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![New drugs
• Ceftaroline fosamil
• is a fifth-generation]cephalosporin antibiotic.
• It is active against methicillin-resistant Staphylococcus aureus (MRSA)
and Gram-positive bacteria.
• It retains the activity of later-generation cephalosporins having broad-
spectrum activity against Gram-negative bacteria.
• It is currently being investigated for community-acquired
pneumonia and complicated skin and skin structure infection.](https://image.slidesharecdn.com/7-190702141805/85/Cephalosporins-21-320.jpg)
![New drugs
• Ceftaroline fosamil
• is a fifth-generation]cephalosporin antibiotic.
• It is active against methicillin-resistant Staphylococcus aureus (MRSA)
and Gram-positive bacteria.
• It retains the activity of later-generation cephalosporins having broad-
spectrum activity against Gram-negative bacteria.
• It is currently being investigated for community-acquired
pneumonia and complicated skin and skin structure infection.](https://image.slidesharecdn.com/7-190702141805/75/Cephalosporins-21-2048.jpg)
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Cephalosporins
- 1. Cephalosporins Jagir R. Patel AsstProfessor Dept. Pharmacology
- 2. Introduction • The cephalosporinsare a class of β-lactam antibiotics originally derived from the fungus Acremonium, which was previously known as "Cephalosporium”
- 3. Classification • 1st Gen:Cephalothin, Cephalexin, Cefazolin Cephradine, Cefadroxil • 2nd Gen: Cefuroxime Cefaclor, Cefoxitin* Cefuroxime axetil • 3rd Gen: Cefotaxime, Cefixime, Ceftizoxime Cefpodoxime proxetil, Ceftriaxone Cefdinir, Ceftazidime Ceftibuten, Cefoperazone Ceftametpivoxil • 4th Gen: Cefepime, Cefpirome • 5th Gen: Ceftaroline fosamil, Ceftolozane, Ceftobiprole
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- 6. Mechanism of resistance •Acquired resistance to cephalosporins could have the same basis as for penicillins, i.e.: • (a) alteration in target proteins (PBPs) reducing affinity for the antibiotic. • (b) impermeability to the antibiotic or its efflux so that it does not reach its site of action. • elaboration of p-lactamases which destroy specific cephalosporins (cephalosporinase).
- 7. 1st Gen • Spectrum •Gram Positive Cocci, including MSSA (Does NOT cover Enterococcus) • Gram Negative Rods • No CNS penetration • Coverage • MSSA • Streptococci Grp A,B,C,G • Strep viridans • S. pneumoniae • H. influenzae • E. coli • Klebsiella pneumoniae • Proteus mirabilis
- 8. Cephalexin • General information:administered orally may not cross the blood brain • Barrier • Side effects • hypersensitivity reactions, leading to fever, skin rashes, angioedema and/or anaphylactic shock consecutive hypersensitivity to penicillins (due to cross reactivity) diarrhea (due to gastrointestinal overgrowth by cephalosporin- resistant bacteria) • Medical uses • treatment of folliculitis, cellulitis and/or impetigo due to staphylococcus and/or streptococcus infection treatment of pharyngitis due to streptococcus infection
- 10. 2nd Gen intermediatespectrum • Same as 1st Generation Plus: • β-lactamase positive H. influenzae • Moraxella catarrhalis • Neisseria meningitidis • E. coli • Klebsiella pneumoniae • Proteus • Oral anaerobes • Cefoxitin & Cefotetan cover B. fragilis
- 11. Cefaclor & Cefuroxime •General information: administered orally may not cross the blood brain • Barrier • Indications: treatment of pharyngitis due to streptococcus infection • -Treatment of pneumonia due to streptococcus, enterobacter, klebsiella, proteus and/or haemophilus infection. • Side effects same as cephalexin
- 12. 3rd broad spectrum •3rd Generation Coverage • Same as 1st Generation Plus: • Expanded gram-negative coverage • Oral anaerobes • S. aureus (OSSA) • Strep pneumoniae • Strep Grp A,B,C,G • Strep viridans • Gram negative rods • N. gonorrhea • All cover B. fragilis EXCEPT cefotaxime & ceftazidime • P. aeruginosa - ceftazidine only
