2. CephalosporinsCephalosporins
B-Lactam antibiotics ( similar to penicillinsB-Lactam antibiotics ( similar to penicillins((
Broad spectrumBroad spectrum
Act by inhibition of cell wall synthesisAct by inhibition of cell wall synthesis
BactericidalBactericidal
Inactive against : enterococci, MRSA,Inactive against : enterococci, MRSA,
legionella , mycoplasma, chlamydia spplegionella , mycoplasma, chlamydia spp..
Widely used in surgical procedures toWidely used in surgical procedures to
reduce the risk of post operative infectionsreduce the risk of post operative infections

4. Classifications of cephalosporinsClassifications of cephalosporins
FIRST GENERATIONFIRST GENERATION
Cephalexin , poCephalexin , po
CefazolinCefazolin
CephalothinCephalothin
Cephradine , poCephradine , po
Active against G+ cocci ( except.enterococci & MRSAActive against G+ cocci ( except.enterococci & MRSA(:(:
s.pneumoniae, s.pyogenes,s. aureus, s.s.pneumoniae, s.pyogenes,s. aureus, s.
epidermidisepidermidis
Indicated for streptococcal pharyngitis ( e.g. cephalexinIndicated for streptococcal pharyngitis ( e.g. cephalexin((
Commonly used ( eg. Cefazolin( as prophylacic forCommonly used ( eg. Cefazolin( as prophylacic for
surgical proceduressurgical procedures..
Modest activity against G- bacteriaModest activity against G- bacteria

5. SECOND GENERATIONSECOND GENERATION
Cefoxitin ( mefoxinCefoxitin ( mefoxin((
Cefuroxime ( zinacef ( Cef. axetil ( zinnatCefuroxime ( zinacef ( Cef. axetil ( zinnat((
Cefaclor ( ceclor ( Cefprozil ( cefzilCefaclor ( ceclor ( Cefprozil ( cefzil((
Mainly effective against G- bacteriaMainly effective against G- bacteria
Modest activity against G+ bacteriaModest activity against G+ bacteria
CefoxitinCefoxitin active against bowel anaerobes (B. fragilisactive against bowel anaerobes (B. fragilis((
CefuroximCefuroxim active against H. influenzae, M. catarrhalis, S. pneumoniaeactive against H. influenzae, M. catarrhalis, S. pneumoniae
Cef. Axetil-Cef. Axetil- oral form of cefuroximoral form of cefuroxim
CefaclorCefaclor active against H. influenzae, M. catarrhalis &E.coliactive against H. influenzae, M. catarrhalis &E.coli
CefprozilCefprozil- similar to cefaclor, c. axetil and augmentin- Liked by children- similar to cefaclor, c. axetil and augmentin- Liked by children
Second Generations are used primarily for URTIs ( acute otitis media,Second Generations are used primarily for URTIs ( acute otitis media,
sinusitis ( and Lower RTIs ( acute exacerbation of chronicsinusitis ( and Lower RTIs ( acute exacerbation of chronic
bronchitisbronchitis((

6. THIRD GENERATIONTHIRD GENERATION
Ceftriaxone ( rocephinCeftriaxone ( rocephin((
Cefotaxime ( claforanCefotaxime ( claforan((
Cetazidime ( fortumCetazidime ( fortum((
Cefoperazone ( cefobidCefoperazone ( cefobid((
Cefixime ( supraxCefixime ( suprax((
They have enhanced G- activity, H. influenzae, N. meningitidis, N.gonorrhea,They have enhanced G- activity, H. influenzae, N. meningitidis, N.gonorrhea,
P. aeruginosae, M. catarrhalis, E.coli, most KlebsiellaP. aeruginosae, M. catarrhalis, E.coli, most Klebsiella
CeftriaxoneCeftriaxone has long half-life . Not advised in neonates (interferes with bilirubinhas long half-life . Not advised in neonates (interferes with bilirubin
metabolismmetabolism((
CefotaximeCefotaxime preferred in neonate ( does not interfere with bilirubin metabolism (,preferred in neonate ( does not interfere with bilirubin metabolism (,
as may ceftriaxoneas may ceftriaxone..
CeftazidimeCeftazidime && cefoperazonecefoperazone have excellent activity against p. aeruginosaehave excellent activity against p. aeruginosae..
CefiximeCefixime has similar activity to amoxicillin & cefaclor for actute otitis mediahas similar activity to amoxicillin & cefaclor for actute otitis media

7. Fourth GenerationFourth Generation
CefipimeCefipime
Active against G+ bacteria than cefazolinActive against G+ bacteria than cefazolin
against s. pyogenes, s.pneumoniae butagainst s. pyogenes, s.pneumoniae but
lower against s. aureus.lower against s. aureus.
Similar to cefotaxime against E.coli & K.Similar to cefotaxime against E.coli & K.
pneumoniae but for p. aeruginosapneumoniae but for p. aeruginosa..

