2.  Cephalosporins are structurally and
pharmacologically related to the penicillins
 They have a beta-lactam ring structure
that interferes with synthesis of the
bacterial cell wall
 Bactericidal Activity

3.  Cephalosporins are bactericidal agents
and have the same mode of action as
other beta-lactam antibiotics (such as
penicillins).
 Cephalosporins disrupt the synthesis of the
peptidoglycan layer of bacterial cell
walls, which causes the walls to break
down and eventually the bacteria die.

4.  Cephalosporins are bactericidal for most of
the following:
 Gram-positive bacteria
 Gram-negative bacteria
 Cephalosporins are used to treat infections
in different parts of the body—the
ears, nose, throat, lungs, sinuses, and
skin, for example.
 Cephalosporins are a newer class
of antibiotics and often are seen as an
alternative to penicillin

5.  Cephalosporins are grouped into
"generations" based on their spectrum of
antimicrobial activity.
 Each newer generation of cephalosporins
has significantly greater gram-negative
antimicrobial properties than the
preceding generation, in most cases with
decreased activity against gram-positive
organisms.
 Fourth generation cephalosporins,
however, have true broad spectrum
activity.

6. Currently there are only two drugs in this
category, Ceftobiprole and Ceftaroline.
These new drugs are also the only β-lactam
antibiotics that are effective
against methicillin-resistant-
Staphylococcus-aureus (MRSA).
They inhibits the 2a penicillin-binding
protein (PBP) of methicillin-
resistant Staphylococcus aureus and the 2x
PBP of Streptococcus pneumoniae, as well
as the classic PBP-2 of MSSA. Ceftobiprole is
resistant to staphylococcal β-lactamase.

7.  MRSA is any strain of Staphylococcus
aureus that has evolved resistance to beta-
lactam antibiotics, which include
the penicillins (methicillin, dicloxacillin, nafc
illin, oxacillin, etc.)
 and the cephalosporins. Strains unable to
resist these antibiotics are classified as
methicillin-sensitive Staphylococcus
aureus, or MSSA.
 resistance does make MRSA infection more
difficult to treat with standard types of
antibiotics and thus more dangerous.

8. Ceftobiprole
Ceftobiprole is a pyrrolidinone-3-
ylidenemethyl cephem. The C-3 side chain
was specifically designed to have a strong
binding affinity to PBP2a and PBP2x. PBP2a is
known to give staphylococci resistance to
other β-lactam drugs and PBPx does the
same for pneumococci.
Ceftobiprole also has a
aminothiazoylhydroxyimino side chain at the
C-7 position which is known to give good
resistance to β-lactamase from S. aureus.
Together these active groups make
Ceftobiprole bactericidal to MRSA.
Ceftobiprole has poor water solubility and is
therefore administered intravenously.
Clinical used:
Methicillin-resistant
Staphylococcus
aureus associated
with endocarditis and
bone and joint
infections
Pneumonia caused
by Penicillin-resistant
Streptococcus
pneumoniae
Pseudomonas
aeruginosa
Enterococci.

15. Ceftaroline
Ceftaroline was developed from the fourth
generation cephalosporin Cefozopran, It
retains the alkoxyimino group at position C-7
from earlier generations so it is fairly stable in
the presence of many β-lactamases.
Since MRSA and penicillin resistant
Streptococcus pneumoniae have resistance
dedicated to new types of PBP, PBP2a and
PBP2x respectively,
both Ceftaroline and Ceftobiprole have C-3
side chains specially engineered to bind
these new PBP. In the case of Ceftaroline this
side chain contains a 2-thioazolythio spacer
linkage optimised for its anti-MRSA activity.]