- 13. Cefotaxime • Administered intramuscularlyand/or IV may cross the blood-brain barrier • Interactions: Cefotaxime + aminoglycosides = nephrotoxicity • ADV: Clostridium difficile-associated diarrhoea and colitis, arrhythmias, anaphylaxis. • Medical uses • Pharyngitis: due to streptococcus infection • Meningitis due to streptococcus, haemophilus and/or neisseria infection Gonorrhea due to neisseria infection • Septicaemia • Surgical prophylaxis Dose: 1-2gm per day
- 14. Ceftriaxone • Administered intramuscularlyand/or IV may cross the blood-brain barrier exctred via urine and faeces • ADV: Anaphylaxis, Clostridium difficile-associated diarrhoea and colitis, hemolytic anemia. • Indications: Uncomplicated Gonorrhoea, Prophylaxis of surgical infections • Contraindications: to hypersensitive to cephalosporins
- 15. 4th gen • Spectrum •Good gram-positive & gram-negative coverage • Anti- Pseudomonal (including ceftazidime resistant isolates) • Penetrates CSF • Limited anaerobic coverage
- 16. Cefepime • Absorption: Rapidlyand almost completely absorbed on IM inj. Time to peak plasma concentration: Approx 1.5 hr (IM); w/in 30 min (IV). • Distribution: Widely distributed in body tissues and fluids; high concentrations in bile. Crosses the blood-brain barrier and enters breast milk (low concentrations). Plasma protein binding: Approx 20%. • Metabolism: Minimally hepatic. • Excretion: Via urine (approx. 85% as unchanged drug). Plasma half-life: Approx 2 hr. • ADV: Neurotoxicity (e.g. encephalopathy, myoclonus, seizures, non- convulsive status epilepticus); Clostridium difficile-associated diarrhoea; anaphylaxis.
- 17. • Indications: • Respiratorytract infections • Skin and skin structure infections • Urinary tract infections • Abdominal infections • Empiric therapy for febrile neutropenic patients • Dose: 1-2gm daily
- 18. Cefpirome • Administration: i.v. •Distribution: Widely distributed into body tissues and fluids; enters breast milk. Protein-binding: 10% • Excretion: Mainly by the kidneys via the urine (80-90% as unchanged); significantly removed by hemodialysis; 2 hrs (elimination half-life); prolonged in renal impairment. • Adv.: Pseudomembranous colitis. • Indications: Susceptible infections
- 19. • diarrhea, nausea,rash, electrolyte disturbances, and pain and inflammation at injection site. vomiting, headache, dizziness, pseudomembranous colitis, superinfection, eosinophilia, nephrotoxicity, neutropenia, thrombocytopenia, and fever. • hypoprothrombinemia and a disulfiram-like reaction with ethanol • Hypersensitive reaactions
- 20. General characteristics • Bactericidal •Bind to Penicillin Binding Proteins • Resistant to Penicillinase, but not other classes of β-lactamases (e.g. Extended Spectrum Beta-Lacatamases or ESBLs) • Renal excretion • Side Effects • Hypersensitivity reactions (Cross-hypersensitivity with penicillins 1-3%) • Superinfections: Enterococci, Enterobacter and Candida
- 21. New drugs • Ceftarolinefosamil • is a fifth-generation]cephalosporin antibiotic. • It is active against methicillin-resistant Staphylococcus aureus (MRSA) and Gram-positive bacteria. • It retains the activity of later-generation cephalosporins having broad- spectrum activity against Gram-negative bacteria. • It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection.
- 22. Ceftolozane • Ceftolozane isa 5th generation cephalosporin antibiotic, • developed for the treatment of infections with gram-negative bacteria that have become resistant to conventional antibiotics. • It was studied for urinary tract infections, intra-abdominal infections and ventilator-associated bacterial pneumonia. Ceftolozane is combined with the β-lactamase inhibitor tazobactam, which protects ceftolozane from degradation. • • Ceftolozane-tazobactam is indicated for the treatment of complicated urinary tract infections and complicated intra abdominal infections.
- 23. Ceftobiprole • Ceftobiprole isa new 5th-generation cephalosporin for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP). • Ceftobiprole has high affinity for PBP2a of methicillin resistant Staphylococcus aureus (MRSA) strains