Besifloxacin is a fluoroquinolone ophthalmic suspension indicated for the treatment of bacterial conjunctivitis in adult and pediatric patients 1 year of age and older. Avoid the use of contact lenses during treatment. Adverse effects are generally limited to ophthalmic-related events and headache. Prolonged use may result in overgrowth of nonsusceptible organisms.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-For topical ophthalmic administration only.
-Wash hand prior to use.
-Remove contact lenses prior to use.
-Prior to administration, invert the closed bottle and shake once.
-Remove the cap while the bottle is in the inverted position and administer one drop into the affected eye(s).
-Avoid contaminating the applicator tip with material from the eye, fingers, or other source.
-Use one bottle per patient; do not share ophthalmic drops.
Conjunctival redness (conjunctival hyperemia) was reported in approximately 2% of patients in besifloxacin clinical trials. Blurred vision, ocular pain, ocular irritation, and ocular pruritus occurred in 1% to 2% of patients.
Headache occurred in 1% to 2% of patients in besifloxacin clinical trials.
Overgrowth of non-susceptible organisms may occur with the prolonged use of besifloxacin which may result in superinfection. If this occurs, discontinue use and institute alternative therapy.
Besifloxacin is for topical ophthalmic use only and should not be injected into the eye.
Patients should not wear contact lenses during the treatment of bacterial conjunctivitis or during the course of therapy with besifloxacin.
There are no available human data for the use of besifloxacin during pregnancy to inform any drug-associated risks; however, the systemic exposure to besifloxacin is low. In animal studies, the No Observed Adverse Effect Level (NOAEL) for embryo-fetal development was 100 mg/kg/day (Cmax 5 mcg/mL or greater than 11,000-times the mean serum concentration measured in humans).
There are no data on the presence of besifloxacin in human milk, the effects on the breastfed infant, or the effects on milk production. It is not known whether measurable concentrations of besifloxacin would be present in maternal milk after topical ocular administration; however, systemic exposure after ocular administration is low. The low maternal serum concentrations (less than 1.3 ng/mL) suggest exposure to a nursing infant would likely be clinically insignificant. The developmental and health benefits of breast-feeding should be considered, along with the mother's clinical need for besifloxacin, and any potential adverse effects on the breastfed infant.
Per the manufacturer, this drug has been shown to be active against most strains of the following microorganisms either in vitro and/or in clinical infections: Aerococcus viridans, CDC coryneform group G, Corynebacterium pseudodiphtheriticum, Corynebacterium striatum, Haemophilus influenzae (beta-lactamase negative), Haemophilus influenzae (beta-lactamase positive), Moraxella catarrhalis, Moraxella lacunata, Pseudomonas aeruginosa, Staphylococcus aureus (MSSA), Staphylococcus epidermidis, Staphylococcus hominis, Staphylococcus lugdunesis, Staphylococcus warneri, Streptococcus mitis, Streptococcus oralis, Streptococcus pneumoniae, Streptococcus salivarius
NOTE: The safety and effectiveness in treating clinical infections due to organisms with in vitro data only have not been established in adequate and well-controlled clinical trials.
For the treatment of bacterial conjunctivitis due to susceptible organisms:
Ophthalmic dosage:
Adults: Instill 1 drop in the affected eye(s) 3 times daily, 4 to 12 hours apart, for 7 days.
Children and Adolescents: Instill 1 drop in the affected eye(s) 3 times daily, 4 to 12 hours apart, for 7 days.
Maximum Dosage Limits:
-Adults
3 drops/eye/day.
-Geriatric
3 drops/eye/day.
-Adolescents
3 drops/eye/day.
-Children
3 drops/eye/day.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustment in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustment in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Besifloxacin products.
Besifloxacin is an 8-chloro fluoroquinolone with an N-1 cyclopropyl group that has activity against Gram-positive and Gram-negative bacteria due to the inhibition of both bacterial DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme required for replication, transcription and repair of bacterial DNA. Topoisomerase IV is an essential enzyme required for partitioning of the chromosomal DNA during bacterial cell division. Besifloxacin is bactericidal with minimum bactericidal concentrations (MBCs) generally within one dilution of the minimum inhibitory concentrations (MICs). In vitro data have demonstrated cross-resistance between besifloxacin and other fluoroquinolones.
Besifloxacin is administered topically to the eye. Systemic absorption is minimal. The average elimination half-life of besifloxacin in plasma after multiple dosing is estimated to be 7 hours.
-Route-Specific Pharmacokinetics
Other Route(s)
Ophthalmic Route
Plasma concentrations of besifloxacin were measured in adult patients with suspected bacterial conjunctivitis who received besifloxacin bilaterally three times a day (16 doses total). After the first and last dose, the maximum plasma besifloxacin concentration in each patient was less than 1.3 ng/mL. The mean besifloxacin Cmax was 0.37 ng/mL on day 1 and 0.43 ng/mL on day 6.