MECHANISM OF ACTION

Inhibit the last step in peptidoglycan synthesis which is a component of bacterial cell wall that provides mechanical stability

PHARMACOKINETICS

DRUGS INDICATIONS (with CONTRAINDICATIONS INTERACTION ADVERSE

ABSORPTION DISTRIBUTION METABOLISM EXCRETION Dosage) EFFECTS

[all Cephalosporins]

Generic name: Bioavailability: Concentrations T1/2: 1 hr [plasma] Against G+ and G- aerobes If skin testing is not Probenecid slows Hypersensitivity rxn
Cefotaxime achieved in CSF feasible, administration of a renal secretion of [anaphylaxis,
adequate for ! administer q4-8 hrs Poor against B. fragilis cephalosporin should be most bronchospasms,
treatment of for serious infections avoided if possible cephalosporins urticarial]
meningitis Empiric treatment of
Classification: 3rd Metabolized in vivo to meningitis in Maculopapular rash
Generation Onset: desacetylcefotaxime nonimmunocmpromised [+fever and
Cephalosporin adult and child eosinophilia]

Community-acquired +Coombs Test [large

Duration of penumonia doses]
Family: ß-lactam action:
antibiotics Hemolysis [rare]

Bone marrow
depression
[`~granulocytopenia]

Potentially
nephrotoxic

Encephalitis

Jaundice [neonates]

Generic name: T1/2: ~ 8 hrs ½ urine Single Dose IM [250 mg + Biliary pseudolithiasis
Ceftriaxone azithromycin]
½ biliary
secretion Mgmt. of urethral, cervical,
rectal, pharyngeal gonorrhea

Empirical tx of meningitis

Severe Lyme dx

CAP

Generic name: T1/2: 1.8 hrs 90% Similar but less potent
Ceftizoxime [administer q8-12 h recovered in activity as Cefotaxime
for serious infections] urine
Less active against S.
Not metabolized pneumoniae

More active against B.

fragilis

Generic name: Oral prodrug Hydrolyzed to Unchanged in Similar, but less potent,
esterases during urine activity against MRSA and
Cefpodoxime absorption to active penicillin susceptible strains
protexil forms [cefpodoxime of S. pneumoniae, S.
and cefditoren, pyogenes, H. influenzae, H.
Cefditoren pivoxil respectively] parainfluenzae and M.
catarrhalis

Generic name: T1/2: 3-4 h Excreted in Orally effective against UTI Reduce dose in px
Cefixime urine caused by E. coli and P. with renal impairment
mirabilis, otitis media by H.
Eliminated in influenza and S. pyogenes
bile
Pharyngitis due to S.
pyogenes

Uncomplicated gonorrhea
[IM>]

Standard Dose [A]: 400

mg/d for 5-7 d; longer for S.
pyogenes

[pediatric 6 mo and older

and less than 45 kg]: 8
mg/kg/d

Generic name: Orally administered similar

in spectrum and
Ceftibuten pharmacokinetics to
cefixime
Cefdinir

Generic name: Only achieves T1/2: 1.5 h [plasma] Renal ¼ to ½ as active against G+ Requires adjustment
Ceftazidime therapeutic as is cefotaxime in renal dysfunction
levels through
parenteral Activity against
administration staphylococci poor
Classification:
Antipseudomonal Act. against
Cephalosporins Enterobacteriaceae similar
to ceftriaxone

Excellent activity against

Family: ß-lactam Pseudomonads
antibiotics
Poor activity against B.
fragilis

Act. enhanced with ß-

lactamase inhibitor
avibactam
[ceftazidime/avibactam]

Generic name: T1/2: 2.5 h renal Structural analog of

Ceftolozane Ceftazidime that has
enhanced act. against
Pseudomonas including
resistant strains through ß-
lactamase overexpression

Ceftolozane/tazobactam,
improves act. against ESBL
producing
Enterobacteriaceae

Generic name: Excellent T1/2: 2 h [serum] renal Parenteral antipseudomonal Encephalopathy

penetration into [“fourth generation”]
Cefipime CSF [animal Nonconvulsive status
models of Similar act. against epilepticus
Cefpirome meningitis] Enterobacteriaceae

Relatively resistant to
AmpC encoded ß-
lactamases

Cefipime susceptible to
varying degrees to
hydrolysis by ESBL and
KPCs; higher act. than
ceftazidime and comparable
act. to cefotaxime for strep
and MRSA

Generic name: Minimal protein Parenteral prep Elimated by G- act. comparable to

Ceftaroline fosamil binding [~20%] rapidly converted to kidneys cefotaxime
active ceftaroline on
 Distribute well IV admin Enhanced G+ act.,
into most tissues especially ability to bind to
Classification: T1/2: 2 h low affinity PBPs
Anti-MRSA
Cephalosporins

Family: ß-lactam
antibiotics

Generic name: IV formulation is a Similar act. to ceftaroline

Ceftobiprole prodrug cleaved to against G+
medocaril active moiety
Appreciable in vitro act,
!Pharmacokinetics against E. faecalis
similar to ceftaroline
G- spectrum includes act.
similar to cefepime against
Pseudomonads spp. And
other G- bacilli