Cephalosporins

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Cephalosporins

  1. 1. CEPHALOSPORINS<br />VIJAY NAGDEV<br />H.O.MU-I<br />CMCH LARKANA<br />
  2. 2. CEPHALOSPORINS<br />A class of beta lactam antibiotics<br />They were first isolated from cultures of cephalosporium acremonium<br />
  3. 3. Mechanism of action<br />Peptidoglycan layer is important for cell wall structural integrity<br />The final step in synthesis of petidoglycan(Transpeptidation) is fascillitated by transpeptidases(pencillin binding proteins)<br />Cephalosporins competitively inhibit PBP and disrupt synthesis of peptidoglycan<br />These are bactricidal agents<br />
  4. 4. Therapeutic uses<br />Pharyngitis<br />Tonsilitis<br />Bronchitis<br />Pneumonia <br />UTI<br />Skin and bone infections(cefazolin and ceftriaxone have good penetration into bone)<br />Meningitis( 3rd generation cephalosporins)<br />Surgical prophylaxis <br />
  5. 5. Adverse effects<br />Diarrhea,nausea,vomitting<br />Pain and inflammation at injection site <br />Pseudomembranous colitis <br />Allergic reactions<br />Disulfiram-like effect(cefamandole,cefoperazone)because these block oxidation of alcohol.<br />Bleeding(cefamandole,cefoperazone,ceftriaxone)because these contain MTT side chain(anti vit-k effect)<br />Seroconversion of direct coombs test from negative to positive.<br />
  6. 6. Pharmacokinetics <br />Except 1st and some of 2ndgeneration,allcephalosporins are adminsteredparentrally<br />Well distributed in body fluids <br />Crosses placenta and secreted in breast milk.<br />Therapeutic levels in CSF are achieved only with 3rd generation cephalosporins<br />20-30% bound to plasma proteins<br />80-90% excreted unchanged in urine<br />Elimination occurs through tubular secretion/glomerular filtration<br />Cefoperazone and ceftriaxone are excreted through bile (can be administered in renal insufficiency) <br />
  7. 7. CLASSIFICATION<br />
  8. 8. GENERATIONS <br />Cephalosporins are divided into five generation based largely on their <br />Spectrum and <br />Resistance to beta lactamases<br />Each newer generation has increased activity against G-ve rods and decreased activity against G+vecocci<br />
  9. 9. First generation<br />
  10. 10. Therapeutic uses<br />Pharyngitis<br />Tonsilitis<br />Otitis<br />Pneumonia<br />UTI <br />Skin infections<br />Bone infections (cefazolin)<br />Surgical prophylaxis (cefazolin is drug of choice ) <br />
  11. 11. Dosage <br />
  12. 12. 2ndgeneration<br />
  13. 13. Therapeutic uses<br />Upper RTI (weaker effect)<br />Pneumonia <br />UTI <br />Skin infections<br />Bone infections<br />Gonorrhea<br />Surgical prophylaxis(cefuroxime 1.5 G 1hour prior )<br />Meningitis (cefuroxime ; but less effective than 3rd generation ) <br />
  14. 14. Dosage <br />
  15. 15. 3rd generation<br />
  16. 16. Therapeutic uses<br />Gonorrhea(single dose of ceftriaxone;1stline drug)<br />Meningitis ( good penetration in CSF)<br />Sepsis<br />Typhoid (4G ceftriaxone/day for 2 days,then 2G/day for 2 days)<br />Surgical prophylaxis <br />UTI<br />Intra-abdominal infections<br />
  17. 17. Dosage <br />
  18. 18. 4thgeneration<br />
  19. 19. Therapeutic uses<br />Upper RTI (weaker effect)<br />Pneumonia<br />UTI<br /> Skin infections<br />Intra abdominal infections <br />Febrile neutropenia<br />
  20. 20. Dosage <br />
  21. 21. 5th Generation<br />CeftarolineFosamil<br />
  22. 22. Ceftarolinefosamil<br />On 29thoctober 2010 ceftaroline was approved by FDA(U.S food and drug administration )<br />It was added as 5th generation cephalosporin<br />In phase III clinical trials it shown non inferior efficacy with same adverse effects to ceftriaxone.<br />
  23. 23. Mechanism of action<br />Same mechanism of action as for other generations<br />While it can bind to and inhibit PBP-2A( PBP produced by MRSA) which is not inhibited by others.<br />
  24. 24. Therapeutic uses<br />Infections caused by MRSA<br />CAP<br />Skin infections <br />
  25. 25. Pharmacokinectis and adverse effects<br />Same as of other generations <br />
  26. 26. THANKS<br />

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