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The ABC of
Moxifloxacin

 Dr. B. K. Iyer
Classification
 Moxifloxacin is a 4th generation fluoroquinolone.
 1st generation
    – Cinoxacin, nalidixic acid, and oxolinic acid
   2nd generation
    – Ciprofloxacin, enoxacin, lomefloxacin, ofloxacin and
      norfloxacin.
   3rd generation
    – Grepafloxacin, levofloxacin, and sparfloxacin
   4th generation
    – Cinafloxacin, gatifloxacin, moxifloxacin &
MOXI
   Each film-coated MOXI tablet
    – contains Moxifloxacin Hydrochloride equivalent to Moxifloxacin
      = 400 mg.
    – is indicated for the treatment of adults with upper and lower
      respiratory tract, skin/skin structure, and intra-abdominal
      infections.
    – safety and tolerability summarized from meta-analysis in over
      4300 patients.
    – exerts its action by inhibiting the bacterial topoisomerases II (DNA
      gyrase) and topoisomerases IV which interferes with bacterial
      DNA replication, transcription, repair, and recombination.
MOXI – Where & how?
Moxi- What?
 Moxifloxacin has a high activity against most
  respiratory pathogens.
 Moxifloxacin has been shown to be effective against
  Gram+ve, Gram-ve, and atypical strains, as well as
  multi-drug resistant Streptococcus pneumoniae.
 Moxifloxacin is effective in controlled studies of
    – community-acquired pneumonia,
    – exacerbations of chronic bronchitis and
    – acute bacterial rhinosinusitis.
                 Expert Opinion on Pharmacotherapy, July 2008, Vol. 9, No. 10 , Pages 1755-1772
MOXI - Why?
   In cases of acute exacerbations of chronic bronchitis
    (AECB) and community-acquired pneumonia (CAP), recent
    guidelines suggest using fluoroquinolone antibiotics as first-
    line therapy. This suggestion is based evidence from several
    trials that show:
    –   Clinical superiority
    –   Microbial superiority.
    –   Shorter hospital stay,
    –   Reduced recurrences, and
    –   Lower costs.
   Fortunately, resistance to these agents is still very low, and
    reserving them for use in populations at risk should preserve
    their effectiveness for some time
MOXI - Against RTI organisms
MOXI - Levels in airway
MOXI - Against Staphylococcus
MOXI - In sinusitis vs. Cefuroxime
MOXI - Benefits

    Moxifloxacin has
    1. A long elimination half-life that permits once-daily
       dosing.
    2. Excellent pharmacokinetic profile characterized by
       respiratory tissue concentrations in upper and lower
       respiratory tissues that significantly exceed serum
       levels,
    3. Excellent pharmacodynamic profile implies that the
       drug can achieve high response rates with shorter
       courses of therapy while minimizing the development
       of resistance.
MOXI - Benefits

    Moxifloxacin has
    1. A postantibiotic effect is observed for both gram-
       positive and gram-negative bacteria.
    1. Balanced system of excretion & so no dosage
       adjustments are required in patients with renal or
       hepatic impairment.
    2. No clinically significant drug interactions due to lack of
       inhibition or stimulation of hepatic metabolism.
MOXI - Outcomes
   In this era of emerging resistance of community-acquired
    respiratory pathogens to cephalosporins and other beta-
    lactams, macrolides, and tetracycline is common.
    – Moxifloxacin has excellent in vitro inhibitory activity against
      antibiotic-resistant S. pneumoniae, beta-lactamase-producing
      Haemophilus sp, and M. catarrhalis, as well as atypical organisms.
    – Emergence of resistance to moxifloxacin is still uncommon,
      including selection of resistance under experimental conditions
      (methicillin-sensitive Staphylococcus aureus, S. pneumoniae).
MOXI - Side effects

 Low photosensitizing potential.
 Negligible sude effects profile
 Common side effects include:
    – Nausea,
    – Vomiting
    – Dizziness
MOXI - Summary of trials
   Moxifloxacin compared to other fluoroquinolone
    antibiotics:
    – significant improvement in the rate of “clinical recovery” (defined
      as the resolution of or reduction in acute signs and symptoms of
      infection) in patients receiving moxifloxacin after 3 to 5 days of
      therapy
   Moxifloxacin compared to other classes of antibiotic drugs

   Moxifloxacin in SSTI
    – Clinical cure/improvement rates at 7–21d after the end of therapy
      were around 90%.
MOXI - Summary of studies

 Moxifloxacin has demonstrated a faster
  resolution of symptoms in community-acquired
  pneumonia and exacerbations of chronic
  bronchitis patients compared with first-line
  therapy together with excellent eradication
  rates.
 The use of moxifloxacin as first-line therapy for
  moderate to severe respiratory infections in the
  community and the hospital has been

