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Antibacterial; β-lactam antibiotic; third
generation cephalosporin.
Third Generation Cephalosporins.
 In the early 1980's parenteral third generation
cephalosporins changed the hospital use of antibiotics.
 The MICs of these cephalosporins are several dozen
times lower than those of first or second generation
cephalosporins for Enterobacteriaceae and they are
much more beta-lactamase stable than second
generation cephalosporins.
 After years of research, is has finally been possible to
develop orally active compounds possessing the same
antibacterial activity as parenteral third generation
cephalosporins, either through the use of prodrugs, or by
modifying the molecular structure of drugs.
 Cefixime is an example of the latter. The vinyl group at
the 3-position of the cephem nucleus is responsible for
the intestinal absorption of the intact molecule, primarily
by a carrier-mediated transport mechanism.
 Thousands of adults have been treated by cefixime for
lower respiratory tract, ear-nose-throat and urinary tract
infections, showing that cefixime is a safe and effective
antimicrobial agent.
 The major clinical indications for cefixime in adults are
bronchial and pulmonary infections, acute otitis or
sinusitis, acute pyelonephritis with no underlying
uropathy, and complicated or uncomplicated lower
urinary tract infections excluding prostatitis. In all cases,
the dosage is 200 mg b.i.d.
 The advances achieved in the field of oral
cephalosporins consist of improved bioavailability
and enhanced intrinsic activity of the compounds.
 Oral absorption is facilitated either by creating
prodrugs or by modifying the compound itself with
addition of the alpha-amino group at position 7 on
the cephem ring or of a vinyl group at position 3.
 Antibacterial activity and resistance to beta-
lactamases are facilitated by the presence of an
amino-2-thiazole heterocycle at position 7,
associated with a methoxy-imino group or an oxy-
imino-acetoxy group
Cefixime
 Cefixime is quickly establishing in Western countries
as a potent broad-spectrum antibiotic with a variety
of indications.
 A multinational, nonrandomized study in Central and
Eastern Europe has confirmed the excellent efficacy of
cefixime in both children and adults.
 In 45 children with acute sinusitis and 50 with acute
otitis media, once-daily cefixime in oral suspension
resulted in clinical cure or improvement in 45 (100%)
and 48 (96%) patients, respectively.
 In 60 adult patients with acute exacerbations of
chronic bronchitis and 12 with pneumonia, cefixime
400 mg resulted in cure or improvement in 59 (98%)
and 12 (100%) patients, respectively.
 Similarly, excellent efficacy was found in adults with
urinary tract infections (UTI), with cure in 80 (94%)
patients
The aim of this study was to evaluate the efficacy of
cefixime in the treatment of community-acquired
infections in a country where parenteral third
generation cephalosporins have been used for a long
time.
The present study was designed to assess the clinical
efficacy, bacteriological eradication rates and
tolerability of cefixime in children with community-
acquired upper RTI (URTI), lower RTI (LRTI) and
uncomplicated urinary tract infections (UTI).
The study was prospective, open, and included 89
patients, from 6 months to 28 years, of both
sexes, with the diagnosis of community-acquired
URTI, LRTI and UTI.
 Data are reviewed for safety from worldwide clinical
trials of 4000 patients and postmarketing studies of
38,000 patients treated with cefixime, a broad-
spectrum, bactericidal, beta-lactam stable, third-
generation cephalosporin.
 Adverse experiences were similar in adults
and children in all groups, with the most
frequent side effects being gastrointestinal in
nature.
 Based on spectrum of activity, classified as a third
generation cephalosporin. Expanded spectrum of
activity against gram-negative bacteria compared with
first and second generation cephalosporins; less
active against Enterobacteriaceae than some other
third-generation cephalosporins.
 Usually bactericidal.
 Like other β-lactam antibiotics, antibacterial activity
results from inhibition of bacterial cell wall synthesis.
 Gram-positive aerobes: Active in vitro and in clinical
infections against Streptococcus pneumoniae1 and
Streptococcus pyogenes (group A β-hemolytic
streptococci). Also active in vitro against S. agalactiae
(group B streptococci) and groups C, F, and G
streptococci.
 Most staphylococci, enterococci, and Listeria
monocytogenes are resistant.
 Strains of staphylococci resistant to penicillinase-
resistant penicillins (oxacillin-resistant [methicillin-
resistant] staphylococci) should be considered
resistant to cefixime, although results of in vitro
susceptibility tests may indicate susceptibility.
 Gram-negative aerobes: Active in vitro and in clinical
infections against Neisseria gonorrhoeae,
Haemophilus influenzae (including β-lactamase-
producing strains), Moraxella catarrhalis (including β-
lactamase-producing strains), Escherichia coli, and
Proteus mirabilis.
 Also active in vitro against H. parainfluenzae,
Klebsiella, Pasteurella multocida, P. vulgaris,
Providencia, Salmonella, Shigella, and Serratia.
Most Enterobacter and Pseudomonas are
resistant.
 Community-acquired infections, such as
AOM, LRTI and UTI, caused by susceptible
pathogens, can be treated with cefixime, as a
good choice for a successful clinical
response.
