ZYMAR
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZYMAR (ZYMAR).
Ofloxacin is a fluoroquinolone antibacterial that inhibits DNA gyrase and topoisomerase IV, enzymes essential for bacterial DNA replication, transcription, repair, and recombination.
| Metabolism | Not extensively metabolized; less than 10% excreted in urine as unchanged drug following ophthalmic administration. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 70% of an administered dose; biliary/fecal excretion accounts for about 30%. |
| Half-life | Terminal elimination half-life is approximately 4.5 hours in adults, supporting twice-daily dosing for ocular infections. |
| Protein binding | Approximately 50% bound to serum proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 1.7 L/kg, indicating extensive distribution into tissues. |
| Bioavailability | Ophthalmic: systemic bioavailability is minimal (less than 5%) following topical ocular administration. |
| Onset of Action | Topical ophthalmic: clinical effect observed within 1 hour following instillation. |
| Duration of Action | Duration of action is approximately 12 hours, correlating with the dosing interval of every 12 hours for ophthalmic use. |
1 drop instilled into the affected eye(s) every 2 hours while awake on Day 1, then 1 drop 4 times daily on Days 2 through 7.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment; systemically absorbed drug is minimal. |
| Liver impairment | No dosage adjustment required for hepatic impairment; systemically absorbed drug is minimal. |
| Pediatric use | Children ≥1 year: same as adult dosing; safety and efficacy in infants <1 year not established. |
| Geriatric use | No specific dose adjustment; use same as adult dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZYMAR (ZYMAR).
| Breastfeeding | It is not known whether gatifloxacin is excreted in human milk after ophthalmic administration. Systemic absorption is low, so minimal excretion is expected. Caution should be exercised when ZYMAR is administered to a nursing woman. M/P ratio: Not available. |
| Teratogenic Risk | ZYMAR (gatifloxacin ophthalmic solution) is pregnancy category C. Systemic exposure is minimal after ocular administration, but no well-controlled studies in pregnant women. In animal studies, gatifloxacin was not teratogenic in rats or rabbits at doses up to 100 mg/kg/day (approximately 2000 times the maximum recommended human ophthalmic dose). However, due to potential risk, use during pregnancy only if clearly needed. First trimester: No known fetal risk; second and third trimester: no known risk. |
■ FDA Black Box Warning
None for ophthalmic use. Systemic fluoroquinolones have black box warnings for tendinitis/tendon rupture, peripheral neuropathy, and CNS effects, but these are not applicable to topical ophthalmic formulations.
| Serious Effects |
["Hypersensitivity to ofloxacin or any other fluoroquinolone."]
| Precautions | ["Prolonged use may result in overgrowth of nonsusceptible organisms including fungi.","Do not inject subconjunctivally or introduce into the anterior chamber of the eye.","Patients should not wear contact lenses during treatment.","Avoid contamination of the dropper tip."] |
Loading safety data…
| Fetal Monitoring | No specific maternal or fetal monitoring is required for ophthalmic use. Standard monitoring for any medication applied during pregnancy applies. |
| Fertility Effects | No studies have assessed the effect of gatifloxacin ophthalmic solution on fertility. Systemic fluoroquinolones have been associated with reproductive toxicity in animal studies at high doses, but relevance to ophthalmic use is negligible due to minimal systemic absorption. |