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K D Tripathi,Sparsh Gupta , S K shriwastav

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  1. 1. CEPHALOSPORINS Dr. Lokendra Sharma Sr Professor Pharmacology S.M.S.Medical College, Jaipur
  2. 2. Introduction Antibacterial agents which inhibit bacterial cell wall synthesis Discovered from a fungal colony in Sardinian sewer water (1948) Cephalosporin C identified in 1961 Generally more resistant to B-lactamases
  3. 3. What are the advantages and disadvantages of cephalosporin? Disadvantages • Polar due to the side chain - difficult to isolate and purify • Low potency - limited to the treatment of urinary tract infections where it is concentrated in the urine • Not absorbed orally Advantages • Non toxic • Lower risk of allergic reactions compared to penicillins • More stable to acid conditions • More stable to b-lactamases • Ratio of activity vs Gram -ve and Gram +ve bacteria is better
  4. 4. What is the mechanism of action of Cephalosporin ?
  5. 5. Write Generation Classification of Cephalosporin.
  6. 6. Write spectrum of different generations cephalosporin.
  7. 7. Cephalosporin Spectrum ABS First Generation Second Generation Third Generation Fourth Generation +Cocci Ө Cocci Ө Cocci Ө Cocci Ө Bacclli Ө Bacclli Ө Bacclli Ө Bacclli Anaerobes Anaerobes Resistance 3 LESS LESS LESS LESS + Bacclli +Cocci +Cocci Ө Cocci + Bacclli + Bacclli +Cocci
  8. 8. Write Pharmacokinetic properties of cephalosporin. Some cephalosporins may be given orally but most are given parenterally (IM or IV). They are widely distributed in the body like penicillins. Some such as CEFOPERAZONE, CEFOTAXIME, CEFUROXIME, CEFTRIAXONE, AND CEFTAZIDIME (third generation) also cross the blood-brain barrier Drugs of choice for meningitis due to Gram-negative intestinal bacteria. Almost all are eliminated via the kidneys and are actively secreted by the renal tubules. CEFAPERAZONE AND CEFTRIAXONE are eliminated through the biliary tract----Q.
  9. 9. Pharmacokinetic properties of cephalosporin
  10. 10. Mention properties of first generation cephalosporin's.  CEPHALOTHIN, CEFAZOLIN, CEFALEXIN. (Streptococcus, pneumococcus but not or methicillin-resistant Staphylococcus).  + Cocci > - Bacilli > + Bacilli > - Cocci > Anaerobics  Do not cross the blood-brain barrier.  Primarily excreted by kidney  Ineffective Pseudomonas aeruginosa, Enterobacter, and indole-positive Proteus species
  11. 11. Write some important properties of Second generation cephalosporin's.  CEFUROXIME, CEFAMANDOLE, CEFOXITIN, CEFACLOR.  - Cocci >+ Cocci > +Bacilli - Bacilli  Cefuroxime cross BBB ,Resistant to beta-lactamase  Do not achieve adequate levels in the CSF.
  12. 12. Mention properties of Third generation cephalosporin's. MOXALACTAM, CEFAPERAZONE, CEFTAZIDIRNE, CEFTRIAXONE. Extended Gram negative coverage, resistant to non-Staphylococcus b-lactamase, Cross the blood-brain barrier. The spectrum is extended to include: Enterobacter, Pseudomonas (ceftazidime and cefaperazone only), Serratia, b- lactamase producing Haemophillus influenza and Neisseria species. Ceftizoxime and moxalactam retain good activity against Bacteroides fragilis. - cocci & Bacilli & Anaerobes > + Cocci & Bacilli
  13. 13. What are the important properties of Fourth generation cephalosporin? CEFEPIME ,CEFPIROME . Comparable to third-generation but more resistant to some beta- lactamases. - cocci & Bacilli (Resistant to 3rd Gn) & > + Cocci & + Bacilli & Anaerobes ----NO
  14. 14. Mention some properties of Fifth Generation cephalosporin . Ceftobiprole and ceftaroline both parental Inhibit Bind to Penicillin binding protein -2a produce by MRSA resistance S Pneumonia Ceftaroline 2010 for MRSA Ceftobiprole – post antibiotic effect on MRSA
  15. 15. What are the adverse effects of cephalosporin ?  Hypersensitivity reactions =similar penicillins.  Nephrotoxicity =CEPHALORIDINE----Q  Intolerance to alcohol (disulfiram like reaction)(Q---- cefamandole, cefotetan, moxalactam, cefoperazone=MTT group)  Diarrhea= oral forms. cephaloridine ,third cefoperazone,cefixime  Superinfection. resistant organisms , fungi, often proliferate
  16. 16. What are the adverse effects of cephalosporin ? BLEEDING  Hyperprothrombinemia= (Q-----MTT group= cefamandole, cefotetan, moxalactam, cefoperazone)  Thrombocytopenia, Platelet dysfunction. Administration of vitamin K (10mg) twice a week can prevent this.  Neutropenia=Rare  Serum sickness=cefaclor ----- Q
  17. 17. ADRs of Cephalosporin • Adverse reactions. • 5-10% cross-sensitivity with pcn allergic pts. • 1-2% hypersensitivity reactions in non-pcn allergic pts. • Broader spectrum leads to opportunistic infections (candidiasis, C. difficile colitis).
