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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