Proparacaine is an ophthalmic ester-type local anesthetic. It is used as a local anesthetic during short corneal and conjunctival procedures, suture or foreign body removal, and for tonometry. Prolonged use is not recommended. Extended use may produce permanent corneal opacification with accompanying vision loss.
Route-Specific Administration
Ophthalmic Administration
-For topical ophthalmic administration only. Do not administer by injection or orally.
-Avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surfaces.
-Prolonged use is not recommended. Extended use may produce permanent corneal opacification with accompanying vision loss.
Local or systemic sensitivity to proparacaine may occasionally occur. After ophthalmic administration, temporary irritation, stinging, burning, conjunctival hyperemia, lacrimation, eyelid numbness, or increased winking may occur. Immediately closing the eye after administration may help reduce this initial discomfort. Some local ocular irritation and stinging may occur several hours after the instillation. Rarely, a severe, immediate-type, apparently hyperallergic corneal reaction may occur. Symptoms include acute, intense, and diffuse epithelial keratitis; a gray, ground-glass appearance; sloughing of large areas of necrotic epithelium; corneal filaments; and, sometimes, iritis with descemetitis. Pupillary dilation or cycloplegic effects (cycloplegia) have rarely been observed with proparacaine hydrochloride. In addition, delayed hypersensitivity reactions resulting in corneal softening and erosion of the corneal epithelium (corneal erosion), conjunctival congestion, and hemorrhage have been reported. Proparacaine blocks epithelial cell mitosis and cellular migration delaying corneal epithelial regeneration. Long-term proparacaine therapy may lead to impaired wound healing, severe keratitis, scarring, permanent corneal opacification, and visual impairment.
Headache has been reported with proparacaine use. Although exceedingly rare, systemic toxicity manifested by central nervous system stimulation followed by depression may occur after ophthalmic application of local anesthetics. Signs and symptoms of systemic toxicity include drowsiness, difficulty breathing, weakness, sudden fatigue, pallor, or irregular heartbeat.
Allergic contact dermatitis with xerosis or drying and fissuring of the fingertips has been reported.
Proparacaine is contraindicated for use in patients with a known hypersensitivity to any component of the solution. Proparacaine is a local ester anesthetic and should not be used in patients with an ester local anesthetic hypersensitivity. Also, ester-type local anesthetics, such as proparacaine, are metabolized to para-aminobenzoic acid (PABA) and should not be used in patients with para-aminobenzoic acid, PABA hypersensitivity.
Proparacaine should be used cautiously and sparingly in patients with cardiac disease or hyperthyroidism. Although rare, systemic toxicity of proparacaine may occur. Signs and symptoms of systemic toxicity include drowsiness, difficulty breathing, weakness, sudden fatigue, pallor, or irregular heartbeat.
Do not administer by either intravenous administration or intramuscular administration. Proparacaine is only for topical ophthalmic use.
Protection of the eye treated with proparacaine is very important, as the eye may be inadvertently damaged while anesthetic effects remain. Patients should avoid touching, rubbing, or wiping the eyes for at least 10 to 20 minutes. Contact lenses should not be inserted until the anesthetic effects of proparacaine have completely waned. Prolonged use may result in permanent corneal opacification, keratitis, scarring, and visual impairment or loss.
Proparacaine should be administered during pregnancy only if clearly needed. The ability of proparacaine to cause fetal harm or to affect reproductive capacity is unknown. Animal reproduction studies have not been conducted.
It is not known whether proparacaine is excreted into breast milk. Use caution if this drug is administered to a woman who is breast-feeding an infant, as many drugs are excreted in human milk.
For ophthalmic anesthesia:
NOTE: Representative ophthalmic procedures in which the preparation provides good local anesthesia include measurement of intraocular pressure, removal of foreign bodies and sutures from the cornea, and conjunctival scraping in diagnosis and gonioscopic examination. Proparacaine is also indicated for use as a topical anesthetic prior to surgical operations such as cataract extraction.
NOTE: Prolonged use of a topical ocular anesthetic may produce permanent corneal opacification with accompanying loss of vision.
-for the removal of foreign bodies and sutures, and for tonometry:
Ophthalmic dosage:
Adults: Instill 1 or 2 drops in the affected eye(s) before the procedure.
Infants, Children, and Adolescents: Instill 1 or 2 drops in the affected eye(s) before the procedure.
Neonates: Instill 1 or 2 drops in the affected eye(s) before the procedure.
-for anesthesia in short corneal and conjunctival procedures:
Ophthalmic dosage:
Adults: Instill 1 drop in the affected eye(s) every 5 to 10 minutes for 5 to 7 doses.
Infants, Children, and Adolescents: Instill 1 drop in the affected eye(s) every 5 to 10 minutes for 5 to 7 doses.
Neonates: Instill 1 drop in the affected eye(s) every 5 to 10 minutes for 5 to 7 doses.
Maximum Dosage Limits:
-Adults
Specific maximum dosage information is not available.
-Geriatric
Specific maximum dosage information is not available.
-Adolescents
Specific maximum dosage information is not available.
-Children
Specific maximum dosage information is not available.
-Infants
Specific maximum dosage information is not available.
-Neonates
Specific maximum dosage information is not available.
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 Proparacaine products.
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, 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.
Proparacaine is administered topically to the eye. Proparacaine is rapid-acting; the onset of anesthesia after a single drop usually begins within 30 seconds and persists for approximately 10 to 20 minutes; rarely reported to last up to 30 minutes.