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
Cephalosporins are bactericidal agents
and have the same mode of action as
other beta-lactam antibiotics (such as
Cephalosporins disrupt the synthesis of the
peptidoglycan layer of bacterial cell
walls, which causes the walls to break
down and eventually the bacteria die.
Cephalosporins are bactericidal for most of
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
Cephalosporins are grouped into
"generations" based on their spectrum of
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
Fourth generation cephalosporins,
however, have true broad spectrum
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
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.
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
aureus, or MSSA.
resistance does make MRSA infection more
difficult to treat with standard types of
antibiotics and thus more dangerous.
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.
with endocarditis and
bone and joint
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
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.]