Locular 0.2% Eye-Drop 5 ml drop

Indications

Brimonidine 0.2% ophthalmic solution is indicated for lowering intraocular pressure in patients with open-angle glaucoma or ocular hypertension

Description

Brimonidine Tartrate ophthalmic solution 0.2% is an alpha adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours postdosing. Fluorophotometric studies in animals and humans suggest that Brimonidine Tartrate has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.

Pharmacology

Brimonidine is an α-2 adrenoreceptor agonist that is more selective for the α-2 adrenoreceptor than α-1. Topical administration of Brimonidine Tartrate eye drops decreases intraocular pressure (IOP) in humans. When used as directed Brimonidine Tartrate have the action of reducing elevated IOP with minimal effect on cardiovascular parametres. Brimonidine Tartrate eye drops have a rapid onset of action with the peak ocular hypotensive effect occurring at two hours post-dosing. The duration of effect is 12 hours or greater. Fluorophotometric studies in animals and humans suggest that Brimonidine Tartrate has a dual mechanism of action. Brimonidine Tartrate eye drops lower IOP by reducing aqueous humor production and enhancing uveoscleral outflow.

Interaction

Although specific drug interaction studies have not been conducted with Brimonidine Tartrate ophthalmic solution 0.2%, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, or anesthetics) should be considered. Alpha-agonists, as a class, may reduce pulse and blood pressure. Caution in using concomitant drugs such as beta-blockers (ophthalmic and systemic), antihypertensives and/or cardiac glycosides is advised. Tricyclic antidepressants have been reported to blunt the hypotensive effect of systemic clonidine. It is not known whether the concurrent use of these agents with Brimonidine Tartrate ophthalmic solution 0.2% in humans can lead to resulting interference with the IOP lowering effect. No data on the level of circulating catecholamines after administration of Brimonidine Tartrate ophthalmic solution 0.2% are available. Caution, however, is advised in patients taking Tricyclic antidepressants which can affect the metabolism and uptake of circulating amines.

Side Effects

Adverse events occurring in approximately 10-30% of the subjects, in descending order of incidence, included oral dryness, ocular hyperemia, burning and stinging, headache, blurring, foreign body sensation, fatigue/drowsiness, conjunctival follicles, ocular allergic reactions, and ocular pruritus. Events occurring in approximately 3-9% of the subjects, in descending order included corneal staining/erosion, photophobia, eyelid erythema, ocular ache/pain, ocular dryness, tearing, upper respiratory symptoms, eyelid edema, conjunctival edema, dizziness, blepharitis, ocular irritation, gastrointestinal symptoms, asthenia, conjunctival blanching, abnormal vision and muscular pain. The following adverse reactions were reported in less than 3% of the patients: lid crusting, conjunctival hemorrhage, abnormal taste, insomnia, conjunctival discharge, depression, hypertension, anxiety, palpitations/arrhythmias, nasal dryness and syncope.