Alcaine^® (Drops) Instructions for Use

Marketing Authorization Holder

Alcon Laboratories, Inc. (USA)

Manufactured By

Alcon-Couvreur N.V., S.A. (Belgium)

ATC Code

S01HA04 (Proxymetacaine)

Active Substance

Proxymetacaine (Rec.INN registered by WHO)

Dosage Form

Alcaine®

Ophthalmic drops 0.5%: dropper bottle 15 ml

Dosage Form, Packaging, and Composition

Ophthalmic drops in the form of a clear solution from colorless to slightly yellowish or slightly yellowish-brownish in color.

Excipients: benzalkonium chloride solution (equivalent to benzalkonium chloride 0.1 mg), glycerol – 24.5 mg, hydrochloric acid and/or sodium hydroxide – q.s., purified water – up to 1 ml.

15 ml – polyethylene dropper bottles “DropTainer^®” (1) – cardboard packs.

Clinical-Pharmacological Group

Local anesthetic for use in ophthalmology

Pharmacotherapeutic Group

Local anesthetic agent

Pharmacological Action

An agent for local anesthesia in ophthalmic practice. The effect begins 30 seconds after instillation and lasts for 15 minutes with a single instillation.

Proxymetacaine inhibits the permeability of cell membranes to sodium ions, which prevents the generation of impulses in nerve endings and the conduction of impulses along nerve fibers.

Pharmacokinetics

After instillation into the conjunctival sac, it is rapidly absorbed and hydrolyzed by plasma esterases. It is excreted by the kidneys as inactive breakdown products.

Indications

In ophthalmology for performing short-term diagnostic and therapeutic procedures requiring rapid and short-term anesthesia: including tonometry, tonoscopy, removal of foreign bodies.

ICD codes

Dosage Regimen

For topical ophthalmic use only. Instill into the conjunctival sac.

For tonometry, administer one to two drops immediately before the procedure.

For superficial foreign body removal or other brief surgical procedures, administer one to two drops. A second drop may be required after five to ten minutes for prolonged manipulation.

For deep ophthalmic anesthesia, instill one drop every five to ten minutes for a total of five to seven instillations.

Do not exceed the minimum number of drops necessary to achieve anesthesia. The maximum safe duration of continuous use has not been established; prolonged use increases the risk of serious corneal damage.

If used concomitantly with other ophthalmic solutions, maintain an interval of at least five minutes between instillations. Apply eye ointments last.

Always replace the cap after use to avoid contamination. Do not touch the dropper tip to any surface, including the eye.

Discard the bottle promptly after the single procedure or course of treatment is completed.

Adverse Reactions

Local reactions: frequent – eye itching, eye irritation, conjunctival hyperemia; infrequent – ulcerative keratitis, keratitis, corneal infiltrates, corneal edema, iritis, descemetitis, severe immediate allergic reactions from the cornea, characterized by diffuse epithelial keratitis with detachment of necrotized epithelium and diffuse stromal edema; rare – development of filamentous keratitis accompanied by diffuse stromal edema; frequency unknown – vision loss, corneal perforation, corneal infection, corneal erosion, corneal clouding, blurred vision, photophobia, mydriasis, eye pain, eye swelling, eye discomfort sensation, eye hyperemia, increased lacrimation.

Systemic reactions rare – hypersensitivity reactions, systemic toxicity manifested by CNS excitation followed by its depression; frequency unknown – fainting.

Contraindications

Hypersensitivity to proxymetacaine.

With caution in patients with allergic reactions, epilepsy, heart disease, hyperthyroidism, and breathing disorders; patients with myasthenia gravis, patients with low plasma acetylcholinesterase content, as well as patients undergoing treatment with cholinesterase inhibitors (as they are more susceptible to the risk of systemic adverse reactions), children under 18 years of age.

Use in Pregnancy and Lactation

Use during pregnancy is not recommended. If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Pediatric Use

Should be used with caution in children and adolescents under 18 years of age (due to the lack of sufficient experience of use in this category of patients).

Special Precautions

Repeated sequential application of proxymetacaine causes a decrease in the duration of its action, which requires additional instillation. However, in this case, there is a high risk of developing infection, clouding, or perforation of the cornea.

If necessary, Proxymetacaine can be used in combination with other ophthalmic drugs. In this case, the interval between their applications should be at least 5 minutes. Eye ointments should be applied last.

Effect on the ability to drive vehicles and mechanisms

During the use of proxymetacaine, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.