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Speaker Presentation.ppt

  • 1.
  • 2. Antibacterial; β-lactam antibiotic; third generation cephalosporin. Third Generation Cephalosporins.
  • 3.  In the early 1980's parenteral third generation cephalosporins changed the hospital use of antibiotics.  The MICs of these cephalosporins are several dozen times lower than those of first or second generation cephalosporins for Enterobacteriaceae and they are much more beta-lactamase stable than second generation cephalosporins.
  • 4.  After years of research, is has finally been possible to develop orally active compounds possessing the same antibacterial activity as parenteral third generation cephalosporins, either through the use of prodrugs, or by modifying the molecular structure of drugs.  Cefixime is an example of the latter. The vinyl group at the 3-position of the cephem nucleus is responsible for the intestinal absorption of the intact molecule, primarily by a carrier-mediated transport mechanism.
  • 5.  Thousands of adults have been treated by cefixime for lower respiratory tract, ear-nose-throat and urinary tract infections, showing that cefixime is a safe and effective antimicrobial agent.  The major clinical indications for cefixime in adults are bronchial and pulmonary infections, acute otitis or sinusitis, acute pyelonephritis with no underlying uropathy, and complicated or uncomplicated lower urinary tract infections excluding prostatitis. In all cases, the dosage is 200 mg b.i.d.
  • 6.  The advances achieved in the field of oral cephalosporins consist of improved bioavailability and enhanced intrinsic activity of the compounds.  Oral absorption is facilitated either by creating prodrugs or by modifying the compound itself with addition of the alpha-amino group at position 7 on the cephem ring or of a vinyl group at position 3.
  • 7.  Antibacterial activity and resistance to beta- lactamases are facilitated by the presence of an amino-2-thiazole heterocycle at position 7, associated with a methoxy-imino group or an oxy- imino-acetoxy group
  • 9.  Cefixime is quickly establishing in Western countries as a potent broad-spectrum antibiotic with a variety of indications.  A multinational, nonrandomized study in Central and Eastern Europe has confirmed the excellent efficacy of cefixime in both children and adults.
  • 10.  In 45 children with acute sinusitis and 50 with acute otitis media, once-daily cefixime in oral suspension resulted in clinical cure or improvement in 45 (100%) and 48 (96%) patients, respectively.  In 60 adult patients with acute exacerbations of chronic bronchitis and 12 with pneumonia, cefixime 400 mg resulted in cure or improvement in 59 (98%) and 12 (100%) patients, respectively.  Similarly, excellent efficacy was found in adults with urinary tract infections (UTI), with cure in 80 (94%) patients
  • 11. The aim of this study was to evaluate the efficacy of cefixime in the treatment of community-acquired infections in a country where parenteral third generation cephalosporins have been used for a long time. The present study was designed to assess the clinical efficacy, bacteriological eradication rates and tolerability of cefixime in children with community- acquired upper RTI (URTI), lower RTI (LRTI) and uncomplicated urinary tract infections (UTI).
  • 12. The study was prospective, open, and included 89 patients, from 6 months to 28 years, of both sexes, with the diagnosis of community-acquired URTI, LRTI and UTI.
  • 13.  Data are reviewed for safety from worldwide clinical trials of 4000 patients and postmarketing studies of 38,000 patients treated with cefixime, a broad- spectrum, bactericidal, beta-lactam stable, third- generation cephalosporin.
  • 14.  Adverse experiences were similar in adults and children in all groups, with the most frequent side effects being gastrointestinal in nature.
  • 15.  Based on spectrum of activity, classified as a third generation cephalosporin. Expanded spectrum of activity against gram-negative bacteria compared with first and second generation cephalosporins; less active against Enterobacteriaceae than some other third-generation cephalosporins.  Usually bactericidal.
  • 16.  Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.
  • 17.  Gram-positive aerobes: Active in vitro and in clinical infections against Streptococcus pneumoniae1 and Streptococcus pyogenes (group A β-hemolytic streptococci). Also active in vitro against S. agalactiae (group B streptococci) and groups C, F, and G streptococci.  Most staphylococci, enterococci, and Listeria monocytogenes are resistant.
  • 18.  Strains of staphylococci resistant to penicillinase- resistant penicillins (oxacillin-resistant [methicillin- resistant] staphylococci) should be considered resistant to cefixime, although results of in vitro susceptibility tests may indicate susceptibility.
  • 19.  Gram-negative aerobes: Active in vitro and in clinical infections against Neisseria gonorrhoeae, Haemophilus influenzae (including β-lactamase- producing strains), Moraxella catarrhalis (including β- lactamase-producing strains), Escherichia coli, and Proteus mirabilis.  Also active in vitro against H. parainfluenzae, Klebsiella, Pasteurella multocida, P. vulgaris, Providencia, Salmonella, Shigella, and Serratia. Most Enterobacter and Pseudomonas are resistant.
  • 20.  Community-acquired infections, such as AOM, LRTI and UTI, caused by susceptible pathogens, can be treated with cefixime, as a good choice for a successful clinical response.