Alcaine®

GoodRx

Proparacaine 0.5% · ophthalmic solution

Local Anesthetic

Approved uses

Corneal anesthesia of short duration (tonometry, gonioscopy, foreign body or suture removal)

1 to 2 drops in each eye as a single instillation before the procedure

Anesthesia is complete within 1 minute and sensitivity returns to baseline by 45 minutes.

Short corneal and conjunctival procedures

1 drop in each eye every 5 to 10 minutes for 5 to 7 doses

Anesthesia starts at 2 minutes, peaks at 15 minutes, and sensitivity is still reduced at 60 minutes.

OFF-LABELNot in the FDA label for this product

Outpatient analgesia for traumatic corneal abrasion

No endorsed regimen, and this entry is not a recommendation. The only randomized trial of take-home proparacaine used a 0.05% dilution; across the trials in the Cochrane review, treatment ran 3 hours to 1 week, most commonly 24 to 48 hours. Neither source states a dosing frequency.

Cochrane · very low certainty

Cochrane review of 9 RCTs and 556 participants: little or no difference from placebo in post-traumatic pain at 24 hours (MD -0.04 on a 10-point scale; 1 RCT, 76 participants) and a 37% higher rate of unresolved epithelial defects (RR 1.37, 95% CI 0.78 to 2.42; 3 RCTs, 221 participants). All outcomes very low certainty, over half the trials at high risk of bias, and the authors do not recommend the practice. The most favorable single trial used dilute 0.05% drops in 33 completers and found better pain reduction than placebo (median VAS improvement 3.9 vs 0.6 cm, P=0.007) with no observed healing delay, but was far too small to detect the complication it is dispensed against.

Sulewski M, Leslie L, Liu SH, Ifantides C, Cho K, Kuo IC. Topical ophthalmic anesthetics for corneal abrasions. Cochrane Database Syst Rev. 2023;8(8):CD015091; Ball IM, Seabrook J, Desai N, Allen L, Anderson S. Dilute proparacaine for the management of acute corneal injuries in the emergency department. CJEM. 2010;12(5):389-396.

Contraindications

Known hypersensitivity to any ingredient of the preparation.

Available Forms

Proparacaine HCl 0.5% (5 mg/mL) ophthalmic solution, 15 mL dropper bottle

Mechanism of Action

Ester-type local anesthetic that blocks voltage-gated sodium channels in the sensory nerve endings of the cornea and conjunctiva, preventing initiation and conduction of the impulse.

Warnings & Precautions

Topical ophthalmic use only: Not for injection.
Corneal opacification: Prolonged use is not recommended; it may produce permanent corneal opacification with accompanying visual loss.
Anesthetic abuse keratopathy: Repeated self-administration produces a nonhealing epithelial defect with a ring-shaped stromal infiltrate that mimics Acanthamoeba keratitis and has led to conjunctival flap and penetrating keratoplasty; in a 19-patient series ring keratitis appeared in 58% of eyes, hypopyon in 42%, and mean time to epithelialization was 20 days.
Outpatient dispensing: A Cochrane review of 9 RCTs and 556 participants found little or no reduction in post-traumatic pain at 24 hours and no evidence of a healing benefit, all outcomes very low certainty; the authors do not recommend the practice.
Solution appearance: Should be clear to straw-color; discard if it becomes darker.
Storage: Refrigerate at 2 to 8 degrees C and keep the bottle in its unit carton to protect from light.

Common Side Effects

Ocular: Occasional temporary stinging, burning, and conjunctival redness.
Ocular, rare: Severe immediate hyperallergic corneal reaction with acute diffuse epithelial keratitis, a gray ground glass appearance, sloughing of large areas of necrotic epithelium, corneal filaments, and sometimes iritis with descemetitis.
Dermatologic: Allergic contact dermatitis with drying and fissuring of the fingertips.

Pregnancy & Lactation

Pregnancy: Former Category C. No animal reproduction studies have been conducted, and it is unknown whether the drug can cause fetal harm or affect reproductive capacity; administer only if clearly needed.

Lactation: Excretion in human milk is unknown.

Pediatric Use

Established in pediatric patients, supported by controlled studies in adults and children over age 12 plus safety data in neonates and other pediatric patients.