5th generation of cephalosporin
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1 5TH GENERATION CEPHALOSPORINS
Dr. PeymaniSara Bakhshi
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Contents• What are Cephalosporins • History of Cephalosporins• Mechanism of action• Generation of Cephalosporins• 5th generation of
Cephalosporins– Ceftobiprole– Ceftaroline– Ceftolozane
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What are Cephalosporins
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• A class of β-lactam antibiotics originally derived from the fungus Acremonium, which was previouslyknown as "Cephalosporium".
• Inhibit wide variety of gram(+) and gram(-) bacteria.
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History of cephalosporins
• Cephalosporium acremonium from a sewer in Sardinia in 1945 by Italian scientist Giuseppe Brotzu.
• Were first sold in 1964Contents
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Core structure
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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.
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Generation of Cephalosporins
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5th generation of Cephalosporins
• developed in the lab to specifically target against resistant strains of bacteria.
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Members of5th Generation Ceftobipr
ole
Ceftaroline
Ceftolozane
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Ceftobiprole
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• 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.
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Ceftobiprole structure
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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.
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Ceftaroline structure
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• 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.
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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.
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Ceftolozane structure
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Thanks For Your Attention
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