ZYMAXID 0.5 % Ophthalmic Solution
DESCRIPTION
11 ZYMAXID ® is a quinolone antimicrobial topical ophthalmic solution for the treatment of bacterial conjunctivitis.
Its chemical name is (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, sesquihydrate.
Its molecular formula is C19H22FN3O4 · 1½ H2O and its molecular weight is 402.42.
Its chemical structure is: ZYMAXID ® is a clear, pale yellow, sterile, preserved aqueous solution with an osmolality of 260-330 mOsm/kg and a pH of 5.1-5.7.
ZYMAXID ® contains the active ingredient gatifloxacin 0.5% (5 mg/mL) and the inactive ingredients benzalkonium chloride 0.005%, edetate disodium, sodium chloride and purified water.
ZYMAXID ® may contain hydrochloric acid and/or sodium hydroxide to adjust pH.
Chemical Structure
CLINICAL STUDIES
14 In two randomized, double-masked, multicenter clinical trials, where patients 1-89 years of age were dosed for 5 days, ZYMAXID ® was clinically superior to its vehicle on day 6 in patients with conjunctivitis and positive conjunctival cultures.
Clinical outcomes for the trials demonstrated clinical success (resolution of conjunctival hyperemia and conjunctival discharge) in 58% (193/333) of patients for the gatifloxacin-treated groups versus 45% (148/325) for the vehicle-treated groups.
Microbiological outcomes for the same clinical trials demonstrated a statistically superior eradication rate for causative pathogens of 90% (301/333) for gatifloxacin vs.
70% (228/325) for vehicle.
Please note that microbiological eradication does not always correlate with clinical outcome in anti-infective trials.
HOW SUPPLIED
16 /STORAGE AND HANDLING ZYMAXID ® (gatifloxacin ophthalmic solution) 0.5% is supplied sterile in a white, low density polyethylene (LDPE) bottle with a controlled dropper tip, and a tan, high impact polystyrene (HIPS) cap in the following size: 2.5 mL in 5 mL bottle: NDC 0023-3615-25 Storage: Store at 15°-25°C (59°-77°F).
Protect from freezing.
RECENT MAJOR CHANGES
Contraindications, Hypersensitivity (4) 09/2016 Warnings and Precautions, Hypersensitivity (5.1) 09/2016
GERIATRIC USE
8.5 Geriatric Use No overall differences in safety or effectiveness have been observed between elderly and younger patients.
DOSAGE FORMS AND STRENGTHS
3 Ophthalmic solution: 0.5% gatifloxacin (5 mg/mL) Ophthalmic solution: 0.5% gatifloxacin (5mg/mL) (3)
MECHANISM OF ACTION
12.1 Mechanism of Action Gatifloxacin is a quinolone antimicrobial [see Microbiology (12.4)].
INDICATIONS AND USAGE
1 ZYMAXID® is indicated for the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Aerobic gram-positive bacteria: Staphylococcus aureus Staphylococcus epidermidis Streptococcus mitis group* Streptococcus oralis* Streptococcus pneumoniae Aerobic gram-negative bacteria: Haemophilus influenzae *Efficacy for these organisms were studied in fewer than 10 infections.
ZYMAXID ® is a quinolone antimicrobial indicated for the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Haemophilus influenzae, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus mitis group, Streptococcus oralis, Streptococcus pneumoniae (1)
PEDIATRIC USE
8.4 Pediatric Use The safety and effectiveness of ZYMAXID ® in infants below one year of age have not been established.
ZYMAXID ® has been demonstrated in clinical trials to be safe and effective for the treatment of bacterial conjunctivitis in pediatric patients one year or older [see Clinical Studies (14)].
PREGNANCY
8.1 Pregnancy Risk Summary There are no available data on the use of ZYMAXID® in pregnant women to inform a drug-associated risk.
Administration of oral gatifloxacin to pregnant rats and rabbits throughout organogenesis did not produce adverse development outcomes at clinically relevant doses.
Administration of gatifloxacin to rats during late gestation through lactation did not produce adverse maternal, fetal or neonatal effects at clinically relevant doses.
Data Animal Data Oral administration of gatifloxacin to pregnant rats throughout organogenesis produced teratogenic effects in rat fetuses, including skeletal/craniofacial malformations, delayed ossification, atrial enlargement, and reduced fetal weight, at doses greater than or equal to 150 mg/kg/day (approximately 600-fold higher than the maximum recommended human ophthalmic dose [MRHOD] for ZYMAXID® of 0.04 mg/kg/day, on a mg/m2 basis).
No teratogenic effects were observed in rat or rabbit fetuses at doses of gatifloxacin up to 50 mg/kg/day (approximately 200- and 400-fold higher than the MRHOD, respectively, on a mg/m2 basis).
In a perinatal/postnatal study in rats, oral administration of gatifloxacin during late gestation through lactation produced an increase in late gestation fetal loss and neonatal/perinatal mortality at 200 mg/kg/day (approximately 800-fold higher than the MRHOD on a mg/m2 basis).
WARNING AND CAUTIONS
5 WARNINGS AND PRECAUTIONS Hypersensitivity (5.1) Growth of Resistant Organisms with Prolonged Use (5.2) Corneal Endothelial Cell Injury (5.3) 5.1 Hypersensitivity Some patients receiving topical ophthalmic gatifloxacin experienced hypersensitivity reactions including anaphylactic reactions, angioedema (including pharyngeal, laryngeal, or facial edema), dyspnea, urticaria, and itching, even following a single dose.
Rare cases of Stevens-Johnson Syndrome were reported in association with topical ophthalmic gatifloxacin use.
If an allergic reaction to gatifloxacin occurs, discontinue the drug [see Patient Counseling Information (17)].
5.2 Growth of Resistant Organisms with Prolonged Use Prolonged use of ZYMAXID ® may result in overgrowth of nonsusceptible organisms, including fungi.
If superinfection occurs, discontinue use and institute alternative therapy.
Whenever clinical judgment dictates, examine the patient with the aid of magnification, such as slit lamp biomicroscopy and where appropriate, fluorescein staining.
5.3 Corneal Endothelial Cell Injury ZYMAXID ® is for topical ophthalmic use.
ZYMAXID ® may cause corneal endothelial cell injury if introduced directly into the anterior chamber of the eye.
INFORMATION FOR PATIENTS
17 PATIENT COUNSELING INFORMATION Avoiding Contamination of the Product Instruct patients to avoid contaminating the applicator tip with material from the eye, fingers, or other source.
Potential for Hypersensitivity Reactions Advise patients to discontinue use immediately and contact the physician at the first sign of a rash or hypersensitivity reaction [see Warnings and Precautions (5.1) and Contraindication (4)].
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DOSAGE AND ADMINISTRATION
2 Day 1: Instill one drop every two hours in the affected eye(s) while awake, up to 8 times.
Day 2 through Day 7: Instill one drop two to four times daily in the affected eye(s) while awake.
Day 1: Instill one drop every two hours in the affected eye(s) while awake, up to 8 times on Day 1.
Days 2 through 7: Instill one drop two to four times daily in the affected eye(s) while awake on Days 2 through 7.
(2)