Moxifloxacin

Moxifloxacin is a synthetic fluoroquinolone antibiotic agent. Bayer AG developed the drug and sells it worldwide (as the hydrochloride) under the brandname Avelox® (in some countries also Avalox®) for oral treatment. Each tablet contains 400mg. In most countries the drug is also available in parenteral form for i.v. infusion of 400mg. Currently, the drug is very popular. more...

Its chemically referred to as (4aS-cis)-1-Cyclopropyl-6-flouro-1,4dihydro-8-methoxy-7-(octahydro-6H-pyrrololpyrindin-6yl-)-4-oxo-quinolinecarboxylic acid monohydrochloride. The molecular formular is C21H24FN3O4.

Mode of Action

Like other fluoroquinolones, moxifloxacin inhibits the bacterial enzyme DNA gyrase (topoisomerase IV) and thus prevents supercoiling of bacterial DNA. This mechanism is lethal to susceptible bacteria. Moxifloxacin is often referred to as chemotherapeutic drug because its mode of action has so far not been noted in any natural occurring or semisynthetic antibiotic.

Distribution

Moxifloxacin is found in high concentrations in body tissues and fluids, such as salvia, nasal and bronchial secrets, sinus mucosa, skin blister fluid, subcutaneous and muscle tissues. Pus does not seem to inhibit the drug's potential to reach effective concentrations in infectious foci easily.

Susceptible Bacteria

A broad spectrum of bacteria is susceptible including, but not limited to, Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus, Klebsiella, Moraxella, Enterobacter, Mycobacteria and Anthrax.

Pharmacodynamic Data including Metabolization/Excretion

• Bioavailability : 86 to 92%, not influenced by meals
• Peak Plasma Level : 0.5 to 4 hours after oral dosing
• Time needed to reach steady-state : at least 3 days
• Half-life in normal individuals : approximately 12 hours, making once-a-day administration feasible
• Fiftytwo (52) percent of the drug is metabolized via glucoronide and sulfate conjugates, which are pharmacological inactive. Enzymes of the CYP-class are not involved.
• The drug and the conjugates are excreted as well in urine and biliar/in feces.

Pharmacokinetic Behaviour in Patients with decreased liver and renal function

Mild, moderate and severe renal function does not alter half-life, metabolization or excretion significantly. The same is true to for mild to moderate liver impairment (Child-Pugh class A and B). Nothing is known about severe liver impairment (Child-Pugh class C).

Uses

• Respiratory infections including acute sinusitis, acute exacerbations of chronic bronchitis and community-acquired pneumonia
• Skin and skin structure infections

Investigational and Off-Label Uses

• Acute mycobacterial infections including tuberculosis as part of a multidrug treatment regime
• The US Working Group on Civilian Biodefense has proposed that moxifloxacin should be used for the postexposure prophylaxis and treatment of Anthrax.

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