PROPARACAINE: 314 Adverse Event Reports & Safety Profile

DESCRIPTION Proparacaine hydrochloride ophthalmic solution USP, 0.5% is a local anesthetic for ophthalmic instillation. Each mL of sterile aqueous solution contains active ingredient: proparacaine hydrochloride 5 mg (0.5%) and inactive ingredients: glycerin (tonicity agent), benzalkonium chloride, 0.01% (preservative) and water for injection (vehicle). The pH may be adjusted with hydrochloric acid and/or sodium hydroxide. At the time of manufacture, the air in the container is replaced by nitrogen. Proparacaine hydrochloride is designated chemically as 2-(Diethylamino) ethyl 3-amino-4-propoxybenzoate monohydrochloride. Graphic formula: C 16 H 26 N 2 O 3

• HCl MW

330.85 CAS-5875-06-9 proparacaine-stru

INDICATIONS AND USAGE Proparacaine Hydrochloride Ophthalmic solution is indicated for topical anesthesia in ophthalmic practice. Representative ophthalmic procedures in which the preparation provides good local anesthesia include measurement of intraocular pressure (tonometry), removal of foreign bodies and sutures from the cornea, conjunctival scraping in diagnosis and gonioscopic examination; it is also indicated for use as a topical anesthetic prior to surgical operations such as cataract extraction.

DOSAGE AND ADMINISTRATION Usual Dosage: Removal of foreign bodies and sutures, and for tonometry: 1 to 2 drops (in single instillations) in each eye before operating. Short corneal and conjunctival procedures: 1 drop in each eye every 5 to 10 minutes for 5 to 7 doses. NOTE: Proparacaine hydrochloride ophthalmic solution USP, 0.5% should be clear, colorless to faint yellow color. If the solution becomes darker, discard the solution. FOR TOPICAL OPHTHALMIC USE ONLY

CONTRAINDICATIONS Proparacaine hydrochloride ophthalmic solution should be considered contraindicated in patients with known hypersensitivity to any of the ingredients of this preparation.

ADVERSE REACTIONS Pupillary dilation or cycloplegic effects have rarely been observed with proparacaine hydrochloride. The drug appears to be safe for use in patients sensitive to other local anesthetics, but local or systemic sensitivity occasionally occurs. Instillation of proparacaine in the eye at recommended concentration and dosage usually produces little or no initial irritation, stinging, burning, conjunctival redness, lacrimation or increased winking. However, some local irritation and stinging may occur several hours after the instillation. Rarely, a severe, immediate-type, apparently hyperallergic corneal reaction may occur which includes 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. Allergic contact dermatitis with drying and fissuring of the fingertips has been reported. Softening and erosion of the corneal epithelium and conjunctival congestion and hemorrhage have been reported. To report SUSPECTED ADVERSE REACTIONS, contact Somerset Therapeutics, LLC at 1- 800-417-9175 or FDA at 1-800 -FDA-1088 or www.fda.gov/medwatch

WARNINGS NOT FOR INJECTION INTO THE EYE - For topical ophthalmic use only. Prolonged use of a topical ocular anesthetic may produce permanent corneal opacification with accompanying loss of vision. Proparacaine ophthalmic solution is indicated for administration under the direct supervision of a healthcare provider. Proparacaine ophthalmic solution is not intended for patient self-administration.

PRECAUTIONS General Proparacaine should be used cautiously and sparingly in patients with known allergies, cardiac disease, or hyperthyroidism. The long-term toxicity of proparacaine is unknown; prolonged use may possibly delay wound healing. Although exceedingly rare with ophthalmic application of local anesthetics, it should be borne in mind that systemic toxicity (manifested by central nervous system stimulation followed by depression) may occur. Protection of the eye from irritating chemicals, foreign bodies and rubbing during the period of anesthesia is very important. Tonometers soaked in sterilizing or detergent solutions should be thoroughly rinsed with sterile distilled water prior to use. Patients should be advised to avoid touching the eye until the anesthesia has worn off. Carcinogenesis, Mutagenesis, Impairment of Fertility Long-term studies in animals have not been performed to evaluate carcinogenic potential, mutagenicity or possible impairment of fertility in males or females.

Pregnancy

Animal reproduction studies have not been conducted with proparacaine hydrochloride ophthalmic solution USP, 0.5%. It is also not known whether proparacaine hydrochloride can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Proparacaine hydrochloride should be administered to a pregnant woman only if clearly needed.

Nursing

Mothers It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when proparacaine hydrochloride is administered to a nursing woman.

Pediatric Use

Safety and effectiveness of proparacaine hydrochloride ophthalmic solution in pediatric patients have been established. Use of proparacaine hydrochloride is supported by evidence from adequate and well-controlled studies in adults and children over the age of twelve, and safety information in neonates and other pediatric patients.

Geriatric

Use No overall clinical differences in safety or effectiveness have been observed between the elderly and other adult patients.