8. PharmacokineticsPharmacokinetics
Cephalosporins are given parenterally and orallyCephalosporins are given parenterally and orally..
Extent of binding to plasma protein vary from one to anotherExtent of binding to plasma protein vary from one to another..
e.g. Cefazolin is 80% protein bound ( hence, long t1/2e.g. Cefazolin is 80% protein bound ( hence, long t1/2((
Cephalexin is 10-15% protein boundCephalexin is 10-15% protein bound
Relatively lipid insoluble ( like penicillinsRelatively lipid insoluble ( like penicillins((
Hence,do not penetrate cells or the CNS, except for third generationsHence,do not penetrate cells or the CNS, except for third generations..
Mostly excreted unchanged by the kidney (glomerular & tubularMostly excreted unchanged by the kidney (glomerular & tubular
secretion (, except, ceftazidime & cefoperazone( glomerularsecretion (, except, ceftazidime & cefoperazone( glomerular((
Probenecid slows their elimination and prolong their half-live ( exceptProbenecid slows their elimination and prolong their half-live ( except
Ceftazidime & cefoperazoneCeftazidime & cefoperazone((
Half-life 30-90 min; ceftriaxone 4-7 hrHalf-life 30-90 min; ceftriaxone 4-7 hr

9. Therapeutic usesTherapeutic uses
11..Alternative to penicillin in allergicAlternative to penicillin in allergic
patientspatients
22..Upper respiratory tract infectionsUpper respiratory tract infections
and otitis mediaand otitis media
cefaclor cefuroxime axetilcefaclor cefuroxime axetil
cefixime cefprozilcefixime cefprozil
33..Septicaemia caused by G- bacteriaSepticaemia caused by G- bacteria
( P.aeruginosae( P.aeruginosae((
A penicillin(eg.Piperacillin/A penicillin(eg.Piperacillin/
Ticarcillin( +aminoglycosideTicarcillin( +aminoglycoside
OROR
A cephalosporin(eg.A cephalosporin(eg.
ceftazidime ( + AGceftazidime ( + AG
44..Urinary tract infectionsUrinary tract infections
Cefuroxime, CefiximeCefuroxime, Cefixime
..55..Prophlaxis in surgeryProphlaxis in surgery
Appendectomy ( bowelAppendectomy ( bowel
anaerobes ( eg. Cefoxitinanaerobes ( eg. Cefoxitin
Obstetrical &gynecological,Obstetrical &gynecological,
urological, orthopedicurological, orthopedic
procedures, etcprocedures, etc
((S. aureus & S. epidermidis (S. aureus & S. epidermidis (
eg. Cefazolineeg. Cefazoline
66..Meningitis- N. MeningitidisMeningitis- N. Meningitidis
CeftriaxoneCeftriaxone
Cefotaxime( pref. in neonateCefotaxime( pref. in neonate((
77..Gonococcal infectionsGonococcal infections
CeftriaxoneCeftriaxone

10. Adverse effectsAdverse effects
11..Hypersensitivity reactions- most commonHypersensitivity reactions- most common
Anaphylaxis, bronchspasm, urticariaAnaphylaxis, bronchspasm, urticaria
Maculopapular rash- more commonMaculopapular rash- more common
22..Nephrotoxicity ; esp. cephradineNephrotoxicity ; esp. cephradine
33..Thrombophlebitis ( i.v adminThrombophlebitis ( i.v admin. (. (
44..SuperinfectionsSuperinfections
55..Diarrhea-oral cephalosporins, cefoperazone,Diarrhea-oral cephalosporins, cefoperazone,
ceftriaxone & moxalactamceftriaxone & moxalactam..
66..cefamandole, moxalactam & cefoperazone may causecefamandole, moxalactam & cefoperazone may cause::
a( bleeding disordersa( bleeding disorders
b( Flushing, tachycardia, vomiting with alcohol intakeb( Flushing, tachycardia, vomiting with alcohol intake