Inhibitors of Cell Wall Synthesis II Flashcards by Rebecca Lea

Q

4 classes of beta-lactams

A

penicillins
cephalosporins
monobactams
carbapenems

ALL CIDALS!

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Q

3 other inhibitors of CWS (not beta-lactams)

A

vancomycin
phosphomycin
bacitracin

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Q

Cephalosporins mechanism of action

A

activate cell wall autolytic enzymes through blocking of terminal cross-linking of peptidoglycan

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Q

ICWS all do what?

A

all lyse cells

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Q

R2 substitutions determine degree of

A

antibacterial activity

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Q

R1 affects

A

pharmacokinetic properties

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Q

Chemically, cephalosporins are a group of antibiotics closely related to _______ and have what structures?

A

penicillin

beta-lactam ring structures

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Q

What advantage do cephalosporins have over penicillins?

A

7-methyl-group in cephalosporins which increases resistance to beta-lactamase

– never 100% resistance due to different types of beta-lactamase

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Q

First generation cephalosporins have what kind of spectrum?

A

narrow

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Q

First generation cephalosporins:

good activity against what kind of bacteria?

A

G+

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Q

First generation cephalosporins:

relatively moderate activity against what kind of bacteria?

A

Gram - (E. Coli, Kiebsiella, Proteus)

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Q

What kind of bacteria is susceptible to first generation cephalosporins?

A

Most G+ cocci

MSSA (enterococci, MRSA, and S. epidermis are resistant)

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Q

First generation cephalosporins:

some are:

A

acid resistant

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Q

First generation cephalosporins:

increased _______

A

beta-lactamase resistance

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Q

First generation cephalosporins:

how are they excreted?

A

renal excretion

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Q

What is the DOC for surgical prophylaxis?

A

cefazolin (parentally given)

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Q

Are first generation cephalosporins the DOFC for MSSA?

A

no - penicillinase-resistance still DOFC

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Q

Second generation cephalosporins:

lower activity against what type of bacteria?

A

G+

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Q

Second generation cephalosporins:

somewhat increased activity against what type of bacteria

A

G-

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Q

Second generation cephalosporins:

do they have antipseudomonal activity?

A

no

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Q

Second generation cephalosporins:

do they have beta-lactamase resistance?

A

yes - increased beta-lactamase resistance

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Q

Second generation cephalosporins:

are they acid resistant?

A

some are

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Q

Second generation cephalosporins:

how are they excreted?

A

mostly through renal excretion

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Q

What are the two first generation cephalosporins?

A

cefazolin - IV, IM

cephalexin - oral

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What are the three second generation cephalosporins?

cefaclor - oral cefuroxime - IV, IM cefprozil - oral

Third generation cephalosporins: what kind of spectrum

broad

What are the four third generation cephalosporins?

Ceftriaxone - IV/IM Cefotaxime Sodium - IV/IM Ceftazidime - IV/IM Cefixime - oral

What is the only third generation cephalospore that is oral?

cefixime

Special characteristics of ceftriaxone? Treats what?

CNS penetration Neisseria

Special characteristics of cefotaxime sodium?

CNS penetration

Ceftazidime used to treat what bacteria?

P. aeruginosa

Third generation cephalosporins: less active against

Gram + cocci

Third generation cephalosporins: much more active against

enterobacteriaceae (penicillinase producing strains)

Third generation cephalosporins: what kind of activity does ceftazidime combined with aminoglycosides treat?

pseudomonas aeruginosa activity

Third generation cephalosporins: how are they administered?

IV/IM and oral

Third generation cephalosporins: increased:

beta-lactamase resistance

Third generation cephalosporins: how are they excreted?

by kidney

What is the drug of choice for N. gonorrhoeae?

Ceftriaxone

In what populations do you not want to use ceftriaxone i?

neonates, billirubin displacement

Third generation cephalosporins can/cannot penetrate CNS without inflammation

can

What is the DOFC for pseudomonas?

antipseudomonas penicillins BUT can use ceftazidime if penicillin allergy

Fourth generation cephalosporins: comparable to what generation

3rd generation

Fourth generation cephalosporins: more resistant to

some beta-lactamases

Fourth generation cephalosporins: given how?

IV

Fourth generation cephalosporins: is/is not antipseudomonal?

IS

Fourth generation cephalosporins: what kind of coverage: gram+ or gram-

Gram+ coverage

Fourth generation cephalosporins: how are they excreted?

renal

Which generation of cephalosporins have the broadest coverage

fourth generation

What do fourth generation cephalosporins treat against?

enterobacteriaceae, MSSA, pseudomonas

What generation of drugs do you use for empirical therapy?

fourth generation - particularly when resistance to beta-lactamases are anticipated

Name one fourth generation cephalosporin?

Cefepime - IV

Fifth generation cephalosporins bind to:

MRSA PBP

Fifth generation cephalosporins do/do not have antipseudomonal activity.

do not

Fifth generation cephalosporins activity against what kind of bacteria?

G+ and G-, approved for CABP

Fifth generation cephalosporins what kind of excretion?

renal

Fifth generation cephalosporins what kind of special coverage? WHY is this special?

MRSA and VRSA coverage THE ONLY BETA LACTAM ACTIVE AGAINST MRSA

Name of one fifth generation cephalosporin

ceftaroline fosamil - IV

What makes fifth generation cephalosporin unique?

mechanistically, ceftaroline can bind to PBP2A with very high affinity - this is the mutated PBP that other beta-lactams cannot bind to

ceftraline fosamil is an exception why?

it is because ONLY beta-lactam active against MRSA still not drug of first choice against MRSA

First or second generation cephalosporins are DOFC for which three bacteria?

E coli Kiebsiella Proteus

Second of third generation cephalosporins are DOFC for which bacteria?

Moraxella catarrhalis

Ceftriaxone or cefixime treat which bacteria?

neisseria gonorrheae | KNOW THIS

What generation of drugs treat salmonella?

third generation cephalosporins

What drug treats penicillin-resistant s. pneumoniae?

ceftriaxone

What is used to treat borrelia burgdorferi?

ceftrioxone (LATE DISEASE ONLY)

Level of safety for cephalosporins?

fairly

Which has more toxicity - cephalosporins or penicillins?

cephalosporins

Risk of ______ with cephalosporins with enterococci, G-bacilli, pseudomembranous colitis or candida

superinfection

What type of reaction can people have after alcohol consumption with cephalosporins?

disulfiram-like reaction (makes drinking intolerable due to hangover) should not drink on this medicine

What percentage of cross sensitivity with penicillin does cephalosporin have?

10%

G.I symptoms commonly associated with cephalosporins?

anorexia, N/V, diarrhea

Dose dependent renal tubular necrosis is associated with what class of drugs?

cephalosporins

Why would you not want to treat something with cephalosporin and aminoglycosides?

synergistic nephrotoxicity (BIG DEAL)

What is the DOFC for pseudomonas?

2 penicillins better than cephamine due to cephamine's renal effects