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