Biomedical Engineering Reference
In-Depth Information
Dosage and Administration
: The recommended dosage regimen
includes two drops into the affected eye every 15 min for the first
6 h followed by two drops every 30 min for the remainder of the
first day. Second-day dosage schedule includes instillation of two
drops every hour. From third to fourteenth day, two drops in the
affected eye every 4 h is recommended. The dosage regimen may
vary depending upon the type of microbial infection affecting the
eye. For example in case of bacterial conjunctivitis, the recom-
mended dosage regimen is one- to two-drop administration into
cul-de-sac every 2 h while awake for 2 days and one or two drops
every 4 h while awake for next 5 days.
Drug Composition
: Each milliliter of Ciloxan
®
consists of active
drug ingredient, ciprofloxacin HCl 3.5 mg equivalent to 3 mg of
base (ciprofloxacin, 0.3 %). Other excipients include sodium acetate,
acetic acid, mannitol (4.6 %), edetate disodium (0.05 %), sodium
hydroxide/hydrochloric acid (pH adjusted to 4.5), and purified
water. Benzalkonium chloride (0.05 %) is used as a preservative.
Pharmacodynamic Profile
: Ciprofloxacin has in vitro activity against
a wide range of gram-negative and gram-positive organisms. The
antibacterial activity results from interference of ciprofloxacin with
enzyme DNA gyrase which is required for bacterial DNA synthesis.
Results demonstrated active performance of Ciloxan
®
against most
strains of the gram-positive and gram-negative bacteria both
in vitro and in clinical infections. Ciprofloxacin is active against
gram-positive bacteria such as
Staphylococcus
(
S
)
aureus
,
S. epider-
midis
,
S. pneumoniae
, viridans group, and gram-negative bacteria
such as
Enterococcus faecalis
,
S. haemolyticus
,
S. hominis
,
S. sapro-
phyticus
, and
S. pyrogenes
. Clinical studies with Ciloxan
®
drops in
patients with corneal ulcers and positive bacterial cultures demon-
strated re-epithelialization in ulcers (92 %). Treatment with
Ciloxan
®
demonstrated eradication of causative pathogens by the
end of treatment regimen.
Pharmacokinetic Profile
: Ciloxan
®
topical drop instillation in each
eye is recommended every 2 h while awake for 2 days followed by
every 4 h for an additional 5 days. Drug concentrations in the
systemic circulation were measured. Cmax for ciprofloxacin was
4.7 ng/mL (approx. 450 times less than simple 250 mg oral
administration). The mean concentration was below 2.5 ng/mL.
Similarly, pharmacokinetic study conducted in equine eyes demon-
strated similar pharmacokinetic profile to those of rabbits and
humans. Post topical application, mean tear concentrations of the
drug remained above the minimum inhibitor concentration
(MIC90) for most pathogenic bacteria in 6 h [
20
].
Adverse Reactions
: Most frequently observed adverse reactions
include local ocular burning or discomfort and development of
