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Pharmacology > Cephalosporins > Flashcards

Cephalosporins Flashcards

0
Q

Discuss the function of the R2 and R1 side-chains present in cephalosporins:

A

R2: confers degree of antibiotic activity
R1: determines pharmacokinetics

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1
Q

Mechanism of action for cephalosporins?

A

Cephalosporins are B-lactams that inhibit transpeptidation and activate autolytic cell wall lysins

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2
Q

Discuss the function of the 7-methyl group found in cephalosporins:

A

The 7-methyl group helps increase resistance to beta-lactamase. therefore cephalosporins are more equipped to deal with penicillinase resistant bacteria than most drugs in the penicillin class are.

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3
Q

List the first generation Cephalosporins and their mode of administration:

A
  1. Cefazolin - IV/IM
  2. Cephalothin - IV/IM
  3. Cephalexin - PO
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4
Q

What is the DOC for surgical prophylaxis?

A

Cefazolin which is administered IV/IM. The only first generation cephalosporin which is adminstered PO is Cephalexin!!

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5
Q

List the characteristics of the first generation cephalosporins:

A
  1. good G+ coverage; some G- coverage
  2. some are acid resistant
  3. renal excretion
  4. increased beta-lactamase resistance
  5. MSSA treatment alternative for people with a penicillin allergey
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6
Q

List the second generation cephalosporins and their mode of administration:

A
  1. Cefaclor: PO
  2. Cefuroxime: IV/IM
  3. Cefprozil: PO
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7
Q

Discuss the characteristics of the second generation cephalosporins:

A
  1. decreased G+ activity
  2. increased G- coverage
  3. not antipseudomonal
  4. some are acid resistant
  5. kidney excretion
  6. increased beta-lactamase resistance
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8
Q

List the third generation cephalosporins:

A
  1. Ceftriaxone
  2. Cefotaxime Sodium
  3. Cefoperazone
  4. Ceftazadime
  5. Cefixime
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9
Q

Which 3rd generation cephalosporins are used in treating pseudomonas aeruginosa?

A

Cefoperazone and ceftazidime

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10
Q

What is the DOC for Niserria gonnorhea?

A

Ceftriaxone, a third generation cephalosporin

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11
Q

which third generation cephalosporins have good CNS penetration?

A

Ceftriaxone, cefotaxime, and cefoperazone

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12
Q

which cephalosporin is metabolized by the liver?

A

cefoperazone

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13
Q

Which of the third generation cephalosporins can be administered orally?

A

cefixime

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14
Q

Discuss the characteristics of 3rd generation cephalosporins:

A
  1. even less G+ activity
  2. increased G-; especially enterobacteria
  3. some are antipseudomonal - cefoperazone, ceftazadime (combine these with aminoglycosides)
  4. some are acid resistant - cefixime
  5. mainly renal excretion - cefoperazone is metabolized by the liver
  6. increased beta-lactamase resistance
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15
Q

Why is ceftriaxone not used in infants?

A

bilirubin displacement

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16
Q

List the fourth generation cephalosporins and their modes of administration:

A
  1. Cefepime - IV
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17
Q

Discuss the characteristics of fourth generation cephalosporins (cefepime):

A
  1. comparable to third generation
  2. increased G+ coverage
  3. increased beta lactamase resistnace
  4. antipseudomonal
  5. broadest coverage
  6. empirical therapy when beta lactamase resistance is expected
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18
Q

What cephalosporin is in the “unnamed generation” and how is it administered?

A

Ceftaroline fosamil - IV

19
Q

Discuss the characteristics of ceftaroline fosamil:

A
  1. G+/G- coverage
  2. approved for CABP treatment
  3. not antipseudomonal
  4. renal excretion
  5. MRSA and VRSA coverage
20
Q

DOC moraxella catarrhalis:

A

second or third generation cephalosporins

21
Q

DOC N. gonnhoreae?

A

Ceftriaxone

22
Q

DOC E. coli, Klebsiella, Proteus?

A

First or second generation cephalosporins

23
Q

DOC for Salmonella?

A

Third generation cephalosporins

24
Q

DOC for MSSA if penicillin allergy?

A

Ceftriaxone

25
Q

DOC for Borrelia burgdorferi late disease?

A

ceftriaxone

early disease is doxycycline or amoxicillin

26
Q

Discuss Cephalosporin toxicity:

A
  1. fairly safe
  2. superinfection
  3. allergy (10% cross sensitivity with PCN)
  4. GI symptoms
  5. positive direct and indirect Coombs test
  6. dose dependent renal tubular necrosis (synergistic toxicity with aminoglycosides)
27
Q

what drugs are monobactams?

