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Flashcards in Antimicrobials Deck (95)
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1

Penicillin G, V
MOA

>Binds penicillin-binding proteins (transpeptidases) and block them from cross-linking w/ peptidoglycan wall -- loss of rigidity, susceptible to rupture.
>Activates autolytic enzymes.

2

Penicillin G, V
Clinical use

>Bactericidal, Penicillinase-sensitive.
>G(+) organisms (S. pneumoniae, GAS, Actinomyces).
>G(-) cocci (N. meningitidis).
>Spirochetes (T. pallidum).

3

Amoxicillin, Ampicillin
MOA

>Extended-spectrum, Bactericidal, Penicillinase-sensitive.
>Binds to transpeptidases and blocks transpeptidase cross-linking w/ cell wall -- susceptible to rupture.
>Activates autolytic enzymes.

4

Amoxicillin, Ampicillin
Clinical use (HHEELPSS)

>H. influenzae, H. pylori, E. coli, Enterococci, L. monocytogenes, Proteus, Salmonella, Shigella.
>Combine w/ Clavulanic acid -- protect against B-lactamase (co-amoxiclav).

5

Amoxicillin, Ampicillin
Toxicity

Pseudomembranous colitis (ex. C. difficile)

6

Dicloxacillin, Nafcillin, Oxacillin
MOA

>Narrow spectrum, Bactericidal, Penicillinase-resistant.
>Binds to pencillin-binding protein and prevents them from cross-linking w/ cell wall -- prone to rupture.
>Activates autolytic enzymes.

7

Dicloxacillin, Nafcillin, Oxacillin
[Clinical use, Toxicity]

>S. aureus (except MRSA due to altered penicillin-binding protein site).
>Toxicity: interstitial nephritis.

8

Piperacillin, Ticarcillin
MOA

>Antipseudomonals, Extended spectrum. Penicillinase-sensitive.
>Binds to transpeptidases and prevents them from cross-linking w/ cell wall -- prone to rupture.
>Activates autolytic enzymes.

9

Piperacillin, Ticarcillin
Clinical use

Pseudomonas
G(-) rods

10

Beta-lactamase inhibitors (CAST)

Clavulanic acid
Sulbactam
Tazobactam
*Add to penicillin antibiotics

11

Cephalosporins
MOA

>B-lactam drugs -- Inhibit cell wall synthesis
*Less susceptible to Penicillinase, unless structural change in binding site.

12

Cephalosporins
Toxicity

Autoimmune hemolytic anemia.
Vit K deficiency.
Disulfiram-like reactions.
Cross-reaction w/ penicillins.
Inc. nephrotoxicity w/ aminoglycosides.

13

Cephalosporins don't cover w/c organisms? (LAME)

Listeria
Atypicals (Chlamydia, Mycoplasma)
MRSA (except ceftaroline)
Enterococci

14

Cephalosporins, gen I
[Drug names, Clinical use]

Cefazolin, Cephalexin
>G(+) cocci
>Proteus, E. coli, Klebsiella (PEcK)
*Cefazolin before surgery for S.aureus infections

15

Cephalosporins, gen II
[Drug names, Clinical use]

Cefoxitin, Cefaclor, Cefuroxime.
>G(+) cocci.
>H. influenzae, Enterobacter, Neisseria, Serratia (HENS).
>Proteus, E.coli, Klebsiella (PEcK).
>Cefoxitin is the only one that covers G(+), G(-), and anaerobes.

16

Cephalosporins, gen III
[Drug names, Clinical use]

Ceftriaxone, Cefotaxime, Ceftazidime.
G(-) resistant to other Beta-lactams.
Can penetrate CSF.
>Ceftriaxone: meningitis, gonorrhea, disseminated Lyme dse.
>Ceftazidime: Pseudomonas

17

Cephalosporins, gen IV
[Drug names, Clinical use]

Cefepime
G(-) organisms.
*Inc. activity vs Pseudomonas, G(+) organisms.

18

Cephalosporins, gen V
[Drug names, Clinical use]

Ceftaroline
Broad G(+/-) coverage
Includes MRSA
*Doesn't include Pseudomonas

19

Carbapenems
Drug names

Imipenem, Meropenem, Ertapenem, Doripenem

20

Carbapenems
MOA

Inhibit cell wall synth by binding to penicillin-binding proteins (same MOA as penicillin).
>Imipenem: broad spectrum, Penicillinase-resistant; Administer w/ Cilastatin (inhibits renal dehydropeptidase I) -- dec. inactivation in renal tubules.

21

Carbapenems
Clinical use

G(+) cocci, G(-) rods, anaerobes.
>Only use in life-threatening infections or if other drugs failed -- major side effects

22

Carbapenems
Toxicity

CNS toxicity (seizures)
GI distress, skin rash
*Meropenem has less risk of seizure and more stable to dehydropeptidase I

23

Vancomycin
MOA

>Binds to D-ala D-ala of cell wall precursors -- inhibits cell wall peptidoglycan formation.
>Resistant bacteria have D-ala D-lac modification.

24

Vancomycin
Clinical use

G(+) only.
Includes MRSA, S. epidermidis, Enterococcus, C. difficile

25

Vancomycin
Toxicity

Generally well-tolerated.
Nephrotoxic, ototoxic.
*Thrombophlebitis -- Red man syndrome: diffuse flushing due to nonspecific mast cell degranulation (pretreat w/ slow-infusing antihistamines).

26

Aminoglycosides
Drug names (GNATS)

Gentamicin, Neomycin
Amikacin, Tobramycin
Streptomycin

27

Aminoglycosides
MOA

Bactericidal.
>Binds to 30s subunit -- inhibits initiation complex -- inhibits transcription of bacterial mRNA, causes misreading of mRNA.
>Needs O2 for uptake (useless w/ anaerobes).

28

Aminoglycosides
Clinical use

Severe G(-) rod infections.
Synergistic w/ Beta-lactams

29

Aminoglycosides
Toxicity

Nephrotoxicity, Ototoxicity.
Neuromuscular blockade.
Teratogen.

30

Tetracyclines
Drug names

Tetracycline
Doxycycline
Minocycline