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Moxifloxacin

  • 1. The ABC of Moxifloxacin Dr. B. K. Iyer
  • 2. Classification  Moxifloxacin is a 4th generation fluoroquinolone.  1st generation – Cinoxacin, nalidixic acid, and oxolinic acid  2nd generation – Ciprofloxacin, enoxacin, lomefloxacin, ofloxacin and norfloxacin.  3rd generation – Grepafloxacin, levofloxacin, and sparfloxacin  4th generation – Cinafloxacin, gatifloxacin, moxifloxacin &
  • 3. MOXI  Each film-coated MOXI tablet – contains Moxifloxacin Hydrochloride equivalent to Moxifloxacin = 400 mg. – is indicated for the treatment of adults with upper and lower respiratory tract, skin/skin structure, and intra-abdominal infections. – safety and tolerability summarized from meta-analysis in over 4300 patients. – exerts its action by inhibiting the bacterial topoisomerases II (DNA gyrase) and topoisomerases IV which interferes with bacterial DNA replication, transcription, repair, and recombination.
  • 4. MOXI – Where & how?
  • 5. Moxi- What?  Moxifloxacin has a high activity against most respiratory pathogens.  Moxifloxacin has been shown to be effective against Gram+ve, Gram-ve, and atypical strains, as well as multi-drug resistant Streptococcus pneumoniae.  Moxifloxacin is effective in controlled studies of – community-acquired pneumonia, – exacerbations of chronic bronchitis and – acute bacterial rhinosinusitis. Expert Opinion on Pharmacotherapy, July 2008, Vol. 9, No. 10 , Pages 1755-1772
  • 6. MOXI - Why?  In cases of acute exacerbations of chronic bronchitis (AECB) and community-acquired pneumonia (CAP), recent guidelines suggest using fluoroquinolone antibiotics as first- line therapy. This suggestion is based evidence from several trials that show: – Clinical superiority – Microbial superiority. – Shorter hospital stay, – Reduced recurrences, and – Lower costs.  Fortunately, resistance to these agents is still very low, and reserving them for use in populations at risk should preserve their effectiveness for some time
  • 7. MOXI - Against RTI organisms
  • 8. MOXI - Levels in airway
  • 9. MOXI - Against Staphylococcus
  • 10. MOXI - In sinusitis vs. Cefuroxime
  • 11. MOXI - Benefits  Moxifloxacin has 1. A long elimination half-life that permits once-daily dosing. 2. Excellent pharmacokinetic profile characterized by respiratory tissue concentrations in upper and lower respiratory tissues that significantly exceed serum levels, 3. Excellent pharmacodynamic profile implies that the drug can achieve high response rates with shorter courses of therapy while minimizing the development of resistance.
  • 12. MOXI - Benefits  Moxifloxacin has 1. A postantibiotic effect is observed for both gram- positive and gram-negative bacteria. 1. Balanced system of excretion & so no dosage adjustments are required in patients with renal or hepatic impairment. 2. No clinically significant drug interactions due to lack of inhibition or stimulation of hepatic metabolism.
  • 13. MOXI - Outcomes  In this era of emerging resistance of community-acquired respiratory pathogens to cephalosporins and other beta- lactams, macrolides, and tetracycline is common. – Moxifloxacin has excellent in vitro inhibitory activity against antibiotic-resistant S. pneumoniae, beta-lactamase-producing Haemophilus sp, and M. catarrhalis, as well as atypical organisms. – Emergence of resistance to moxifloxacin is still uncommon, including selection of resistance under experimental conditions (methicillin-sensitive Staphylococcus aureus, S. pneumoniae).
  • 14. MOXI - Side effects  Low photosensitizing potential.  Negligible sude effects profile  Common side effects include: – Nausea, – Vomiting – Dizziness
  • 15. MOXI - Summary of trials  Moxifloxacin compared to other fluoroquinolone antibiotics: – significant improvement in the rate of “clinical recovery” (defined as the resolution of or reduction in acute signs and symptoms of infection) in patients receiving moxifloxacin after 3 to 5 days of therapy  Moxifloxacin compared to other classes of antibiotic drugs  Moxifloxacin in SSTI – Clinical cure/improvement rates at 7–21d after the end of therapy were around 90%.
  • 16. MOXI - Summary of studies  Moxifloxacin has demonstrated a faster resolution of symptoms in community-acquired pneumonia and exacerbations of chronic bronchitis patients compared with first-line therapy together with excellent eradication rates.  The use of moxifloxacin as first-line therapy for moderate to severe respiratory infections in the community and the hospital has been