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9.CEPHALOSPORIN (therapeutic use (upper resp. tract & otitis media…
9.CEPHALOSPORIN
therapeutic use
utk yg sensitive pen.
upper resp. tract & otitis media
cefaclor
cefixime
cefprozil
cefuroxime axetil
Septicaemia (sbb Pseudomonas a.)
ceftazidime (+aminoglcoside)
UTI
Cefuroxime,
Cefixime
prophylaxis
Meningitis-
Ceftriaxone
Cefotaxime-neonate
gonorrhea
Ceftriaxone
pharmacokinetic
ROA
oral
parenteral
cefazolin-high protein bound
long t1/2
cephalexin-sikit protein bound
lipid insoluble (mcm penicillin)
except 3rdG
excreted kidney
probenecid
increase t1/2
except ceftazidime & cefoperazone
ADR
Hypersensitivity
Nephrotoxicity
Thrombophlebitis (inflam vein)
Superinfections
diarrhea (oral)
cephalosporins,
cefoperazone,
ceftriaxone
bleeding
cefamandole,
cefoperazone
cefoxitin?
classification
1st generation
G+ve
penicillinase-producing
MSSA (methicillin-susceptible staph. & strep- methicillin berkesan)
though bukan pilihan
kurang G-ve
Proteus mirabilis,
some Escherichia coli,
Klebsiella pneumoniae
Proteus,
Serratia
eg
Cephradine (oral)
Cephalothin
Cephalexin (oral)
Cefazolin
usually for prophylaxis
x BBB
2nd generation
sikit G+ve
G-ve
eg
Cefoxitin
-bleeding
bowel anaerobes
Cefuroxime
H. influenzae,
M. catarrhalis,
S. pneumoniae
Cefaclor
influenzae,
M. catarrhalis
E.coli
Cefprozil
children
cefamandole (s/e bleeding)
primarily for upper resp. tract
acute otitis media (infame middle ear)
sinusitis
Lower resp. tract
acute exacerbation
chronic bronchitis
x BBB
3rd generation
G- activity
H. influenzae,
N. meningitidis,
N.gonorrhea,
P.
aeruginosae,
M. catarrhalis,
E.coli,
most Klebsiella
eg
Ceftriaxone
long half-life
x neonate
interferes with bilirubin
metabolism
gonorrhea ('the only USA')
Cefotaxime
neonate
Ceftazidime
p. aeruginosae.
cefoperazone
p. aeruginosae.
Cefixime
otitis media
x 1sr choice-susceptiblity decrease (kurang berkesan)
sangat sikit G+Ve
can BBB
4th generation
eg
Cefepime
P. aeruginosa
wider G+ve
G-ve
C ada zwitterion
can penetrate outer membrane G-ve
resistance B-lactamase
can BBB
5th generation
Ceftobiprole
kuat P. aeruginosa
less susceptible to resistance (bagus)
'ceftaroline'
x pseudomonas
x VRE
ceftolozane
cIAI
Complicated
Intra-abdominal Infections
cUTI
Complicated Urinary
Tract Infections
.+ tazobactam (B-lactamase inhibitor)
x boleh
LAME
legionella
atypical
mycoplasma
chlamydia
MRSA
enterococci
lactam antibiotic
sama mcm penicillin
broad spectrum
bactericidal: inhibit cell wall synthesis
prophylactic