ALTAFLUOR BENOX
Clinical safety rating
cautionComprehensive clinical and safety monograph for ALTAFLUOR BENOX (ALTAFLUOR BENOX).
Comprehensive clinical and safety monograph for ALTAFLUOR BENOX (ALTAFLUOR BENOX).
FDA: For topical ophthalmic anesthesia and as a disclosing agent during ophthalmic procedures (e.g., tonometry, gonioscopy, removal of foreign bodies, sutures).Off-label: No well-established off-label uses.
ALTAFLUOR BENOX is a combination of benoxinate, a local anesthetic that reversibly blocks sodium ion channels in nerve cell membranes, stabilizing the neuronal membrane and inhibiting the initiation and conduction of nerve impulses, and fluorescein, a fluorescent dye that stains epithelial defects in the cornea. Local anesthetic effect occurs within seconds.
| Metabolism | Systemic absorption is minimal after ophthalmic administration. Benoxinate is hydrolyzed by plasma esterases; metabolites are excreted renally. Fluorescein is metabolized via glucuronidation in the liver and excreted primarily in urine. |
| Excretion | Renal: ~80% as unchanged drug; biliary/fecal: ~20% as metabolites (glucuronide conjugates). |
| Half-life | Terminal elimination half-life: 1.0–1.5 hours in adults with normal renal function; prolonged to 6–10 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | ~40–45% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Vd: 1.2–1.8 L/kg (total body water distribution with moderate tissue binding; higher Vd may reflect extensive extravascular distribution). |
| Bioavailability | Topical ophthalmic: minimal systemic absorption (<1% of dose enters systemic circulation). |
| Onset of Action | Topical ophthalmic: within 1 minute (anesthesia); peak effect: 5–15 minutes post-instillation. |
| Duration of Action | Topical ophthalmic: 15–30 minutes of superficial anesthesia. For infiltrative procedures (e.g., cataract surgery): 30–60 minutes of deep anesthesia. |
| Molecular Weight | Propranolol: 259.34 Da; Benoxinate (as HCl): 378.9 Da; Fluorescein: 332.31 Da |
1-2 drops of 0.4% benoxinate hydrochloride ophthalmic solution instilled into the conjunctival sac prior to diagnostic procedures or surgery.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dose adjustment required; systemic absorption minimal. |
| Liver impairment | No dose adjustment required; systemic absorption minimal. |
| Pediatric use | Not recommended for pediatric use; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use with caution due to possible increased sensitivity. |
| 1st trimester | Avoid use. Propranolol (component) has been associated with fetal bradycardia, hypoglycemia, and growth restriction. Benoxinate (sodium fluorescein) is an ophthalmic diagnostic agent with limited systemic absorption; however, the presence of propranolol necessitates caution. |
| 2nd trimester | Use only if potential benefit outweighs risk. Monitor fetal growth and heart rate. |
| 3rd trimester | Avoid near term due to risk of neonatal bradycardia, hypoglycemia, and respiratory depression from propranolol. |
Clinical note
Comprehensive clinical and safety monograph for ALTAFLUOR BENOX (ALTAFLUOR BENOX).
| Placental transfer | Propranolol crosses the placenta readily (cord blood concentrations approximate maternal levels). Benoxinate has minimal systemic absorption; placental transfer negligible. |
| Breastfeeding | Propranolol is excreted into breast milk in small amounts (infant dose ~0.1% of maternal weight-adjusted dose). Monitor infant for bradycardia, hypotension, and hypoglycemia. Benoxinate has minimal systemic absorption; unlikely to be excreted. Use caution with high doses or in premature infants. |
| Lactation Rating | L3 (Moderately Safe) - propranolol component |
| Teratogenic Risk | ALTAFLUOR BENOX contains fluorescein sodium and benoxinate hydrochloride. Fluorescein is not systemically absorbed in significant amounts after topical ophthalmic administration. No teratogenic effects are expected in any trimester. Benoxinate is an ester-type local anesthetic; systemic absorption is minimal. No known teratogenic risk. |
| Fetal Monitoring | No specific maternal-fetal monitoring required due to topical administration and minimal systemic absorption. Standard prenatal care is sufficient. |
| Fertility Effects | No known adverse effects on fertility. Reproductive toxicity studies are not available but systemic exposure is negligible. |
■ FDA Black Box Warning
WARNING: CORNEAL TOXICITY AND IRREVERSIBLE CORNEAL DAMAGE. Prolonged use of topical anesthetics, including ALTAFLUOR BENOX, can result in delayed healing, corneal erosion, ulceration, perforation, and permanent vision loss. Use only for short-term procedures in a controlled clinical setting. Do not dispense to patients for self-administration.
| Serious Effects |
Hypersensitivity to any component (propranolol, benoxinate, fluorescein)Cardiogenic shockSinus bradycardiaHeart block greater than first degreeBronchial asthmaSevere COPDUncompensated heart failure
| Precautions | For topical ophthalmic use only. Not for injection., Prolonged use may cause corneal toxicity; avoid repeated instillation., Patients should avoid touching or rubbing the eye until anesthesia wears off., Use with caution in patients with known hypersensitivity to ester-type anesthetics or fluorescein., May cause transient stinging, burning, or conjunctival hyperemia., Soft contact lenses should be removed before application and may be stained by fluorescein. |
| Food/Dietary | No specific food interactions. Avoid alcohol as it may increase risk of dizziness or syncope during eye procedures. |
| Clinical Pearls | ALTAFLUOR BENOX (benzocaine 20% and fluorescein 0.25%) ophthalmic solution is used for corneal anesthesia and fluorescein staining. Apply 1-2 drops topically before procedures. Avoid prolonged use as benzocaine can cause corneal toxicity and delay healing. Fluorescein may stain soft contact lenses permanently; remove before use. Use with caution in patients with sulfonamide allergy (possible cross-reactivity with fluorescein). After use, patients should not rub eyes to prevent corneal abrasion. |
| Patient Advice | Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before use and wait at least 15 minutes before reinserting. · Temporary blurred vision and stinging may occur; avoid driving until vision clears. · Do not use more often or longer than prescribed to prevent eye damage. · Tell your doctor if you have sulfa allergy or if you are pregnant or breastfeeding. |
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