ring)
  • monobactam (no ring)
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4
Q

ß-lactamases (mechanism)

A

-many gram - bacteria possess. Altered transpeptidase that can reversibly bind ß-lactams, allowing them to stay active

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5
Q

ß-lactamase inhibitor (mechanism, exs)

A
  • bulky ß-lactam that irreversibly binds ß-lactamases
  • given with regular ß-lactam antibiotic in combination to allow it to work again
  • ex: clavulinic acid, tazobactam, sulbactam
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6
Q

Avibactam (drug class)

A
  • broad spectrum ß-lactamase inhibitor

- given with 3rd gen. cephalosporin (ceftazidine)

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7
Q

Penicillin G (class, target bacteria)

A

Common penicillin, good vs. gram +/- cocci, anaerobes, anything else that doesn’t produce ß-lactamase. Acid labile (broken down by stomach acid)

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8
Q

Oxacillin, Cloxacillin, Dicloxacillin (class, features, target bacteria, non-target bacteria)

A

Acid-stable, ß-lactamase resistant penicillins.

  • good vs. ß-lactamase staph, penicillin-susceptible strep and pneumococci
  • NOT GOOD vs enterococci, gram - rods/cocci, anaerobes
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9
Q

Amoxicillin

A

Acid stable, extended spectrum penicillin. Good vs. gram -.

  • ß-lactamase susceptible, so combo with ßLI (Augmentin = clavulanic acid + amoxicillin)
  • Used for sinusitis, UTIs, LRT, otitis.
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10
Q

Penicillins (route of administration, clearance time, side effects, allergy replacement)

A
  • given oral, IV
  • 3-4 hour clearance, so multiple dose/day
  • little side effects, but rash, diarrhea, nausea
  • if allergy, all penicillins. Give 2nd gen.+ cephalosporins instead
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11
Q

Cephalosporins (route, elimination, uses

A

-oral/IV
-kidney elimination, dont give to renal insufficient
-used vs. sinusitis, otitis, LRT. 4th gen. vs. MRSA
-can have hypersensitivity reactions- anaphylaxis, fever, skin rash, nephritis, granulocytopenia, hemolytic anemia
-

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12
Q

Cefazolin (class, spectrum, special use)

A

1st gen. cephalosporin

  • broad spectrum, better vs. gram +
  • used prophylactically in surgery
  • no CNS penetration
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13
Q

Cefamandole (class, spectrum, special use)

A

2nd gen. cephalosporin

  • broad spectrum like 1st gen., improved gram - activity
  • no cross-reactive allergy with penicillin, so used as replacement
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14
Q

Ceftazidime (class, spectrum, special use)

A

3rd gen. cephalosporin

  • improved gram - but weakened gram + activity
  • not effective alone against constitutive ßL
  • Avycaz: ceftazidime + ßLI (avibactam)
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15
Q

Cefepime (class, spectrum, special use)

A

4th gen. cephalosporin

  • broadest spectrum cephalosporin, vs gram +/- good
  • penetrates CNS
  • used vs p. aeruginosa, haemophilus, enterobactericiae, s. aureus, s. pneumoniae, nesseria, penicillin-resistant streptococci
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16
Q

Ceftolozane (class, spectrum, special use)

A

5th gen. cephalosporin

  • used vs. resistant gram - bacteria like pseudomones, complicated UTIs or intrabdominal
  • Given with tazobactam (ßLI) to extend half life
17
Q

Ceftaroline/ceftobiprole

A

cephalosporins for MRSA (late gen.)

  • given IV
  • broad spectrum
18
Q

Monobactams (class, special property, spectrum, ex)

A
  • resistant to ß-lactamases
  • active vs. gram - rods (like pseudomones, serratia)
  • no activity vs. gram +
  • given IV, no cross reaction with penicillin, no side effects
  • ex: aztreonam
19
Q

Carbapenems (class, spectrum, use, side effects)

A
  • broad spectrum, used for mixed infections
  • resistant vs. serine ß-lactamases
  • penetrate CNS, excreted renally
  • cross react with penicillin
  • side effects: vomiting, diarrhea, skin rash, penicillin allergy
20
Q

Imipenem

A

Carbapenem, inactivated in renal tubules

21
Q

Cilastatin

A

Improves half life of carbanepems by inhibiting renal dehydropeptidase

22
Q

Meropenem

A

carbapenem, resistant to renal dehydropeptidase so better half life

23
Q

Vancomycin (class, spectrum, mechanism, side effects)

A

glycopeptide
-active vs. gram +, especially staph
-bactericidal vs growing cells: binds peptidoglycan unit, preventing proper incorporation, weakening wall and lysis
-resistance via D-ala D-ala–>D-ala D-lactic acid
-penetrates CNS
-used in combo with aminoglycosides vs. enterococci
side effects: minor (phlebitis, chills, fever, nephrotoxicity, ototoxicity)
-given IV, oral for enterococci
-other glycopeptides: teicoplanin, televancin

24
Q

Dalbavancin (class, use, spectrum)

A

derivative of teicoplanin (glycopeptide)

  • good as vancomycin but less frequent dosing (2x week)
  • Good for skin infections of MDR gram +
25
Q

Oritavancin (class, spectrum, special use)

A

vancomycin derivative

-like dalbavancin, good vs. MDR gram + skin infections, but only need 1x dose!!!

26
Q

Daptomycin (class, mechanism, clinical use)

A

Causes bacterial pore to leak K+, killing cell WITHOUT rupture (no toxin release)
-good vs SSTI gram +, MRSA

27
Q

Brilacidin (class, mechanism, spectrum, improvement vs other in class)

A

daptomycin mechanism

  • broad spectrum (+/-) including MRSA
  • single dose (daptamycin 7 days
28
Q

Polymyxins

A

Perforate gram - inner/outer membranes

-used topically in neosporin

29
Q

Drugs targeting cell wall precursors (3)

A

Fosfomycin, bacitracin, d-cycloserine

30
Q

Fosfomycin (class, mechanism, spectrum, use)

A

prevents NAM–>NAG by binding enzyme, MurA

  • active vs. gram +/-. Synergeistic with others.
  • Used vs. UTIs
31
Q

Bacitracin (mechanism, spectrum, use)

A

Inhibits lipid phosphate dephosphorylation of phosphorylated lipid carrier of peptidoglycan units

  • good vs. gram +
  • topical use due to nephrotoxicity
32
Q

D-cycloserine

A

competitive inhibitor of d-alanine racemase and ligase (becomes incorporated into D-ala D-ala instead of D-ala)

  • Used in combination vs. TB
  • serious side effects: CNS toxicity (headaches, tremors, convulsions, psychosis)

Microbiology (10 decks)

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