A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Ocuflox Pharmacology, Pharmacokinetics, Studies, Metabolism - Ofloxacin (ophthalmic)
Ocuflox Pharmacology, Pharmacokinetics, Studies, Metabolism - Ofloxacin (ophthalmic)
CLINICAL PHARMACOLOGY
Pharmacokinetics
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 OCUFLOX® 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
OID dosing for 10 ½ 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 pg/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 pg/g.
Corneal tissue concentrations
of 4.4 pg/mL were observed four hours after beginning topical
ocutar application of two drops of OCUFLOX® every 30 minutes.
Ofloxacin was excreted in the urine
primarily unmodified.
Microbiology
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:
Staphylococcus aureus
Staphylococcus epidermidis
Streptococcus pneumoniae
AEROBES, GRAM-NEGATIVE:
Enterobacter cloacae
Haemophilus influenzae
Proteus mirabiis
Pseudomonas aeruginosa
Serratia marcescens *
ANAEROBIC SPECIES:
*Efficacy for this organism
was studied in fewer than 10 infections.
The safety and effectiveness
of OCUFLOX® in treating ophthalmologic infections due to the
following organisms have not been established in adequate and well-controlled
clinical trials. OCUFLOX®
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:
Staphylococcus hominus
Enterococcus faecalis
Staphylococcus simulans
Listeria monocytogenes
Streptococcus pyogenes
Staphylococcus capitilis
AEROBES, GRAM-NEGATIVE:
Acinetobacter calcoaceticus
var. anitratus
Kiebsiella pneumoniae
Acinetobacter calcoaceticus
var. Iwoffii
Moraxella (Branhamella) catarrhalis
Citrobacter diversus
Moraxella lacunata
Citrobacter freundii
Morganella morganli
Enterobacter aerogenes
Neisseria gonorrhoeae
Enterobacter agglomerans
Pseudomonas acidovorans
Escherichia coli
Pseudomonas fluorescens
Haemophilus parainfluenzae
Shigella sonnei
Kiebsiella oxytoca
OTHER:
Clinical Studies
Conjunctivitis: In
a randomized, double-masked, multicenter clinical trial, OCUFLOX®
solution was superior
to its vehicle after
2 days of treatment
in patients with conjunctivitis
and positive conjunctival
cultures. Clinical outcomes for the trial demonstrated a clinical
improvement rate of 86% (54/63) for the ofloxacin treated group
versus 72% (48/67) for the placebo
treated group after 2
days of therapy. Microbiological outcomes for the same clinical
trial demonstrated an eradication
rate for causative pathogens
of 65% (41/63) for the ofloxacin treated group
versus 25% (17/ 67) for the vehicle
treated group after 2
days of therapy. Please note that microbiologic eradication
does not always correlate with clinical outcome in anti-infective
trials.
Corneal Ulcers: In
a randomized, double-masked, multi-center clinical trial of 140
subjects with positive
cultures, OCUFLOX® treated subjects had an overall clinical
success rate (complete
re- epithelialization and no
progression of the
infiltrate for two
consecutive visits) of 82% (61/74) compared to 80% (53/66) for the
fortified antibiotic
group, consisting of 1.5% tobramycin
and 10% cefazolin solutions. The median
time to clinical success
was 11 days for the ofloxacin treated group
and 10 days for the fortified treatment
group.
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