BESIVANCE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BESIVANCE (BESIVANCE).
BESIVANCE is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, thereby blocking DNA replication and leading to bacterial cell death.
| Metabolism | BESIVANCE is not extensively metabolized. Following topical ocular administration, systemic exposure is low; the minimal metabolism that occurs is primarily via glucuronidation and oxidation. |
| Excretion | Primarily excreted unchanged in urine (approximately 50-60%) and feces (approximately 20-30%); biliary excretion contributes to fecal elimination. |
| Half-life | Terminal half-life of approximately 1.5-2 hours in adults; prolongation in renal impairment. |
| Protein binding | Approximately 60% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.35 L/kg, indicating distribution into extracellular fluid and tissues. |
| Bioavailability | Low systemic bioavailability after topical ocular administration (less than 0.1%) due to limited corneal penetration and nasolacrimal drainage. |
| Onset of Action | Onset of antibacterial effect within 30 minutes following topical ocular administration; peak tear concentrations achieved within 5-15 minutes. |
| Duration of Action | Duration of action extends to 4-6 hours based on tear film concentrations; dosing every 8 hours for 7 days ensures sustained antibacterial coverage. |
| Molecular Weight | 606.7 |
One drop instilled into the affected eye(s) three times daily for 7 days.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dosage adjustment required in renal impairment. |
| Liver impairment | No dosage adjustment required in hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients below 1 year of age have not been established. For patients 1 year and older, dosing is as per adult dosing. |
| Geriatric use | No specific dose adjustment is required for elderly patients; dosing is the same as for younger adults. |
| 1st trimester | No adequate studies in pregnant women. Use only if potential benefit justifies potential risk to fetus. |
| 2nd trimester | No adequate studies in pregnant women. Use only if potential benefit justifies potential risk to fetus. |
| 3rd trimester | No adequate studies in pregnant women. Use only if potential benefit justifies potential risk to fetus. |
Clinical note
Comprehensive clinical and safety monograph for BESIVANCE (BESIVANCE).
| Placental transfer | Unknown; systemic absorption after topical ophthalmic administration is minimal, but theoretical potential exists. |
| Breastfeeding | Systemic absorption is negligible; however, caution is advised in nursing mothers due to potential for ocular irritation or systemic effects in infant. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to besifloxacin or any component of the formulation
| Precautions | Topical ophthalmic use only, not for injection, Prolonged use may result in overgrowth of non-susceptible organisms including fungi, Anaphylaxis and other serious hypersensitivity reactions have been reported with systemic fluoroquinolones, Avoid contact lens wear during treatment of bacterial conjunctivitis, Safety and efficacy in pediatric patients below 1 year of age have not been established |
| Food/Dietary | No clinically significant food interactions reported. |
| Clinical Pearls |
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| Lactation Rating |
| L2 |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. Based on animal data, there is no evidence of teratogenicity at clinically relevant doses. In rats and rabbits, ocular administration of besifloxacin during organogenesis showed no fetal malformations. However, systemic exposure is minimal. Risk cannot be completely excluded; use only if potential benefit justifies potential risk to the fetus. |
| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond standard obstetrical care, given minimal systemic absorption. However, monitor for signs of maternal hypersensitivity or ocular adverse effects. |
| Fertility Effects | No studies on fertility in humans. In animal studies, besifloxacin did not impair fertility in rats at doses up to 100 mg/kg/day (systemic exposure). Clinically relevant effects are unlikely due to low systemic absorption. |
| BESIVANCE (besifloxacin ophthalmic suspension) is a fluoroquinolone antibiotic indicated for bacterial conjunctivitis. Shake well before use. Avoid wearing contact lenses during treatment. Not for injection or subconjunctival use. Monitor for hypersensitivity reactions. Use with caution in patients with known fluoroquinolone allergy. |
| Patient Advice | Shake the bottle well before each use. · Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and do not reinsert during treatment. · Apply the prescribed number of drops into the affected eye(s) as directed. · Do not share the medication with others. · Wash hands before and after use. |