9. Cephalosporins Flashcards
List the 1st generation cephalosporins.
- Cephalothin
- Cefazolin
- Cefalexin/Cephalexin
- Cephadroxil
- Cephradine
“lothi, zoli and lexi”
List the 2nd generation cephalosporins.
- Cefuroxime
- Cefoxitin
- Cefamandole
- Cefuroxime-axetil
- Cefaclor
- Cefprozil
- Cefotetan
- Cefonicid
“roxi, foxi, mandi and falco”
List the 2nd generation drugs that are given oral.
- Cefuroxime -axetil
- Cefaclor
List the 2nd genetation drugs that are given parenterally.
- Cefuroxime
- Cefoxitin
- Cefamandole
List the 3rd generation cephalosporins.
- Cefotaxime
- Cefoperazine
- Ceftriaxone
- Ceftazidime
- Ceftibuten
- Cefixime
- Ceftizoxime
“taz and triax taxi to the opera zone”
List the 4th generation cephalosporins.
- Cefepime
- Ceftolozon
List the 5th generation cephalosporins.
- Ceftolozane
- Ceftaroline
What spectrum does cephalosporins cover?
- Generally better Gram - and worse Gram + coverage as the generation advances, until…
- 4th and 5th generations are broad-spectrum (similar to ESPs spectrum, BUT ineffective against Enterococci and Listeria)
- Generally good for oral anaerobes, but not other anaerobes (ESPs better for anaerobes)
- Resist B-lactamases, but not altered PBPs or ESBLs
What are the indications for first generation cephalosporins?
Best effect against Gram + (↑ affin for Staph PBPs) + worst effect against Gram-. (UTIs by “PEK” Proteus, E. coli and Klebsiella often sensitive, however).
What spectrum does second generation cephalosporins cover?
Second Generation are worse for, but still effective against, Gram + and better effect against Gram -.
What spectrum does third generation cephalosporins cover?
even weaker effect against Gram+ and even better effect against Gram- (Salmonella, Shigella, H. influenzae etc.)
What are the indications for Cefepime?
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).
What are the indications for 5th generation cephalosporins?
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-!)
What is the route of administration of the 1st generation cephalosporins?
- Parenteral: Cephalothin, Cefazolin
- Oral: Cefalexin
What are the indications of Cefazolin?
Cefazolin is a DOC for surgical prophylaxis due to ↑ tissue penetration.
What are the indications for Cefalexin?
Uncomplicated skin / resp. infections (cellulitis, abscess, strep throat)
What are the side effects of cephalosporins?
Generally low toxicity and ok in pregnancy
- Allergy - cross-rxn with penicillin in about 10%
- GI effects: diarrhea, dysbacteriosis (esp. ceftriaxone, cefoperazone via bile!)
- Hematological rxns (hemolytic anemia)
- Seizures (at high serum level)
- Interstitial Nephritis
- Alcohol Intolerance - cefoperazone and cefamandole cause aldehyde dehydrogenase inhibition; AKA “disulfiram-like effect”.
What are the pharmacokinetic parameters of Cephalosporins?
- Tissue penetration increases with generation (ceftazidime, cefepime are DOC in meningitis); reach therapeutic levels in gallbladder
- Admin every 8-12 hrs (2-3x/day) with some exceptions:
- ceftriaxone, ceftibuten and cefixime given 1x/day
- cefotaxime given 3-4x/day
- Eliminated unchanged in kidney, except:
- cefotaxime is partly metabolized
- ceftriaxone, cefoperazone partly eliminated via bile
What are the indications for second generation cephalosporins?
- Middle severity RTI and UTIs, including “HENS” H. flu, Neisseria, Serratia.
What are the routes of administration for the second generation cephalosporins?
-
Parenteral:
- Cefuroxime
- Cefoxitin
- Cefamandole
-
Oral: for sinusitis, otitis, lower RTI (S. pneumo, H. flu, Klebs)
- Cefuroxime-Axetil
- Cefaclor
What are the indications for Cefoxitin?
Cefoxitin is good for Gram - anaerobes (B. fragilis) in peritonitis/diverticulitis.
What are the indications for thrid generation cephalosporins?
- First choice in pyelonephritis + orals used for severe UTIs
- Parenterals in pneumonia, meningitis
What are the routes of administration of third generation cephalosporins?
Parenteral:
- Cefotaxime - partly metabolized
- Cefoperazone - alcohol intolerance effect.
- Ceftriaxone
- Ceftazidime
Oral:
- Ceftibuten
- Cefixime
What are the indications for Cefoperazone?
Cefoperazone is non-DOC for Pseudomonas, high dose only.
What spectrum does Ceftriaxone cover and what are some indications for its use?
- Meningitis by Neisseria, H. flu, and pneumococci. (may add vancomycin for resistant S. pneumo or ampicillin for resistant Listeria)
- Endocarditis by S. viridans / H. flu; empirical sepsis tx; gonorrhea and Lyme
- Better Gram+ effect than other 3rd gens: DOC in penicillin-resistant pneumococcal infections
What are some possible side effect of Ceftriaxone?
Ceftriaxone can cause pseudocholelithiasis via biliary sludging.
What are the indications for Ceftazidime?
Ceftazidime is especially good for Gram - including Pseudomonas (“ICU” abx) in nosocomial / ventilator pneumonia.
What is the route of administration of the 5th generation cephalosporins?
Parenteral administration
What are important considerations to remember about Ceftolozane?
Ceftolozane does not have a Gram+ effect! and its given with tazobactam B-Lase inhibitor.
Does ceftaroline have any gram - effect?
Ceftaroline has a bad Gram- effect!
