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Pharmacology (Topic C) > 9. Cephalosporins > Flashcards

9. Cephalosporins Flashcards

1
Q

List the 1st generation cephalosporins.

A
  1. Cephalothin
  2. Cefazolin
  3. Cefalexin/Cephalexin
  4. Cephadroxil
  5. Cephradine

“lothi, zoli and lexi”

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2
Q

List the 2nd generation cephalosporins.

A
  1. Cefuroxime
  2. Cefoxitin
  3. Cefamandole
  4. Cefuroxime-axetil
  5. Cefaclor
  6. Cefprozil
  7. Cefotetan
  8. Cefonicid

“roxi, foxi, mandi and falco”

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3
Q

List the 2nd generation drugs that are given oral.

A
  1. Cefuroxime -axetil
  2. Cefaclor
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4
Q

List the 2nd genetation drugs that are given parenterally.

A
  1. Cefuroxime
  2. Cefoxitin
  3. Cefamandole
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5
Q

List the 3rd generation cephalosporins.

A
  1. Cefotaxime
  2. Cefoperazine
  3. Ceftriaxone
  4. Ceftazidime
  5. Ceftibuten
  6. Cefixime
  7. Ceftizoxime

“taz and triax taxi to the opera zone”

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6
Q

List the 4th generation cephalosporins.

A
  1. Cefepime
  2. Ceftolozon
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7
Q

List the 5th generation cephalosporins.

A
  1. Ceftolozane
  2. Ceftaroline
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8
Q

What spectrum does cephalosporins cover?

A
  1. Generally better Gram - and worse Gram + coverage as the generation advances, until…
  2. 4th and 5th generations are broad-spectrum (similar to ESPs spectrum, BUT ineffective against Enterococci and Listeria)
  3. Generally good for oral anaerobes, but not other anaerobes (ESPs better for anaerobes)
  4. Resist B-lactamases, but not altered PBPs or ESBLs
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9
Q

What are the indications for first generation cephalosporins?

A

Best effect against Gram + (↑ affin for Staph PBPs) + worst effect against Gram-. (UTIs by “PEK” Proteus, E. coli and Klebsiella often sensitive, however).

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10
Q

What spectrum does second generation cephalosporins cover?

A

Second Generation are worse for, but still effective against, Gram + and better effect against Gram -.

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11
Q

What spectrum does third generation cephalosporins cover?

A

even weaker effect against Gram+ and even better effect against Gram- (Salmonella, Shigella, H. influenzae etc.)

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12
Q

What are the indications for Cefepime?

A

Cefepime is administered parenteral only and is broad spectrum antibiotic. It has medium effect against Gram + (except MRSA) and highly effective for Gram - including Pseudomonas; good for meningitis (↑ CNS entry).

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13
Q

What are the indications for 5th generation cephalosporins?

A

Fifth generation cephalosporins are good for Gram +s and even MRSA! (except ceftolozane!). Also great effect for Gram - including Pseudomonas and Acinetobacter RTIs (exc. ceftar-!)

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14
Q

What is the route of administration of the 1st generation cephalosporins?

A
  1. Parenteral: Cephalothin, Cefazolin
  2. Oral: Cefalexin
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15
Q

What are the indications of Cefazolin?

A

Cefazolin is a DOC for surgical prophylaxis due to ↑ tissue penetration.

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16
Q

What are the indications for Cefalexin?

A

Uncomplicated skin / resp. infections (cellulitis, abscess, strep throat)

17
Q

What are the side effects of cephalosporins?

A

Generally low toxicity and ok in pregnancy

  1. Allergy - cross-rxn with penicillin in about 10%
  2. GI effects: diarrhea, dysbacteriosis (esp. ceftriaxone, cefoperazone via bile!)
  3. Hematological rxns (hemolytic anemia)
  4. Seizures (at high serum level)
  5. Interstitial Nephritis
  6. Alcohol Intolerance - cefoperazone and cefamandole cause aldehyde dehydrogenase inhibition; AKA “disulfiram-like effect”.
18
Q

What are the pharmacokinetic parameters of Cephalosporins?

A
  1. Tissue penetration increases with generation (ceftazidime, cefepime are DOC in meningitis); reach therapeutic levels in gallbladder
  2. Admin every 8-12 hrs (2-3x/day) with some exceptions:
    • ceftriaxone, ceftibuten and cefixime given 1x/day
    • cefotaxime given 3-4x/day
  3. Eliminated unchanged in kidney, except:
    • cefotaxime is partly metabolized
    • ceftriaxone, cefoperazone partly eliminated via bile
19
Q

What are the indications for second generation cephalosporins?

A
  1. Middle severity RTI and UTIs, including “HENS” H. flu, Neisseria, Serratia.
20
Q

What are the routes of administration for the second generation cephalosporins?

A
  1. Parenteral:
    • ​​Cefuroxime
    • Cefoxitin
    • Cefamandole
  2. Oral: for sinusitis, otitis, lower RTI (S. pneumo, H. flu, Klebs)
    • Cefuroxime-Axetil
    • Cefaclor
21
Q

What are the indications for Cefoxitin?

A

Cefoxitin is good for Gram - anaerobes (B. fragilis) in peritonitis/diverticulitis.

22
Q

What are the indications for thrid generation cephalosporins?

A
  1. First choice in pyelonephritis + orals used for severe UTIs
  2. Parenterals in pneumonia, meningitis
23
Q

What are the routes of administration of third generation cephalosporins?

A

Parenteral:

  1. Cefotaxime - partly metabolized
  2. Cefoperazone - alcohol intolerance effect.
  3. Ceftriaxone
  4. Ceftazidime

Oral:

  1. Ceftibuten
  2. Cefixime
24
Q

What are the indications for Cefoperazone?

A

Cefoperazone is non-DOC for Pseudomonas, high dose only.

25
Q

What spectrum does Ceftriaxone cover and what are some indications for its use?

A
  1. Meningitis by Neisseria, H. flu, and pneumococci. (may add vancomycin for resistant S. pneumo or ampicillin for resistant Listeria)
  2. Endocarditis by S. viridans / H. flu; empirical sepsis tx; gonorrhea and Lyme
  3. Better Gram+ effect than other 3rd gens: DOC in penicillin-resistant pneumococcal infections
26
Q

What are some possible side effect of Ceftriaxone?

A

Ceftriaxone can cause pseudocholelithiasis via biliary sludging.

27
Q

What are the indications for Ceftazidime?

A

Ceftazidime is especially good for Gram - including Pseudomonas (“ICU” abx) in nosocomial / ventilator pneumonia.

28
Q

What is the route of administration of the 5th generation cephalosporins?

A

Parenteral administration

29
Q

What are important considerations to remember about Ceftolozane?

A

Ceftolozane does not have a Gram+ effect! and its given with tazobactam B-Lase inhibitor.

30
Q

Does ceftaroline have any gram - effect?

A

Ceftaroline has a bad Gram- effect!

Pharmacology (Topic C) (20 decks)

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