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5TH GENERATION
CEPHALOSPORINS
Dr. Peymani
Sara Bakhshi
1
Contents
• What are Cephalosporins
• History of Cephalosporins
• Mechanism of action
• Generation of Cephalosporins
• 5th generation of Cephalosporins
– Ceftobiprole
– Ceftaroline
– Ceftolozane
Sara Bakhshi
2
What are
Cephalosporins
Sara Bakhshi
3
• A class of β-lactam antibiotics originally derived from
the fungus Acremonium, which was previously
known as "Cephalosporium".
• Inhibit wide variety of gram(+) and gram(-) bacteria.
Sara Bakhshi
4
Contents
History of
cephalosporins
• Cephalosporium acremonium
from a sewer in Sardinia in 1945 by
Italian scientist Giuseppe Brotzu.
• Were first sold in 1964
Sara Bakhshi
5
Contents
Core
structure
Sara Bakhshi
6
Contents
Mechanism of
action
• Disrupt the synthesis of the
peptidoglycan layer forming the
bacterial cell wall.
• Beta-lactam antibiotics mimic the
D-Ala-D-Ala site, thereby
irreversibly inhibiting PBP
crosslinking of peptidoglycan.
Sara Bakhshi
7
Contents
Generation of
Cephalosporins
Sara Bakhshi
8
Contents
5th generation
of
Cephalosporins
• developed in the lab to specifically
target against resistant strains of
bacteria.
Sara Bakhshi
9
Contents Members
Members of
5th Generation
Sara Bakhshi
10
•Ceftobiprole
•Ceftaroline
•Ceftolozane
Contents
Ceftobiprole
Sara Bakhshi
11
Contents Members
• Ceftobiprole is effective against methicillin-
resistant Staphylococcus aureus (MRSA)
• for the treatment of hospital-acquired
pneumonia (HAP), excluding ventilator-
associated pneumonia (VAP), and community-
acquired pneumonia (CAP)
• It is mainly excreted renally.
Ceftobiprole
structure
Sara Bakhshi
12
Contents Members
Ceftaroline • With activity against aerobic and
anaerobic gram(+) and aerobic gram(-)
bacteria .
• Associated with skin and respiratory
infections.
• Also has activity against methicillin-
resistant Staphylococcus aureus and
Streptococcus pneumonia.
Sara Bakhshi
13
Contents Members
Ceftaroline
structure
Sara Bakhshi
14
Contents Members
• FDA has approved Ceftaroline
Fosamil under the trade name
Teflaro.
• Indicated for the treatment of
adults with acute bacterial skin
and skin structure infections
(ABSSSI)
• Also for the treatment of
community-acquied bacterial
pneumonia (CABP)
 Caused by susceptible Gram+ and Gram- microorganisms, such as
Staphylococcus aureus (including methicillin-susceptible and -resistant isolates),
Streptococcus pyogenes Streptococcus agalactiae, E-coli, Klebsiella pneumoniae ,
and Klebsiella oxytoca.
 Caused by susceptible Gram+ and Gram- bacteria, such as Streptococcus
pneumoniae (including cases with concurrent bacteremia), Staphylococcus
aureus (methicillin-susceptible isolates only), Haemophilus influenzae ,
Klebsiella pneumoniae , Klebsiella oxytoca , and E-coli.
Sara Bakhshi
15
Contents Members
Ceftolozane
(Zerbaxa)
• Anew option for treatment of
Complicated Intra-abdominal
Infections (cIAI), and Complicated
Urinary Tract Infections (cUTI).
• Is combined with the β-lactamase
inhibitor tazobactam, as multi-
drug resistant bacterial infections
will generally show resistance to
all β-lactam antibiotics unless this
enzyme is inhibited.
Sara Bakhshi
16
Contents Members
Ceftolozane
structure
Sara Bakhshi
17
Contents Members
Thanks For Your Attention
Sara Bakhshi
18
Contents

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5th generation of cephalosporin

  • 2. Contents • What are Cephalosporins • History of Cephalosporins • Mechanism of action • Generation of Cephalosporins • 5th generation of Cephalosporins – Ceftobiprole – Ceftaroline – Ceftolozane Sara Bakhshi 2
  • 4. • A class of β-lactam antibiotics originally derived from the fungus Acremonium, which was previously known as "Cephalosporium". • Inhibit wide variety of gram(+) and gram(-) bacteria. Sara Bakhshi 4 Contents
  • 5. History of cephalosporins • Cephalosporium acremonium from a sewer in Sardinia in 1945 by Italian scientist Giuseppe Brotzu. • Were first sold in 1964 Sara Bakhshi 5 Contents
  • 7. Mechanism of action • Disrupt the synthesis of the peptidoglycan layer forming the bacterial cell wall. • Beta-lactam antibiotics mimic the D-Ala-D-Ala site, thereby irreversibly inhibiting PBP crosslinking of peptidoglycan. Sara Bakhshi 7 Contents
  • 9. 5th generation of Cephalosporins • developed in the lab to specifically target against resistant strains of bacteria. Sara Bakhshi 9 Contents Members
  • 10. Members of 5th Generation Sara Bakhshi 10 •Ceftobiprole •Ceftaroline •Ceftolozane Contents
  • 11. Ceftobiprole Sara Bakhshi 11 Contents Members • Ceftobiprole is effective against methicillin- resistant Staphylococcus aureus (MRSA) • for the treatment of hospital-acquired pneumonia (HAP), excluding ventilator- associated pneumonia (VAP), and community- acquired pneumonia (CAP) • It is mainly excreted renally.
  • 13. Ceftaroline • With activity against aerobic and anaerobic gram(+) and aerobic gram(-) bacteria . • Associated with skin and respiratory infections. • Also has activity against methicillin- resistant Staphylococcus aureus and Streptococcus pneumonia. Sara Bakhshi 13 Contents Members
  • 15. • FDA has approved Ceftaroline Fosamil under the trade name Teflaro. • Indicated for the treatment of adults with acute bacterial skin and skin structure infections (ABSSSI) • Also for the treatment of community-acquied bacterial pneumonia (CABP)  Caused by susceptible Gram+ and Gram- microorganisms, such as Staphylococcus aureus (including methicillin-susceptible and -resistant isolates), Streptococcus pyogenes Streptococcus agalactiae, E-coli, Klebsiella pneumoniae , and Klebsiella oxytoca.  Caused by susceptible Gram+ and Gram- bacteria, such as Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible isolates only), Haemophilus influenzae , Klebsiella pneumoniae , Klebsiella oxytoca , and E-coli. Sara Bakhshi 15 Contents Members
  • 16. Ceftolozane (Zerbaxa) • Anew option for treatment of Complicated Intra-abdominal Infections (cIAI), and Complicated Urinary Tract Infections (cUTI). • Is combined with the β-lactamase inhibitor tazobactam, as multi- drug resistant bacterial infections will generally show resistance to all β-lactam antibiotics unless this enzyme is inhibited. Sara Bakhshi 16 Contents Members
  • 18. Thanks For Your Attention Sara Bakhshi 18 Contents