  18. 18. ADRs of Cephalosporin Hypersensitivity
  19. 19. Adverse effects of cephalosporin
  20. 20. What are the clinical uses of cephaloporin A cephalosporin with or without aminoglycoside 1st Trt Klebsiella pneumococci. First GN surgical prophylaxis (Cefazolin) of wound infection. Third GN meningitis due to, meningococci, and Haemophillus influenza. CEFTRIAXONE= TOC beta-lactamase producing Neisseria gonorrhea. E coli(G1), Salmonella Typhoid,Parathyphoid=CEFTRIAXONE H .Ducreyi= CEFTRIAXONE Pseudo Pseudomalli=CEFTRIAXONE
  21. 21. Write indications of cephalosporin's.
  22. 22. Cephalosporin's First Generation Second Generation Third Generation Fourth Generation * Oral Agent CEFADROXIL * (tissue) CEFACLOR * CEFDINIR CEFEPIME (100% renal) CEFAZOLIN (surgical prophylaxis) CEFAMANDOLE CEFOPERAXONE CEFPIROME CEFELIXIN * (bile) CEFONICID CEFOTAXIME (prototype) CEFIPIME CEPHALOTHIN (prototype) (IM pain) CEFORANIDE CEFTAZIDIME (Thrombocytopeni) CEPHAPRIN CEFOTETAN (anaerobics) CEFTIBUTEN CEPHRADINE * (diarrhoea) CEFOXITIN (prototype ) CEFTIZOXIME CEFUROXIME (BBB) MOXALACTAM CEFTRIAXONE (MDR Typhoid)
  23. 23. Key points for clinical uses of Cephalosporins First Generation: Cefazolin: Drug of choice for surgical prophylaxis Second Generation: Cefotetan, Cefmetazole & Cefoxitin: Active against anaerobes like Bacteroides fragilis Third Generation: Cefazidime( maximum), Ceftolozane & Cefoperazone: Active against Pseudomonas Fifth Generation: Ceftaroline & Ceftobiprole: Approved for community acquired pneumonia & MRSA infection Reference: Garg GR, Gupta S. Review of Pharmacology, 13th edition.
  24. 24. Key points for clinical uses of Cephalosporins • No Cephalosporin is active against E. fecalis, MRSA and L. monocytogenes • Cefazidime+ Aminoglycoside : Treatment of choice for pseudomonas infections • Cefazolin: Drug of choice for surgical prophylaxis • Ceftriaxone & Cefoperazone: Secreted in the bile.
  25. 25. GUIDANCE OF ANTIMICROBIAL THERAPY • Minimum inhibitory concentration: lowest concentration of antibiotic that inhibits visible growth • Minimum bactericidal concentration: lowest concentration of antibiotic that kills 99.9% of the inoculum • Serum bactericidal title: dilution of serum that kills 99.9% of the inoculum • Synergy test: synergistic activity of multiple antibiotics For lecture only
  26. 26. An ideal antibiotics • Broad-spectrum • Did not induce resistance • Selective toxicity, low side effects • Preserve normal microbial flora For lecture only
  27. 27. Q. 1 Which cephalosporins are secreted in the bile? Ceftriaxone and Cefoperazone
  28. 28. Q. 2 Which Cephalosporin is used as a DOC in surgical prophylaxis? Cefazoline
  29. 29. Q. 3 ADRs of ceftriaxone, when used chronically. Biliary sludging syndrome, cholelithiasis
  30. 30. Q. 4 Which Cephalosporins are active against pseudomonas? Ceftazidime (Max.), ceftolozane and cefoperazone
  31. 31. Q. 5 Treatment of choice for pseudomonas infection. Ceftazidime and aminoglycosides
  32. 32. Q. 6 DOC for melioidiosis. Ceftazidime
  33. 33. Q.7 ADRs of cephalosporins. Hypersensitivity reactions, Neutropenia with ceftazidime
  34. 34. Q. 8 Ceftriaxone is first choice drug for- Gonorrhoea, Salmonellosis, E. coli sepsis, Proteus, Haemophilus, Bacterial Meningitis
  35. 35. THANK YOU