A

aztreonam

28
Q

Discuss the characteristics of monobactams (aztreonams):

A
  1. monocyclic b-lactam rings
  2. fairly resistant to beta lactamase
  3. only aerobic G- rods (pseudomonas, serratia, proteus, and Klebseilla)
  4. parenteral administration
  5. no cross sensitivity with other beta-lactams
  6. very few side effects
29
Q

what are the three carbapenems?

A
  1. imipenem
  2. meropenem
  3. ertapenem
30
Q

what broad drug category do carbapenems fall into?

A

beta-lactam drugs

31
Q

Discuss the main difference between imipenem and meropenem:

A

Imipenem can be degraded in the renal tubule by dihydropeptidases and therefore must be administered with cilastatin (a dihydropeptidase inhibitor). meropenem on the other hand is not susceptible to dihydropeptidases and can be administered alone

32
Q

List the characteristics of Imipenem and Meropenem:

A
  1. Broad spectrum (G+/G- coverage)
  2. pseudomonas may develop resistance rapidly (administer with aminoglycosides to prevent this)
  3. stable against beta-lactamase
  4. DOC for penicillinase producing Enterobacters
  5. Imipenem can cause seizures (less likely with meropenem)
  6. IV administration
33
Q

List the traits of Eratopenem:

A
  1. highly stable against beta-lactamase
  2. good G+/G- coverage, especially enterobactericeae
  3. not as good pseudomonal coverage (choose a different carbapenem)
  4. IV/IM administration
  5. renal elimination
34
Q

What are the four cell wall inhibitors that are not beta-lactam drugs?

A
  1. Vancomycin
  2. Bacitracin
  3. Phosphomycin
  4. Cycloserine
35
Q

Describe the mechanism of action for vancomycin and how bacteria could develop a resistance to this antibiotic:

A

Vancomycin works to sterically inhibit transpeptidation. It does so by binding to D-ala, D-ala. If bacteria alter the D-ala binding site vancomycin can no longer block transpeptidation.

36
Q

Discuss vancomycin usage:

A

Vancomycin is extremely helpful in treating penicillinase resistant staphylococcus aureus (MRSA). it can only be used in treating G+ infections (penicillin allergic patients). Treats these infections parenterally.
Vancomycin is given orally in the case of superinfection treatment. (C. diff or staphylococcus) For C. diff it is the second choice next to metronidazole.

37
Q

Vancomycin toxicity:

A
  1. thrombophlebitis (injection site)
  2. ototoxicity
  3. nephrotoxicity
  4. red man syndrome (red flush due to histamine release)
38
Q

Discuss the mechanism of action for fosfomycin:

A

Fosfomycin is a structural analog of phosphophenylpyruvate and blocks one of the first steps in peptidoglycan synthesis. It blocks the reduction of NAG to NAM. It is structurally unrelated to the other inhibitors of cell wall synthesis

39
Q

Discuss the characteristics of fosfomycin:

A
  1. works well against G+/G- bacteria
  2. PO
  3. renal excretion
  4. used to treat uncomplicated lower UTIs
  5. synergistic activity when taken with aminoglycosides, beta-lactam or fluoroquinolone
40
Q

Discuss the mechanism of Bacitracin:

A

Bacitracin prevents the peptidoglycan subunits from being transported across in cell membrane.

41
Q

Discuss the characteristics of Bacitracin:

A
  1. Parenteral (rare) or topical
  2. G+ coverage
  3. commonly used in combo with neomycin or polymyxins which are active against G-
  4. parenteral use can cause nephrotoxicity
  5. most commonly used after superficial skin and eye injury to prevent infection
42
Q

Describe the mechanism of action for cylcoserine:

A

Cycloserine is a D-ala structural analog and prevents the addition of D-ala onto the pentapeptide.

43
Q

Describe the characteristics of cycloserine:

A
  1. used as a secondary line of treatment for TB and uncomplicated UTIs
  2. can be bactericidal or bacteriostatic
  3. adverse affects most commonly involve the CNS
44
Q

DOC for enterobacter, citrobacter and serratia

A

carbapenem

45
Q

DOC for methicillin resistant s. aureus:

A

vancomycin

46
Q

DOC for Bacillus species (non anthracis):

A

vancomycin

Pharmacology (7 decks)

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