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Pharmacology Exam II
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Cephalosporins are a class of
beta lactam antibiotics
Advantages of cephalosporins over PCNs
more stable against beta lactamases
broad specturm
cephalosporins can by hydrolyzed by
extended specturn beta lactamases
cephalosporins are not active against
enterococci
L monocytogenes
cephalosporins have a similar nucleus compared to PCNs but have
a second R group option
First synthetic cephalosporin
cefalothin
Cephalosporin mechanism of action
disruption of synthesis of the peptidoglycan layer of bacterial cell walls (same as other beta lactams)
less susceptible to penicillinases
cephalosporins are grouped by "generation" which distinguishes their
antimicrobial properties
First generation cephalosporins are very active against
gram positive cocci
first generation cephalosporins are not generally active against
methicillin resistant strains of staph
Each newer generation of cephalosporins contains
a broader spectrum of action
First generation cephalosporins
cephalothin
cephalexin
cefazolin
cephradine
cephapirin
First generation cephalospoins that may be used orally
cephalexin
cephradine
cefadroxil
urin concentrations of 1st gen ceph.
very high
tissue vs blood concentrations of 1st gen ceph.
lower in tissues than in blood
excretion of 1st gen cephs.
renal
decreased by probenecid
Only first gen. cephalosporin still in use
cefazolin
0.5g-2g q8h
Dose adjustments for 1st gen. ceph must be made based on
renal function
Uses of oral 1st gen cephalosporins
UTI
Streptococcal
cellulitis
soft tissue abscess
Uses of cefazolin (IV)
surgical prophylaxis (drug of choice)
staph or strep infections in pt with PCN allergy
cannot be used for meningitis
Second generation cephalosporins
cefamandole
cefonicid
cefuroxime
cefaclor
cefprozil
and structurally related cephamycins
Cephamycins
cefoxitin
cefmetazole
cefotetan
activity against anaerobes
2nd generation cephalosporin spectrum
greater gram negative specturm than 1st
more resistant to b-lactamase
no activity against enterococci or pseudomonas
Oral 2nd gen cephalosporins
cefuroxime
cefaclor
cefproxil
loracarbef
Usual dose of 2nd gen cephs
adult 10-15mg/kg
higher in children (20-40mg/kg max of 1 gram)
2nd gen Cephs are not active against PCN resistant pneumococci except
cefuroxime
Second generation cephalosporin dosing depends on
renal function
oral 2nd gen cephs active against H influenzae or Moraxella are primarily used to treat
sinusitis
otitis
lower RTIs
2nd gen. cephs have activity against _____ and can therefore be used to treat ____ and ____.
activity against anaerobes
peritonitis
diverticulitis
Used to treat community aquired pneumonia
cefuroxime
Cefuroxime should not be used to treat
meningitis
3rd generation cephalosporins
cefoperazone
cefotaxime
ceftriaxone
ceftazidime
ceftizoxime
cefixime
cefpodoxime
cefdinir
3rd gen cephs have _____ when compared to 2nd generation
expanded gram negtative coverage
3rd gen cephs are effective against
b-lactamase producing strains of haemophilus and neisseria
Only two drugs with useful activity against P aeruginosa (pseudomonas)
ceftazidime
cefoperazone
achieve leves in CSF to inhibit most pathogens influding gram-negative rods except pseudomonas
3rd generation cephalosporins
Only 3rd gen cephs that do not require renal dosing
cefoperazone
ceftriaxone
3rd gen cephs should be avoided in treatment of
enterobacter (emergence of resistance)
Approved for treatment of meningitis except that caused by l monocytogenes
ceftriaxone
cefotaxime
Clinical uses of Ceftriaxone and Cefotaxime
meningitis + vancomycin
treatment of sepsis of unknown cause
used in neutropenic immunocomprimised pt + aminoglycoside
treating hospital aquired infections
Only recommended treatmenf for gonorrhea in the US
ceftriaxone
cefixime
4th generation cephalosporins
cefepime
cefluprenam
cefoselis
cefozopran
cefpirome
cefquinome
Fourth Gen Cephalosporins
extended spectrum
greater b-lactamase resistance
can cross BBB
used in Pseudomonas aeruginosa
more resistance to lactamases produced by enterobacter
Cefepime uses
pseudomonas
enterobacter
haemophilus
neisseria
penetrates CSF
B-lactam antibiotics with activity against MRSA
currently under development
ceftaroline fosamil
ceftobiprole medocaril
increased PCN binding protein 2a
Common ADRs with cephalosporins
diarrhea
nausea
rash
electrolyte disturbance
pain at injection site
Infrequent ADRs with cephalosporins
vomiting
headache
dizziness
candidiasis
pseudomembranous colitis
eosinophilia and or fever
Cephalosporin allergies
hypersensitivity reactions identical to those of PCN
Some patients with PCN allergy can tolerate cephalosporins, pt with history of anaphylaxis to PCN should _____
not take cephalosporins
Toxicities of cephalosporins
thrombophlebitis
interstitial nephritis (renal) or tubular necrosis
Drug withdrawn from market due to tubular necrosis
cephaloridine
Cephalosporins containing a methylthiotetrazole group frequently cause ____. Can be avoided with the use of ____.
hypoprothrombinemia
bleeding disorders
disulfiram like reactions
vitamin K 10mg 2x weekly (for bleeding)
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Author
Rx2013
ID
65116
Card Set
Pharmacology Exam II
Description
Cephalosporins
Updated
2011-02-09T02:05:44Z
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