1 ml of solution contains 5 mg Proxymetacaine hydrochloride.
Excipients/Inactive Ingredients: Preservative: 1 ml of solution contains 0.1 mg benzalkonium chloride.
Benzalkonium chloride, glycerol, hydrochloric acid and/or sodium hydroxide (to adjust pH), purified water.
Pharmacotherapeutic Group: Local anaesthetics. ATC Code: S01 HA 04.
Pharmacology: Mechanism of action: Proxymethacaine hydrochloride is a surface anesthetic of the ester-type. The surface anesthetics cause a reversible block of conduction through nerve fibers, leading to local anesthesia. The main site of anesthetic action is the nerve cell membrane where proxymetacaine interferes with the large transient increase in the membrane permeability to sodium ions that is internally 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. The exact mechanism by which proxymetacaine and other local anesthetics influence the permeability of the cell membrane is unknown; however, several studies indicate that local anesthetics may limit sodium ion permeability through the lipid layer of the nerve cell membrane. This limitation prevents the fundamental change necessary for the generation of the action potential.
Pharmacodynamics: Proxymetacaine solution is a rapid acting local anesthetic suitable for ophthalmic use. The onset of anesthesia usually begins within seconds and lasts a relatively short period of time.
Clinical efficacy and safety: Proxymetacaine is an established medication.
Pediatric population: The safety and efficacy of Proxymetacaine eye drops in children has not been established.
Pharmacokinetics: Absorption: After topical administration, the local and systemic exposure of proxymetacaine has not been determined. However, quick onset of anesthesia within 30 seconds suggests the compound is rapidly absorbed and persists for a relatively short period of time (about 15-20 minutes).
Distribution: Information on the distribution of proxymetacaine is not available.
Biotransformation: Proxymetacaine is hydrolyzed by plasma esterases, and to a much lesser extend in the liver, to PABA metabolite (p-aminobenzoic acid).
Elimination: Proxymetacaine is only given topically. Information on its elimination is not available.
Linearity/non-linearity: The linearity of the pharmacokinetics for proxymetacaine is not known.
Pharmacokinetic/pharmacodynamic relationship(s): Since ocular or systemic exposure is not known after topical ocular administration, pharmacokinetic/pharmacodynamics relationships for proxymetacaine have not been established.
Toxicology: Preclinical safety data: Following topical ocular administration, proparacaine elicited delayed corneal wound healing and corneal epithelial toxicity in rabbits.
ALCAINE ophthalmic solution contains proxymetacaine hydrochloride, a local anesthetic.
ALCAINE ophthalmic solution is indicated for surface anesthesia in ophthalmologic procedures, such as: tonometric measure of the intraocular pressure, removal of foreign bodies and sutures, conjunctival and corneal scraping, gonioscopic examinations, and other cases where surface anesthesia is indicated.
Posology: For tonometry and other procedures of short duration, instill 1 or 2 drops just prior to evaluation.
For minor surgical procedures such as foreign body or suture removal, instill 1 to 2 drops every 5 to 10 minutes for 1 to 3 doses.
For prolonged anesthesia as in cataract extraction, instill one or two drops in the eye (s) every 5 to 10 minutes for 3 to 5 doses.
Pediatric population: The safety and efficacy of Proxymetacaine Eye Drops in children has not been established.
Use in Elderly Patients: No information is available to suggest dosage adjustment in patients above 65 years of age.
Use in patients with hepatic or renal impairment: The safety and efficacy of ALCAINE ophthalmic solution in patients with hepatic or renal impairment have not been established.
Method of administration: For ocular use.
Shake well before use.
To prevent contamination of the dropper tip and solution, care must be taken not to touch the eyelids, surrounding areas or other surfaces with the dropper tip. Keep the bottle tightly closed when not in use.
After cap is removed, if tamper evident snap collar is loose, remove before using product.
If more than one topical ophthalmic product is being used, the products must be administered at least 5 minutes apart. Eye ointments should be administered last.
Nasolacrimal occlusion or gently closing the eyelid after administration is recommended. This may reduce the systemic absorption of medicinal products administered via the ocular route and result in a decrease in systemic adverse reactions.
In the event of overdose or accidental ingestion, systemic effects may manifest as central nervous system (CNS) stimulation and may include nervousness, tremors or convulsions; followed by depression in CNS which may result in loss of consciousness and respiratory depression.
Hypersensitivity to the active substance or to any of the excipients.
For surface anesthesia in ophthalmology. Not for injection.
Local anesthetics should be used with caution in patients with cardiac disease or hyperthyroidism.
Prolonged use of a topical ocular anesthetic may diminish duration of anesthesia.
Prolonged use or abuse may lead to corneal epithelial toxicity, and may manifest as epithelial defects which may progress to permanent corneal damage (See Adverse Reactions).
Advise patients that, due to the effect of the anesthetic, their eyes will be insensitive and that care should be taken to avoid accidental eye injuries.
Protect the eye from irritants, rubbing, and foreign bodies during period of anesthesia.
Proxymetacaine may cause allergic contact dermatitis. Avoid contact of ALCAINE ophthalmic solution with the skin.
ALCAINE ophthalmic solution contains benzalkonium chloride which may cause eye irritation and is known to discolour soft contact lenses. Additionally, contact lens wear is not recommended until the anesthetic effect has worn-off.
Effects on ability to drive and use machines: Temporary blurred vision or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs after administration, the patient must wait until the vision clears before driving or using machinery.
Fertility: Studies have not been performed to evaluate the effect of topical ocular administration of ALCAINE ophthalmic solution on fertility.
Pregnancy: There are no or limited amount of data from the use of ophthalmic proxymetacaine in pregnant women.
ALCAINE ophthalmic solution is not recommended during pregnancy.
Breast-feeding: It is unknown whether topical proxymetacaine/metabolites are excreted in human milk; however, a risk to the suckling child cannot be excluded. A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from ALCAINE ophthalmic solution therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.
Tabulated list of adverse reactions (Clinical Trials):
Tabulated list of adverse reactions (Post-marketing Surveillance):
The following adverse reactions have been identified from post-marketing surveillance following administration of ALCAINE ophthalmic solution. Frequencies cannot be estimated from the available data. Within each System Organ Class, adverse reactions are presented in order of decreasing seriousness.
Click on icon to see table/diagram/image
Additionally, uncontrolled use or abuse of the product may lead to ocular lesions due to the toxic effects of the anesthetic to the epithelium (see Precautions).
No clinically relevant interactions have been described.
Incompatibilities: Not applicable.
Store refrigerated between 2 °C - 8 °C.
Do not use this medicine after the expiry date which is stated on the packaging.
Discard 4 weeks after first opening.
S01HA04 - proxymetacaine ; Belongs to the class of local ophthalmologic anesthetics.
Ophth soln 0.5% (clear, colourless to light yellowish / brownish solution) x 15 mL.