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Spring Exam #1 - Cephalosporins
n/a
30
Pharmacology
Graduate
03/27/2010

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Term
1st generation cephalosporins
Definition
cephalothin
cephapirin
cephradine
cephalexin
cefazolin
cefadroxil
Term
2nd generation cephalosporins
Definition
cefamandole
cefaclor
cefuroxime
cefoxitin
cefotetan
cefprozil
loracarbef
cefmatazole
cefonicid
Term
3rd generation cephalosporin
Definition
ceftriaxone
ceftazidime
cefotaxime
ceftizoxime
cefixime
ceftibuten
cefditoren pivoxil
cefoperazone
cefpodoxime
cefdinir
Term
4th generation cephalosporin
Definition
cefepime
Term
ceftriaxone
Definition
3rd gen. cephalosporin with LONGEST half-life: 8 hrs (most have T1/2= 1-3 hrs)
Term
1st & 2nd generation cephalosporins
Definition
these do NOT have good penetration into CNS, even meninges are inflamed = NOT RECOMMENDED for Meningites or Brain Abscesses
Term
3rd generation cephalosporins except cefuroxime
Definition
drugs that DO enter CNS and ARE used for Meningitis
Term
Pharmacokinetics of most Cepahlosporins except 3rd generation cefoperazone and ceftriaxone
Definition
excreted by kidney via glomerular filtration & tubular secretion;
doses should be adjusted for renal failure;
probenicid slows tubular secretion of most of these drugs
Term
3rd generation ceftriaxone and cefoperazone
Definition
drugs excreted in the bile rather than by the kidneys;
Dosage adjustment with renal failure is NOT REQUIRED
Term
5 - 10% cross-allergenicity
Definition
percentage of people that are cross-allergenic between penicillins and cephalosporins;
allergic rxns occur less frequently in cephalosporins;
Term
Pts should NOT take cephalosporins in this situation --> switch to another antibiotic
Definition
If a pt has a SEVERE IMMEDIATE rxn to penicillins, what should they do if given an Rx for a cephalosporin?
Term
Adverse Events associated with cephalosporins
Definition
hypersensitivity and allergic rxns - urticaria, pruritus, angioedema, bronchospasm, maculopapular rash, fever;
Intolerance of alcohol - disulfiram-like rxn;
Bleeding disorders - prothrombin deficiency, thrombocytopenia, platelet dysfunction;
Nephrotoxicity;
Superinfection w/ opportunistic microorganisms;
Seizures
Term
cefazolin, cefmetazole, cefamandole, cefotetan, cefoperazone
Definition
cephalosporins that cause both intolerance of alcohol (disulfiram-like rxns) AND bleeding disorders (prothrombin deficiency, thrombocytopenia, platelet dysfunction)
Term
Bleeding disorders caused by cephalosporins
Definition
Administer vitamin K (10 mg twice/wk) to prevent these
Term
destruction of beta-lactam rings
Definition
most important resistance mechanism to cephalosporins
Term
limit or restrict usage of cepahlosporins
Definition
best way to minimize resistance to cephalosporins
Term
MRSA (methicillin-resistant Staph. aureus) and Enterococci
Definition
NONE of the cephalosporins have activity against these bugs
Term
1st generation cephalosporins (cefazolin & cephalexin)
Definition
good activity against Gram (+) bacteria & modest activity against Gram (-) bacteria;
Activity against most gram (+) cocci (EXCEPT MRSA);
Good activity against some Gram (-) enterics: PECK - Proteus, E.coli, Klebsiella;
Term
cefazolin (1st generation)
Definition
drug of choice for surgical prophylaxis
Term
Clinical Uses for 1st generation Cephalosporins (cefazolin, cephalexin)
Definition
one is a drug of choice for surgical prophylaxis;
alternative agent for penicillin for Staph and Strep infections with mild penicillin allergic rxns;
Used for UTIs;
SHOULD NOT be used for serious systemic infections;
Term
2nd generation cephalosporins (cefaclor, loracarbef, cefoxitin, cefuroxime, cefprozil)
Definition
less activity against Gram (+) bacteria but INCREASED activity against Gram (-) bacteria;
subset has activity against B. fragilis anaerobe;
subset good against agents that cause sinusitis & otitis media (S. pneumoniae, H. influenzae, M. Catarrhalis, S. Pyogenes);
one has coverage over Strep. Pneumoniae --> useful against CAP;
NOT effective against Pseudomonas aeruginosa
Term
Clinical Uses for 2nd generation Cephalosporins (cefaclor, loracarbef, cefoxitin, cefuroxime, cefprozil)
Definition
Tx sinusitis, otitis media, and lower respiratory tract infections (e.g. Community acquired pneumonia);
Tx mixed anaerobe infections (peritonitis and diverticulitis);
NOT used for meningitis
Term
cefoxitin (2nd generation)
Definition
subset of 2nd gen. drugs that has good activity against anaerobe B. fragilis
Term
cefuroxime, cefprozil, cefaclor, loracarbef (2nd gen)
Definition
subset of 2nd gens good for bugs that cause sinusitis and otitis media (S. pneumoniae, H. influenzae, M. catarrhalis, S. pyogenes)
Term
cefuroxime (2nd gen)
Definition
2nd generation ceph that has coverage against Strep. pneumoniae --> useful against Community Acquired Pneumonia (CAP)
Term
3rd generation cephalosporins (ceftriaxone, cefixime, ceftizoxime, ceftazidime) - BROAD SPECTRUM Cephs
Definition
broad-spectrum cephalosporins;
more active than 2nd gen against Gram (-) b/c resistant to beta-lactamases;
Less active than 1st gen against gram (+) cocci;
Useful against Gram (-) bacilli resistant to other cephs, penicillins, and aminoglycosides;
activity against Enterobacter sp. but SHOULD NOT BE USED CLINICALLY since mutants that express chromosomal beta-lactamase emerge rapidly during treatment;
Term
cefixime, ceftriaxone
Definition
1st line drugs for gonorrhea caused by N. gonnorrhoeae;
Term
ceftriaxone, ceftizoxime, ceftazidime (3rd gen)
Definition
able to penetrate CNS and can be used to treat Meningitis cause by pneumococci, meningococci, H. influenzae;
NOT useful if Listeria monocytogenes is causative agent (Use ampicillin instead)
Term
ceftriaxone (3rd gen)
Definition
used for treating neurologic complicatios of Lyme dx caused by Borrelia burgdorferi
Term
4th generation cephalosporin - cefepime
Definition
extended spectrum of activity and are resistant against deactivation by plasmid and chromosomal beta-lactamases;
useful against Gram (-) bacteria (Peudomonas aeruginosa, some Enterobacteriae);
More useful for enterobacter infections (e.g. UTI);
Used for penicillin-resistant Streptococci;
Penetrates into CNS and useful for treating Meningitis
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