Fluorescein; proparacaine is a topical combination of a disclosing agent and local anesthetic indicated for ocular procedures, such as tonometry, gonioscopy, removal of corneal foreign bodies and other short corneal or conjunctival procedures, requiring a disclosing agent with a rapidly acting anesthetic agent of short duration. Prolonged use of a topical ocular anesthetic may result in permanent corneal opacification with accompanying visual loss and is not recommended. Although exceedingly rare with ophthalmic application of local anesthetics, systemic toxicity manifested by central nervous system stimulation followed by depression can occur.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-For topical application to the eye only.
-Thoroughly rinse tonometers that have been soaked in sterilizing or detergents with sterile distilled water prior to use.
-To avoid contamination, do not touch the tip of the dropper used to dispense solution to any surface.
-Replace container closure immediately after using.
-Protect the eye from irritating chemicals, foreign bodies, and rubbing during the anesthesia period. Advise patients to avoid touching the eye until anesthesia has worn off.
Although exceedingly rare with ophthalmic application of local anesthetics, systemic toxicity manifested by central nervous system stimulation followed by depression can occur.
Prolonged use of a topical ocular anesthetic may result in permanent corneal opacification with accompanying visual impairment and is not recommended.
Prolonged use of fluorescein; proparacaine may result in impaired wound healing.
Ocular irritation (i.e., stinging and burning) and conjunctival hyperemia have been reported after ocular administration anesthetics. Rarely, a severe, immediate-type, apparent hyper-allergic, corneal reaction with acute, intense and diffuse epithelial keratitis, a gray, ground glass appearance, sloughing of large areas of necrotic epithelium, corneal filaments, and occasionally, iritis with descemetitis has occurred after use of ocular anesthetics.
Allergic contact dermatitis with accompanying drying and fissuring of the fingertips has been reported with the use of fluorescein; proparacaine.
Use fluorescein; proparacaine with caution and sparingly in patients with known allergies.
Use fluorescein; proparacaine with caution and sparingly in patients with cardiac disease.
Use fluorescein; proparacaine with caution and sparingly in patients with hyperthyroidism.
Use fluorescein; proparacaine during pregnancy only if clearly needed. It is not known if fluorescein; proparacaine can cause fetal harm when administered to a pregnant woman or affect reproduction capacity. Animal reproduction studies have not been conducted with fluorescein; proparacaine.
Use fluorescein; proparacaine with caution in a breast-feeding woman. It is not known if fluorescein; proparacaine is excreted in human milk.
For use as ophthalmic anesthesia during procedures requiring a disclosing agent in combination with an anesthetic:
Ophthalmic dosage (routine ophthalmic anesthesia):
Adults: 1 to 2 drops (in single installations) into affected eye(s) before removal of foreign bodies, sutures, or tonometry.
Ophthalmic dosage (deep ophthalmic anesthesia):
Adults: 1 drop into affected eye(s) every 5 to 10 minutes for 5 to 7 doses.
Maximum Dosage Limits:
-Adults
7 drops/eye per procedure.
-Geriatric
7 drops/eye per procedure.
-Adolescents
Safety and efficacy have not been established.
-Children
Safety and efficacy have not been established.
-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 adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments 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 Fluorescein; Proparacaine products.
Fluorescein is a fluorescent dye that responds to electromagnetic radiation and light at wavelengths of 465 to 490 nanometers and emits light at wavelengths of 520 to 530 nanometers. Thus, the fluorescein hydrocarbon is excited by blue light and emits yellowish-green light. After application of fluorescein to the eye, a slit lamp is used to visualize the anterior ocular surface. Proparacaine prevents the initiation and transmission of nerve impulses by stabilizing the neuronal membrane, so that the neuron is less permeable to ions. Specifically, proparacaine interferes with the large transient increase in the membrane permeability to sodium ions that is normally produced by a slight depolarization of the membrane. As the anesthetic action progressively develops in a nerve, the threshold for electrical stimulation gradually increases and the safety factor for conduction decreases. When this action is sufficiently well-developed, a block of conduction is produced. Proparacaine may limit sodium ion permeability by closing the pores through which the ions migrate in the lipid layer of the nerve cell membrane. Decreased sodium ion permeability may prevent the fundamental change necessary for the generation of the action potential.
Fluorescein; proparacaine is administered topically to the eye. Fluorescein undergoes rapid metabolism to fluorescein monoglucuronide. Fluorescein and its metabolites are primarily eliminated by renal excretion. The estimated renal clearance and hepatic clearance (due to conjugation) of fluorescein are 1.75 mL/minute/kg and 1.5 mL/minute/kg, respectively.
Affected cytochrome P450 isoenzymes and drug transporters: none
-Route-Specific Pharmacokinetics
Other Route(s)
Ophthalmic Route
When administered via topical ophthalmic preparation fluorescein is highly water-soluble and thereby readily diffuses through intercellular fluid spaces. Staining is enhanced with cell degeneration or death, which increases membrane permeability. Staining is increased by rapid stromal diffusion and can manifest whenever there is a disruption of the cell-cell junctions. After administration of a single drop of proparacaine to ocular tissues, the onset of anesthesia begins within 30 seconds and lasts for at least 15 minutes.