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
Ciloxan Pharmacology, Pharmacokinetics, Studies, Metabolism - Ciprofloxacin HCl (ophthalmic)
Ciloxan Pharmacology, Pharmacokinetics, Studies, Metabolism - Ciprofloxacin HCl (ophthalmic)
CLINICAL PHARMACOLOGY
Systemic Absorption
Absorption studies in humans with the ciprofloxacin ointment have not
been conducted, however, based on studies with ciprofloxacin solution,
0.3%, mean maximal concentrations are expected to be less than 2.5 ng/mL.
Microbiology
Ciprofloxacin has in vitro activity against a wide range of gram-negative
and gram-positive organisms. The bactericidal action of ciprofloxacin
results from interference with the enzyme DNA gyrase which is needed for
the synthesis of bacterial DNA.
Ciprofloxacin has been shown to be active against most strains of the
following microorganisms both in vitro and in clinical infections
(See INDICATIONS section).
Aerobic gram-positive microorganisms:
Staphylococcus aureus (methicillin-susceptible strains)
Staphylococcus epidermidis (methicillin-susceptible strains)
Streptococcus pneumoniae
Streptococcus Viridans Group
Aerobic gram-negative microorganisms:
Haemophilus influenzae
The following in vitro data are available; but their clinical
significance in ophthalmologic infections is unknown.
The safety and effectiveness of ciprofloxacin in treating conjunctivitis
due to these microorganisms have not been established in adequate and
well controlled trials.
The following organisms are considered susceptible when evaluated using
systemic breakpoints. However, a correlation between the in vitro
systemic breakpoint and ophthalmological efficacy has not been established.
Ciprofloxacin exhibits in vitro minimal inhibitory concentrations
(MIC’s) of 1ng/mL or less (systemic susceptible breakpoint) against most
(³90%) strains of the following ocular
pathogens.
Aerobic gram-positive microorganisms:
Bacillus species
Corynebacterium species
Staphylococcus haemolyticus
Staphylococcus hominis
Aerobic gram-negative microorganisms:
Acinetobacter calcoaceticus
Enterobacter aerogenes
Escherichia coil
Haemophilus parainfluenzae
Kiebsielle pneumoniae
Moraxella catarrhalis
Neisseria gonorrhoeae
Proteus mirabilis
Pseudomonas aeruginosa
Serratia marcesens
Most strains of Burkholderia cepacia and some strains of Stenotrophomonas
maltophilia are resistant to ciprofloxacin as are most anaerobic bacteria,
including Bacteroides fragilis and Clostridium difficile.
The minimal bactericidal concentration (MBC) generally does not exceed
the minimal inhibitory concentration (MIC) by more than a factor of 2.
Resistance to ciprofloxacin in vitro usually develops slowly (multiplestep
mutation).
Ciprofloxacin does not cross-react with other antimicrobial agents such
as betalactams or aminoglycosides; therefore, organisms resistant to these
drugs may be susceptible to ciprofloxacin. Organisms resistant to ciprofloxacin
may be susceptible to betalactams or aminogylcosides.
Clinical Studies
In multicenter clinical trials, approximately 75% of the patients with
signs and symptoms of bacterial conjunctivitis and positive conjunctival
cultures were clinically cured and approximately 80% had presumed pathogens
eradicated by the end of treatment (day 7).
ANIMAL PHARMACOLOGY
Ciprofloxacin and related drugs have been shown to cause arthropathy
in immature animals of most species tested following oral administration.
However, a one month topical ocular study using immature Beagle dogs did
not demonstrate any articular lesions.
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