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CEPHALOSPORINS
Dr. Lokendra Sharma
Sr Professor Pharmacology
S.M.S.Medical College,
Jaipur
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
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
What is the mechanism of action of
Cephalosporin ?
Write Generation Classification of Cephalosporin.
Write spectrum of different generations cephalosporin.
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
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.
Pharmacokinetic properties of cephalosporin
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
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.
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
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
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
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
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
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).
ADRs of Cephalosporin
Hypersensitivity
Cephalosporins
Adverse effects of cephalosporin
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
Cephalosporins
Write indications of cephalosporin's.
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)
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.
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.
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
Cephalosporins
An ideal antibiotics
• Broad-spectrum
• Did not induce resistance
• Selective toxicity, low side effects
• Preserve normal microbial flora
For lecture only
Q. 1 Which cephalosporins are secreted in the bile?
Ceftriaxone and Cefoperazone
Q. 2 Which Cephalosporin is used as a DOC in surgical prophylaxis?
Cefazoline
Q. 3 ADRs of ceftriaxone, when used chronically.
Biliary sludging syndrome, cholelithiasis
Q. 4 Which Cephalosporins are active against pseudomonas?
Ceftazidime (Max.), ceftolozane and cefoperazone
Q. 5 Treatment of choice for pseudomonas infection.
Ceftazidime and aminoglycosides
Q. 6 DOC for melioidiosis.
Ceftazidime
Q.7 ADRs of cephalosporins.
Hypersensitivity reactions, Neutropenia with ceftazidime
Q. 8 Ceftriaxone is first choice drug for-
Gonorrhoea, Salmonellosis, E. coli sepsis, Proteus, Haemophilus, Bacterial Meningitis
THANK YOU

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Cephalosporins

  • 1. CEPHALOSPORINS Dr. Lokendra Sharma Sr Professor Pharmacology S.M.S.Medical College, Jaipur
  • 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. 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. What is the mechanism of action of Cephalosporin ?
  • 6. Write spectrum of different generations cephalosporin.
  • 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. 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.
  • 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. 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. 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. 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. 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. 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. 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. 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).
  • 20. Adverse effects of cephalosporin
  • 21. 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
  • 23. Write indications of cephalosporin's.
  • 24. 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)
  • 25. 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.
  • 26. 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.
  • 27. 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
  • 29. An ideal antibiotics • Broad-spectrum • Did not induce resistance • Selective toxicity, low side effects • Preserve normal microbial flora For lecture only
  • 30. Q. 1 Which cephalosporins are secreted in the bile? Ceftriaxone and Cefoperazone
  • 31. Q. 2 Which Cephalosporin is used as a DOC in surgical prophylaxis? Cefazoline
  • 32. Q. 3 ADRs of ceftriaxone, when used chronically. Biliary sludging syndrome, cholelithiasis
  • 33. Q. 4 Which Cephalosporins are active against pseudomonas? Ceftazidime (Max.), ceftolozane and cefoperazone
  • 34. Q. 5 Treatment of choice for pseudomonas infection. Ceftazidime and aminoglycosides
  • 35. Q. 6 DOC for melioidiosis. Ceftazidime
  • 36. Q.7 ADRs of cephalosporins. Hypersensitivity reactions, Neutropenia with ceftazidime
  • 37. Q. 8 Ceftriaxone is first choice drug for- Gonorrhoea, Salmonellosis, E. coli sepsis, Proteus, Haemophilus, Bacterial Meningitis

Editor's Notes

  1. Active against Gram negative organisms (Escherichia co1i Kiebsiella pneumoniae, and the indole negative Proteus mirabilis). Effective against some anaerobic cocci (Peptococcus and Peptosteptococcus, but NOT Bacteroides fragilis).
  2. The spectrum is extended to more Gram negative bacteria Enterobacter species, Klebsiella species, and indole-positive Proteus species. Also, Haemophilus influenza is covered by cefuroxime, cefamandole, cefaclor; Bacteroides fragilis by cefoxitin