OFLOXACIN- ofloxacin solution
Pack Pharmaceuticals, LLC
Chemical Name: (±)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H pyrido [1,2,3-de]-1,4 benzoxazine-6-carboxylic acid.
Contains: Active: ofloxacin 0.3% (3 mg/mL)
Preservative: benzalkonium chloride (0.005%)
Inactives: sodium chloride and water for injection. May also contain hydrochloric acid and/or sodium hydroxide to adjust pH.
Ofloxacin ophthalmic solution is unbuffered and formulated with a pH of 6.4 (range 6.0 to 6.8). It has an osmolality of 300 mOsm/kg. Ofloxacin is a fluorinated 4-quinolone which differs from other fluorinated 4-quinolones in that there is a six member (pyridobenzoxazine) ring from positions 1 to 8 of the basic ring structure.
Serum, urine and tear concentrations of ofloxacin were measured in 30 healthy women at various time points during a ten-day course of treatment with ofloxacin ophthalmic solution. The mean serum ofloxacin concentration ranged from 0.4 ng/mL to 1.9 ng/mL. Maximum ofloxacin concentration increased from 1.1 ng/mL on day one to 1.9 ng/mL on day 11 after QID dosing for 10 1/2 days. Maximum serum ofloxacin concentrations after ten days of topical ophthalmic dosing were more than 1000 times lower than those reported after standard oral doses of ofloxacin.
Tear ofloxacin concentrations ranged from 5.7 to 31 mcg/g during the 40 minute period following the last dose on day 11. Mean tear concentration measured four hours after topical ophthalmic dosing was 9.2 mcg/g.
Corneal tissue concentrations of 4.4 mcg/mL were observed four hours after beginning topical ocular application of two drops of ofloxacin ophthalmic solution every 30 minutes. Ofloxacin was excreted in the urine primarily unmodified.
Ofloxacin has in vitro activity against a broad range of gram-positive and gram-negative aerobic and anaerobic bacteria. Ofloxacin is bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Ofloxacin is thought to exert a bactericidal effect on susceptible bacterial cells by inhibiting DNA gyrase, an essential bacterial enzyme which is a critical catalyst in the duplication, transcription, and repair of bacterial DNA.
Cross-resistance has been observed between ofloxacin and other fluoroquinolones. There is generally no cross-resistance between ofloxacin and other classes of antibacterial agents such as beta-lactams or aminoglycosides.
Ofloxacin has been shown to be active against most strains of the following organisms both in vitro and clinically, in conjunctival and/or corneal ulcer infections as described in the INDICATIONS AND USAGE section.
|AEROBES , GRAM - POSITIVE :||AEROBES , GRAM - NEGATIVE :|
|Staphylococcus aureus||Enterobacter cloacae|
|Staphylococcus epidermidis||Haemophilus influenza|
|Streptococcus pneumoniae||Proteus mirabilis|
|ANAEROBIC SPECIES :||Pseudomonas aeruginosa|
|Propionibacterium acnes||Serratia marcescens *|
The safety and effectiveness of ofloxacin ophthalmic solution in treating ophthalmologic infections due to the following organisms have not been established in adequate and well-controlled clinical trials. Ofloxacin ophthalmic solution has been shown to be active in vitro against most strains of these organisms but the clinical significance in ophthalmologic infections is unknown.
|AEROBES , GRAM - POSITIVE :|
|Enterococcus faecalis||Staphylococcus hominus|
|Listeria monocytogenes||Staphylococcus simulans|
|Staphylococcus capitis||Streptococcus pyogenes|
|AEROBES , GRAM - NEGATIVE :|
|Acinetobacter calcoaceticus var . anitratus||Klebsiella pneumoniae|
|Acinetobacter calcoaceticus var . lwoffii||Moraxella ( Branhamella ) catarrhalis|
|Citrobacter diversus||Moraxella lacunata|
|Citrobacter freundii||Morganella morganii|
|Enterobacter aerogenes||Neisseria gonorrhoeae|
|Enterobacter agglomerans||Pseudomonas acidovorans|
|Escherichia coli||Pseudomonas fluorescens|
|Haemophilus parainfluenzae||Shigella sonnei|
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