WARNING:
Fluoroquinolones, including AVELOX,® are associated with an increased risk of tendinitis and tendon rupture in all ages. This risk is further increased in older patients usually over 60 years of age, in patients taking corticosteroid drugs, and in patients with kidney, heart or lung transplants (see WARNINGS).
To reduce the development of drug-resistant bacteria and maintain the effectiveness of AVELOX and other antibacterial drugs, AVELOX should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
DESCRIPTION
AVELOX (moxifloxacin hydrochloride) is a synthetic broad spectrum antibacterial agent and is available as AVELOX Tablets for oral administration and as AVELOX I.V. for intravenous administration. Moxifloxacin, a fluoroquinolone, is available as the monohydrochloride salt of 1-cyclopropyl-7-[(S,S)-2,8-diazabicyclo[4.3.0]non-8-yl]-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3 quinoline carboxylic acid. It is a slightly yellow to yellow crystalline substance with a molecular weight of 437.9. Its empirical formula is C21H24FN3O4*HCl and its chemical structure is as follows:
AVELOX Tablets are available as film-coated tablets containing moxifloxacin hydrochloride (equivalent to 400 mg moxifloxacin). The inactive ingredients are microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, hypromellose, titanium dioxide, polyethylene glycol and ferric oxide.
AVELOX I.V. is available in ready-to-use 250 mL latex-free flexibags as a sterile, preservative free, 0.8% sodium chloride aqueous solution of moxifloxacin hydrochloride (containing 400 mg moxifloxacin) with pH ranging from 4.1 to 4.6. The appearance of the intravenous solution is yellow. The color does not affect, nor is it indicative of, product stability. The inactive ingredients are sodium chloride, USP, Water for Injection, USP, and may include hydrochloric acid and/or sodium hydroxide for pH adjustment. AVELOX I.V. contains approximately 34.2 mEq (787 mg) of sodium in 250 mL.
CLINICAL PHARMACOLOGY
Absorption
Moxifloxacin, given as an oral tablet, is well absorbed from the gastrointestinal tract. The absolute bioavailability of moxifloxacin is approximately 90 percent. Co-administration with a high fat meal (i.e., 500 calories from fat) does not affect the absorption of moxifloxacin.
Consumption of 1 cup of yogurt with moxifloxacin does not significantly affect the extent or rate of systemic absorption (AUC).
The mean (± SD) Cmax and AUC values following single and multiple doses of 400 mg moxifloxacin given orally are summarized below.
|
|
Cmax
(mg/L) |
AUC
(mg•h/L) |
Half-life
(hr) |
Single Dose Oral
Healthy (n = 372) |
3.1 ± 1 |
36.1 ± 9.1 |
11.5 - 15.6* |
|
Multiple Dose Oral |
|
|
|
|
Healthy young male/female (n = 15) |
4.5 ± 0.5 |
48 ± 2.7 |
12.7 ± 1.9 |
|
Healthy elderly male (n = 8) |
3.8 ± 0.3 |
51.8 ± 6.7 |
|
|
Healthy elderly female (n = 8) |
4.6 ± 0.6 |
54.6 ± 6.7 |
|
|
Healthy young male (n = 8) |
3.6 ± 0.5 |
48.2 ± 9 |
|
|
Healthy young female (n = 9) |
4.2 ± 0.5 |
49.3 ± 9.5 |
|
* Range of means from different studies
The mean (± SD) Cmax and AUC values following single and multiple doses of 400 mg moxifloxacin given by 1 hour I.V. infusion are summarized below.
|
|
Cmax
(mg/L) |
AUC
(mg•h/L) |
Half-life
(hr) |
|
Singe Dose I.V. |
|
|
|
|
Healthy young male/female (n = 56) |
3.9 ± 0.9 |
39.3 ± 8.6 |
8.2 - 15.4* |
|
Patients (n = 118) |
|
|
|
|
Male (n = 64) |
4.4 ± 3.7 |
|
|
|
Female (n = 54) |
4.5 ± 2 |
|
|
|
less than 65 years (n = 58) |
4.6 ± 4.2 |
|
|
|
greater than or equal to 65 years ( n = 60) |
4.3 ± 1.3 |
|
|
|
Multiple Dose I.V. |
|
|
|
|
Healthy young male (n = 8) |
4.2 ± 0.8 |
38 ± 4.7 |
14.8 ± 2.2 |
|
Healthy elderly (n = 12; 8 male, 4 female) |
6.1 ± 1.3 |
48.2 ± 0.9 |
10.1 ± 1.6 |
|
Patients† (n = 107) |
|
|
|
|
Male (n = 58) |
4.2 &plu |
