Classification of Cephalosporin Antibiotics

Cephalosporin drugs are beta lactam antibiotics that inhibit the cell wall of bacteria.
Cephalosporin C was first isolated from a fungus named as Cephalosporium acremonium by Dr.
Abraham in 1948. These are bactericidalantibiotics as they kill the micro-organisms when used at
therapeutic dose.
Mode of Action:
The mechanism of action of cephalosporin drugs is similar to penicillin. They inhibit the
enzymes that are necessary for the synthesis of cell wall of bacteria by combing with penicillin
binding proteins (PBP). Remember their bactericidal activitydoes not depend upon the
concentration of drug.
Classification of Cephalosporin:
Cephalosporins can be classified by different ways such as classification based upon;

Spectrum

Generation

Chemical structure

Resistance to beta lactamases

Clinical pharmacology

But most renowned type of classification is based on generation. Cephalosporin drugs are divided
into different generations depending upon their microbialspectrum.
1.

First generation

2.

Second generation

3.

Third generation

4.

Fourth generation

5.

Fifth generation

First Generation:
The optimum activity of all first generation cephalosporin drugs is against gram-positive
bacteria

such

as

staphylococci and streptococci.

They

also

have

little

gram-

negative spectrum.
The list of drugs is as follows.
Cephalosporin Dose

Route

Dosing
Interval

Spectrum

Renal

1st Generation (Narrow Spectrum)

Cefazolin

1-2gm

IV/IM 8

Cephalothin

1-2gm

IV/IM 4-6

Cephapirin

0.5-1gm

IV/IM 4-6

Cephalexin

250-500mgPO

b;Staphylococcus yes

Cefadroxil

500mg

PO

12

aureus. c

250mg

PO

Cephradine

<500mg> PO

yes
yes
Streptococci

yes

yes
yes

12

Second Generation:
The drugs that come under second generation have more spectra against gram-negative
bacteria (Haemophilus influenzae, Enterobacter aerogenes) in comparison to the first
generation. Their gram positive spectrum is less than thefirst generation.

Cephalosporin Dose

Route

Dosing
Interval

Spectrum

Renal

2nd Generation (Intermediate Spectrum)

Cefamandole
Cefuroxime
Cefoxitin

1-2gm

IV/IM

4-6

Escherichia

0.75-1.5gm

IV/IM

Klebsiella, Proteus,

250-500mg

PO

12

Haemophilus

1-2gm

IV/IM

4-6

Cefotetan

1-2gm

IV/IM

12

Cefmetazole

2gm

IV

6-12

Cefaclor

250-500mg

PO

influenzae,
Moraxella
catarrhalis.

coli,yes
yes
yes
yes
yes
yes

Cefprozil

250-500mg

PO

12-24

yes

Cefpodoxime

200-400mg

PO

12

yes

Loracarbef

200-400mg

PO

12

yes

Third Generation:
Third generation cephalosporin drugs are broad spectrum and the effective against both gram
positive and gram negative bacteria. However their optimumactivity is against gram negative
bacteria.

Cephalosporin Dose

Route

Dosing
Interval

Spectrum

Renal

3rd Generation (Broad Spectrum)

Cefotaxime

1-2gm IV/IM 6-8

Ceftriaxone

1-2gm IV/IM 12-24

Pseudomonas

Ceftizoxime

1-2gm IV/IM 8-12

Serratia;

Ceftazidime

1-2gm IV/IM 8

gonorrhoeae;activity for

Cefoperazone

1-2gm IV/IM 12

aureus,

Cefixime

400mg PO

24

200mg PO

12

yes
aeruginosa

e;

Neisseriayes
S.yes

Streptococcus

pneumoniae,Enterobacteriaceae
yes

Fourth Generation:
These are extended spectrum antibiotics. They are resistant to beta lactamases.

Cephalosporin Dose Route

Dosing
Interval

4th Generation (Broad Spectrum)

Spectrum

Renal

Their

spectra

comparable
Cefipime

2gm

is
to

12 hours 3rdgeneration but theyYes

IV

show more resistance

to betalectamases
Fifth Generation:
These are extended spectrum antibiotics.

Cephalosporin

Dose

Route

Dosing
Interval

Spectrum

5th Generation (Extended Spectrum)

Ceftaroline

600 mg

IV

12 hours

Ceftobiprole

500mg

IV

12 hours

Pneumonia,

skin and soft

tissue infections
Methicillin-resistant Staphyloc
occus aureus

References:
1.

The Merck Manual of Medical Information. Mark H. Beers et al., eds. 2ndHome Edition.
Whitehouse Station, NJ: Merck; 2003.

2.

Tumah H. Fourth-generation cephalosporins: in vitro activity against nosocomial gramnegative bacilli. Chemotherapy. 2005 May;51(2-3):80-5.

3.

Brunton LL, Parker K, Blumenthal D, et al. The goodman and gilmans manualof
pharmacological therapeutics. McGraw-Hill Professional, 2007.

4.

Henry F. Chambers. Beta-Lactam & Other Cell Wall- & Membrane-ActiveAntibiotics.

Basic & Clinical Pharmacology, edited by Bertram G. Katzung. McGraw Hill, USA, 2007.