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Avelox

Clinical Pharmacology
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Clinical Pharmacology

Avelox

Mean Steady-State Plasma Concentrations of Moxifloxacin Obtained With Once Daily Dosing of 400 mg Either Orally (n=10) or by I.V. Infusion (n=12)


Distribution

Moxifloxacin is approximately 30-50% bound to serum proteins, independent of drug concentration. The volume of distribution of moxifloxacin ranges from 1.7 to 2.7 L/kg. Moxifloxacin is widely distributed throughout the body, with tissue concentrations often exceeding plasma concentrations. Moxifloxacin has been detected in the saliva, nasal and bronchial secretions, mucosa of the sinuses, skin blister fluid, subcutaneous tissue, skeletal muscle, and abdominal tissues and fluids following oral or intravenous administration of 400 mg. Moxifloxacin concentrations measured post-dose in various tissues and fluids following a 400 mg oral or I.V. dose are summarized in the following table. The rates of elimination of moxifloxacin from tissues generally parallel the elimination from plasma.

Moxifloxacin Concentrations (mean ± SD) in Tissues and the Corresponding Plasma Concentrations After a Single 400 mg Oral or Intravenous Dose §


Tissue or Fluid N Plasma Concentration (µg/mL) Tissue or Fluid Concentration (µg/mL or µg/g) Tissue Plasma Ratio:
Respiratory        
Alveolar Macrophages 5 3.3 ± 0.7 61.8± 27.3 21.2 ± 10.0
Bronchial Mucosa 8 3.3 ± 0.7 5.5± 1.3 1.7 ± 0.3
Epithelial Lining Fluid 5 3.3 ± 0.7 24.4± 14.7 8.7 ± 6.1
Sinus        
Maxillary Sinus Mucosa 4 3.7 ± 1.1† 7.6± 1.7 2.0 ± 0.3
Anterior Ethmoid Mucosa 3 3.7 ± 1.1† 8.8± 4.3 2.2 ± 0.6
Nasal Polyps 4 3.7 ± 1.1† 9.8± 4.5 2.6 ± 0.6
Skin, Musculoskeletal        
Blister Fluid 5 3.0± 0.5‡ 2.6± 0.9 0.9 ± 0.2
Subcutaneous Tissue 6 2.3± 0.4# 0.9± 0.3* 0.4 ± 0.6
Skeletal Muscle 6 2.3± 0.4# 0.9± 0.2* 0.4 ± 0.1
Intra-Abdominal        
Abdominal tissue 8 2.9± 0.5 7.6 ± 2.0 2.7 ± 0.8
Abdominal exudate 10 2.3 ± 0.5 3.5 ±1.2 1.6 ± 0.7
Abscess fluid 6 2.7± 0.7 2.3 ±1.5 0.8±0.4
§all moxifloxacin concentrations were measured 3 hours after a single 400 mg dose, except the abdominal tissue and exudate concentrations which were measured at 2 hours post-dose and the sinus concentrations which were measured 3 hours post-dose after 5 days of dosing.
† N = 5
‡ N = 7 D
#N = 12
* Reflects only non-protein bound concentrations of drug.

Metabolism>

Brand Name: Avelox
Generic Name: Moxifloxacin HCL
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